Bristol-myers Squibb Compnay

Albany Molecular Research, Inc.

Pliant Therapeutics, Inc.

Eisai R&d Management Co., Ltd.

Cytokinetics, Inc.

Qi Gao

Shuang Liu

Chenkou Wei

Matthew L Isherwood

Shan-Ming Kuang

David R Kronenthal

Yuping Qiu

Chong-Hui Gu

Chiajen Lai

Nachimuthu Soundararajan

Victor W Rosso

Chung-Pin H Chen

Shawn K Pack

Xinhua Qian

Pierre Sirard

Ramakrishnan Chidambaram

Min Hu

Kenneth J Natalie, Jr

Jean Lajeunesse

Benjamin Cohen

Katerina Leftheris

Soojin Kim

Fukang Yang

John D Matiskella

Dalian Zhao

Yi Xiao

Martin D Eastgate

Gregory L Beutner

Michael Shawn Lawler

Jacob Cha

Yadagiri R Pendri

David Kenneth Leahy

Bin Zheng

Nicolas Cuniere

Matthew Pfeiffer

Christopher S Regens

Denise Andersen

Jun Qiu

Michael G Fakes

Xiaohua Huang

Rasidul Amin

Wenhao Hu

Feng Qian

Friedrich Mayerl

Yuh-Lin Allen Yang

Robert Droghini

Nathan Reising

Erqing Tang

Blisse J Vakkalagadda

Thorsten Rosner

Carolyn S Wei

Srividya Ramakrishnan

Lopa V Desai

Jian Wang

Paul C Lobben

Neil A Strotman

Keming Zhu

Anne I Song

Roberto Droghini

Norma Tom

Yuh-lin Allen Yang

Jaquan Kalani Levons

Bing-Shiou Yang

Monica Fitzgerald

Michael Bryan Hay

Dawn DiGiugno Parker

Venkatramana M Rao

Susanne Kiau

Blisse Vakkalagadda

Matthew Isherwood

Jr Kenneth J Natalie

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 invention relates to an improved process for synthesizing N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide of the formula: (I) Compound (I) is currently in clinical trials for the treatment of myeloproliferative disorders, such as polycythaemia vera, thrombocythaemia and primary myelofibrosis. 

Process for the preparation of N,N-dicyclopropyl-4-(1,5-dimethyl-1H-pyrazol-3-ylamino)-6-ethyl-1-methyl-1,6-dihydroimidazo[4,5-d]pyrrolo[2,3-b]pyridine-7-carboxamide

The present disclosure generally relates to a crystalline form of 6-[(4S)-2-methyl-4-(naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form, as well of methods of using a crystalline form in the treatment of depression and other conditions and methods for obtaining such crystalline form.

Crystalline form of 6-[(4S)-2-methyl-4-(2-naphthyl)-1,2,3,4-tetrahydroisoquinolin-7-yl]pyridazin-3-amine

Novel [1,2,4]triazolo[1,5-]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention.

Crystalline forms of (S)-7-([1,2,4]triazolo[1,5-a ]pyridin-6-yl)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydroisoquinoline and use thereof

Novel [1,2,4]triazolo[1,5-a]pyridinyl-6-yl-substituted tetrahydroisoquinolines are described in the present invention. These compounds and crystalline forms SA1 and N-2 are used in the treatment of various neurological and physiological disorders. Methods of making these compounds and crystalline forms SA-1 and N-2 are also described in the present invention.

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The present disclosure generally relates to a crystalline form of methyl ((1S)-1-(((2S)-2-(5-(4'-(2-((2S)-1-((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-5-yl)-4-biphenylyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt. The present disclosure also generally relates to a pharmaceutical composition comprising a crystalline form, as well of methods of using a crystalline form in the treatment of Hepatitis C and methods for obtaining such crystalline form.

Crystalline form of methyl ((1S)-1-((25)-2-(5-(4'-(2-((25)-1((2S)-2-((methoxycarbonyl)amino)-3-methylbutanoyl)-2-pyrrolidinyl)-1H-imidazol-2-yl)-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamate dihydrochloride salt

A process is provided for preparing triazole substituted azaindoleoxoacetic piperazine derivative. Novel intermediates produced in the above process, and novel N-1 and amorphous forms of a 1,2,3-triazole substituted azaindoloxoacetic piperazine derivatives and processes for producing such novel forms are also provided.

Process for preparing triazole substituted azaindoleoxoacetic piperazine derivatives and novel salt forms produced therein

Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-yl)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine its salts and solvates thereof are herein set forth, as are pharmaceutical compositions comprising the crystalline form(s), as well of methods of using the crystalline form(s) in the treatment of HIV and/or AIDS, and methods for obtaining such crystalline form(s).

The instant invention provides crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione; processes for the production of such crystalline materials; pharmaceutical compositions comprising such crystalline materials; and methods of treating HIV or AIDS with such crystalline materials or such pharmaceutical compositions.

Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-C]pyridine-3-yl]-ethane-1,2-dione

The instant disclosure provides crystalline forms of 1-benzoyl-4-[2-[4,7-dimethoxy-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-c]pyridin-3-yl]-1,2-dioxoethyl]-piperazine, salts and solvates thereof. The present disclosure also generally relates to pharmaceutical compositions comprising the crystalline form(s), as well of methods of using the crystalline form(s) in the treatment of HIV and/or AIDS, and methods for obtaining such crystalline form(s).

Certain novel 1H-cycloundeca[1,2-b:5,6-b']biscyclohepta(b)pyran analogs are useful as antitumor agents.

Culture of Eupenicillium brefeldianum

A compound isolated from Eupricillium brefeldionum having the structure: ##STR1## is a useful antitumor agent.

1H-cycloundeca[1,2-b:5,6-b']biscyclohepta(b)pyrans useful as antitumor

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Franklin Park, NJ, United States of America

Qi Gao