Neurogen Corporation

Wallace C Pringle

Alan J Hutchison

John M Peterson

Taeyoung Yoon

Dario Doller

Linda M Gustavson

Yang Gao

He Zhao

Timothy M Caldwell

Yiping Shen

Cheryl K Steenstra

Helen Yin

Andrew Y Thurkauf

Bertrand Leo Chenard

Rajagopal Bakthavatchalam

Jiong Lan

Robert W DeSimone

George P Luke

Xiao-shu He

Kyungae Lee

Linghong Xie

Manuka Ghosh

Ping Ge

Guiying Li

James G Tarrant

Alan J Hutchinson

Joseph W Ochterski

Mary-Margaret E O'Donnell

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

Compounds of Formula I are provided, in which variables are as described herein:  Such compounds 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).

Substituted 1-benzyl-4-substituted piperazine 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

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

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Guilford, CT, United States of America

Wallace C Pringle