Pharmacia & Upjohn Company

Pfizer Corporation

The Upjohn Co.

Other

Pharmacia Corporation

Pharmacia & Upjohn

Michael D Ennis

Kristine E Frank

Jian-Min Fu

Robert Louis Hoffman

Patrick Robert Verhoest

Eric Jon Jacobsen

Brad A Acker

Jeffrey W Corbett

Arthur Glenn Romero

Chiu-Hong Lin

Donald J Rogier

William W McWhorter, Jr

Susanne R Haadsma-Svensson

Jed F Fisher

Jeanette Kay Morris

David John Anderson

Per A Carlsson

Hakan V Wikstrom

Bengt R Andersson

Nils P Stjernlof

Stig Thomas Elebring

Jackson B Hester, Jr

Bruce Nelsen Rogers

Richard Charles Thomas

Ruth Elizabeth TenBrink

Toni-Jo Poel

Kjell Anders Svensson

Robert A Lahti

Susan L Vander Velde

John C Sih

Douglas K Hutchinson

Kjell A Svensson

Robert B McCall

William H Darlington

Rebecca M Olson

Nabil B Ghazal

Robert L Hoffman

Mark E Baze

The present invention relates to compounds of Formula I, or a stereoisomer thereof, a pharmaceutically acceptable salt thereof, or a prodrug thereof. The compounds of the inventions are CRFreceptor antagonists. Compounds of the invention are useful for treating, in a warm-blooded animal, particularly a mammal, and more particularly a human, various disorders that are associated with CRF or CRFreceptors, or disorders the treatment of which can be effected or facilitated by antagonizing CRFreceptors.

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This invention relates to compounds of Formula I, a stereoisomer thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, or a pharmaceutically acceptable salt of a prodrug thereof. The compounds interact with CRFreceptors, including human CRFreceptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety-related disorders such as anxiety, and mood disorders such as major depression.

Substituted pyrimidine derivatives

Substituted aryl pyrazine derivatives of the formula I as defined herein,and their use in treating anxiety disorders, depression and stress related disorders are disclosed.

Substituted aryl 1, 4-pyrazine derivatives

This invention relates to substituted pyrimidinone and pyrimidithione derivatives that bind with high affifnity to CRF1 receptors, including human CRF1 receptors. This invention also relates to methods of using the compounds of the invention to treat a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders or diseases, particularly anxiety disorders, and depression and stress related disorders.

Substituted pyrimidinones and pyrimidinthiones

Substituted aryl 1,4-pyrazine derivatives of formula I as defined hereinand their use in treating anxiety disorders, depression and stress related disorders are disclosed.

Substituted aryl 1,4-pyrazine derivatives

The present invention provides substituted pyrazine derivatives of Formula I,that are CRFreceptor antagonists, including human CRFreceptors. This invention also relates to use of compounds of the invention for treating a disorder or condition, the treatment of which can be effected or facilitated by antagonizing a CRF receptor, such as CNS disorders, particularly anxiety-related disorders and mood disorders.

Substituted pyrazine derivatives

Disclosed are compounds of Formula (I):wherein R-R, p and q have any of the values described in the specification, as well as pharmaceutical salts thereof, and pharmaceutical compositions containing such compounds or salts. The compounds and salts are 5-HT ligands and are useful for treating diseases, disorders, and/or conditions in a mammal wherein activity of a 5-HT receptor is implicated. The compounds and salts are particularly useful for treating diseases of the central nervous system.

Substituted azepino[4,5b]indole derivatives

The present invention provides compounds of formula I:wherein R, R, X and Y have any of the values defined in the specification, as well as pharmaceutical compositions comprising the compounds. The invention also provides therapeutic methods as well as processes and intermediates useful for preparing compounds of formula (I).

Tetracyclic azepinoindole compounds

The present invention provides 2,3,4,4,5,9-hexahydro-1H-pyrido[4,3-b]indoles and 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles. These compounds are 5-HT ligands that are useful for treating diseases wherein modulation of 5-HT activity is desired.

Therapeutic 1H-pyrido [4,3-b] indoles

Substituted azepino&lsqb;4,5b&rsqb;indoline derivatives

Certain 2,3,4,5-tetrahydro-1H-&lsqb;1,4&rsqb;diazepino&lsqb;1,7-a&rsqb;indoles are 5-HT ligands and are useful for treating diseases wherein modulation of 5-HT activity is desired.

2,3,4,5-Tetrahydro-1H-&lsqb;1,4&rsqb;diazepino&lsqb;1,7-a&rsqb;indole compounds

Substituted azepino&lsqb;4,5b&rsqb;indole derivatives

A process for preparing a compound of the formula I:

Phenyloxazolidinones having a C-C bond to 4-8 membered heterocyclic rings

Growing community of inventors

Portage, MI, United States of America

Michael D Ennis