Wyeth

Genetics Institute, Inc.

Pfizer Corporation

Lihren Chen

John C McKew

Katherine Lin Lee

James D Clark

Fuk-Wah Sum

Mark L Behnke

Baihua Hu

Paresh Thakker

Steve Yikkai Tam

Wei Li

Kevin Pong

Steven Y Tam

Valerie Clerin

Suzana Marusic

Neal Green

Jason Shaoyun Xiang

Jasbir S Seehra

Jean E Bemis

Yibin Xiang

Richard Vargas

Cara Williams

Audrey Molina Davies

Gary Paul Stack

John L Knopf

Eddine Saiah

Douglas Wilson

Tarek Suhayl Mansour

Jinbo Lee

Frank Eldridge Lovering

Zhao-Kui Wan

Eva Deanna Binnun

Neelu Kaila

Steve Yik-Kai Tam

Huan-Qiu Li

Jianchang Li

Yuchuan Wu

Vipin Suri

Manus Ipek

John Caedmon Mckew

James Donald Clark

Mark Leo Behnke

John C Mckew

This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase Aenzymes (cPLA), more particularly including inhibitors of cytosolic phospholipase Aalpha enzymes (cPLA&#x3b1;). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.

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This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase Aenzymes, and for the medical treatment, prevention and inhibition diseases and disorders including asthma, stroke, atherosclerosis, multiple sclerosis, Parkinson's disease, arthritic disorders, rheumatic disorders, central nervous system damage resulting from stroke, central nervous system damage resulting from ischemia, central nervous system damage resulting from trauma, inflammation caused or potentiated by prostaglandins, inflammation caused or potentiated by leukotrienes, inflammation caused or potentiated by platelet activation factor, pain caused or potentiated by prostaglandins, pain caused or potentiated by leukotrienes, and pain caused or potentiated by platelet activation factor.

Methods for the use of inhibitors of cytosolic phospholipase A2

This invention provides methods for treating in mammals asthma and asthmatic conditions using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase Aenzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Methods for treating asthmatic conditions

This invention relates to inhibiting 11&#x3b2;HSD1.

11-beta HSD1 inhibitors

This invention provides methods for treating in mammals arthritic or rheumatic disorders using substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase Aenzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.

Methods for treating arthritic disorders

A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.

Process for making an aldehyde

The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection, autoimmune disease or graft vs. host disease.

Dihydrodipyrazolopyridinone inhibitors of B7-1

Dihydropyrazolo&lsqb;3,4-d&rsqb;thieno&lsqb;2,3-B&rsqb;pyridinone inhibitors of B7-1

Inhibitors of cytosolic phospholipase A2

The present invention provides a compound of formula I and the use thereof for the immunotherapeutic treatment of transplant rejection or autoimmune disease.

Dihydrodipyrazolopyridinylbenzamide and -sulfonamide inhibitors of B7-1

N-benzhydryl indole compounds

This invention provides substituted indole and indoline compounds useful in inhibiting phospholipase activity, particularly including cytosolic phospholipase A2 (cPLA2) activity, as well as pharmaceutical compositions containing the compounds and methods of using them to treat various maladies, including pain and inflammatory conditions.

Inhibitors of phospholipase enzymes

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Cambridge, MA, United States of America

Lihren Chen