One Organic Chemist One Day............Honouring Profiles of leading Organic Chemists brought to you by DR ANTHONY MELVIN CRASTO, worlddrugtracker, helping millions, amcrasto@gmail.com, +91 9323115463, India, skype amcrasto64
DR ANTHONY MELVIN CRASTO Ph.D ( ICT, Mumbai) , INDIA 29Yrs Exp. in the feld of Organic Chemistry,Working for GLENMARK PHARMA at Navi Mumbai, INDIA. Serving chemists around the world. Helping them with websites on Chemistry.Million hits on google, world acclamation from industry, academia, drug authorities for websites, blogs and educational contribution
Shaughnessy Robinson received a B.S. in Chemistry from Wright State University, OH. He worked at Sterling Winthrop and Pfizer for many years doing synthetic and computational chemistry on a variety of small molecule drug discovery programs. He is currently employed by Schrödinger, Inc. in the Drug Discovery Applications Group.
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Application
Filed:
September 17, 2015
Publication date:
March 10, 2016
Inventors:
Jeremy Robert Greenwood, Geraldine C.
Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy
Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Grant
Filed:
January 10, 2013
Date of Patent:
December 15, 2015
Assignee:
Nimbus Iris, Inc.
Inventors:
Geraldine C. Harriman, Ronald T. Wester,
Donna L. Romero, Shaughnessy Robinson, Mee Shelley, Matthew David
Wessel, Jeremy Robert Greenwood, Craig E. Masse, Rosana
Kapeller-Libermann
Abstract: The present
invention provides quinazoline and quinoline compounds, compositions
thereof, and methods of using the same. Also disclosed is the activity
of such compounds as inhibitors of IRAK enzymes.
Type:
Application
Filed:
April 21, 2015
Publication date:
November 19, 2015
Inventors:
Donna L. Romero, Shaughnessy Robinson,
Jeremy Robert Greenwood, Mee Shelley, Craig E. Masse, Geraldine C.
Harriman
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Grant
Filed:
January 8, 2014
Date of Patent:
November 3, 2015
Assignee:
Nimbus Iris, Inc.
Inventors:
Jeremy Robert Greenwood, Geraldine C.
Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy
Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Application
Filed:
February 25, 2014
Publication date:
January 22, 2015
Applicant:
Nimbus Iris, Inc.
Inventors:
Donna L. Romero, Matthew David Wessel,
Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah
Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse,
Mee Shelley
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Application
Filed:
January 8, 2014
Publication date:
July 10, 2014
Applicant:
Nimbus Iris, Inc.
Inventors:
Jeremy Robert Greenwood, Geraldine C.
Harriman, Rosana Kapeller-Libermann, Craig E. Masse, Shaughnessy
Robinson, Donna L. Romero, Mee Shelley, Ronald T. Wester
Abstract: The present
invention provides thienopyrimidine and thienopyridine compounds,
compositions thereof, and methods of using the same for the treatment of
diseases mediated by IRAK enzymes. Such diseases include inflammatory
and proliferative diseases.
Type:
Grant
Filed:
January 10, 2012
Date of Patent:
April 22, 2014
Assignee:
Nimbus Iris, Inc.
Inventors:
Donna L. Romero, Matthew David Wessel,
Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah
Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse,
Mee Shelley
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Application
Filed:
January 10, 2013
Publication date:
September 5, 2013
Applicant:
NIMBUS IRIS, INC.
Inventors:
Geraldine C. Harriman, Ronald T. Wester,
Donna L. Romero, Shaughnessy Robinson, Mee Shelley, Matthew David
Wessel, Jeremy Robert Greenwood, Craig E. Masse, Rosana
Kapeller-Libermann
Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
Type:
Application
Filed:
January 10, 2012
Publication date:
November 8, 2012
Applicant:
NIMBUS IRIS, INC.
Inventors:
Donna L. Romero, Matthew David Wessel,
Shaughnessy Robinson, Jeremy Robert Greenwood, Karl Shawn Watts, Leah
Lynn Frye, Geraldine C. Harriman, Alan Franklin Corin, Craig E. Masse
Abstract: Compounds of the
general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5,
R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their
preparation and their use as antimicrobial agents.
