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Curriculum
Vitae Mark
Brian Anderson, PhD .....................
THERAPEUTIC AREAS: Drug discovery, operational leadership in identifying, evaluating and developing novel
preclinical drug development opportunities and candidates; progressing into IND-enabling studies and into human clinical trials.
Understanding
applicable genetics and pathogenesis as it applies to the discovery process. Work with the establishment
of the infrastructure to build products. Manage the operational aspects of partner alliances; oversee the development
and maintenance of and adherence to all collaborative agreements as they apply to the science and product pipeline. Ensure
appropriate communications as it applies to the science. Lead, design & development as translational medicine with experience
in cancer/oncology; infectious diseases; neurology; neurodegeneration; cardiovascular; multiple kinase targets; anti-virals,
HIV, genetic, epigenetic and metabolic targets; bacterial and fungal targets; thrombosis; endocrine; inflammation, cell adhesion,
pulmonary, adverse drug reactions; chemical biology, chemical proteomics, vascular disrupting and vascular targeting agents,
tubulin agents, Alzheimer's disease, and ischemia-reperfusion inhibitors. I
bring more than eighteen years experience from the biotechnology and pharmaceutical industry directing numerous R&D
programs. In these roles, I have been responsible for establishing company’s strategic R&D roadmap and to provide exemplary scientific input into the company’s
research and development programs in order to support the overall corporate strategy. Strong Translational Science background advancing the company's product
pipeline and mentoring talent management essential to program success, the development and retention of a highly
competitive workforce, planning for changing pipeline dynamics interoperating the corporate vision to tangible deliverables.
Also, I have demonstrated a driven talent in setting and managing the scientific and technical direction; IND development
of all invented, existing and/or anticipated products for filling the pipeline to drive profits. I participate as
a translational clinical development team member; work as an international and US collaborations lead. Working to that
end in an advisory capacity I understand the importance of timely reporting to management boards, directing the
scientific vision and driving the direction of the company. I have been responsible for the professional development
in all aspects of the biology, pathology and chemistry from "principle to practice", so to encourage the drug
development pipeline. I have spent my career targeting highly effective science, bringing forward strong teams, so
to produce a healthy and robust preclinical development pipeline in pharmaceuticals. - Lead process efficiency initiatives related
to cross-company, cross-program global operations to promote organizational effectiveness
- Clinical
pathology & chemistry panel review, translational research, adverse drug-drug interactions, personalized medicine approach
using data to drive selection process.
- Formulation evaluation for small molecules,
heterocycles, natural products, proteins, and antisense RNA compounds etc
- Expand profiles to
include difficult therapeutic areas as novel compounds as well as polymorphs, salt forms, prodrugs, DSC, TGA, pre-IND API
stability studies, C-of-A's, and Top-quality technology transfer packages enabling bench-to-CRO API syntheses
- Implement strategic business acumens to ensure best practices and eliminate redundancies, TPP and IND preparation,
INN/USAN proprietary names, and ATC Codes
- Drive International and US joint collaborative research
committees (JCRC); board meetings; steering committees; and strategic think tanks; and provided scientific expertise on in-licensing
opportunities
- Recruit and develop key scientific talent
- New
technology evaluations and review
- Lead Confidential M&A discussions
- Pharmacology (pharmacokinetics/ADME, pharmacodynamics, pharmacotherapeutics, & Toxicology) in SXR matrix
- Track record of building and mentoring fully integrated chemistry drug discovery engines (e.g. CFU/H2L, In Silico
Chemistry/SBDD, Analytical, Medicinal/Chemical Biology/Chemical Proteomics, In Silico Sciences, SBDD, pre-formulations,
early API stability, and bench top-to CRO scale-up and technology transfer packages, Chemical Toxicology)
- Predicting blood-brain barrier (BBB) permeable compounds
- Direct international and
US multidisciplinary CSO's/CRO's/CMO's.
- Track-record of leadership, scientific vision, problem
solver, timelines, IND's, budgets, etc
- Track record of small molecules, heterocycles, natural
products, proteins, carbohydrates, antisense RNA, etc
- Track record in strategic disease areas
of cancer/oncology, infectious disease, neurodegeneration /neurology (Alzheimer's), HIV, thrombosis, inflammation, etc
- Track record of important targets kinases, genetic disease links, metabolic, bacterial, fungal, endocrine, cardiovascular,
pulmonary, cell adhesion, tubulin agents, ischemia-reperfusion inhibitors, etc
- Track record
of driving ideas into the clinic, being a passionate leader, drug hunter, mentoring talent, inventor, team player, and creating
fun top-quality high-performance teams
OVERVIEW OF INTELLECTUAL PROPERTIES:
100+ US & international issued and pending patent applications covering novel therapeutic agents,
HIV maturation inhibitors, novel agents for treating HIV, novel antiviral (HIV) agents, blood brain barrier permeable anti-cancer
agents, methods for treating brain cancer, novel anti-tumor agents, caspase activators and inducers of apoptosis, genetic
predisposition as it applies to disease, Alzheimer's disease (neurodegeneration), non-peptide GnRH agents, kinases, etc. The
end result is a history of multiple agents in the clinic. See list below. PUBLICATIONS
HIGHLIGHTS: 50+ publications, many cited in diverse areas and novel agents with potent anti-maturation activity
against HIV-1, discovery of novel agents for treating brain cancer, SAR of novel anticancer agents, experimental therapeutics,
new methodologies, etc., additional publications are in progress. Examples: 2008 review on vascular disrupting and vascular
targeting agents (in press), 2003 Annual Reports in Medicinal Chemistry, Burger's Medicinal Chemistry Chapter 22 (1994), ACS
and international symposia posters, papers on mechanism of action studies as it relates to disease targets and the development
of novel compounds, MRSA strategies, and many international collaboration presentations. See list below. 2011 February - R&D Directions; Notable People in R&D. Article of
one of nine people recognized in the February issue of "R&D Directions" for the top noteworthy 2010 leaders
who have made lasting contributions in research; Notable People in R&D, page 16 2011. http://www.pharmalive.com/magazines/randd/
Industrial Experience Mark Anderson, Mark Brian Anderson NOVABAY PHARMA (OCTOBER 2009 - PRESENT) EMERYVILLE, CA. Chief Scientific Officer: Provide senior
technical leadership by formulating and advocating a science and technology vision that complements the business vision
as a vibrant up and coming biotech, driving the capability investment strategy, expanding the technical integration
across capability groups to help assure regional, national, and international impact in the biological, chemical, materials
sciences in developing novel therapeutics. Streamline the operating model driving growth of innovative opportunities
and managing multiple business profit driven platforms. Mentor talent, establish and achieve the strategic goals of the
organization in collaboration with the Novabay leadership team by leading the strategic scientific planning effort, development
of critical new science and technology capabilities that are required to build and grow research programs, attract and anchor
effective collaborations and productive partnerships, maintain a competitive market position, and deliver highly impactful
science in key areas as outlined by the board of directors and scientific advisory board. Overall business understanding including experience in business development and licensing contracts.
Manage scientific staff in all areas of discovery and development in biology, chemistry, pathology and clinical
development as they relate to the team development in the pursuit of novel drug targets in novel, relevent therapeutic
areas. Strong networking
skills with experts in academia & industry. A solid record of maintaining and developing successful relationships with
opinion leaders and investigators in multiple stages of critical care as it relates to the investigation of infectious
disease and inflamation. Collaborations & Licensing: Alcon
Pharmaceuticals, Galderma Pharmaceuticals; senior member of license acquisition team for the licensing of potential research
(idea to IND) and/or drug agents suitable for clinical development (IND to NDA).
BIOTECH PHARMA SOLUTIONS (MARCH 2009 - SEPTEMBER 2009) OFFICES IN BOSTON, MA AND SALT
LAKE CITY, UT. http://www.biotechpharmasolutions.com/
Services:
As a consulting chief scientific officer (CSO) I have shepherded preclinical drug development projects, pathology, chemistry,
biology, formulations, understanding toxicology to promote clinical drug development programs from "principal
to practice" that is cost effective and in reasonable time, with entrepeneurial minded thinking. In the role as
a consulting CSO in multiple therapeutic areas, I have been responsible for advancing the company's product pipeline; setting
and managing the scientific and technical direction; IND track development of all invented, existing or anticipated products
in the pipeline; formulation strategies; a vital clinical development team member; international and US collaborations lead;
advising the board and management on the scientific vision and direction of the company; and responsible for the professional
development of the science and staff. The design, formulation, clinical development and marketing of novel microRNAs
(antagomirs) for the treatment of human pathologies. Furthermore, I have developed highly effective business acumens
that help direct the creation of a healthy robust prioritized preclinical IND pipeline in a reasonable timeframe, that is
growth oriented to improve financial conditions reducing over all risk.
Preclinical Drug Development Consultant Formulation Development Problem Resolution CRO Selection and Management Acquisition Pharmaceutical Drug Development Mentoring Quality Assurance/GMP Assistance Pharmaceutical Regulatory Affairs/CMC CRO Management Confidential In-Licensing and M&A Discussion Lead Invention
Generation Opportunity Model Assessment Competitive Landscaping Assessment INN/USAN & ATC Codes Evaluating Research Tools (e.g. equipment, chemical proteomics, chemical biology,
chemical toxicology) Think Tank and Personalized Medicine Discussions; (cancer, infectious disease, inflamitory
disease, HIV, neurology) Help with 21 & 37 Codes of Federal Regulations Focused Change Management and
more.
Examples: Cancer (brain, melanoma, etc), Infectious disease (bacterial & fungal); HIV
infection; Neurodegenerative (Alzheimer's & Parkinson's); Cell Adhesion mediated diseases (inflammation, cancer metastasis,
etc); Genetic disease (antisense RNA); and therapeutic agent types: small molecules; natural products; heterocycles; peptides
and proteins; antisense RNA; agents targeting metalloenzymes; complex carbohydrates; and chemical combinations to form novel
hybrids.
MYRIAD GENETICS & MYRIAD
PHARMACEUTICALS (DEC. 2003 - MARCH 2009, 5.5 YEARS) SALT LAKE CITY, UTAH.
Vice President of Research; Chemistry:
Responsible for setting and managing the overall scientific, technical direction, and IND track development of all invented,
existing or anticipated products in the pipeline; clinical development team member; and responsible for: the professional
development of the scientific staff. The results were to put five compounds into clinical development. The most advanced and
patented compounds target brain cancer, neurology, metastatic cancers and HIV (vide infra patents).
Clinical
Pipeline: AzixaTM (MPC-6827) Non-Small-Cell Lung Cancer Phase 2; AzixaTM (MPC-6827) Melanoma
Phase 2; AzixaTM (MPC-6827) Glioblastoma Phase 2; ViveconTM (MPC-9055) HIV Maturation Phase 1; MPC-2130
Metastatic & Blood Cancers Phase 1; MPC-0920 Thrombosis Phase 1; MPC-3100 for Cancer; and work on FlurizanTM
(tarenflurbil) for Alzheimer's. Composition of matter, clinical use patents, and IND's to fully enable the pipeline (vide
infra patents).
Preclinical Pipeline: Responsible for the chemistry drug discovery engine
and program management to produce IND-Ready agents. Examples: MPI-0443803 (drug resistant cancers and brain cancer; including
prodrugs); MPI-451936 HIV (HIV fusion inhibitor) and MPI-461359 HIV (Maturation); MPC-2130 (chemical MOA); backup for MPC-0920;
follow on agents for MPC-3100 ( in clinical development); MPI-442690( backup for Alzheimer's Disease); prodrugs for treating
neurodegenerative disease agents; novel compounds and novel drug combinations for neurodegenerative disease programs including
prodrugs and formulations; blood-brain-barrier predictions; chemical proteomic programs and strategies; and numerous oncology,
antiviral, and kinase targets that are clinically-relevant and clinically-important; novel drug-drug combinations for treating
diseases; drug delivery formulations; and numerous invention disclosures for novel agents and therapeutic targets and enzymes
(vide infra patents).
Intellectual Properties (IP): Track record of a close, effective,
and productive relationship with the IP department. In addition, a recent review on VDA's and VTA's is published.
Licensing & Collaborations: Joint collaborative research committee with Abbott Labs; member of Myriad's
in-license acquisition teams for the in-licensing of potential research (idea to IND) and/or drug agents suitable for clinical
development (IND to NDA).
Track record: Effective leadership and management business acumens;
multiple program portfolio management resulting in compounds in the clinic; multidisciplinary program management; worked
closely with pharmacology/ADME TOX and discovery biology; medicinal chemistry chemical biology; exploitation of pharmacology
and biologic results for the SXR chemical drug design matrix; a fully integrated chemistry department (medicinal, analytical,
structure-based drug design, chemistry follow up/hit-to-lead, pre-IND scale up); chemical proteomics with coordination of
chemistry & biology teams; share management responsibilities for the site as a member of the senior management team; numerous
patents, invention disclosures and expert relationship with the intellectual property department; active discussions in personalized
medicine; translational research/medicine; 1-5 year budgets; hiring; annual reviews; and 21 & 37 codes of federal regulations.
The result is a fun, innovative, fast-paced, results-driven, strategic, and team-oriented drug discovery engine with a clear
focus on the programs and corporate objectives. The return on the R&D investment is multiple drug agents in the clinic.
ELITRA PHARMACEUTICALS INC. (JUNE 2002
- NOV. 2003, 1.5 YEARS) SAN DIEGO, CA.
Senior Director of Drug Discovery Chemistry R&D: Share management
responsibilities for the site as a member of the senior scientific staff, mentored the microbiology teams, and manage a large
portfolio of projects focused on discovering, developing, and commercializing novel small molecule drugs for the treatment
of drug resistant infectious disease with high unmet needs.
