Wyeth

Genetics Institute, Inc.

Pfizer Corporation

John C McKew

Lihren Chen

Katherine Lin Lee

James D Clark

Fuk-Wah Sum

Mark L Behnke

Baihua Hu

Paresh Thakker

Jasbir S Seehra

Jean E Bemis

Wei Li

Yibin Xiang

Kevin Pong

Steve Yikkai Tam

Steven Y Tam

Valerie Clerin

Suzana Marusic

Frank Eldridge Lovering

Neelu Kaila

Richard Vargas

Cara Williams

John L Knopf

Eddine Saiah

Douglas Wilson

Tarek Suhayl Mansour

Jinbo Lee

Zhao-Kui Wan

Jason Shaoyun Xiang

Eva Deanna Binnun

Huan-Qiu Li

Jianchang Li

Manus Ipek

Vipin Suri

Yuchuan Wu

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

Novel compounds are disclosed which inhibit the activity of phospholipase enzymes in a mammal, particularly cytosolic phospholipase A. Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.

Inhibitors of phospholipase enzymes

Novel compounds are disclosed which inhibit the activity of phospholipase enzymes, particularly cytosolic phospholipase A . Pharmaceutical compositions comprising such compounds and methods of treatment using such compositions are also disclosed.

Inhibitors of cytosolic phospholipase A2

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.

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Arlington, MA, United States of America

John C McKew