Achillion Pharmaceuticals, Inc.

Michael Pucci

Jason Allan Wiles

Milind Deshpande

Qiuping Wang

Barton James Bradbury

Edlaine Lucien

Akihiro Hashimoto

Godwin Pais

Ha Young Kim

Avinash S Phadke

Akhiro Hashimoto

Godwin Clarence Gilroy Pais

Yongsheng Song

Disclosed herein are hydroxylthienoquinolones and related compounds and their pharmaceutically acceptable salts useful as antiviral agents and having the general formula in which the variables R, R, and Rare defined herein. Certain compounds provided herein possess potent antibacterial, antiprotozoal, or antifungal activity and are particularly efficacious for the treatment of MRSA infections. The invention also provides pharmaceutical compositions, pharmaceutical compositions containing a hydroxylthienoquinolone in combination with one or more other active agent, and methods of treating microbial infections in animals by administering an effective amount of a hydroxylthienoquinolone or related compound to an animal suffering from a microbial infection.

Hydroxylthienoquinolones and related compounds as anti-infective agents

The invention provides certain compounds and salts of Formula I and Formula II: which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A, R, R, R, R, R, Aand Rare defined herein.

Isothiazoloquinolones and related compounds as anti-infective agents

The invention provides compound and salts of Formula I and II, disclosed herein, which includes compounds of Formula A and Formula B: Such compounds possess useful antimicrobial activity. The variables R, R, R, R, R, and Rshown in Formula A and B are defined herein. Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in animals.

8-methoxy-9H-isothiazolo[5,4-b]quinoline-3,4-diones and related compounds as anti-infective agents

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Kensington, CT, United States of America

Michael Pucci