Clinical Pipeline: Evaluate potential
in-license opportunities for clinical development (IND to NDA), ensuring that the potential in-licensing IND package was complete,
feasible, and a reasonable estimate for moving towards a successful NDA;
Preclinical pipeline:
Responsible for the chemistry drug discovery engine and program management to produce IND-Ready agents from internal efforts
and with multiple international and US collaborations. Elitra's drug discovery collaborations included Merck & Co. (US),
LG Life Sciences (Korea), BioLeads (EU), Kaken (Japan), and deCODE genetics (Reykjavik, Iceland and US facility). Designed
the chemistry drug discovery plans for SBIR grants (e.g. chemical compound design for Yersinia pestis a Gram-negative
rod-shaped bacterium belonging to the family Enterobacteriaceae); and reviewed the competitive landscape of bacterial and
fungal drugs.
Track-record of mentoring top-performing teams by ensuring the capture of ideas
and intellectual properties (Idea to IP); member of multiple joint collaborative research committees (JCRC's); the utilization
of genetic, biologic, pharmacokinetic (ADMET), safety, and pharmacodynamic (PD) data into the matrix of medicinal chemistry
drug design; member of in-license acquisition teams for in-licensing of potential drug agents for the clinic (IND to NDA);
development of effective business acumens; and familiar with WHO/INN/USAN, and ATC codes.
Simultaneously
managed multi-phased and multi-focused collaborations (JCRC's); experienced manager of CRO's/CMO's; and experienced
in the design and development of new therapeutic agents exploiting Elitra's proprietary bacterial and fungal genetic targets.
These proprietary platforms were highly valued for drug discovery and chemical biology to elucidate the molecular pathways
that are fundamental in cellular, developmental, and the biology of diseases of novel and established drugs.
Mentor
talent in Microbiology and Cell-Based assays (6); Pharmacology (ADMET and Pharmacodynamic) team (4); and the Analytical
team (2); managed the drug discovery chemistry with LG (8) and deCODE (8), worked with CRO's.
Plan and
execute multiyear budgets for multiple departments (chemistry, bioanalytical, microbiology, pharmacology/ADMET and
pharmacodynamics groups). Maintain high scientific standards (>95% HPLC purity); developed business acumens for the internal
analog progression of preclinical agents towards IND-ready candidates; collaboratively work with screening, informatics, biology,
analytical chemistry, microbiology, joint collaborations, and CROs. Review HTS and UHTS screening hits; scientifically contribute
to SAR and SXR (DMPK/ADMET) of collaborations; de novo drug discovery; managed the Microbiology and Cell-Based assays
(6), ADMET and Pharmacology team (4), Analytical (2). Chemistry (LG 8 and deCODE 8), CROs. Work closely with human resources
for recruiting, hiring and annual reviews.
Genetic and therapeutic targets for the discovery
of new agents for the treatment of bacterial infections as a high priority as many know pathogens show resistance to know
antibacterial agents. The medical need is for antibacterial agents for Gram-positive, Gram-negative and/or broad spectrum
agents and to investigate agents for drug resistant infectious bacterial induced disease. The focus was the discovery and
development of novel antibacterial and antifungal drug candidates identified by proprietary screening technologies of the
bacterial and fungal genomes (functional genomics), with internal and collaborative chemistry drug discovery programs. Elitra
identified more than 6,000 essential genes in eleven bacterial and fungal pathogens and were discovering new classes of compounds
utilizing its internal high throughput screening capabilities. The approach was enabling true functional genomics on a genome-wide
scale and to identify all of the essential genes directly in the key pathogenic organisms. The technology also elucidated
known and potential new targets of established clinically used bacterial and fungal drugs. 2004 Elitra's assets acquired by
Rx3 now Trius and Mycota now Merck.
PFIZER LA JOLLA LABS, AGOURON PHARMACEUTICALS (OCT. 1997 - JUNE 2002,
5 YEARS).
Associate Director of Medicinal Chemistry: share management responsibilities
for the department as a member of the senior scientific staff.
Recipient of the Agouron Pharmaceuticals
President's Award in drug discovery research (January 1999). Associate Director of Medicinal Chemistry
Duties: Foster a team-oriented approach in chemistry and projects; worked with upper management to maintain a focus on corporate
needs and the corporate pipeline. Project leader (GnRH), and project member of several drug discovery projects and directly
contributed to multiple patent applications. Direct line management on average of more than 20 PhD/MS chemists, and 4 students.
Focus on teamwork and drug candidate compounds for GnRH, cancer related to kinases, and ideas for novel anti-virals. Additional
contributions: actively participated in the oncology and viral discovery groups. Clinical pipeline: Driver of Pfizer's protocols for moving into first in human
studies and beyond.
Preclinical Pipeline: Participated in numerous drug discovery projects, one
candidate compound awarded, and responsible for the project leadership of the GnRH project, and the progression of candidate
for IND/Clinical considerations, directly contribute to the chemical lead discovery and lead optimizations, and developed
the small molecule antagonist project from the initial HTS screening hits, through the novel molecular rearrangement to give
the key lead series, through a full medicinal chemistry team lead SAR optimization including early DMPK/ADMET, Safety, biomarkers,
and pharmacodynamic data integration into further lead optimizations, to the presentation of several potent viable lead series
exhibiting metabolic stability, sufficient Cmax, long T1/2, etc. as potential drug development candidate compounds. Additional
project considerations included: verification of medical need, marketing and commercial considerations in collaboration with
the global management teams.
Project teams consisted of ~ 11 PhD/MS chemists, ~5 PhD/MS pharmacologists,
~2 PhD/MS DMPK specialists, ~6+ PhD/MS biologists including assorted marketing and development teams, etc. In addition to
the GnRH project, I had the pleasure of participating in several kinase structure-based-drug-design projects and in multiple
combinatorial chemistry projects. As an associate director and scientist, I personally contributed to the design, and submission,
of many new ideas into the Pfizer idea bank for new drug core structures and combinatorial library expansion opportunities.
Associate Director; scientific duties activities included fostering a team-oriented approach in the department and in projects; conducted team meetings (as
the project leader) and action item follow up for lead optimization to candidate compound projects; participated in cross-site
Pfizer scientific meetings in medicinal chemistry and in combinatorial discussions; attend departmental meetings and senior
staff meetings. Responsible for line management of several PhD/MS chemistry teams in the medicinal chemistry department. Conceive,
design and execute on novel chemical series for active research projects; actively support all intellectual property needs
related to associated projects, and directly contribute scientifically to patent filings. Actively support all aspects of
medicinal chemistry in the department and directly contributed chemical agents for screening and medicinal chemistry lead
optimization. Participated in SBDD (structure-based drug design) kinase teams and in targeted/combinatorial drug design strategies
for hit and lead optimizations; personally contributed to novel synthesis ideas and opportunities for developing the new Pfizer
screening libraries; team member of the Pfizer La Jolla oncology discovery advisory group (project leaders & internal
experts).
Internal Collaborations ADMET; worked closely with biology and pharmacology
colleagues and teams for the advancement of projects and fostered open discussion of the biological results; worked with
upper management to maintain a focus on corporate needs, compound advancement criteria, and critical path discussions.
Microwave-accelerated chemical lead series optimizations, microwave cyclization methods, microwave
nitrations, and novel exploratory microwave chemistry experiments (PersonalChemistry, CEM, Mars, Milestones); made proposals
in supercritical fluid synthetic chemistries; coordinate with computational colleagues to develop pharmacophores and pharmacophore
designed targeted libraries for the GnRH and other projects; contributed to budgets and capital equipment.
LIGAND PHARMACEUTICALS - GLYCOMED INC. (APRIL 1992 - SEPT. 1997, 5.5 YEARS).
Senior Research Scientist and International Project Leader reporting directly to John Musser, Ph.D. Chief
Scientific Officer / Chief Operating Officer. A demonstrated ability to define and drive the vision for scientific growth
and demonstrated the ability to effectively plan, implement, and manage a diverse portfolio of research projects. International Collaborations: Sankyo-Glycomed (Japan-USA) international
collaboration leader and member of the joint collaborative research committee in the discovery of novel agents to treat, cancer,
cell adhesion, inflammation, pulmonary disease, and diseases related to aberrant cell adhesion. Established drug candidate
selection criteria for advanced preclinical and clinical studies. Extensive international collaboration with the Canadian
Alberta Research Council (ARC).
USA Collaborations: Johns Hopkins Asthma and Allergy Center,
Baltimore, MD.; The University of Michigan Medical School Department of Pathology for in vivo lung injuries; The
University of Michigan Medical School Department of Pharmacology for ex vivo and in vivo cardiac ischemia/reperfusion
injuries, rat model of pulmonary Granulomatous Vasculitis, and a new in vitro cell-based membrane attack complex
assay for the selection and research evaluation of selectin inhibitors; The MD Anderson Cancer Center in Houston Texas for
the use of cell adhesion / anti-inflammatory agents in cancer; and finally The University of Michigan at Kalamazoo (cytokine
release related to cell adhesion). Selected experiments were carefully controlled, appropriate, and fully monitored in mice,
rats, rabbit, Guinea Pigs, and some primates. Main therapeutic areas included: Cancer, Asthma, Cardiac Ischemia-Reperfusion
injury, Granulomatous Vasculitis, Inflammation, and Cell Adhesion (E-, L-, and P-Selectins). GM acquired by LGND 1995.
Senior Research Scientist/Project Leader activities included: Find and optimize R&D hit to lead
and lead to potential IND opportunities; patenting agents with specific and dual pharmacophobic activities; utilized de
novo pharmacophore designs; solid-phase (resin) syntheses; discrete parallel methodologies (Advanced ChemTech 496-MOS);
approaches using Chiron Mimotope (PIN) technologies; solid-phase medicinal chemistry directed combinatorial technology (resins
focusing on spatially-addressable systems), and peptidomimetics. Maintain high scientific standards; worked within the established
matrix management and line management systems to supply agents for testing and collaborations. Was responsible for the design,
synthesis and characterization of several novel chemical analogs and series of agents, identified natural products as cell
adhesion inhibitors, developed new molecular hybrids and small molecules to act as glycomimetics of Sialyl Lewisx
and Sialyl Lewisa to inhibit cell adhesions related to disease and cancer; and directly contributed to the developing
patent estates. Developed the structure activity relationships for key chemical series, utilized the data from additional
cell-based cell adhesion assays and drug metabolism data to further develop potential drug candidates. Worked with outside
CROs to perform scale-up modifications for agents that were potential candidates for development consideration. Worked closely
with screening, cell-based assays, and cell-based rolling assay, cancer cell adhesion assay, and in vivo adhesion
model teams to obtain data and discuss the scientific results. Additional work was performed by making novel sulfatoids and
sulfates as sialic acid mimics. Was promoted to Senior Research Scientist from Scientist III (July 1994).
Education Mark Anderson, Mark Brian Anderson UNIVERSITY OF MASSACHUSETTS 2009: Clinical Pathology and Nutritional
Sciences Department. Professor Eugene Rogers, Program Director. Clinical Pathology Certification: Clinical
Pathology combines the theoretical and technical knowledge of human anatomy and physiology, clinical chemistry, genetics,
immunology, microbiology, hematology, histocompatibility, cellular pathology and other fields as they pertain to the clinical
Pathology combines the theoretical and technical knowledge of human anatomy and physiology, clinical chemistry, genetics,
immunology, microbiology, hematology, histocompatibility, cellpathology and other fields as they pertain to the diagnosis,
monitoring and prevention of disease. HARVARD UNIVERSITY DECEMBER
1989 - APRIL 1992: NSF Postdoctoral Research Fellow with Professor Yoshito Kishi.
Department of Chemistry and
Chemical Biology: Palytoxin (PTX) is a complex marine natural product with 71 asymmetric centers isolated from soft coral
and is considered to be one of the most toxic non-peptide substances known second to maitotoxin. Palytoxin targets the sodium-potassium
pump protein via binding and "locking" it in a position allowing passive transport of both the sodium and potassium
ions, thereby destroying the ion gradient that is essential for most cells. Toxicity symptoms are angina-like chest pains,
tachycardia, unstable blood pressure, hemolysis, asthma-like breathing difficulties, and exaggerated T-wave in electreocardiograms
wherein these symptoms are rapid and death usually follows in minutes.
Synthesis and purifications of the synthetic
bioisostere incorporated PTX from the palytoxin carboxylic acid (PTC) derived from the selective hydrolysis of the vinylogous
urea portion of PTX. Specially trained in the handling of PTX and PTC from a former Japanese Prof. Kishi group member.
Synthesis and incorporation of novel vinylogous urea bioisosteres of Palytoxin (PTX) into Palytoxin carboxylic acid
(PTC), and the construction of many Palytoxin model systems. Methods included Kishi's Nickel‑Chromium coupling for the
synthesis of the C‑1 to C‑16 and C‑l to C‑25 Palytoxin model systems, worked on new synthetic building
blocks, and carbon-glycosides. Testing of the novel palytoxin analogs were done at the Harvard University Medical School.
PURDUE UNIVERSITY AUGUST 1984 - DECEMBER 1989: Ph.D., NSF and NIH Graduate Research Associate with
Professor Phil. L. Fuchs "New Methodologies Directed towards the Total Synthesis of Cytochalasins C&D."
The Cytochalasins can be used as chemical "molecular tools" to better understand actin polymerization, cell motility,
ruffling, cell division, contraction, cell stiffness, cytoskeletal movement and other biological processes.
Constructed
many advanced intermediates and novel building blocks employing unique Diels-Alder reactions, an intramolecular chiral acyl
transfer strategy, "tried and true" vinyl sulfone technologies, new cyclopentenylations, anhydrous cerium (III)
chloride methodologies, allylsilanes, "BEST" reagents for nucleophilic and electrophilic mercaptanylations, silicon
and tin.
