Neurogen Corporation

Synaptic Pharmaceutical Corporation

Novartis Ag

H. Lunbeck A/s

Yasuchika Yamaguchi

Wai C Wong

Stewart Alwyn Noble

Mohammad R Marzabadi

Ping Ge

Dario Doller

Raymond F Horvath

Taeyoung Yoon

Kevin J Hodgetts

Stéphane De Lombaert

Bernd Kaiser

Lu Yan Zhang

Cunyu Zhang

Jianhua Huang

Heinrich R&uuml;eger

Peter B&uuml;hlmayer

Xuechun Zhang

Jim Darrow

Kevin Hodggetts

This invention is directed to bicyclic and tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of this invention and a pharmaceutically acceptable carrier. The invention provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides the use of a compound of the invention for the preparation of a pharmaceutical composition for treating an abnormality, wherein the abnormality is alleviated by decreasing the activity of a human Y5 receptor.

Selective NPY (Y5) antagonists

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

Diarylpyrimidine compounds of Formula I are provided, wherein.or a pharmaceutically acceptable salt thereof, wherein: These compounds are useful in the treatment of a number of CNS and periphereal disorders, particularly stress, anxiety, depression, cardiovascular disorders, and eating disorders. Methods of treatments of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of Formula I 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.

2,5-diarypyrimidine compounds

This invention is directed to tricyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

Selective NPY (Y5) antagonists (tricyclics)

This invention is directed to bicyclic compounds which are selective antagonists for NPY (Y5) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

Selective NPY (Y5) antagonists (bicyclics)

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Guilford, CT, United States of America

Yasuchika Yamaguchi