John DeMattei - San Diego CA, US Sagar Shakya - Longmont CO, US Paul J. Nichols - Boulder CO, US Bradley R. Barnett - Boulder CO, US Bruno P. Hache - Boulder CO, US Matthew Charles Evans - Macclesfield, GB James Gair Ford - Macclesfield, GB John Leonard - Macclesfield, GB
Assignee:
Array BioPharma Inc. - Boulder CO AstraZeneca AB - Sodertalje
International Classification:
C07C 235/08
US Classification:
5483044
Abstract:
Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X, X, X, R, Rand Rare as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
John Demattei - Berthoud CO, US Sagar Shakya - San Diego CA, US Anthony D. Piscopio - Longmont CO, US Bruno P. Hache - Boulder CO, US Matthew Charles Evans - MacclesField, GB James Gair Ford - Macclesfield, GB Simon Mark Pointon - Macclesfield, GB Koen Peeters - Wetteren, BE Timothy John Lilley - Macclesfield, GB John Leonard - Macclesfield, GB
Assignee:
Array BioPharma Inc. - Boulder CO AstraZeneca AB - Sodertalje
International Classification:
C07D 235/04 C07D 403/02 C07D 235/18
US Classification:
5483047, 5483061, 5483107
Abstract:
Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1:.
John Demattei - Berthoud CO, US Sagar Shakya - San Diego CA, US Anthony D. Piscopio - Longmont CO, US Bruno P. Hache - Boulder CO, US Matthew Charles Evans - MacclesField, GB James Gair Ford - Macclesfield, GB Simon Mark Pointon - Macclesfield, GB Koen Peeters - Wetteren, BE Timothy John Lilley - Macclesfield, GB John Leonard - Macclesfield, GB
John Demattei - Berthoud CO, US Sagar Shakya - Longmont CO, US Anthony D. Piscopio - Boulder CO, US Bruno P. Hache - Boulder CO, US Matthew Charles Evans - Cheshire, GB James Gair Ford - Cheshire, GB Simon Mark Pointon - Cheshire, GB Koen Peeters - Mont-Saint-Guibert, BE Timothy John Lilley - Cheshire, GB John Leonard - Manchester, GB
Assignee:
ARRAY BIOPHARMA INC. - Boulder CO
International Classification:
C07D 235/04 C07C 229/60 C07C 205/58
US Classification:
5483044, 560 47, 562437
Abstract:
Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X, X, X, Rand Rare as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.
Crystalline Forms And Processes For The Preparation Of Pg12 Receptor Agonists
The present invention relates to salts of 2-(2-((4-(((4-chlorophenyl)(phenyl)-carbamoyloxy)methyl)cyclohexyl)methoxy)acetamido)ethanesulfonic acid (Compound 1) and crystalline forms, solvates and hydrates thereof. The present invention further relates to processes and intermediates useful in the preparation of Compound I and salts, solvates and hydrates thereof. Crystalline forms, salts, solvates and hydrates of the present invention and pharmaceutical compositions thereof are useful in the treatment of for example, pulmonary arterial hypertension (PAH); platelet aggregation; coronary artery disease; myocardial infarction; transient ischemic attack; angina; stroke; ischemia-reperfusion injury; restenosis; atrial fibrillation; blood clot formation; atherothrombosis; asthma or a symptom thereof; a diabetic-related disorder; glaucoma or other disease of the eye with abnormal intraocular pressure; hypertension; inflammation; psoriasis; psoriatic arthritis; rheumatoid arthritis; Crohn's disease; transplant rejection; multiple sclerosis; systemic lupus erythematosus (SLE); ulcerative colitis; atherosclerosis; acne; type I diabetes; type 2 diabetes; sepsis; and chronic obstructive pulmonary disorder (COPD).
- Alameda CA, US Khalid Shah - Half Moon Bay CA, US Sagar Shakya - San Diego CA, US Peter Wong - Brisbane CA, US Courtney S. Johnson - West Lafayette IN, US Melanie Janelle Bevill - West Lafayette IN, US Stephan D. Parent - West Lafayette IN, US
International Classification:
C07D 215/48
Abstract:
The present invention relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid crystalline salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.
Crystalline Forms And Salt Forms Of A Kinase Inhibitor
- Alameda CA, US Khalid Shah - Half Moon Bay CA, US Sagar Shakya - San Diego CA, US Peter Wong - Brisbane CA, US Courtney S. Johnson - West Lafayette IN, US Melanie Janelle Bevill - West Lafayette IN, US Stephan D. Parent - West Lafayette IN, US
International Classification:
C07D 215/48
Abstract:
The present invention relates to crystalline forms of the free base of the c-Met inhibitor, Compound 1. The invention also relates to crystalline forms of salts of Compound 1. The invention also relates to pharmaceutical compositions comprising the solid polymorphs of the free base and salts of Compound 1. The invention further relates to methods of treating a disease, disorder, or syndrome mediated at least in part by modulating in vivo activity of a protein kinase.
Crystalline L-Arginine Salt Of (R)-2-(7-(4-Cyclopentyl-3- (Trifluoromethyl)Benzyloxy)-1,2,3, 4-Tetrahydrocyclo-Penta [B]Indol-3-Yl)Acetic Acid(Compound1) For Use In Sipi Receptor-Associated Disorders
- San Diego CA, US Ryan O. Castro - San Diego CA, US Mark Allen Hadd - San Diego CA, US You-An Ma - Poway CA, US Antonio Garrido Montalban - San Diego CA, US Jaimie Karyn Rueter - San Diego CA, US Lee Alani Selvey - Longview WA, US Sagar Raj Shakya - San Diego CA, US Marlon Carlos - Chula Vista CA, US
International Classification:
C07D 209/94 C07C 279/12
Abstract:
The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1Preceptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).
Arena Pharmaceuticals since 2009
Associate Fellow
Array BioPharma 2000 - 2009
Research Investigator
Apotex Pharmachem inc. 1996 - 2000
R&D chemist
Hauser Inc 1995 - 1996
Chemist
Education:
University of Colorado at Boulder 1992 - 1995
Postdoc, Synthetic Organic Chemistry
University of Ottawa 1987 - 1992
Ph.D., Synthetic Medicinal Chemistry
Skills:
Organic Chemistry Organic Synthesis Drug Discovery Chemistry Medicinal Chemistry Technology Transfer Analytical Chemistry Hplc Drug Development Gmp Drug Design Lc Ms Cmc Chromatography Process Chemistry Nmr Ind High Performance Liquid Chromatography Spectroscopy Synthetic Organic Chemistry Lead Change Parallel Synthesis
Languages:
English
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