Teaching Assistant Experience
General Chemistry TA: These courses introduced concepts such
as stoichiometry, prediction of reaction products, thermodynamics, nuclear chemistry, electrochemistry, chemical kinetics,
Conservation of energy, Conservation of mass, Law of constant composition, Gas laws, Solubility, Acid-base chemistry, Chemical
bonding, Chemical equilibria and the basics of physical chemistry.
General Chemistry Laboratory TA: These courses
applied the concepts acquired in the lectures and applied them in a supervised laboratory setting.
Organic Chemistry
(Chemistry for Medicine/Health Care Fields): These courses were focused on those entering the medical and healthcare fields.
Topics introduced the study of organic structures, properties, composition, reactions and preparation (by synthesis or by
other means) of chemical compounds that contain carbon, basic nomenclature and an introduction to compounds that may contain
any number of other elements, including hydrogen, nitrogen, oxygen, the halogens as well as phosphorus, silicon and sulfur.
Organic Chemistry Laboratory TA (Chemistry for Medicine/Health Care Fields): These courses applied the concepts
acquired in the lectures and applied them in a supervised laboratory setting.
Organic Chemistry (Chemistry for
Chemistry Majors): These courses were focused on those majoring in chemistry. Topics include the study of organic structures,
properties, composition, reactions and preparation (by synthesis or by other means) of chemical compounds that contain carbon,
nomenclature, examples that contain any number of other elements, including hydrogen, nitrogen, oxygen, the halogens as well
as phosphorus, silicon and sulfur. The study and application of organic chemistry for medicinal chemistry lie on a continuum,
but individuals with interests in these areas have one thing in common; they seek to understand how chemical structure correlates
with biological activity.
UNIVERSITY OF MINNESOTA AUGUST 1980 - JUNE 1984: B.S. degree in chemistry
with a focus on biochemistry and microbiology. Conducted undergraduate research & thesis (CHM 3499) in the biogenesis
of alkaloids (heterocyclic syntheses and plant chemical biology), the biology of plant natural product syntheses, and secondary
plant metabolites with the late Professor Edward Leete (08Feb1992).
Niacin (vitamin B3 or nicotinic acid), is
a vitamin that prevents the deficiency disease pellagra. However the tetrahydronicotinic acids are also proposed as intermediates
in the biosynthesis of secondary plant metabolites and alkaloids.
Undergraduate Thesis (CHM 3499): "Studies
Directed Toward The Synthesis of 1,2,3,6‑Tetrahydronicotinic Acid and Retronecine for Their Use In Plant Biomimetic
Syntheses", and studies in the biogenesis of alkaloids. Additional studies were on electrode surface modifications with
chemically modified riboflavins for studying the biology and reduction potential of important enzymes with Professor M. T.
Stankovich.
Lakewood Community College/Century College January 1979 - May 1980 main studies in biology and general
credits.
AWARDS:
2011 - R&D Directions Notable People in R&D. Article of one of nine people recognized in
the February issue of "R&D Directions" under Notable People in R&D, page 16 2011. http://www.pharmalive.com/magazines/randd/ Professional Associations: American Chemical Society, New York Academy of Sciences, etc.
Awards:
Agouron Pharmaceuticals "President's Award in Drug Discovery (January 1999).
Strathmore's Who's Who in Leadership
and Achievement (2003).
United Who's Who of Executives and Professionals (2003). Multiple Continuing Education
Certificates (CE).
INTERESTS: Personal interests: Passion of Drug Discovery, love of golf, fishing, sailing, skiing, travel,
languages, art, literature, etc.
Useful Software: MS Word, Front Page, PowerPoint, Adobe, ISIS, Excel, SciFinder,
Spotfire, Pipeline Pilot, Group resource and modeling software Beilstein, ISIS base, Accelrys, Schrodinger, etc. LANGUAGES:
English, German, French, Swedish, Japaneese, Spanish
PATENTS & PATENT APPLICATIONS IN THE PUBLIC DOMAIN
Application number: 12/500,449. Publication number: US 2010/0068197
A1. Filing date: Jul 9, 2009. PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF CELL PROLIFERATION AND THE USE THEREOF. Disclosed
are compounds of Formula I effective as cytotoxic agents. The compounds of this invention are useful in the treatment of a
variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. Inventors: MARK B. ANDERSON,
J. Adam Willardsen, Warren S. Weiner, Kazuyuki Suzuki, Robert J. Halter, In Chul Kim, Matthew Reeder, Ashantai Yungai.
Patent number: 7714022. Filing date: Mar 27, 2008. Issue date: May 11, 2010. Application
number: 12/057,140. PYRROLE DERIVATIVES AS THERAPEUTIC COMPOUNDS. Novel pyrrole derivatives are disclosed as Aβ42-lowering
agents for the treatment and prevention of neurodegenerative disorders characterized by the formation or accumulation of amyloid
plaques comprising the Aβ42 peptide. Inventors: Warren S. Weiner, Rachel M. Slade, Yevgeniya I. Klimova, Ruth J. Walton,
Mark B. Anderson
Application number: 12/574,632. Publication number: US 2010/0093773 A1. Filing
date: Oct 6, 2009. METHODS OF TREATING CANCER. Disclosed is (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride
effective as a vascular disrupting agent. (4-Methoxy-phenyl)-methyl-(2-methyl-quinazolin-4-yl)-amine hydrochloride is useful
in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs, and
in particular to its use in treating cancer. Inventors: MARK LAUGHLIN, Mark B. Anderson, Adam Willardsen, Chris Pleiman.
Application
number: 12/500,863. Publication number: US 2010/0069383 A1. Filing date: Jul 10, 2009. COMPOUNDS AND THERAPEUTICAL USE THEREOF.
Disclosed are 4-arylamino-quinazolines and analogs thereof that are effective as activators of caspases and inducers of apoptosis.
The compounds of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth
and spread of abnormal cells occurs. Inventors: MARK B. ANDERSON, J. Adam Willardsen, Warren S. Weiner, Ashantai Yungai, Robert
J. Halter, Yevgeniya Klimova, Kazuyuki Suzuki, Matthew Reeder.
Application number: 12/719,672. Publication number: US
2010/0184975 A1. Filing date: Mar 8, 2010. The invention provides novel compounds useful for the treatment of neurodegenerative
disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(═O)OH, -L-CH═CHC(═O)OH,
-L-C(═O)NH2, -L-C(═0)NH(C1-3alkyl), -L-C(═O)N(C1-3alkyl)2, etc. Inventors: Rachel Slade, Yevgeniya Klimova,
Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz.
Patent
number: 7595401. Filing date: May 14, 2007. Issue date: Sep 29, 2009. Application number: 11/748,362. THERAPEUTIC COMPOUNDS
AND THEIR USE IN CANCER. The invention relates to compounds of Formula I. Inventors: Ashok C. Bajji, Se-Ho Kim, Benjamin Markovitz,
Richard Trovato, Rajendra Tangallapally, Mark B. Anderson, Daniel Wettstein, Mark Shenderovich, John A. Vanecko.
Application
number: 12/780,828. Publication number: US 2010/0292255 A1. Filing date: May 14, 2010. The invention provides novel therapeutic
compounds, pharmaceutical compositions comprising these compounds, and methods for using these compounds and compositions
to treat diseases and disorders, such as cancer. Inventors: Ashok C. Bajji, Se-Ho Kim, Rajendra Tangallapally, Benjamin J.
Markovitz, Richard Trovato, Mark B. Anderson, Daniel A. Wettstein, Mark D. Shenderovich.
Application number: 12/794,300. Publication number: US
2010/0240630 A1. Filing date: Jun 4, 2010. The invention relates to compounds, pharmaceutical compositions and methods useful
for treating viral infection. Inventors: Dange Vijay KUMAR, Kraig M. Yager, David A. Gerrish, Christophe Hoarau, Mark B. Anderson.
PATENTS:
2009
- WO/2009/065035 BAJJI, Ashok C.; KIM, Se-Ho; TANGALLAPALLY, Rajendra; MARKOVITZ, Benjamin; TROVATO, Richard;
ANDERSON, Mark B.; WETTSTEIN, Daniel; SHENDEROVICH, Mark. Therapeutic Compounds And Their Use In Treating Diseases
And Disorders. The invention provides novel therapeutic compounds, pharmaceutical compositions comprising these compounds,
and methods for using these compounds and compositions to treat diseases and disorders, such as cancer.
2008 - Patent Number: 2008097341 (application serial number US2007/074478) Kraig
M. Yager, In Chul Kim, David Gerrish, Mark B. Anderson. ANTIVIRAL COMPOUNDS AND USE THEREOF. / COMPOSÉS ANTIVIRAUX
ET LEUR UTILISATION. The invention relates to compounds, pharmaceutical compositions and methods useful for treating
viral infection. L'invention concerne des composés, des compositions pharmaceutiques et des procédés
qui s'utilisent pour traiter une infection virale.
2008
- CIP of PCT/US06/000056 Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath; Zhang,
Hong; Suzuki, Kazuyuki. PREPARATION OF SUBSTITUTED QUINAZOLINAMINES AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS.
U.S. Pat. Appl. Publ. (2008), 50pp., Cont.-in-part of Appl. No. PCT/US06/000056. CODEN: USXXCO US 2008004297 A1 20080103 CAN
148:121727 AN 2008:12280. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable,
pharmacokinetics).
2007 - WO 2007095383 Walton, Ruth J.; Slade, Rachel M.; Willardsen, J. Adam; Weiner, Warren S.; Anderson, Mark B..
PRODRUGS OF PH ALKANOIC ACIDS WITH ENHANCED DELIVERY TO THE BRAIN OR ACROSS THE BLOOD-BRAIN-BARRIER FOR TREATMENT
OF DEMENTIA. PCT Int. Appl. (2007), 56pp. CODEN: PIXXD2 WO 2007095383 A2 20070823 CAN 147:285038 AN 2007:941178.
PCT/US2007/004189. Abstract: The invention relates prodrugs of phenyl alkanoic acids. The prodrugs of the invention can enhance
and/or improve delivery of the phenyl alkanoic acid moiety to a desired target tissue. (drug design, drug discovery, blood
brain barrier, SAR, SXR, Alzheimer's, synthesis, bioavailable, drug delivery, pharmacokinetics).
2007 - WO 2007076161 Bajji, Ashok C.;
Kim, Se-Ho; Trovato, Richard; Mchugh, Robert J.; Markovitz, Benjamin; Anderson, Mark B.. PREPARATION OF OXAZOLE DERIVATIVES
AS ANTIVIRAL AGENTS. PCT Int. Appl. (2007), 116pp. CODEN: PIXXD2 WO 2007076161 A2 20070705 CAN 147:143467 AN 2007:729694.
PCT/US2006/049558. Abstract: Methods and pharmaceutical compositions for treating and/or delaying the onset of viral infection
are provided. The pharmaceutical compositions include compounds having an oxazole core. Additionally, the compositions can
be used to treat cardiovascular disorders and cancer. (drug design, drug discovery, SAR, SXR, HIV, antiviral, synthesis).
2007 - WO 2007002411, CA 2609280 Arranz
Plaza, Esther; Yager, Kraig M.; Gerrish, David Allen; Anderson, Mark B.; Kim, In Chul; Kumar, Dange Vijay. ANTIVIRAL
COMPOUNDS. . International Application Number: PCT/US2006/024493. PCT Int. Appl. (2007), 91pp. CODEN:
PIXXD2 WO 2007002411 A1 20070104 CAN 146:100898 AN 2007:14669. 04.01.2007 C07J 53/00 PCT/US2006/024493 MYRIAD GENETICS, INC.
The invention relates to compounds, pharmaceutical compositions and methods useful for treating viral infection. (drug design,
drug discovery, SAR, SXR, HIV, antiviral, synthesis).
2007 -
US 20070299258, WO 2007134298 Bajji, Ashok C.; Kim, Se-Ho; Markovitz,
Benjamin; Trovato, Richard; Tangallapally, Rajendra; Anderson, Mark B.; Wettstein, Daniel; Shenderovich, Mark; Vanecko, John
A. PREPARATION OF SUBSTITUTED PURINAMINES AS ANTITUMOR AGENTS. PCT Int. Appl. (2007), 477pp. CODEN: PIXXD2
WO 2007134298 A2 20071122 CAN 148:11252 AN 2007:1332992. PCT/US2007/068899. Abstract: Compounds of the formula (I) (II) (III)
in which A is chosen from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group. B is chosen
from a substituted or unsubstituted aryl, heteroaryl, heterocyclic, or carbocyclic group Rl is chosen from hydro, alkyl, aryl,
heteroaryl, amino, halo, sulfur, and thioalkyl. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor,
synthesis, purine, pharmacokinetics, ADME).
2007 - WO 2007038684,
CA 2623558, PCT/US2006/037903 Weiner, Warren S.; Slade,
Rachel M.; Klimova, Yevgeniya I.; Walton, Ruth J.; Anderson, Mark B.. PYRROLE DERIVATIVES AS THERAPEUTIC COMPOUNDS.
PYRROLE DERIVATIVES AS AMYLOID BETA 42-LOWERING AGENTS, THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS, AND USE IN THERAPY.
PCT Int. Appl. (2007), 84pp. CODEN: PIXXD2 WO 2007038684 A2 20070405 CAN 146:379817 AN 2007:384648. PCT/US2006/037903. Abstract:
Novel pyrrole derivatives are disclosed as Aβ42-lowering agents for the treatment and prevention of neurodegenerative
disorders characterized by the formation or accumulation of amyloid plaques comprising the Aβ42 peptide. (drug design,
drug discovery, blood brain barrier, SAR, SXR, Alzheimer's, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics,
ADME).
2006 - WO 2006135383 Bajji, Ashok; Morham, Scott; Anderson, Mark B.; McHugh, Robert J.; Trovato, Richard; Weiner, Warren S.; Kim,
Se-Ho. INDAZOLES: PREPARATION OF INDAZOLES FOR TREATING VIRAL INFECTION AND OTHER DISEASES MEDIATED
BY RHO KINASE. PCT Int. Appl. (2006), 221pp. CODEN: PIXXD2 WO 2006135383 A2 20061221 CAN 146:62713 AN 2006:1338316.
