Bristol-myers Squibb Compnay

Boguslaw Mudryk

Martin D Eastgate

Yi Xiao

James H Simpson

Jonathan Clive Tripp

Ke Chen

Michael S Bultman

Richard J Fox

Dayne Dustan Fanfair

Thomas E La Cruz

Christina Ann Risatti

Maxime C Soumeillant

Rulin Zhao

Bang-Chi Chen

Nicolas Cuniere

Huiping Zhang

Lucius Rossano

Bei Wang

Jing Liang

Dau-Ming Hsieh

Adrian David

Xinhua Qian

Jianji Wang

Michael E Randazzo

Peng Geng

Carolyn S Wei

Thomas M Razler

Kishta Katipally

Ye Zhu

Steven R Wisniewski

Ronald Carrasquillo

Eric C Huang

Andrew Lee

John V Duncia

Michael G Yang

Rafael Shapiro

David R Kronenthal

Percy H Carter

Zili Xiao

Matthew Richard Oberholzer

Zhongping Shi

Rao S Bhandaru

Disclosed is a process for preparing Compound 8: comprising the step of reacting Compound of 7: wherein R is Calkyl or benzyl in the presence of a base. Also disclosed are intermediates and processes for preparing the intermediates.

Process for preparing tetrahydrocarbazole carboxamide compound

Disclosed is a process for preparing Compound 8: (8) comprising the step of reacting Compound of 7: (7) wherein R is C1-8 alkyl or benzyl in the presence of a base. Also disclosed are intermediates and processes for preparing the intermediates.

A method for making the compound is set forth utilizing the starting material 

Methods for the preparation of HIV attachment inhibitor piperazine prodrug compound

A method for making the compound is set forth utilizing the starting material wherein R&#x2550;&#x2014;H, alkyl, aryl, &#x2014;SOR, &#x2014;C(O)OR, and &#x2014;C(O)NR; where R&#x2550;&#x2014;H, C-Calkyl, -aryl, and &#x2014;CHAryl.

Methods for the Preparation of HIV attachment inhibitor piperazine prodrug compound

A process for the preparation of the compound of Formula I is set forth utilizing the starting compound 1 and the acid chloride compound 

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino) pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R, R, R, R, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.

Substituted pyrrolidine-2-one compounds

The present invention provides a novel antagonist or partial agonists/antagonist of MCP-1 receptor activity: N-((1R,2S,5R)-5-tert-butylamino)-2-((S)-2-oxo-3-(6-(trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide, or a pharmaceutically acceptable salt, solvate or prodrug, thereof, having an unexpected combination of desirable pharmacological characteristics. Crystalline forms of the present invention are also provided. Pharmaceutical compositions containing the same and methods of using the same as agents for the treatment of inflammatory diseases, allergic, autoimmune, metabolic, cancer and/or cardiovascular diseases is also an objective of this invention. The present disclosure also provides a process for preparing compounds of Formula (I), including N-((1R,2S,5R)-5-(tert-butylamino)-2-((S)-2-oxo-3-(6-trifluoromethyl)quinazolin-4-ylamino)pyrrolidin-1-yl)cyclohexyl)acetamide: wherein R, R,R, R, and are as described herein. Compounds that are useful intermediates of the process are also provided herein.

[object Object]

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described. These compounds can be useful as factor Xa inhibitors.

Efficient synthesis of 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones

A novel process and intermediates thereof for making 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones of the type shown below from appropriate phenyl hydrazines is described.  These compounds can be useful as factor Xa inhibitors.

Process for preparing 4,5-dihydro-pyrazolo[3,4-c]pyrid-2-ones

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East Windsor, NJ, United States of America

Boguslaw Mudryk