Type:
Application
Filed:
November 22, 2011
Publication date:
March 15, 2012
Inventors:
Steven Joseph Brickner, Jinshan Michael
Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael
A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang,
Shaughnessy Robinson
Abstract: Compounds of the
general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5,
R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their
preparation and their use as antimicrobial agents.
Type:
Application
Filed:
December 20, 2010
Publication date:
April 21, 2011
Inventors:
Steven Joseph Brickner, Jinshan Michael
Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Michael
A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang,
Shaughnessy Robinson
Abstract: Compounds of the
general Formula I, wherein X1, X2, X3, X4, X5, X6, X7, R1, R2, R4, R5,
R6, R7, R8, R9, R10, Y1, n, m, p and q are defined as above, their
preparation and their use as antimicrobial agents.
Type:
Application
Filed:
May 8, 2008
Publication date:
November 13, 2008
Inventors:
Steven Jospeh BRICKNER, Jinshan Michael
Chen, Zhengong Bryan Li, Anthony Marfat, Mark Joseph Mitton-Fry, Micheal
A. Plotkin, Usa Datta Reilly, Chakrapani Subramanyam, Zhijun Zhang,
Shaughnessy Robinson
Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders
Divya Chaudhary has been working in the pharmaceutical and biotechnology industry in drug discovery and development of small molecules and biologics for autoimmune diseases and oncology at Wyeth, Pfizer, and Nimbus Discovery. She received her Ph.D. from University of Alabama at Birmingham at the Comprehensive Cancer Center, working on regulation of oncogene expression, and did postdoctoral fellowships at University of Michigan and Genentech in molecular oncology and signal transduction.
Summary
Created
value in pharmaceutical R&D organizations in small molecule and
biologics drug discovery and development. Strong experience in strategic
thinking and innovation, communication and diligence, and effective
management of projects with diverse functional teams.
Effectivey managed external partners and client relations
Mentored staff as they enter and grow in organizations
Unique combination of a deep scientific and a strategy consulting experience
Disease areas experience in inflammation, autoimmune diseases, respiratory diseases, and immuno-oncology
Specialized in commercialization and operations strategy in life
sciences, pharmacology, biochemistry, cell biology, CRO and supply
chain, and program and alliance management
Managed Markets Strategy for Commercialization of Bio-Pharmaceutical Products
Conducted subnational market analysis and created Tableau dashboard
tools for a newly launched therapeutic to help define local market
strategies
Conducted primary research with physicians, academics, and key opinion
leaders for development insights and commercial assessments for multiple
assets
Analyzed physician and patient data to understand segmentation/
positioning and building patient journey and treatment flow models
Refined a revenue model by performing sensitivity analysis, for the purpose of projecting revenue scenarios
Conducted due diligence for private equity client evaluating a medium sized pharmaceutical company’s assets
Developed product positioning strategies for cell immunotherapy product in hematology
Assessed global opportunities in vaccines; conducted research for HEOR
analysis data inputs for the purpose of asset prioritization
Led preclinical discovery in a virtual CRO outsourced model, contributing to successful series B and program transaction
Contributed to the selection of IRAK4 inhibitor development candidates resulting in program partnering with Genentech
Communicated lead candidate profiles and timelines for board meetings
and external discussions, and for diligence discussions and evaluation
Initiated and fast tracked the oncology project strategy with staff embedded at a CRO
Managed the early efforts to initate the ACC inhibitor evaluation in tumor cell lines
Developed the preclinical markers approach working with a CRO to contribute to the program's oncology strategy
Advanced critical business development objectives in the areas of cancer and autoimmune disease
Evaluated and critiqued multiple target ideas; initiated and implemented two programs
Proposed, planned, and led TYK2 inhibitor lead optimization biology effort
Project
management for IRAK4 inhibitor and ACC inhibitor programs lead
discovery efforts, with contract research organization, for both fee for
service and full time equivalent resourced projects
Recent Advances in the Discovery of Small Molecule Inhibitors of Interleukin-1 Receptor-Associated Kinase 4 (IRAK4) as a Therapeutic Target for Inflammation and Oncology Disorders
Drug Metabolism, Pharmacokinetics, Clinical Pharmacology & Investigative Toxicology
Bengaluru, India
SubrahmanyamVangala is Vice President, DMPK, Clinical Pharmacology
& Investigative Toxicology at Advinus Therapeutics in Bangalore,
India. He has 22 years of pharmaceutical industry experience at major
pharmaceutical companies in USA including American Cyanamid/Wyeth,
Purdue Pharma (PP), JNJ and Shire. He returned to India in 2008 as Vice
President of DMPK and Toxicology at Sai Advantium Pharma (SAP). He built
DMPK departments ground up at PP and JNJ. At SAP, he built the
infra-structure for DMPK & Toxicology groups for integrated drug
discovery support of Medicinal Chemistry programs. For the last 16 years
he managed DMPK, Toxicology and Pharmacology groups at various
capacities.