PCT/US2005/027730. Abstract: Methods and pharmaceutical compositions for treating and/or delaying the onset of viral infection
are provided. The pharmaceutical compositions include compounds having an indazole core. Additionally, the compositions can
be used to treat cardiovascular disorders and cancer. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics,
pharmacodynamics, ADME).
2006 - WO 2006074223, CA 2593005 Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Jiang, Songchun;
Halter, Robert J.; Slade, Rachel; Klimova, Yevgeniya. PHARMACEUTICAL COMPOUNDS AS ACTIVATORS OF CASPASES AND INDUCERS
OF APOPTOSIS AND THE USE THEREOF. International Application Number: PCT/US2006/000176. PCT Int. Appl. (2006), 97
pp. CODEN: PIXXD2 WO 2006074223 A2 20060713 CAN 145:145755 AN 2006:676927. Disclosed are 1-arylamino-phthalazines, 4-arylamino-benzo[d][1,2,3]triazines,
and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful
in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. (drug
design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, ADME).
2006 - US 20080051398, WO 2006074187, CA 2592971 Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath. METHOD OF TREATING
BRAIN CANCER. International Application Number: PCT/US2006/000122. PCT Int. Appl. (2006), 90 pp. CODEN: PIXXD2 WO
2006074187 A2 20060713 CAN 145:145733 AN 2006:675266. 13.07.2006 A61K 39/395 PCT/US2006/000122 MYRIAD GENETICS, INC. Disclosed
are 4-arylamino-quinazolines and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds
of this invention are useful in the treatment of a variety of clinical conditions in which uncontrolled growth and spread
of abnormal cells occurs, and in particular to the use of these compounds in treating brain cancer. http://www.freepatentsonline.com/y2008/0051398.html (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, pharmacokinetics,
pharmacodynamics, ADME).
2006 - WO 2006074147, CA 2592900 Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam; Sirisoma, Nilantha
Sudath; Zhang, Hong; Suzuki, Kazuyuki. NITROGEN CONTAINING BICYCLIC COMPOUNDS AND THERAPEUTICAL USE THEREOF.
International Application Number: PCT/US2006/000056. 13.07.2006 C07D 401/00 MYRIAD GENETICS, INC. Disclosed are 4-arylamino-quinazolines
and analogs thereof effective as activators of caspases and inducers of apoptosis. The compounds of this invention are useful
in the treatment of a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs. (drug
design, drug discovery, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics).
2006 - WO 2006074147 Cai, Sui Xiong; Anderson,
Mark B.; Willardsen, Adam; Sirisoma, Nilantha Sudath; Zhang, Hong; Suzuki, Kazuyuki. PREPARATION OF 4-ARYLAMINO-QUINAZOLINES
AND THEIR ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS OF APOPTOSIS. PCT Int. Appl. (2006), 133 pp. CODEN: PIXXD2
WO 2006074147 A2 20060713 CAN 145:145736 AN 2006:678591. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis,
oral, bioavailable, pharmacokinetics).
2006 - WO 2006041874,
CA 2582674, PCT/US2005/035747 Slade, Rachel; Klimova, Yevgeniya;
Halter, Robert J.; Yungai, Ashantai J.; Weiner, Warren S.; Walton, Ruth J.; Willardsen, Jon Adam; Anderson, Mark B.; Zavitz,
Kenton. COMPOUNDS FOR ALZHEIMER'S DISEASE. International Application Number: PCT/US2005/035747. PCT Int.
Appl. (2006), 300 pp. CODEN: PIXXD2 WO 2006041874 A2 20060420 CAN 144:412361 AN 2006:361235. 20.04.2006 C07D 209/04 MYRIAD
GENETICS, INC. (drug design, drug discovery, blood brain barrier, SAR, SXR, Alzheimer's, synthesis, pharmacokinetics, pharmacodynamics,
ADME).
2006 - US 7101878, WO 20040010033 (2004), WO00/20358 Anderson, Mark Brian; Vazir, Haresh N.; Luthin, David Robert; Paderes,
Genevieve Deguzman; Pathak, Ved P.; Christie, Lance Christopher; Hong, Yufeng; Tompkins, Eileen Valenzuela; Li, Haitao; Faust,
James. NON-PEPTIDE GNRH AGENTS, METHODS AND INTERMEDIATES FOR THEIR PREPARATION. PCT/US2007/068899. Also
see Appl. No. 9/763,216. PCT Filed Aug. 20, 1999, PCT No. PCT/US99/18790 § 371(c)(1), (2), (4) Date Feb. 20, 2001, PCT
Pub. No. WO00/20358, PCT Pub. Date Apr. 13, 2000. Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing
hormone are described. Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites
are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating
fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates
useful in their preparation are also described. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor,
synthesis, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2006
- WO 2006074187 Cai, Sui Xiong; Anderson, Mark B.; Willardsen, Adam;
Sirisoma, Nilantha Sudath. PREPARATION OF 4-ARYLAMINO-QUINAZOLINES AND ANALOGS AS ACTIVATORS OF CASPASES AND INDUCERS
OF APOPTOSIS. PCT Int. Appl. (2006), 90 pp. CODEN: PIXXD2 WO 2006074187 A2 20060713 CAN 145:145733 AN 2006:675266.
(drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics,
pharmacodynamics, ADME).
2005 - WO 20050250846, USPTO Application:
20050250846 Mark B. Anderson, Lance Christopher Christie, Quyen-Quyen
Thuy Do, Yufeng Hong, Haitao Li, Ranjan Jagath Rajapakse, Eric T. Sun, Eileen Valenzuela Tompkins, Jun Feng, Ved P. Pathak.
USPTO Application #: 20050250846. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE.
Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds
and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive
disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release
is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described. (drug
design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics,
ADME).
2005 - US 6903132 Anderson, Mark B.; Christie,
Lance Christopher; Do, Quyen-Quyen Thuy; Feng, Jun; Hong, Yufeng; Li, Haitao; Pathak, Ved P.; Rajapakse, Ranjan Jagath; Sun,
Eric T.; Tompkins, Eileen Valenzuela. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE.
Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are described. Such compounds
and their pharmaceutically acceptable salts, prodrugs, and active metabolites are suitable for treating mammalian reproductive
disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the
compounds and intermediates useful in their preparation are also described. (drug design, drug discovery, blood brain barrier,
SAR, SXR, prodrugs, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2004 - US 20040053951 Christie, Lance C.; Anderson, Mark B.; Feng, Jun;
Hong, Yufeng; Pathak, Ved P.; Rajapakse, Ranjan J.; Tompkins, Eileen V.; Vazir, Haresh; Li, Haitao. NON-PEPTIDE GNRH
AGENTS, PHARMACEUTICAL COMPOSITIONS, AND METHODS FOR THEIR USE. Pfizer Inc. No. 10364193 filed on 02/11/2003. Abstract:
Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are described. Such agents are useful for
treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where
suppression of gonadotropin release is indicated. United States Application 20040053951 A1. (drug design, drug discovery,
SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, pharmacodynamics, ADME).
2004
- US 20040014787 Mark B. Anderson; Lance Christopher Christie, Ballwin; Quyen-Quyen Thuy Do; Jun Feng; Yufeng
Hong, San; Haitao Li, San Diego; Ved P. Pathak, San Diego; Ranjan Jagath Rajapakse; Eric T. Sun, San; Eileen Valenzuela Tompkins.
US 20040014787A1. 2004/0014787 Al. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR USE.
Agouron Pharmaceuticals, Inc. Appl. No.: 10/459,364. Filed: Jun. 11, 2003 Related U.S. Application Data. Provisional
application No. 60/388,788, filed on Jun. 13, 2002. Abstract: Non-peptide GnRH agents capable of inhibiting the effect of
gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, pro- drugs, and
active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone- dependent tumors as well
as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds
and intermediates useful in their preparation are also described. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis,
oral, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2004
- US 6833372 Christie, Lance C.; Anderson, Mark B.; Feng, Jun; Hong, Yufeng; Pathak, Ved P.; Rajapakse, Ranjan
J.; Tompkins, Eileen V.; Vazir, Haresh; Li, Haitao. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS, AND METHODS
FOR THEIR USE. Pfizer Inc. No. 10364193 filed on 02/11/2003 Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing
hormone are described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent
tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. (drug design, drug discovery,
SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, ADME).
2003
- WO 2003106446, CA 2489252 Anderson, Mark Brian; Christie, Lance
Christopher; Do, Quyen-Quyen Thuy; Feng, Jun; Hong, Yufeng; Li, Haitao; Pathak, Ved Prakash; Rajapakse, Ranjan Jagath; Sun,
Eric Tak On; Tompkins, Eileen Valenzuela. NON-PEPTIDE GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THEIR
USE. (PREPARATION OF FURANCARBONYLHYDRAZINES AS INHIBITORS OF GONADOTROPIN-RELEASING HORMONE.) 24.12.2003
A61K 31/341 PCT/IB2003/002379 PFIZER INC. PCT Int. Appl. (2003), 115 pp. CODEN: PIXXD2 WO 2003106446 A1 20031224 CAN 140:42021
AN 2003:1006973. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.
(drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, prodrugs, pharmacokinetics, pharmacodynamics,
active metabolites, ADME).
2003 - WO 2003068769, CA 2418712 Christie, Lance; Anderson, Mark, Brian; Feng, Jun; Hong, Yufeng; Pathak,
Ved, Prakash; Rajapakse, Ranjan, Jagath; Tompkins, Eileen, Valenzuela; Vazir, Haresh; Li, Haitao. NON-PEPTIDE COMPOUNDS
AFFECTING THE ACTION OF GONADOTROPIN-RELEASING HORMONE (GNRH). International Application Number: 21.08.2003 C07D
405/12 PCT/IB2003/000316 PFIZER INC. Non-peptide GnRH agents that inhibit the effect of gonadotropin-releasing hormone are
described. Such agents are useful for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well
as for regulating fertility, where suppression of gonadotropin release is indicated. The compound have the following structure:
(Formula I). Canadian Patent (CA) of US 6833372. (CA 2418712) Non-peptide gnrh agents, pharmaceutical compositions, and methods for their
use|Agents et compositions pharmaceutiques non peptidiques anti-gnrh et methodes d'utilisation. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, pharmacodynamics,
ADME).
2003 - US 6670167, US 20030235899 (2003) EP 1096014 (2001)
Chen, Ping; Anderson, Mark; Deng, Ya-Li; Gaur, Smita; Kan, Chen Chen; Luo, Chun; Lundgren, Karen; Margosiak,
Stephen; Nguyen, Binh; O'Connor, Patrick; Register, James; Russell, Anna Tempczyk; Sarup, Jay. CATALYTIC DOMAIN OF THE HUMAN EFFECTOR CELL CYCLE CHECKPOINT PROTEIN
KINASE CHK1 MATERIALS AND METHODS FOR IDENTIFICATION OF INHIBITORS THEREOF The present invention relates to the identification, isolation and purification of the
catalytic domain of the human effector checkpoint protein kinase (hChk1). A 1.7Å crystal structure of the hChk1 kinase
domain in the active conformation is reported herein. The kinase domain of hChk1 and its associated crystal structure is described
for use in the discovery, identification and characterization of inhibitors of hChk1. This structure provides a three-dimensional
description of the binding site of the hChk1 for structure-based design of small molecule inhibitors thereof as therapeutic
agents. Inhibitors of hChk1 find utility in the treatment of hyperproliferative disorders such as HIV and cancer. http://www.wikipatents.com/6670167.html
(drug design, drug discovery, SAR, SXR, cancer, tumor, crystal structure, kinase).
2003 - US 6646137 Anderson, Mark Brian; Polinsky, Alexander; Hong, Yufeng; Gregor,
Vlad Edward. NON-PEPTIDE GNRH AGENTS. Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing
hormone are of the following general formula, where X1, X2, Y, and Z are defined variables: STR1 Such compounds and their
pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive
disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release
is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described. (drug
design, drug discovery, SAR, SXR, prodrugs, cancer, tumor, synthesis, pharmacokinetics, pharmacodynamics, ADME).
2003 - EP 1334972 Anderson, Mark
B.; Christie, Lance C.; Feng, Jun; Hong, Yufeng; Li, Haitao; Pathak, Ved P.; Rajapakse, Ranjan; Tompkins, Eileen; Vazir, Haresh
N. PREPARATION OF NON-PEPTIDE COMPOUNDS AFFECTING THE ACTION OF GONADOTROPIN-RELEASING HORMONE (GNRH). International
Application Number: Eur. Pat. Appl. (2003), 1 p. CODEN: EPXXDW EP 1334972 A1 20030813 CAN 139:179968 AN 2003:626431. (drug
design, drug discovery, SAR, SXR, cancer, tumor, synthesis).
2002
- WO 2002098363, CA 2449843 Sun, Eric T.; Anderson, Mark B.; Anderes,
Kenna L.; Christie, Lance C.; Do, Quyen-Quyen T.; Feng, Jun; Goetzen, Thomas; Hong, Yufeng; Iatsimirskaia, Eugenia A.; Li,
Haitao; Luthin, David R.; Paderes, Genevieve D.; Pathak, Ved P.; Rajapakse, Ranjan Jagath; Shackelford, Scott; Tompkins, Eileen
Valenzuela; Truesdale, Larry K.; Vazir, Haresh. NON-PEPTIDE FURANYL GNRH AGENTS, PHARMACEUTICAL COMPOSITIONS AND METHODS
FOR THEIR USE, AND PROCESSES FOR PREPARING THEM AND THEIR INTERMEDIATES. PCT Int. Appl. (2002), 243 pp. CODEN: PIXXD2
WO 2002098363 A2 20021212 CAN 138:24635 AN 2002:946059. PCT/US2002/017846. Abstract: Non-peptide GnRH agents capable of inhibiting
the effect of gonadotropin-releasing hormone are described. Such compounds and their pharmaceutically acceptable salts, prodrugs,
and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as
well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds
and intermediates useful in their preparation are also described. (drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis,
pharmacokinetics, pharmacodynamics, ADME).
