Pharmacia & Upjohn Company

Pfizer Corporation

Xenon Pharmaceuticals Inc.

Osi Pharmaceuticals, Inc.

Pharmacia & Upjohn

Jian-Min Fu

Kristine E Frank

Michael D Ennis

Robert Louis Hoffman

Patrick Robert Verhoest

Jeffrey W Corbett

Jeanette Kay Morris

Eric Jon Jacobsen

Donald J Rogier

Brad A Acker

William W McWhorter, Jr

Jed F Fisher

Zaihui Zhang

Shaoyi Sun

Sultan Chowdhury

Serguei Sviridov

Rajender Kamboj

Shifeng Liu

Mikhail A Chafeev

Vishnumurthy Kodumuru

Melwyn A Abreo

Mark W Holladay

Nagasree Chakka

Duanjie Hou

Michael D Winther

Vandna Raina

Heinz W Gschwend

Chi Tu

Wenbao Li

Sengen Sun

Arlindo Lucas Castelhano

Arthur Glenn Romero

Daniel F Harvey

Mehran Seid Bagherzadeh

Mikhail Kondratenko

Robert Fraser

Cindy J Hudson

Kashinath Sadalapure

This invention is directed to the use of SCD-1 inhibitors of the formula (I): where x, y, V, W, G, J, L, M, R2, R3, R5, R5a, R6, R6a, R7, R7a, R8 and R8a are defined herein, in combination with other drug therapies to treat adverse weight gain. 

Combination therapy

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (Ia): where x, y, W, V, R, R, R, R, R, R, R, R, R, R, Rand Rare defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.

Pyridazine derivatives and their use as therapeutic agents

Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): 

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

Therapeutic compounds

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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The present invention relates to novel pyrazolo[1,5-a]pyridine derivatives of general formula I: that bind with high affifnity to 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 disorders, and depression and stress related disorders.

Pyrazolo[1,5-a]pyridine derivatives and their use as neurotransmitter modulators

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

Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) Rand Rare independently selected from H, Me or OMe.

Pyrrolo[1,2-b]pyridazine compounds and their uses

Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I): including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.

Pyrrolo[1,2-B]pyridazine compounds and their uses

Disclosed are novel CRF receptor antagonists and their use as treatment of a variety of disorders, including disorders manifesting hypersecretion of CRF or associated with CRF or CRF receptors, such as anxiety, and depression. CRF receptor antagonists of the invention have the structure of formula (I):including stereoisomers or mixture of stereoisomers, pharmaceutically acceptable prodrugs, or pharmaceutically acceptable salts thereof, wherein in formula (I) R is H or Me.

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

The present invention provides compounds of Formula (I):

Indoles and indolines having 5-HT activity

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.

Growing community of inventors

Kalamazoo, MI, United States of America

Jian-Min Fu