Dr. Subrahmanyam received his PhD (1987) in Molecular Toxicology from
Department of Biochemistry at Memorial University, Canada. Following
PhD, he completed 2 year postdoctoral training in the Department of
Molecular Toxicology at University of Colorado and heldResearch
Assistant Professor Position in the School of Public Health at
University of California, Berkeley for 3 years, before joining the
industry. He chaired the inaugural Land-O’-Lakes Drug Metabolism and
Applied Pharmacokinetics Conference(1998) and 1st and 2nd
Idiosyncratic Drug toxicity conferences (1998 and 2000). He gave guest
lecturers as invited speaker at several international conferences
related to ADME/Predictive toxicology. In 2005 he received Excellence
in Science Award from JNJ. Since 2010 serving as editor of the STM
Journal of Toxicology: Research and Reviews.Served on international
advisory board for journal Current Pharmacogenomics and Personalized
Medicine (CPPM-2012 & 2013). He published ~40 research articles and
reviews including several invited book chapters.
Research Interest
Drug discovery & development relating to DMPK; Clinical
pharmacology; Investigative toxicology; Biomarkers and molecular
diagnostics.
Shire Human Genetic Therapies · Toxicology & Pharmacology
USA · Lexington
Sep 2001–Nov 2006
Site Head/Research Fellow
Johnson & Johnson · Pharmacokinetics and Drug Metabolism
USA · Raritan, New Jersey
Sep 1992–Jan 1998
Senior Scientist
American Cyanamid Company/Lederle Laboratories/Wyeth Research · Pharmacokinetics, Pharmacodynamics, Biotransformation
USA · Pearl River New York and Princeton, New Jersey
Jan 1989–Aug 1992
University of California, Berkeley · School of Public Health
USA · Berkeley
Feb 1988–
Aug 2001
Group Leader
Purdue Pharma L.P. · Pharmacokinetics and Drug Metabolism
USA · Ardsley, New York
Jan 1987–
Dec 1988
University of Colorado at Boulder · Molecular Toxicology at School of Pharacy
USA · Boulder, Colorado
Jan 1986–Dec 1986
University of Toronto
University of Toronto, School of Medicine · Biochemistry and Pathology
Canada · Toronto
Education
Jan 1981–Dec 1985
Memorial University of Newfoundland
Biochemistry of Cancer · PhD
Canada · St. John's, Newfoundland
Summary
Experienced
professional who excels in both scientific and regulatory expertise for
drug discovery and development success. Strong track record of
accomplishment in building infra-structures and integrating departments
into effective, value-added support for R&D organizational success..
Primary areas of expertise include Toxicology, Pharmacology, DMPK,
Bioanalytical, Clinical Pharmacology and Investigative/Mechanistic
Toxicology. Experienced in both small molecule and biotechnology-based
drug platforms. Some experience with large molecule drug development.
Therapeutic areas of expertise include CNS, Neuro-degenerative diseases,
Metabolic disorders, Inflammation, Oncology, Anti-infectives and
Women's Health (eg, SERMs).
In
the last 4 years of my tenure at SAI, I established the infra structure
for drug discovery support services relating to Pharmacology, ADME and
Toxicology screening. Designed the laboratories that included 20,000 SF,
hired about 40 plus scientists (including 5 Associate Directors as
group managers), and established validated protocols for ADMET services,
Supported ADMET services for several biotech companies in US and Europe.