2001 - US 6218426 (2001), WO 1999/044987 (1999) Anderson, Mark; Polinsky, Alexander;
Hong, Yufeng; Gregor, Vlad. NON-PEPTIDE GnRH AGENTS 10.09.1999 C07C 279/12 PCT/US1999/004457. PCT Int. Appl.
(1999), 90 pp. CODEN: PIXXD2 WO 9944987 A1 19990910 EP1068178, WO09944987. CA2322444 CAN 131:214183 AN 1999:576906
AGOURON PHARMACEUTICALS, INC. Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are
of general formula (I), where X1, X2, Y, and Z are defined variables. Such compounds and their pharmaceutically acceptable
salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid
hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods
for synthesizing the compounds and intermediates useful in their preparation are also described. (SAR, SXR, synthesis).
2000 - US 7101878, WO 2000020358, EP1105120 (2000), WO 0020358 (2000) Anderson, Mark Brian; Vazir, Haresh N.; Luthin, David Robert; Paderes, Genevieve Deguzman; Pathak,
Ved P.; Christie, Lance Christopher; Hong, Yufeng; Tompkins, Eileen Valenzuela; Li, Haitao; Faust, James. NON-PEPTIDE
GNRH AGENTS, METHODS AND INTERMEDIATES FOR THEIR PREPARATION. PCT Int. Appl. (2000), 444 pp. CODEN: PIXXD2 WO 2000020358
A2 20000413 CAN 132:279106 AN 2000:241135. (drug design, drug discovery, synthesis, SAR, SXR).
1999 - WO 9929705 Anderson, Mark B.;
Kobayashi, Yoshiyuki; Itoh, Kazuhiro; Holme, Kevin R.; Cui, Jingrong; Fugedi, Peter; Peto, Csaba F.; Wang, Li; Vazir, Harish.
PREPARATION OF SIALYL LEWISX AND SIALYL LEWISA GLYCO-MIMETICS AS SELECTIN INHIBITORS. PCT Int. Appl. (1999),
184 pp. CODEN: PIXXD2 WO 9929705 A2 19990617 CAN 131:45047 AN 1999:390408. (drug design, drug discovery, synthesis, SAR, SXR).
1999 - WO 9944987 Anderson,
Mark; Polinsky, Alexander; Hong, Yufeng; Gregor, Vlad. PREPARATION OF N-(HETERO)AROYL-N-(GUANIDINOMETHYLARYLMETHYL)-N-[(POLY)CYCLYLMETHYL)]AMINES
AS NON-PEPTIDE GONADOTROPIN RELEASING HORMONE INHIBITORS. PCT Int. Appl. (1999), 90 pp. CODEN: PIXXD2 WO 9944987
A1 19990910 CAN 131:214183 AN 1999:576906. (drug design, drug discovery, synthesis, SAR, SXR).
1999 - WO 9929706 Anderson, Mark B.;
Levy, Daniel E.; Holme, Kevin R. PREPARATION OF DISALICYLATE ANALOG BASED SIALYL LEWISX MIMETICS AS ANTIINFLAMMATORY
AGENTS AND SELECTIN RECEPTORS. PCT Int. Appl. (1999), 104 pp. CODEN: PIXXD2 WO 9929706 A2 19990617 CAN 131:45048
AN 1999:390409. (drug design, drug discovery, synthesis, SAR, SXR).
1999
- US 6218426, EP1068178, WO09944987, CA2322444 US Patent 6,218,426
M. B. Anderson, A. Polinsky, Y. Hong, Vlad. E. Gregor. NON-PEPTIDE GNRH AGENTS. EP1068178, WO09944987. CA2322444.
(drug design, drug discovery, synthesis, SAR, SXR).
1998 - US
CIP of US 5837689 Anderson, Mark B.; Levy, Daniel E.; Tang, Peng Cho;
Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWIS-X MIMETICS CONTAINING NAPHTHYL BACKBONES AS SELECTIN
INHIBITORS. U.S. (1998), 48 pp., Cont.-in-part of U. S. Ser. No. 446,185. CODEN: USXXAM US 5837689 A 19981117 CAN
130:14166 AN 1998:752223. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - US CIP of US 5789385 Anderson, Mark
B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga; Cui, Jing Rong. PREPARATION OF SIALYL LEWIS
X MIMETICS CONTAINING PHENYL BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 55 pp. Cont.-in-part of U.S. Ser. No.
446,185. US 5789385 A 19980804 CAN 129:161815 AN 1998:534879. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - US 5837690 B. N. Narasinga Rao, M.B. Anderson, and J. H. Musser. DERIVATIVES OF TRITERPENOID
ACIDS AND USES THEREOF. International Patents: AU6529194. Abstract: Derivatives of triterpenoid acids and
uses thereof.: United States Patent 5837690 Abstract: Triterpenoid acid derivatives are described that exhibit dual pharmacophobic
activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and that thus have significant
applications for the treatment or prevention of certain diseases including cancer and diseases associated with the inflammatory
process as well as applications for the diagnosis of disease. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - US 5837689 M. B. Anderson, D. Levy,
P. Tang, J. H. Musser, B. N. N. Rao, SIALYL LEWIS-X MIMETICS CONTAINING NAPHTHYL BACKBONES. International
Patents: AU2137297, WO9731006. Abstract: Sialyl lewis-x mimetics containing naphthyl backbones: United States Patent 5837689
(drug design, drug discovery, synthesis, SAR, SXR).
1998 - US 5789385, WO 9730984 (1997) M. B. Anderson, D. Levy, P. Tang, J. H. Musser,
B. N. N. Rao, J. Cui, SIALYL LEWISX MIMETICS CONTAINING PHENYL BACKBONES. AU2136597, WO9730984.
(drug design, drug discovery, synthesis, SAR, SXR). 1997 - WO 9730984 (drug design, drug discovery, synthesis, SAR, SXR).
1998 - US 5763582 B. N. Narasinga Rao, M.B. Anderson, and J. H. Musser. DERIVATIVES OF TRITERPENE
ACIDS AND USES THEREOF. Abstract: Triterpenoid acid derivatives are described that
exhibit dual pharmacophobic activities, specifically selectin ligand and leukotriene biosynthetic inhibitory activities, and
that thus have significant applications for the treatment or prevention of certain diseases including cancer and diseases
associated with the inflammatory process as well as applications for the diagnosis of disease. (drug design, drug discovery,
synthesis, SAR, SXR).
1998 - U.S. (1998), 48 pp., Cont.-in-part
of U. S. Ser. No. 446,185. US 5837689 Anderson, Mark B.; Levy, Daniel
E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWISX MIMETICS CONTAINING NAPHTHYL
BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 48 pp., Cont.-in-part of U. S. Ser. No. 446,185. US 5837689 A 19981117
CAN 130:14166 AN 1998:752223. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - CIP of US 5837689 Anderson, Mark
B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWIS-X MIMETICS CONTAINING
NAPHTHYL BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 48 pp., Cont.-in-part of U. S. Ser. No. 446,185. CODEN: USXXAM
US 5837689 A 19981117 CAN 130:14166 AN 1998:752223. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - CIP of US 5789385 Anderson,
Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga; Cui, Jing Rong. PREPARATION OF SIALYL LEWISX
MIMETICS CONTAINING PHENYL BACKBONES AS SELECTIN INHIBITORS. U.S. (1998), 55 pp., Cont.-in-part of U.S. Ser. No.
446,185. CODEN: USXXAM US 5789385 A 19980804 CAN 129:161815 AN 1998:534879. (drug design, drug discovery, synthesis, SAR,
SXR).
1997 - WO 9731007, AU1975297 Anderson, Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION
OF SIALYL LEWISX MIMETICS CONTAINING FLAVANOID BACKBONES AS SELECTIN INHIBITORS. PCT Int. Appl. (1997), 160 pp. CODEN:
PIXXD2 WO 9731007 A1 19970828 CAN 127:248358 AN 1997:579729. (drug design, drug discovery, synthesis, SAR, SXR).
1997 - WO 9731006 Anderson,
Mark B.; Levy, Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWISX MIMETICS CONTAINING
NAPHTHYL BACKBONES AS SELECTIN INHIBITORS. PCT Int. Appl. (1997), 178 pp. CODEN: PIXXD2 WO 9731006 A1 19970828 CAN
127:248357 AN 1997:579728. (drug design, drug discovery, synthesis, SAR, SXR).
1997 - WO 9731007 Anderson, Mark B.; Levy,
Daniel E.; Tang, Peng Cho; Musser, John H.; Rao, Narasinga. PREPARATION OF SIALYL LEWISX MIMETICS CONTAINING FLAVANOID
BACKBONES AS SELECTIN INHIBITORS. PCT Int. Appl. (1997), 160 pp. CODEN: PIXXD2 WO 9731007 A1 19970828 CAN 127:248358
AN 1997:579729. (drug design, drug discovery, synthesis, SAR, SXR).
1997
- US 5695738 M.B. Anderson and J. H. Musser, STEROIDAL C-GLYCOSIDES.
Glycomed Incorporated U.S. (1997), 20 pp. US 5695738 A 19971209 CAN 128:75635 AN 1997:803505. Abstract: Compositions of sterodial
glycosides are described wherein the glycoside is linked directly, or indirectly to a desired steroidal compound via a carbon,
or similar stable linkage, and methods of using the compositions to treat patients by binding to and/or blocking cellular
receptors for a variety of diseases including cancer, inflammation, and autoimmune diseases. (drug design, drug discovery,
synthesis, SAR, SXR).
1997 - US 5688922 B.N. Narasinga Rao, M. B. Anderson, and J. H. Musser. Substituted
Fucopyranosides. SUBSTITUTED FUCOPYRANOSIDES 2-Chloromethyl-3-(tri-O-benzyl-α-L-C-fucopyranoside)-1-propene and methods of making
the same are described. Methods of combining this substituted fucopyranose with triterpenoid acid also are described. (drug
design, drug discovery, synthesis, SAR, SXR).
1997 - US 5679644 B.N. Narasinga Rao, M. B. Anderson, and J. H. Musser. METHODS OF TREATING DISEASES USING TRITERPENOID ACID
DERIVATIVES. (Triterpenoid acid derivatives, dual pharmacophobic activities, selectin ligand and leukotriene biosynthetic
inhibitory activities, cancer, diseases associated with the inflammatory process, diagnosis of disease, drug design, drug
discovery, synthesis, SAR, SXR, inflammation).
1997 - US 5643884 Anderson, Mark Brian; Musser, John Henry. LUPANE TRITERPENOID
DERIVATIVES. PCT Int. Appl. (1995), 42 pp. CODEN: PIXXD2 WO 9504526 A1 19950216 CAN 122:256432 AN 1995:516374, AU7520594,
CA2169291, EP0714291, WO9504526.US Patent Issued on July 1, 1997, United States Patent 5643884 (drug design, drug discovery, synthesis, SAR, SXR, HIV,
antiviral, cancer, tumor).
1997 - US 5624909 B.N. Narasinga Rao, M. B. Anderson, J. J. Nalway, and J. H. Musser. DERIVATIVES OF TRITERPENE
ACIDS AS INHIBITORS OF CELL ADHESION MOLECULES ELAM-1 (E-SELECTIN) AND LECAM-1 (L-SELECTIN). Abstract: Derivatives
of triterpenoid acids as inhibitors of cell-adhesion molecules ELAM-1 (e-selectin) and LECAM-1 (l-selectin): United States
Patent 5624909 (Triterpenoid acid derivatives, dual pharmacophobic activities, selectin ligand and leukotriene biosynthetic
inhibitory activities, cancer, diseases associated with the inflammatory process, diagnosis of disease, drug design, drug
discovery, synthesis, SAR, SXR, inflammation).
1996 - WO 9636627
Anderson, Mark Brian; Musser, John H. PROCESS FOR THE PREPARATION
OF ACTIVATED GLYCOMIMETIC C-GLYCOSIDES AS SELECTIN INHIBITORS. PCT Int. Appl. (1996), 132 pp. CODEN: PIXXD2 WO 9636627
A1 19961121 CAN 126:89699 AN 1997:51546. (drug design, drug discovery, synthesis, SAR).
1996 - US
5527890, CA 2160370, EP 0693079, AU 6529194, WO 9424145 M.B.
Anderson, B. N. Narasinga Rao, and J. H. Musser. DERIVATIVES OF TRITERPENE ACIDS AND USES THEREOF. International
Patents: CA2160370, EP0693079, AU6529194, WO9424145. United States Patent 5527890 (Triterpenoid acid derivatives, dual
pharmacophobic activities, selectin ligand and leukotriene biosynthetic inhibitory activities, cancer, diseases associated
with the inflammatory process, diagnosis of disease, drug design, drug discovery, synthesis, SAR, SXR, inflammation).
1996 - US 5519008, AU 5160093, AU 675085,
EP 0691813, AU 675085, WO 9405152 B.N. Narasinga Rao, M. B. Anderson, J. J. Nalway, and J. H. Musser. DERIVATIVES
OF TRITERPENE ACIDS AS INHIBITORS OF CELL ADHESION MOLECULES ELAM-1 (E-SELECTIN) AND LECAM-1 (L-SELECTIN). International
Patents: AU5160093, AU675085, EP0691813, AU675085, WO9405152. United States Patent 5519008 Abstract: Triterpenoid acid
derivatives have been found to have structures similar to natural ligands to the extent that these derivatives bind to natural
selectin receptors including endothelial leukocyte adhesion molecule-1 (ELAM-1) and leukocyte/endothelial cell adhesion molecule-1
(LECAM-1). The molecules can be administered to the patients by themselves or in pharmaceutical formulations; in order to
alleviate inflammation and/or treat other abnormalities associated with the excessive binding of leukocytes to endothelial
receptors. (drug design, drug discovery, synthesis, SAR, SXR).
