Achillion Pharmaceuticals, Inc.

Anacor Pharmaceuticals, Inc.

Suoming Zhang

Avinash S Phadke

Xiangzhu Wang

Atul Agarwal

Jacob J Plattner

Milind Deshpande

Dawei Chen

Venkat Rao Gadhachanda

Vincent S Hernandez

Michael Richard Kevin Alley

Xianfeng Li

Cuixian Liu

Ding Zhou

Fernando Rock

Eric Easom

Charles Z Ding

Shouming Li

Jesse Quinn

Akihiro Hashimoto

Godwin Pais

Tsutomu Akama

Yasheen Zhou

Yang Liu

Ha Young Kim

Yanchen Zhang

James A Nieman

Shouming Lee

Cuixan Liu

This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections.

Boron-containing small molecules

The invention provides pharmaceutical compositions comprising a compound of formula or a pharmaceutically acceptable salt or hydrate thereof. The compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication, and the invention provides methods for treating Hepatitis C infections.

4-amino-4-oxobutanoyl peptides as inhibitors of viral replication

The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R-R, R, R, R, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.

Macrocyclic peptides as inhibitors of viral replication

The invention provides 4-amino-4-oxobutanoyl peptides of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R, R-R, R, R, R, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. The 4-amino-4-oxobutanoyl peptides disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptides and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a 4-amino-4-oxobutanoyl peptides as the only active agent or may contain a combination of a 4-amino-4-oxobutanoyl peptides and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.

This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections.

The invention provides cyclic carboxamide compounds and analogues thereof of Formula I and the pharmaceutically salts and hydrates thereof. The variables R, R, R-R, R, R, R, M, n, T, Y, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain cyclic carboxamide compounds and cyclic carboxamide analogues disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more cyclic carboxamide compounds or cyclic carboxamide analogues and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain a cyclic carboxamide compound or cyclic carboxamide analogue as the only active agent or may contain a combination of a cyclic carboxamide compound or cyclic carboxamide analogue and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections.

Cyclic carboxamide compounds and analogues thereof as of hepatitis C virus

The present invention provides tertiary amine substituted peptides of Formula (I) useful as inhibitors of HCV replication. The variables R and R-Rin Formula I are described herein. The invention also includes methods for preparing such compounds. The present invention further includes pharmaceutical compositions containing tertiary amine substituted peptides and methods for using such compounds, including methods for using the compounds to treat hepatitis C infection.

Tertiary amine substituted peptides useful as inhibitors of HCV replication

The invention provides heteroaryl substituted thiazolo compounds of Formula I and II and pharmaceutically acceptable salts thereof. The variables A and Rto Rare defined herein. The invention also includes methods for preparing compounds and salts of Formula I and II. The present invention also includes pharmaceutical compositions containing heteroaryl substituted thiazolo compounds and methods for using heteroaryl substituted thiazolo compounds, including methods for using the compounds in the treatment of hepatitis C virus.

Heteroaryl substituted thiazoles

The invention provides amino-substituted aminothiazole compounds of Formula I and Formula II where A is a group of the formula: and the variables X, Y, R, and Rto Rare described herein. These compounds are prodrugs of compounds useful as inhibitors of viral replication. Compositions containing such compounds, and methods of treating viral infections with these compounds, as well as to processes and intermediates useful for preparing such compounds are also provided by the invention.

Substituted aminothiazole prodrugs of compounds with anti-HCV activity

The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar, R, R, R, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds 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. 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.

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Palo Alto, CA, United States of America

Suoming Zhang