The animal facilities are accredited by Indian CPCSEA and American
AAALAC authorities. Selected areas of in vitro and in vivo laboratories
are also approved for conducting radiolabel studies. ADME services
include in vivo PK in rodents, mass balance, tissue distribution,
protein binding, caco-2/mdck permeability, CYP profiling (competitive
inhibition,time-based inhibition, phenotyping), metabolic stability,
profiling & metabolite ID, GSH-trapping of reactive intermediates,
physico-chemical properties (solubility, stability, pka, logP, logD).
Toxicology services include: acute, DRF, pivotal one month tox,
(includes: clinical observations, clinical pathology, hematology,
histopathology, toxicokinetics), genetic toxicology (AMES, micronucleus
tests).
Pharmacology services include radioligand binding assays, cell based
assays, in vivo models of pharmacology (pain, neurodegenerative diseases
and inflammation)
For a smooth operational excellence, appropriate processes are put in
place to avoid delays and ensure high quality and timely delivery of
results and reports to the clients.
Communication excellence of all employees is considered number one
piority and appropriate training is provided for all departmental
personnel.
Safe laboratory practices has been made mandatory with appropriate
training recommendations are made for employees by "Health & Safety
Environment" department.
Budget projections based on business needs and for strategic growth are
provided to senior executives with rational justifications.
Provided
PK and Toxicology support for "Enzyme Replacement Therapy" programs.
Managed outsourcing of all PK and Toxicology studies. Designed and
reviewed protocols, analyzed PK and Toxicology data, reviewed reports,
presented at Senior management meetings. Projected quarterly budgets and
provided appropriate justifications. During this job, I had an
opportunity to learn drug discovery/development processes and associated
regulatory challenges for large molecule biologics.
•Built a strong DMPK department from a size of 4 to 28 scientists (Total of 7 PhD: 4 direct reports (2 GL, 1 RS and 1 PS).
•Included experts in compartmental & non-compartmental methods of
PK/TK (GLP), allometric scaling, IV/IVC of ADME, metabolite ID (LC/MS),
in vitro DDI, absorption, transporter, biliary excretion studies.
Evaluation of novel technologies (metabonomics, reactive metabolites,
RED for protein binding).
•Established a competitive DMPK Dept, attracting the best talent from
major Pharma including Merck, Aventis, Pfizer, Schering, Roche.
•Participated in project teams for preclinical development. Provided
preclinical strategies, proposals, and timelines. Provided critical,
expert input in go/no go decisions.
•Managed annual DMPK budget of up to 8 MM (USD). Prepared budgets,
short/long-term strategies, requested appropriate human and capital
resources for dept growth. Balanced in-house and out-sourced activities,
with >90% in-house capacity by 2006 compared to <10% in 2001.
Justified the purchase of LTQ-Orbitrap to Senior management and finance
department and established the state-of-the-art technology for DM
studies.
• Active and lead role in the global harmonization of CYP-DDI assays.
Identified similarities and differences in processes, assay methods for
DDI studies at other JNJ companies. Where needed, harmonized assay
protocols in consensus with other DMPK leaders at JNJ.
•Collaborated with Mechanistic Toxicology group to provide DMPK support
to address specific project related safety issues. Key management
representative for “Hepatotoxicity Expert Group” for evaluation of
hepatotoxicity mechanisms.
•Delegated resources to collaborate with CATD (Computer Aided Trial
Design) group for PK-PD model development using preclinical data.
•Participated in due-diligence teams for in-licensing candidates by reviewing the Preclinical data packages.
•Successfully completed year long “Management Fundamentals” training course at JNJ.
– (3 years 6 months)Ardsley, Westchester, New York
•Managed
8–10 scientists including 4 PhD’s. Established drug metabolism
laboratory that was non-existent at Purdue. Managed the PKDM group,
supported discovery and development projects- including in vitro/in vivo
DM, in vitro DDI, writing preclinical sections for NDA/IND.
•Represented the project teams and sub-teams for DMPK, toxicology, bioanalytical, activities.
•Established hepatocyte cell culture methods, developed cryopreserved
hepatocytes banks and validated their use for drug metabolism and CYP
induction studies.
•Established HPLC/MS coupled to radiometric detection for metabolite
separation and identification to support preclinical and clinical
programs.