1996
- CA 2221589, AU 5855296, EP 0828729, WO 9636627 CA2221589, AU5855296,
EP0828729, WO9636627: COLLECTION OF ACTIVATED GLYCOSIDE COMPOUNDS AND THEIR BIOLOGICAL USE. Anderson, Mark
Brian and Musser, John H. US patent pending. (drug design, drug discovery).
1995 - WO 9504526 Anderson, Mark Brian; Musser,
John Henry. LUPANE TRITERPENOID DERIVATIVES. PCT Int. Appl. (1995), 42 pp. CODEN: PIXXD2 WO 9504526 A1 19950216
CAN 122:256432 AN 1995:516374. (drug design, drug discovery, synthesis, SAR).
1994 - WO 9424145 Rao, Narasinga; Anderson,
Mark Brian; Musser, John Henry. PREPARATION OF GLYCYRRHETINIC ACID DERIVATIVES AS SELECTIN LIGANDS AND LEUKOTRIENE
BIOSYNTHESIS INHIBITORS. PCT Int. Appl. (1994), 49 pp. CODEN: PIXXD2 WO 9424145 A1 19941027 CAN 122:240077 AN 1995:468527.
(drug design, drug discovery, synthesis, SAR, SXR).
1994 - WO
9405152 Rao, Narasinga; Anderson, Mark Brian; Naleway, John J.; Musser,
John Henry. DERIVATIVES OF TRITERPENOID ACIDS AS INHIBITORS OF CELL-ADHESION MOLECULES ELAM-1 (E-SELECTIN) AND LECAM-1
(L-SELECTIN). PCT Int. Appl. (1994), 77 pp. WO 9405152 A1 19940317 CAN 120:315817 AN 1994:315817. (drug design, drug
discovery, synthesis, SAR, SXR).
PUBLICATIONS & REVIEWS 2011 NVC-422 topical gel for the treatment of impetigo. Susan M. Iovino, Kenneth D. Krantz ,
Daisy M. Blanco, Josefina A. Fernández, Naomi Ocampo, Azar Najafi, Bahram Memarzadeh, Chris Celeri, Dmitri Debabov,
Behzad Khosrovi, and Mark Anderson*. Int J Clin Exp Pathol 2011;4(6):xxx-xxx. Received June 8, 2011; accepted July 19, 2011;
Epub July, 2011, published July, 2011 (IJCEP1106003). In press in http://www.ijcep.com/Forthcomings.html
2011
Bioorganic & Medicinal Chemistry Letters. Timothy P. Shiau, Eric D. Turtle, Charles Francavilla, Nichole J. Alvarez, Meghan
Zuck, Lisa Friedman, Donogh J. R. O’Mahony, Eddy Low, Mark B. Anderson, Ramin (Ron) Najafi, Rakesh K. Jain; Novel 3-chlorooxazolidin-2-ones as antimicrobial agents.Bioorganic & Medicinal Chemistry Letters 2011; (21) 3025-3028.
2011 Bioorganic & Medicinal Chemistry Letters. Eddy Low, Bum Kim, Charles Francavilla, Timothy P. Shiau,
Eric D. Turtle, Donogh J. R. O’Mahony,Nichole Alvarez, Ashley Houchin, Ping Xu, Meghan Zuck, Chris Celeri, Mark B. Anderson,Ramin
(Ron) Najafi, Rakesh K. Jain. Structure stability/activity relationships of sulfone stabilizedN,N-dichloroamines . Bioorganic & Medicinal Chemistry Letters 2011; (21) 3682-3685.
2011 Bioorganic &
Medicinal Chemistry Letters . Charles Francavilla, Eric D. Turtle, Bum Kim, Donogh J. R. O’Mahony, Timothy P. Shiau,
Eddy Low, Nichole J. Alvarez, Chris E. Celeri, Louisa D’Lima, Lisa C. Friedman, Francis S. Ruado, Ping Xu, Meghan E.
Zuck, Mark B. Anderson, Ramin (Ron) Najafi, Rakesh K. Jain; Novel N-chloroheterocyclic antimicrobials. Bioorganic & Medicinal Chemistry Letters 2011; (21) 3029-3033.
2011 - 3rd Anti
Infectives Summit Q & A Online Interview. January 24 - 26, 2011, The Westin Philadelphia, PA. 2011 WHS/SAWC-NeutroPhase® with Sorbact® Dramatically Enhances the Speed of Wound Healing.
John R. Crew, MD, Randell Varilla, RN, MSN, Allan Rocas III, RN, BSN, CWCN, Lu Wang, PhD, Dmitri Debabov, PhD, Ron Najafi,
PhD, Mark Anderson PhD. Wound Care Center, Seton Medical Center, 1900 Sullivan Avenue, Daly City, CA 94015; and NovaBay Pharmaceuticals,
Inc. 5980 Horton Street, Suite 550, Emeryville, CA 94608.
2011 ARVO- Aganocide®Compounds Effective Against
Ophthalmic Pathogens. K.Najafi, A. Jekle, D. Debabov, S. Wilmarth, R. Jain, C. Celeri, M. Zuck, T. Shiau, C. Francavilla,
E. Low and M. Anderson. Ophthalmology, Eye Institute of Marin, San Rafael, CA; and NovaBay Pharmaceuticals, Inc., Emeryville,
CA 94608.
2011 Simon Conference-NVC-422
Prevents Urinary Catheter Blockage and Encrustation. S. A. Rani, C. Celeri, L. Friedman, D. Debabov, R. Najafi, M. Anderson.
NovaBay Pharmaceuticals, Inc., Emeryville, CA 94608.
2010 - Scientific American Magazine: Nice
Germs Finish Last: "Good Samaritan" Bacteria Provide New Clues in Antibiotic Resistance Resistant. Bacteria help their kin survive antibiotics,
but at a cost. By Melinda Wenner Moyer. November 2, 2010. The findings could spur scientists to develop better antibiotics.
If indole allows pathogenic bacteria to withstand antibiotics, it may be possible to thwart drug resistance by blocking indole
signaling with small molecules, Collins says. Alternatively, "the findings suggest the possibility that scientists could
one day use indole or an indole-based therapeutic, if proven safe, to help beneficial bacteria outcompete pathogenic bacteria
in the urinary tract or intestinal system," says Mark Anderson, chief scientific officer of Emeryville, Calif.-based
NovaBay Pharmaceuticals, which develops drugs for antibiotic-resistant infections.
2010 Poster - Infectious Diseases Society; "S.
Ibrahim, D. Debabov, M. Ghannoum, M. Anderson, B. Memarzadeh. In vitro evaluation of the antifungal activity
of NVC-422 (N,N-dichloro-2,2-dimethyltaurine) using a novel cadaver nail model. Infectious Diseases Society of America (IDSA)
48th Annual Meeting, Vancouver, October 21-24, 2010".
2010 Poster - Interscience Conference; M. Zuck, K. Hybiske, D. Debabov, M. Anderson. NVC-422:
Towards Developing Preclinical Infected Tissue Models. Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC),
Boston, September 12-15, 2010
2010
Poster - Interscience Conference; S. A. Rani, C. Celeri, D. Debabov, R. Najafi, M. Anderson. Efficacy of NVC-422, a Novel
Derivative of N-Chlorotaurine, in controlling crystalline Proteus mirabilis biofilm formation on urinary catheters. Interscience
Conference on Antimicrobial Agents and Chemotherapy (ICAAC), Boston, September 12-15, 2010
2010 Poster - Interscience Conference; M. Nagl, C. Martini, A. Hammerer-Lercher,
M. Zuck, D. Debabov, M. Anderson Anticoagulant Effects of N-Chlorotaurine and the Analogs N-monochloro-2-2-dimethyltaurine
and N,N-dichloro-2,2-dimethyltaurine. Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC), Boston, September
12-15, 2010
2009 - AACR Poster #5569 Christopher
M. Pleiman, Adam Willardsen, In Chul Kim, Warren S. Weiner, Chad Bradford, Bruce Roth, Harry Austin, Robert J. Halter, Chris
Jolley, Gary Mather, Kenton Zavitz, Mark Anderson, Joshua Jones and Robert O. Carlson. Characterization of an orally
bioavailable homolog of MPC-6827 (MPI-443803) that maintains high brain penetration. AACR 100th
Meeting April 18-22, 2009. Denver, CO. Poster #5569. (drug design, drug discovery, blood brain barrier,
SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2009 - Current Bioactive Compounds (Review) Paul R. Sebahar, J. Adam
Willardsen and Mark B. Anderson. Anticancer Agents: VTA or VDA. Current Bioactive
Compounds, 2009, 5(1), 79-97. (vascular disrupting agents, vascular targeting agents, tumor, cancer, drug
design, drug discovery, review).
2009 - AACR Poster #2706 AACR Poster
March 30, 2009. Nilantha Sirisoma, Azra Pervin, Hong Zhang, Songchun Jiang, J. Adam Willardsen, Mark B. Anderson, Gary Mather,
Christopher M. Pleiman, Shailaja Kasibhatla, Ben Tseng, John Drewe, Sui Xiong Cai. Discovery of N-(4-Methoxyphenyl)-N,2-dimethylquinazolin-4-amine,
MPC-6827, a Potent Apoptosis Inducer and Efficacious Anticancer Agent with High Blood Brain Barrier Penetration. AACR
2009 Abstract #2706. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable,
pharmacokinetics, pharmacodynamics, ADME).
2009 - Journal of Medicinal Chemistry Nilantha Sirisoma, Azra Pervin, Hong Zhang, Songchun Jiang, J. Adam Willardsen, Mark B. Anderson,
Gary Mather, Christopher M. Pleiman, Shailaja Kasibhatla, Ben Tseng, John Drewe, Sui Xiong Cai. DISCOVERY OF N-(4-METHOXYPHENYL)-N,2-DIMETHYLQUINAZOLIN-4-AMINE,
A POTENT APOPTOSIS INDUCER AND EFFICACIOUS ANTICANCER AGENT WITH HIGH BLOOD BRAIN BARRIER PENETRATION. J. Med. Chem.,
2009, 52 (8), 2341-2351 - DOI: 10.1021/jm801315b web publication
date 18 March 2009. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable,
pharmacokinetics, pharmacodynamics, ADME).
2008 - Bioorganic
& Medicinal Chemistry Letters David Gerrish, In Chul Kim, Dange V. Kumar, Harry Austin, Jennifer E. Garrus,
Vijay Baichwal, Michael Saunders, Rena S. McKinnon, Mark B. Anderson, Robert Carlson, Esther Arranz-Plaza, Kraig M. Yager.
TRITERPENE BASED COMPOUNDS WITH POTENT ANTI-MATURATION ACTIVITY AGAINST HIV-1. Bioorganic & Medicinal
Chemistry Letters 18 (2008) 6377-6380. (drug design, drug discovery, SAR, SXR, HIV, antiviral, synthesis, pharmacokinetics,
pharmacodynamic considerations, ADME).
2008 - Journal of Medicinal Chemistry Nilantha Sirisoma, Shailaja Kasibhatla, Azra Pervin, Hong Zhang, Songchun Jiang, J. Adam Willardsen, Mark Anderson,
Christopher M. Pleiman, Ben Tseng, John Drewe, Sui Xiong Cai. DISCOVERY OF 2-CHLORO-N-(4-METHOXYPHENYL)-N-METHYLQUINAZOLIN-4-AMINE
(EP128265, MPI-0441138) AS AN INDUCER OF APOPTOSIS WITH IN VIVO ACTIVITY. J. Med. Chem. 2008, 51,
4771-4779. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics,
pharmacodynamics, ADME).
2008 - ACS Poster MEDI-101 Cai,
Sui Xiong; Sirisoma, Nilantha; Pervin, Azra; Zhang, Hong; Jiang, Songchun; Baichwal, Vijay; Willardsen, J. Adam; Anderson,
Mark; Pleiman, Christopher M.; Tseng, Ben; Kasibhatla, Shailaja; Drewe, John. DISCOVERY OF 2-CHLORO-N-(4-METHOXYPHENYL)-N-METHYLQUINAZOLIN-4-AMINE
(EP128265, MPI-0441138) AS A POTENT APOPTOSIS INDUCER USING ANTICANCER SCREENING APOPTOSIS PROGRAM (ASAP), A CELL- AND CASPASE-BASED
PLATFORM. Abstracts of Papers, 235th ACS National Meeting, New Orleans, LA, United States, April 6-10, 2008 (2008),
MEDI-101. CODEN: 69KNN3 AN 2008:389655. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis,
oral, bioavailable). (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable,
pharmacokinetics).
2008 - AACR Poster #1265 Nilantha
Sirisoma, Azra Pervin, Hong Zhang, Songchun Jiang, Vijay Baichwal, J. Adam Willardsen, Mark Anderson, Christopher M. Pleiman,
Ben Tseng, Shailaja Kasibhatla, John Drewe, Sui Xiong Cai. 2-CHLORO-N-(4-METHOXYPHENYL)-N-METHYLQUINAZOLIN-4-AMINE
(EP128265, MPI-0441138) AS AN INDUCER OF APOPTOSIS WITH IN VIVO ACTIVITY. AACR April 12-16, 2008, San Diego, California,
99th Meeting Abstract # 1265. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral,
bioavailable,pharmacokinetics, pharmacodynamics, ADME).
