Neurogen Corporation

Ping Ge

Raymond F Horvath

Taeyoung Yoon

Dario Doller

Kevin J Hodgetts

Cunyu Zhang

Alan J Hutchison

John M Peterson

Yang Gao

Stephane De Lombaert

Linghong Xie

Yasuchika Yamaguchi

Joseph W Ochterski

Bingsong Han

Jiong Lan

Yuelian Xu

Stéphane De Lombaert

Timothy M Caldwell

Wallace C Pringle

Bernd Kaiser

Lu Yan Zhang

Robert Ohliger

Jianhua Huang

Stėphane DeLombaert

Xuechun Zhang

Jim Darrow

Kevin Hodggetts

Dipiperazinyl ketones and related analogues are provided, as are methods for their preparation and use. Such compounds may generally be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and therapeutic methods are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

Dipiperazinyl ketones and related analogues

Thiazole amides, imidazole amides and related analogues of the Formula: are provided, in which variables are as described herein. Such compounds may be used to modulate ligand binding to histamine H3 receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of central nervous system (CNS) and other disorders in humans, domesticated companion animals and livestock animals. Compounds provided herein may be administered alone or in combination with one or more other CNS agents to potentiate the effects of the other CNS agent(s). Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting histamine H3 receptors (e.g., receptor localization studies).

Thiazole amides, imidazole amides and related analogues

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

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

N-phenyl benzimidazolecarboxamide and N-phenyl indolecarboxamide derivatives

Aminoalkyl substituted pyrrolo&lsqb;3,2-e&rsqb; pyridine and pyrrolo&lsqb;2,3-b&rsqb;pyrimidine derivatives: modulators of CRF1 receptors

Aminoalkyl substituted pyrrolo &lsqb;3,2-E&rsqb;pyridine and pyrollo &lsqb;2,3-b&rsqb;pyrimidine derivatives: modulators of CRF1 receptors

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Durham, CT, United States of America

Ping Ge