•Established high throughput screening methods for discovery support -
Fluorescence cytotoxicity assays using hepatocytes, bDNA assay for
cytochrome P450 induction in hepatocytes.
•Established CYP enzyme ID methods using - correlation analysis,
recombinant enzymes and specific inhibitor assays. Developed and
validated the use of characterized bank (16 subjects) of human liver
microsomes for CYP ID studies.
•Established drug interaction studies using microsomes, recombinant
enzymes and hepatocytes. Made recommendations for clinical drug
interaction program. Established high-throughput fluorescence P450
inhibition screens for discovery support, Coordinated mass-spec
activities for metabolite identification.
•Played key role in help building a Discovery Support program that was
non-existent at Purdue. Provided strategies on how a discovery support
group could help in lead selection and optimization. Identified industry
experts in heading this group.
•Coordinated contract laboratory activities for drug metabolism studies
in hepatocytes/microsomes, CYP enzyme ID, induction, inhibition,
genotyping and Caco-2 permeability studies.
•Established collaborative efforts with academia for assessing
mechanisms of drug toxicity using cellular models and selecting lead
candidates from backups.
– (5 years 6 months)Pearl River, New York (AMC) & Princeton, New Jersey (Wyeth)
•As
a principal investigator, conducted extensive hands-on toxicokinetics
analysis in accordance with GLP. Supported all non-GLP and GLP
toxicology including acute, sub-chronic and chronic studies.
•As a study director and principal investigator designed and conducted
PK (Bioavailability), mass-balance, protein binding, in vivo/in vitro
DM, (CYP isozyme ID, CYP-DDI) studies.
-Conducted hands-on investigative studies to elucidate the mechanisms
underlying long plasma 14C-half life (>22 days) of a drug candidate.
Collaborated with Analytical Development group to conduct amino acid
analysis of plasma proteins and with academia to urinalysis of
endogenous metabolic products. The investigations revealed a novel
mechanism of one-carbon recycling of carbon released from the drug and
incorporation into amino acids, proteins and nucleic acids.
-Conducted hands-on studies and evaluated non-CYP mediated phase-1 and
phase 2 DM for selected preclinical drug candidates based on
strucutre-activity relations. These enzymes include molybdenum
hydroxylases (aldehyde and xanthine oxidses), monoamine oxidases,
carboxylesterases, amidases and UDP-glucuronosyl trnsferases.
-Established recombinant human (rh) CYP-isozyme banks (from cDNA
expressed E.coli cells) for routine drug metabolism studies. Validated
the rhCYP isoforms using standard probe substrates and HPLC analysis.
-Participated in LC-NMR evaluation in collaboration with Bruker for drug metabolism and metabolite-ID studies.
-Supervised two technical assistants. Prepared reports and DM sections of IND/NDA sections for regulatory submissions.
-Supervised a group of four scientists (1 PhD and 3 graduate students).
-Designed in vitro and in vivo metabolism and molecular toxicology
studies using isolated enzyme systems (microsomes, recombinant CYP
enzymes, prostaglandin H synthase, myeloperoxidase etc), cell cultures
(HL-60 cells, human lymphocytes) and in vivo mouse models.
-Established measurement of oxidative DNA damage techniques for
assessing non-genotoxic events in chemical carcinogenesis using HL-60
cells and mouse models (Collaborated with Dr. Bruce Ames laboratory at
Department of Biochemistry for measurement of oxidative DNA damage by
HPLC-Electrochemical detection methods).
-Conducted mechanistic drug metabolism studies using hemeprotein
peroxidases. Investigated novel cooperative interactions of heme and
apoprotein in catalyzing drug metabolism.
-Lectured “Chemical Carcinogenesis” course to graduate students.
Conducted
hands-on in vitro drug metabolism and molecular toxicology experiments
utilizing hepatocytes. Mastered in-situ liver perfusion techniques for
isolating hepatocytes from rats. Developed techniques for measuring
various biochemical and molecular end- points of cell death (GSH
depletion, ATP depletion, inhibition of protein and RNA synthesis,
covalent binding to proteins and DNA etc.).
Conducted Drug Metabolism and toxicity studies in bone marrow
homogenates and bone marrow stromal cells. Evaluated role of cytokines
and other growth factors in bone marrow toxicity
Supervised one technician and one graduate student.