2007 - Purdue University
Invited Lecture on Neurodegenerative and Alzheimer's disease Anderson, Mark B. Invited
Lecture for the Purdue University Special Topics Presentation: ALZHEIMER'S DISEASE - TARGETING AMYLOID. October
5th, 2007, West Lafayette, Indiana. (Alzheimer's, SXR, SAR, drug design, drug discovery, competitive analysis,
review).
2006 - Journal of Medicinal Chemistry Li,
Haitao; Anderes, Kenna L.; Kraynov, Eugenia A.; Luthin, David R.; Do, Quyen-Quyen; Hong, Yufeng; Tompkins, Eileen; Sun, Eric
T.; Rajapakse, Ranjan; Pathak, Ved P.; Christie, Lance C.; Vazir, Haresh; Castillo, Rosemary; Gregory, Margaret L.; Castro,
Mary; Nared-Hood, Karen; Paderes, Genevieve; Anderson, Mark B.. DISCOVERY OF A NOVEL, ORALLY ACTIVE, SMALL MOLECULE
GONADOTROPIN-RELEASING HORMONE (GNRH) RECEPTOR ANTAGONIST. [ERRATUM TO DOCUMENT CITED IN CA145:020415]. Journal of
Medicinal Chemistry (2006), 49(19), 5849. CODEN: JMCMAR ISSN:0022-2623. CAN 145:347819 AN 2006:844175. (drug design, drug
discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics,
ADME).
2006 - Journal of Medicinal Chemistry Li,
Haitao; Anderes, Kenna L.; Kraynov, Eugenia A.; Luthin, David R.; Do, Quyen-Quyen; Hong, Yufeng; Tompkins, Eileen; Sun, Eric
T.; Rajapakse, Ranjan; Pathak, Ved P.; Christie, Lance C.; Vazir, Haresh; Castillo, Rosemary; Gregory, Margaret L.; Castro,
Mary; Nared-Hood, Karen; Paderes, Genevieve; Anderson, Mark B.. DISCOVERY OF A NOVEL, ORALLY ACTIVE, SMALL MOLECULE
GONADOTROPIN-RELEASING HORMONE (GNRH) RECEPTOR ANTAGONIST. Journal of Medicinal Chemistry (2006), 49(11), 3362-3367.
CODEN: JMCMAR ISSN:0022-2623. CAN 145:20415 AN 2006:376441. (drug design, drug discovery, blood brain barrier, SAR, SXR, cancer,
tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2003
- Journal of Pharmacology and Experimental Therapeutics Anderes, Kenna L.; Luthin, David R.; Castillo, Rosemary;
Kraynov, Eugenia A.; Castro, Mary; Nared-Hood, Karen; Gregory, Margaret L.; Pathak, Ved P.; Christie, Lance C.; Paderes, Genevieve;
Vazir, Haresh; Ye, Qiang; Anderson, Mark B.; May, John M. BIOLOGICAL CHARACTERIZATION OF A NOVEL, ORALLY ACTIVE SMALL
MOLECULE GONADOTROPIN-RELEASING HORMONE (GNRH) ANTAGONIST USING CASTRATED AND INTACT RATS. Journal of Pharmacology
and Experimental Therapeutics (2003), 305(2), 688-695. CODEN: JPETAB ISSN:0022-3565. CAN 139:270462 AN 2003:329596. (drug
design, drug discovery, blood brain barrier, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics,
ADME, chemical biology).
2003 - Journal of Organic Chemistry Shackelford, Scott A.; Anderson, Mark B.; Christie, Lance C.; Goetzen, Thomas; Guzman, Mark C.; Hananel, Martha A.;
Kornreich, Wayne D.; Li, Haitao; Pathak, Ved P.; Rabinovich, Alex K.; Rajapakse, Ranjan J.; Truesdale, Larry K.; Tsank, Stella
M.; Vazir, Haresh N. ELECTROPHILIC TETRAALKYLAMMONIUM NITRATE NITRATION. II. IMPROVED ANHYDROUS AROMATIC AND HETEROAROMATIC
MONONITRATION WITH TETRAMETHYLAMMONIUM NITRATE AND TRIFLIC ANHYDRIDE, INCLUDING SELECTED MICROWAVE EXAMPLES. Journal
of Organic Chemistry (2003), 68(2), 267-275. CODEN: JOCEAH ISSN:0022-3263. CAN 138:169603 AN 2002:943438. Note erratum to
CA138:169603 Journal of Organic Chemistry (2003), 68(7), 2986. CODEN: JOCEAH ISSN:0022-3263. CAN 140:41589 AN 2003:135779.
(drug design, drug discovery, SAR, SXR, synthesis, nitration).
2003 - Annual Reports
in Medicinal Chemistry (Review) Anderson, Mark B.; Roemer, Terry; Fabrey, Robyn. PROGRESS
IN ANTIFUNGAL DRUG DISCOVERY. Annual Reports in Medicinal Chemistry (2003), 38 163-172. CODEN: ARMCBI ISSN:0065-7743.
CAN 140:228118 AN 2003:836070. (antiinfective, infective, fungal, review).
2002
- Pharmaceutical Research Iatsimirskaia, Eugenia A.; Gregory, Margaret L.; Anderes, Kenna
L.; Castillo, Rosemary; Milgram, K. Eric; Luthin, David R.; Pathak, Ved P.; Christie, Lance C.; Vazir, Haresh; Anderson, Mark
B.; May, John M. EFFECT OF TESTOSTERONE SUPPRESSION ON THE PHARMACOKINETICS OF A POTENT GNRH RECEPTOR ANTAGONIST.
Pharmaceutical Research (2002), 19(2), 202-208. CODEN: PHREEB ISSN:0724-8741. CAN 137:73535 AN 2002:200606. (drug design,
drug discovery, SAR, SXR, cancer, tumor, synthesis, oral, bioavailable, pharmacokinetics, pharmacodynamics, ADME).
2002 - Bioorganic & Medicinal Chemistry Letters Luthin, David
R.; Hong, Yufeng; Tompkins, Eileen; Anderes, Kenna L.; Paderes, Genevieve; Kraynov, Eugenia A.; Castro, Mary A.; Nared-Hood,
Karen D.; Castillo, Rosemary; Gregory, Margaret; Vazir, Haresh; May, John M.; Anderson, Mark B. CHARACTERIZATION OF
MONO- AND DIAMINOPYRIMIDINE DERIVATIVES AS NOVEL, NONPEPTIDE GONADOTROPIN RELEASING HORMONE (GNRH) RECEPTOR ANTAGONISTS.
Bioorganic & Medicinal Chemistry Letters (2002), 12(24), 3635-3639. CODEN: BMCLE8 ISSN:0960-894X. CAN 139:17096 AN 2002:878755.
(drug design, drug discovery, SAR, SXR, cancer, tumor, synthesis, bioavailable, pharmacokinetics, pharmacodynamics, ADME,
chemical biology).
2002 - Bioorganic & Medicinal Chemistry Letters Luthin, David R.; Hong, Yufeng; Pathak, Ved P.; Paderes, Genevieve; Nared-Hood, Karen D.; Castro, Mary A.; Vazir,
Haresh; Li, Haitao; Tompkins, Eileen; Christie, Lance; May, John M.; Anderson, Mark B. THE DISCOVERY OF NOVEL SMALL
MOLECULE NON-PEPTIDE GONADOTROPIN RELEASING HORMONE (GNRH) RECEPTOR ANTAGONISTS. Bioorganic & Medicinal Chemistry
Letters (2002), 12(23), 3467-3470. CODEN: BMCLE8 ISSN:0960-894X. CAN 138:378559 AN 2002:846220. (drug design, drug discovery,
SAR, SXR, cancer, tumor, synthesis, pharmacokinetics, pharmacodynamics, ADME).
2001
- Combinatorial Chemistry Symposium M. B. Anderson, V. Pathak, Y. Hong, L. Christie, R.
Rajapakse, Q. Do, H. Li, E. Tompkins, J. Feng, D. Luthin, K. Nareed-Hood, M. Castro, S. Barnum , J. May, E. Iatsimirskaia,
M. Gregory, Kenna Anderes, R. Castillo, G. Paderes. THE POWER OF MEDICINAL & COMBINATORIAL CHEMISTRIES IN DRUG
DISCOVERY--AN ILLUSTRATION. UCSD San Diego Combinatorial Chemistry Symposium, CA 13 July 2001. (drug design, drug
discovery, SAR, SXR, combinatorial, synthesis)
2001 - Australia Peptide Symposium
Poster Haitao Li, Quyen-Quyen Do, Yufeng Hong, Eileen Tompkins, Ved Pathak, Lance Christie,
David Luthin, Genevieve Paderes, Haresh Vazir, and Mark B Anderson. DISCOVERY AND OPTIMIZATION OF POTENT SMALL MOLECULE
GNRH (GONADOTROPIN RELEASING HORMONE) ANTAGONISTS 4th Australia Peptide Symposium Poster Oct 7-12 2001.
(drug design, drug discovery, synthesis, SAR, SXR).
2000 - Society of Toxicology M. B. Anderson, V. Pathak, Y. Hong, L. Christie, R. Rajapakse, Q. Do, H. Li, E. Tompkins,
J. Feng, D. Luthin, K. Nareed-Hood, M. Castro, S. Barnum , J. May, E. Iatsimirskaia, M. Gregory, Kenna Anderes, R. Castillo,
G. Paderes. THE POWER OF PARALLEL MEDICINAL CHEMISTRY IN DRUG DISCOVERY--AN ILLUSTRATION. Society of Toxicology,
Irvine, CA 6 June 2000. (drug design, drug discovery, synthesis, SAR, SXR, review).
1998
- Journal of Pharmacology and Experimental Therapeutics Kilgore, Kenneth S.; Powers,
Karen L.; Imlay, Michelle M.; Malani, Anu; Allen, Douglas I.; Beyer, Jennifer T.; Anderson, Mark B.; Warren, Jeffrey S. THE
CARBOHYDRATE SIALYL LEWISX (SLEX) SULFATED GLYCOMIMETIC GM2941 ATTENUATES GLUCAN-INDUCED PULMONARY GRANULOMATOUS VASCULITIS
IN THE RAT. Journal of Pharmacology and Experimental Therapeutics (1998), 286(1), 439-446. CODEN: JPETAB ISSN:0022-3565.
CAN 129:184095 AN 1998:454322. http://jpet.aspetjournals.org/cgi/content/full/284/1/427 (drug design, drug discovery, synthesis,
SAR, SXR, pulmonary, lung, disease).
1998 - Journal of Pharmacology and Experimental
Therapeutics Kilgore, Kenneth S.; Tanhehco, Elaine J.; Park, James L.; Naylor, Keith B.;
Anderson, Mark B.; Lucchesi, Benedict R. REDUCTION OF MYOCARDIAL INFARCT SIZE IN VIVO BY CARBOHYDRATE-BASED GLYCOMIMETICS.
Journal of Pharmacology and Experimental Therapeutics (1998), 284(1), 427-435. CODEN: JPETAB ISSN:0022-3565. CAN 128:212667
AN 1998:53500. http://jpet.aspetjournals.org/cgi/content/full/284/1/427 (drug design, drug discovery, synthesis, SAR, SXR,
cardiovascular).
1998 - American Journal of Respiratory Cell and Molecular Biology Kim, Mi-Kyeong; Brandley, Brian K.; Anderson, Mark B.; Bochner, Bruce S. ANTAGONISM
OF SELECTIN-DEPENDENT ADHESION OF HUMAN EOSINOPHILS AND NEUTROPHILS BY GLYCOMIMETICS AND OLIGOSACCHARIDE COMPOUNDS.
American Journal of Respiratory Cell and Molecular Biology (1998), 19(5), 836-841. CODEN: AJRBEL ISSN:1044-1549. CAN 130:123771
AN 1998:758109. (drug design, drug discovery, synthesis, SAR, SXR, pulmonary).
1998
- Journal of Pharmacology and Experimental Therapeutics Kilgore, Kenneth S.; Powers, Karen
L.; Imlay, Michelle M.; Malani, Anu; Allen, Douglas I.; Beyer, Jennifer T.; Anderson, Mark B.; Warren, Jeffrey S. THE
CARBOHYDRATE SIALYL LEWISX (SLEX) SULFATED GLYCOMIMETIC GM2941 ATTENUATES GLUCAN-INDUCED PULMONARY GRANULOMATOUS VASCULITIS
IN THE RAT. Journal of Pharmacology and Experimental Therapeutics (1998), 286(1), 439-446. CODEN: JPETAB ISSN:0022-3565.
CAN 129:184095 AN 1998:454322. (drug design, drug discovery, synthesis, SAR, SXR).
1998
- Journal of Pharmacology and Experimental Therapeutics Kilgore, Kenneth S.; Tanhehco,
Elaine J.; Park, James L.; Naylor, Keith B.; Anderson, Mark B.; Lucchesi, Benedict R. REDUCTION OF MYOCARDIAL INFARCT
SIZE IN VIVO BY CARBOHYDRATE-BASED GLYCOMIMETICS. Journal of Pharmacology and Experimental Therapeutics (1998), 284(1),
427-435. CODEN: JPETAB ISSN:0022-3565. CAN 128:212667 AN 1998:53500. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - ISHR XX Annual Meeting Anderson, M.B., Lucchesi, B.R., Kilgore,
K.S., et al., INHIBITORS OF SELECTIN-MEDIATED CELL ADHESION. New Frontiers in Cardiovascular Research, International
Society for Heart Research (ISHR) XX Annual Meeting, University of Michigan, Ann Arbor, Michigan August 9-12, 1998. (drug
design, drug discovery, synthesis, SAR, SXR).
