Neurogen Corporation

Achillion Pharmaceuticals, Inc.

G.d. Searle & Company

The United States of America As Represented by the Department of Health

Novartis International Pharmaceutical, Ltd.

Other

Pfizer Corporation

National Institutes of Health

Andrew Y Thurkauf

Alan J Hutchison

Jun Yuan

He Zhao

John M Peterson

Xi Chen

Jennifer N Tran

Raymond F Horvath

Xiaoyan Zhang

Avinash S Phadke

Dawei Chen

Shouming Li

Milind Deshpande

Xiangzhu Wang

Cuixian Liu

Kenner C Rice

Yang Gao

Arthur E Jacobson

Yiping Shen

Jesse Quinn

Junko Ohkanda

George D Maynard

Pamela Ann Albaugh

Xiao-shu He

Nancy M Gray

Patricia C Contreras

Rajagopal Bakthavatchalam

Mariena V Mattson

Suoming Zhang

Renata Xavier Kover

Bertrand Leo Chenard

Kenneth Shaw

Charles A Blum

Kevin J Hodgetts

Wayne D Bowen

Brian R De Costa

Marlys Hammond

Daniel L Rosewater

Stanislaw Rachwal

James E Krause

Robbin M Brodbeck

John Tallman

Thomas L O'Donohue

Lilian A Radesca

Silva Terdjanian

Vinod Singh

Bingsong Han

Scott A Mitchell

Robert W DeSimone

George P Luke

Taeyoung Yoon

Linghong Xie

Richard Louis Elliott

Michael A Rogawski

Wallace C Pringle

Xiao Shu He

LuYan Zhang

James A Monn

Salva Terdjanian

Richard L Elliot

Al Hutchison

Shunichi Yamaguchi

J Michael Walker

Liu Cuixian

Quinn Jesse

The invention provides packaged pharmaceutical preparations of Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.

Aryl imidazoles and related compounds as C5a receptor modulators

Amino methyl imidazoles of Formula I are provided: wherein R, R, R, R, R, R, and Rare defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.

Amino methyl imidazoles and related compounds as C5a receptor modulators

The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A, A, R, R, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

Substituted aryl acylthioureas and related compounds; inhibitors of viral replication

Substituted arylthiourea compounds of Formula I, and the pharmaceutically acceptable salts of such compounds, useful as antiviral agents, are provided herein. Certain substituted arylthioureas disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. Pharmaceutical compositions containing one or more substituted arylthiourea compounds and one or more pharmaceutically acceptable carriers, excipients, or diluents are provided herein. Such pharmaceutical compositions may contain a substituted arylthiourea as the only active agent or may contain a combination of a substituted arylthiourea derivative and one or more other pharmaceutically active agents. Methods of treating Hepatitis C viral infections in mammals are also provided herein.

Substituted arylthiourea derivatives useful as inhibitors of viral replication

Substituted aryl thioureas and related compounds; inhibitors of viral replication

The present invention provides compounds of Formula 1, wherein the variables Ar, A, A, A, A, R, R, R, V, W, X, and Y are defined herein. Certain compounds of Formula 1 described herein possess potent antiviral activity. The invention also provides compounds of Formula 1 that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compounds of Formula 1, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula 1 effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula 1 as a single active agent or administering a compound of Formula 1 in combination with on or more other therapeutic agent.

Azabenzofuran substituted thioureas; inhibitors of viral replication

Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and RR, and R-Rare defined herein. These compounds are selective modulators of MCHreceptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.

Melanin concentrating hormone receptor ligands

This invention relates to low molecular weight, non-peptidic, non-peptidomimetic, organic molecules that act as modulators of mammalian complement C5a receptors, preferably ones that act as high affinity C5a receptor ligands and also to such ligands that act as antagonists or inverse agonists of complement C5a receptors. Preferred compounds of the invention possess some or all of the following properties in that they are: 1) multi-aryl in structure, 2) heteroaryl in structure, 3) a pharmaceutically acceptable oral dose can provide a detectable in vitro effect, 4) comprise fewer than four or preferably no amide bonds, and 5) capable of inhibiting leukocyte chemotaxis at nanomolar or sub-nanomolar concentrations. This invention also relates to pharmaceutical compositions comprising such compounds and the use of such compounds in treating a variety of inflammatory and immune system disorders. Additionally, this invention relates to the use such compounds as probes for the localization of C5a receptors.

High affinity small molecule C5a receptor modulators

The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptos. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.

Amino methyl imidazoles as C5a receptor modulators

Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein:

1-phenyl-4-benzylpiperazines dopamine receptor subtype specific ligands

The invention provides compounds and pharmaceutically acceptable salts of Formula Iwherein the variables A, A, R, R, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease. Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.

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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Branford, CT, United States of America

Andrew Y Thurkauf