Kosan Biosciences Incorporated

University of Pennsylvania

Pfizer Corporation

Simon James Shaw

David C Myles

Mark A Burlingame

Kurt Frederick Sundermann

Gary W Ashley

Amos B Smith, Iii

Yandong Li

Daniel V Santi

Christopher Carreras

Yaoquan Liu

Hong Fu

Yue Chen

Yong Li

Brian Scott Freeze

Tomoyasu Hirose

Hao Zheng

Ignació Brouard Martin

6- and 7-substituted coumarin and related 6- and 7-substituted 1H-quinolin-2-one compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the 7-substituted coumarin and related 7-substituted 1H-quinolin-2-one compounds mimic or exceed the high level of pharmacological activity of discodermolide. In other embodiments, their preparation involves more readily available materials, higher yield processes and/or simpler synthetic sequences. In yet other embodiments, the compounds of the invention represent structurally simpler, therapeutically active analogues of discodermolide than heretofore known and may be useful as microtubule stabilizers and, inter alia, for treating and/or preventing cancer and other diseases, disorders, and/or conditions mediated by the stabilization of microtubules.

Discodermolide analogues and methods of their use

15-fluoroketolides of the formula having improved activity and safety, compositions comprising them, and methods for their preparation and use in the treatment of bacterial infections.

7-quinolyl ketolide antibacterial agents

Compounds having a structure according to formula (I) where R, R, R, R, R, and Rare as defined herein, are useful as prokinetic agents.

Motilide compounds

Compounds and methods useful for the synthesis of (+)-discodermolide, a naturally occurring microtubule stabilizing agent useful as an anti-cancer agent.

Compounds useful for the synthesis of (+)-discodermolide and methods thereof

Synthetic methods and intermediates useful in the preparation of lactone containing compounds such as discodermolide and compounds which mimic the chemical or biological activity of discodermolide are provided.

Synthetic techniques and intermediates for polyhydroxy dienyl lactones and mimics thereof

Synthetic discodermolide analogs having utility as antiproliferative agents, having a structure represented by formula A where Rthrough Rand Xare as defined herein.

Synthetic discodermolide analogs

Various macrolide compounds such as those having the following formulas are provided where the variables have the values provided herein.

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San Francisco, CA, United States of America

Simon James Shaw