1998 - ISHR XX Annual Meeting Powers, K.L., Kilgore, K.S., Anderson, M.B., Warren, J.S. STRUCTURAL ANALYSIS OF GLYCOMIMETIC INHIBITORS
OF P-SELECTIN-MEDIATED NEUTROPHIL ADHESION. NEW FRONTIERS IN CARDIOVASCULAR RESEARCH, INTERNATIONAL SOCIETY FOR HEART RESEARCH
(ISHR) XX ANNUAL MEETING, UNIVERSITY OF MICHIGAN, ANN ARBOR, MICHIGAN August 9-12, 1998. See Journal of Molecular
and Cellular Cardiology, 1998, 30(7), A233 poster 2. (drug design, drug discovery, synthesis, SAR, SXR).
1998 - American Journal of Respiratory Cell and Molecular Biology Kim,
Mi-Kyeong; Brandley, Brian K.; Anderson, Mark B.; Bochner, Bruce S. ANTAGONISM OF SELECTIN-DEPENDENT ADHESION OF HUMAN
EOSINOPHILS AND NEUTROPHILS BY GLYCOMIMETICS AND OLIGOSACCHARIDE COMPOUNDS. American Journal of Respiratory Cell
and Molecular Biology (1998), 19(5), 836-841. CODEN: AJRBEL ISSN:1044-1549. CAN 130:123771 AN 1998:758109. (drug design, drug
discovery, synthesis, SAR, SXR).
1998 - Additional Information Anderson, M.B., Kilgore, K.S., et al. ADDITIONAL NOVEL GLYCOMIMETICS THAT
ATTENUATED GLUCAN-INDUCED PULMONARY GRANULOMATOUS VASCULITIS IN THE RAT. UNPUBLISHED.
1997 - Poster & Lecture Lucchesi, B.R., Kilgore, K.S., Anderson, M.B., et al REDUCTION OF MYOCARDIAL INFARCT SIZE
IN VIVO BY GLYCOMIMETICS. American Heart Association (AHA) San Diego, CA 1997. (drug design, drug discovery, synthesis,
SAR, SXR, cardiovascular).
1997 - Journal of Surgical Research Garcia-Criado, F. J.; Palma-Vargas, J. M.; Valdunciel-Garcia, J. J.; Gomez-Alonso, A.; Srivastava, O.; Ezrin, A.;
Anderson, M. B.; Toledo-Pereyra, L. H. SULFO-LEWISX DIMINISHES NEUTROPHIL INFILTRATION AND FREE RADICALS WITH MINIMAL
EFFECT ON SERUM CYTOKINES AFTER LIVER ISCHEMIA AND REPERFUSION. Journal of Surgical Research (1997), 70(2), 187-194.
CODEN: JSGRA2 ISSN:0022-4804. CAN 127:219160 AN 1997:545222. (drug design, drug discovery).
1996 - Tokyo, Japan Anderson, Mark B and guest. Presentations on cell adhesion
and new in vivo pulmonary model related to cell adhesion events. Sankyo Co., Tokyo, Japan.
1996 - Pharmaceutical News Musser, John H.; Anderson, Mark B.; Fugedi,
Peter. GLYCOMIMETICS: AN APPROACH TO DISCOVERING LEADS FOR NOVEL THERAPEUTICS. Pharmaceutical News (1996),
3(5), 11-17. CODEN: PHNEEP ISSN:1071-894X. CAN 126:54385 AN 1997:38145. (drug discovery, review).
1996 - International Medicinal Chemistry Symposium Poster Anderson, M.
B., Kilgore, K, FROM THE PHARAOH'S TOMB TO THE PHARMACY. International Medicinal Chemistry Symposium, September
1996. (drug discovery, drug design)
1996 - Drug News & Perspectives Musser, John H.; Fugedi, Peter; Anderson, Mark Brian; Rao, Narasinga; Peto, Csaba; Tyrrell, Dave; Holme, Kevin; Tressler,
Rob. CARBOHYDRATES AS A SOURCE OF MOLECULAR DIVERSITY FOR DRUG DISCOVERY. Drug News & Perspectives (1996),
9(3), 133-141. CODEN: DNPEED ISSN:0214-0934. CAN 126:98689 AN 1997:30187. (drug design, drug discovery, review).
1996 - ACS Pacific Regional Conference Anderson, M.B., Lucchesi,
B.R., Kilgore, K.S., et al GLYCOMIMETICS AND GRANULOMATOUS VASCULITIS. ACS Pacific Regional Conference, San
Francisco, October 1996.
1995 - J Allergy Clinical Immunology M. K. Kim, B. K. Brandley, M. B. Anderson and B. S. Bochner, ANTAGONISM OF HUMAN NEUTROPHIL (NEU) AND EOSINOPHIL
(EOS) ADHESION BY GLYCOMIMETICS AND OLIGOSACCHARIDE COMPOUNDS. The American Academy of Allergy and Immunology, abstract
in J. Allergy Clin Immunol., 1995, 95:220. (drug design, drug discovery, synthesis, SAR).
1995 - Current Pharmaceutical Design Musser, John H.; Anderson, Mark B.; Levy,
Daniel E. GLYCOMIMETICS AS SELECTIN INHIBITORS. Current Pharmaceutical Design (1995), 1(2), 221-32. CODEN:
CPDEFP ISSN:1381-6128. CAN 124:193057 AN 1996:90745. (drug design, drug discovery, review).
1994 - XVIIth International Carbohydrate Symposium B. N. Narasinga Rao, M.
B. Anderson, J. H. Musser, J. H. Gilbert, M. E. Schaefer, C. Foxall and B. K. Brandley, IDENTIFICATION OF
NOVEL SELECTIN INHIBITORS USING SLEX PHARMACOPHORE BASED SEARCH. XVIIth International Carbohydrate Symposium,
July 17‑22, 1994, Ottawa, Canada. (drug design, drug discovery).
1994 - Journal
of Biological Chemistry Rao, B. N. Narasinga; Anderson, Mark B.; Musser, John H.; Gilbert,
James H.; Schaefer, Mary E.; Foxall, Carrol; Brandley, Brian K. SIALYL LEWIS X MIMICS DERIVED FROM A PHARMACOPHORE
SEARCH ARE SELECTIN INHIBITORS WITH ANTI-INFLAMMATORY ACTIVITY. Journal of Biological Chemistry (1994), 269(31),
19663-6. CODEN: JBCHA3 ISSN:0021-9258. CAN 121:148348 AN 1994:548348. (drug design, drug discovery, synthesis, SAR, SXR, inflammation,
chemical biology).
1994 - International Business Communications Presentation Anderson, M. B., GLYCOMIMETIC INHIBITORS OF SELECTINS. TARGETING CELL ADHESION MOLECULES FOR THERAPEUTIC
APPLICATION. Sheraton Society Hill Hotel Philadelphia, PA. International Business Communications. December 1‑2,
1994. (drug design, drug discovery, SAR, SXR).
1994 - Immunological Implications
of Shock, Trauma and Sepsis B. K. Brandley, N. Rao, M. B. Anderson, H. Lopez, STRATEGIES
FOR THE DESIGN AND USE OF CARBOHYDRATES AND THEIR DERIVATIVES AS ANTI‑INFLAMMATORY THERAPEUTICS. For a Meeting
on Immunological Implications of Shock, Trauma and Sepsis in Munich, March 2‑6, 1994. (drug design, drug discovery,
shock, trauma, sepsis).
1994 - Burger's Medicinal Chemistry Chapter 22 John H. Musser, Péter Fügedi and Mark Brian Anderson. CHAPTER TWENTY‑TWO:
CARBOHYDRATE BASED THERAPEUTICS. Burger's Medicinal Chemistry, Fifth Edition 1994, pages 901‑947. (drug design,
drug discovery, review).
1991 - Tetrahedron Letters Anderson,
M. B.; Lamothe, M.; Fuchs, P. L. SYNTHESIS VIA VINYL SULFONES. 41. CYTOCHALASIN, NATURAL PRODUCT
SUPPORT STUDIES. 16. INTRAMOLECULAR ACYLATION OF AN ALPHA-SULFONYL ANION GENERATED VIA HALOGEN-METAL EXCHANGE OF AN
ALPHA-HALOSULFONE BEARING AN UNSYMMETRICAL ANHYDRIDE. Tetrahedron Letters (1991), 32(35), 4457-60. CODEN:
TELEAY ISSN:0040-4039. CAN 115:255658 AN 1991:655658. (synthesis, cytochalasin, natural product).
1991 - Synthetic Communications Lamothe, M.; Anderson, M. B.; Fuchs,
P. L. SYNTHESIS VIA VINYL SULFONES. 40. CYTOCHALASIN, NATURAL PRODUCT SUPPORT STUDIES. 15. SCOPE
AND LIMITATIONS IN THE USE OF ALPHA-SILYL AND ALPHA-STANNYL SULFONES AS LATENT ALPHA-SULFONYL ANIONS. Synthetic Communications
(1991), 21(15-16), 1675-93. CODEN: SYNCAV ISSN:0039-7911. CAN 115:255715 AN 1991:655715. (synthesis, cytochalasin, natural
product).
1990 - Rapid Commun Mass Spectrom Wood,
K. V.; Rothwell, A. P.; Anderson, M. B.; Fuchs, P. L. THE INTRAMOLECULAR MIGRATION OF A TRIMETHYLSILYL GROUP LOCATED
ALPHA TO A SULFONE IN SUBSTITUTED CYCLOHEXYL SYSTEMS. Rapid Communications in Mass Spectrometry (1990), 4(1), 1-4.
CODEN: RCMSEF ISSN:0951-4198. CAN 114:6582 AN 1991:6582. (synthesis, cytochalasin, natural product).
1990 - Organic Mass Spectrometry Wood, K. V.; Rothwell, A. P.; Anderson,
M. B.; Lamothe, M.; Fuchs, P. L. MASS SPECTRA OF SUBSTITUTED O-TRIMETHYLSILYLPHENYL SULFONES. Organic Mass
Spectrometry (1990), 25(8), 423-5. CODEN: ORMSBG ISSN:0030-493X. CAN 114:6593 AN 1991:6593. (synthesis, cytochalasin, natural
product).
1990 - Journal of Organic Chemistry Anderson,
M. B.; Fuchs, P. L. SYNTHESIS VIA VINYL SULFONES. 37. CYTOCHALASIN, NATURAL PRODUCT SUPPORT STUDIES.
11. ALPHA-SILYL SULFONES AS LATENT ALPHA-SULFONYL ANIONS. FLUORIDE-PROMOTED INTRAMOLECULAR 1,2-ADDITIONS TO ALDEHYDES AS THE
BASIS OF A NEW CYCLOPENTENYLATION STRATEGY. Journal of Organic Chemistry (1990), 55(1), 337-42. CODEN: JOCEAH ISSN:0022-3263.
CAN 112:35729 AN 1990:35729. (synthesis, cytochalasin, natural product).
1989 -
Purdue Thesis Anderson, Mark Brian. NEW METHODOLOGIES DIRECTED TOWARDS THE TOTAL
SYNTHESIS OF CYTOCHALASIN, NATURAL PRODUCT C AND D. (1989), 498 pp. CAN 114:101467 AN 1991:101467. (synthesis, cytochalasin,
natural product).
1988 - Rapid Commun Mass Spectrom Wood,
Karl V.; Rothwell, Arlene P.; Anderson, Mark B.; Fuchs, P. L. EVIDENCE FOR COMPETITIVE INTRAMOLECULAR TRIMETHYLSILYL
REARRANGEMENT TO OXYGEN AND SULFUR IN BETA-TRIMETHYLSILYLETHYLTHIOL ESTERS. Rapid Communications in Mass Spectrometry
(1988), 2(2), 38-40. CODEN: RCMSEF ISSN:0951-4198. CAN 112:35953 AN 1990:35953. (synthesis, cytochalasin, natural product).
1988 - Journal of Organic Chemistry Anderson,
M. B.; Ranasinghe, M. G.; Palmer, J. T.; Fuchs, P. L. CYTOCHALASIN, NATURAL PRODUCT SUPPORT STUDIES. 10. NUCLEOPHILIC
AND ELECTROPHILIC MERCAPTANYLATIONS VIA 2-(TRIMETHYLSILYL)ETHANETHIOL-DERIVED REAGENTS. Journal of Organic Chemistry
(1988), 53(13), 3125-7. CODEN: JOCEAH ISSN:0022-3263. CAN 109:170526 AN 1988:570526. (synthesis, cytochalasin, natural product).
1987 - Synthetic Communications Anderson, M.
B.; Fuchs, P. L. CYTOCHALASIN, NATURAL PRODUCT SUPPORT STUDIES. PART 9. AN EFFICIENT METHOD FOR CONVERSION OF CARBOXYLIC
ACID DERIVATIVES TO ALLYLSILANES. Synthetic Communications (1987), 17(6), 621-35. CODEN: SYNCAV ISSN:0039-7911. CAN
108:150550 AN 1988:150550. (synthesis, cytochalasin, natural product).
Key Words: chemistry, medicinal chemistry, biology, chemical biology, business
acumen, Harvard, Purdue, University of Minnesota, drug design, small molecule, drug discovery, chemical proteomics, Director,
Senior Director, Vice President, CHEMISTRY, MEDICINAL CHEMISTRY, BUSINESS ACUMENS, DRUG DESIGN, ADMET, SMALL MOLECULE, INTELLECTUAL
PROPERTIES, PATENTS, CANCER, INFECTIOUS DISEASE, HIV, ANTIVIRAL, ALZHEIMERS DISEASE, ALZHEIMERS, BLOOD BRAIN BARRIER, VASCULAR
DISRUPTING AGENTS, VASCULAR TARGETING AGENTS, vascular targeting agents, prodrugs, PRODRUGS, , kinase, KINASE, CASPASE, drug
design, admet, infectious disease, apoptosis, APOPTOSIS, patents, cancer, endocrine, antiviral, gnrh, GNRH, Selectin, pathology,
neurology, cell adhesion, glycomimetic, mark anderson, mark brain anderson, chief scientific officer, CSO.
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