Neurogen Corporation

Sloan-kettering Institute for Cancer Research

Novartis Ag

Novartis International Pharmaceutical, Ltd.

Taeyoung Yoon

Raymond F Horvath

Alan J Hutchison

Jun Yuan

Ping Ge

Dario Doller

Kevin J Hodgetts

Wallace C Pringle

Rajagopal Bakthavatchalam

Timothy M Caldwell

Stéphane De Lombaert

Cunyu Zhang

Xiaozhang Zheng

Samuel J Danishefsky

Charles A Blum

He Zhao

Linda M Gustavson

John M Peterson

Yang Gao

Cheryl K Steenstra

Lu Yan Zhang

Andrew Y Thurkauf

George D Maynard

Ting-Chao Chou

Robert W DeSimone

Gary Mark Coppola

Xiao-shu He

Erik Meredith

Kyungae Lee

Thomas A Gilmore

Christoph Gaul

Maurice Van Eis

Moo Je Sung

Anette Von Matt

Yiping Shen

Matthew D Shair

Harry Brielmann

Nian Liu

Michael Paul Capparelli

Yasuchika Yamaguchi

Bernd Kaiser

Alan J Hutchinson

Helen Yin

Xuechun Zhang

Jim Darrow

Stėphane DeLombaert

Markus Rolf Dobler

Karoline K Mosny

Ge Ping

T-c Chou

Sarah Siska

Jr Charles Francis Jewell

The present invention provides compounds of Formula (I) or (II) salt form or prodrug thereof, wherein variables are defined herein, that are modulators of metalloproteases such as matrix metalloproteases (MMPs) and ADAMs. The compounds or compositions described herein can be used to treat diseases associated with metalloprotease activity including, for example, arthritis, cancer, cardiovascular disorders, skin disorders, inflammation or allergic conditions. 

3-aryl-5,6-disubstituted pyridazines

The present invention provides compounds of the following structure;A-L1-B&#x2014;C-Dthat are useful for treating or preventing conditions or disorders associated with DGAT1 activity in animals, particularly humans.

Organic compounds

Biaryl piperazinyl-pyridine analogues are provided, of the Formula: wherein variables are as described herein. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using such compounds to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Biaryl piperazinyl-pyridine analogues

Substituted quinazolin-4-ylamine analogues are provided. Such compounds are ligands that may be used to modulate specific receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies. 

Substituted quinazolin-4-ylamine analogues

Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).

Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues

Novel 5-substituted-2-arylpyridine compounds are provided. Such compounds can act as selective modulators of CRF receptors. The 5-substituted-2-arylpyridine compounds provided herein are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

5-substituted-2-arylpyridines

Arylpyrazine compounds are provided, including arylpyrazines that can bind with high affinity and high selectivity to CRFreceptors, including human CRFreceptors. The invention thus includes methods for treatment of disorders and diseases associated with CRFreceptors, including CNS-related disorders and diseases, particularly affective disorders and diseases, and acute and chronic neurological disorders and diseases.

Substituted arylpyrazines

Novel 5-substituted-2-arylpyrazine compounds are provided. Such compounds can act as selective modulators or CRF receptors. Compounds of the invention are provided by the following formula:  The 5-substituted-2-arylpyrazine compounds provided herein are useful in the treatment of a number of CNS and periphercal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds provided are also useful as probes for the localization of CRF receptors and as standards in assays for CRF receptor binding. Methods of using the compounds in receptor localization studies are given.

5-substituted-2-arylpyrazines

Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5a receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5a receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies 

Substituted biaryl amides as C5A receptor modulators

Substituted biaryl amides of Formula I are provided. Such compounds are ligands that may be used to modulate C5receptor activity in vivo or in vitro, and are particularly useful in the treatment of conditions associated with pathological C5receptor activation in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for using them to treat such disorders are provided, as are methods for using such ligands for receptor localization studies.

Substituted biaryl amides as C5a receptor modulators

N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives

Pyrimido &lsqb;4,5,b&rsqb;indolizine derivatives and aza analogues thereof; CRF1 specific ligands

Certain isoquinolinamine and phthalazinamine derivatives: corticotropin-releasing factor receptor CRF1 specific ligands

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Guilford, CT, United States of America

Taeyoung Yoon