Merck + Co., Inc.

Velicept Therapeutics, Inc.

Dupont Pharmaceuticals Company

B3ar Therapeutics, Inc.

Other

Merck Sharp + Dohme Corp.

Pliant Therapeutics, Inc.

Mirati Therapepeutics, Inc.

Dalian Zhao

John Y Chung

Bingidimi Itute Mobele

Raymond E Stevens

David L Hughes

Cheng Yi Chen

Richard D Tillyer

Lushi Tan

Michael Ernest Pierce

Lilian Alicia Radesca

Anusuya Choudhury

Katerina Leftheris

Feng Xu

Robert D Larsen

Joseph F Payack

Ian W Davies

David J Mathre

Ekaterina Albert

Michel M Chartrain

Zhonghua Zhang

Qi Gao

Jacob Cha

Emily Marie Rigsbee

James M McNamara

Paul O'Shea

Christopher Roberge

Patricia Andres

Xin Wang

Jian Wang

Edward J J Grabowski

Aquiles E Leyes

Jean-Francois Marcoux

Zhiwei Cao

David Boardman

Anthony On-Ping King

This application relates to solabegron zwitterion useful for the treatment of lower urinary tract symptoms such as, for example, overactive bladder and prostate disorders. Additionally, this application relates to pharmaceutical compositions and methods of treatment utilizing the solabegron zwitterion for treating lower urinary tract symptoms. This application also relates to methods of preparing solabegron hydrochloride from the solabegron zwitterion.

Solabegron zwitterion and uses thereof

Provided herein are integrin inhibitors, compositions thereof, and methods of their uses. Crystalline forms of salts of the inhibitors are also described, along with methods of preparing the crystalline forms. X-ray powder diffraction data, thermogravimetric analysis, and differential scanning calorimetry data are provided for the crystalline forms. The integrin inhibitors are useful for treatment of, inter alia, fibrotic diseases.

Integrin inhibitor and uses thereof

The present invention relates to malate salt of a multi-tyrosine kinase inhibitor. In particular, the present invention relates to crystalline forms of the malate salt of multi-tyrosine kinase inhibitor N-(3-fluoro-4-((2-(5-(((2-methoxyethyl)amino)methyl)pyridin-2-yl)thieno[3,2-b]pyridin-7-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide (S)-2-hydroxysuccinate (1:1), pharmaceutical compositions comprising the crystalline form, processes for preparing the crystalline form and methods of use therefore.

Crystalline salt of a multi-tyrosine kinase inhibitor, method of preparation, and use thereof

Novel crystalline forms of two indole compounds connected to phenoxyalkylcarboxylic acid groups are selective PPAR gamma partial agonists that are useful in the treatment of type 2 diabetes, hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. The novel crystal forms include a crystalline free acid dihydrate and crystalline free acid anhydrate of one compound and several crystalline forms of the free acid and the sodium salt of the second compound. The invention also relates to pharmaceutical compositions comprising these novel crystal forms, processes to prepare the crystal forms and their pharmaceutical compositions, and uses of the crystal forms in the treatment of type 2 diabetes and other PPAR gamma modulated diseases.

Crystalline forms of antidiabetic compounds

This invention encompasses a novel process for synthesizing compounds represented by formula A:

Synthesis of methylthiophenyl hydroxyketones

The present invention provides novel methods for the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1- benzoxazin-2-one of formula (VI-i) ##STR1## which is useful as a human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

Asymmetric synthesis of benzoxazinones

An efficient method for the quantitative preparation and isolation of a compound of formula I ##STR1## or its enantiomer, a chiral mediator used in enantioselective synthesis.

Efficient synthesis of a chiral mediator

Compound 9 is prepared by a 9-step ##STR1## process in an overall yield of about 35% from 3-acetylpyridine. Compound 10 is prepared by a seven-step ##STR2## process in an overall yield of about 30% from 3-acetyl pyridine. These compounds are key intermediates in the synthesis of Compound 11, an important .beta.-3 agonist useful in the treatment of obesity and diabetes. ##STR3##

Process for

Pyridyl ethylation of lactam derivatives

Pyridyl ethylation of lactams

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Fanwood, NJ, United States of America

Dalian Zhao