Kosan Biosciences Incorporated

John R Carney

Brian Walter Metcalf

Gary W Ashley

Peter J Licari

Robert L Arslanian

Chaitan Khosla

Hugo Menzella

Janice Lau Wee

Li Tang

Ralph C Reid

Yong Li

Lawrence Cadapan

The invention provides novel compounds that may be used as intermediates in the preparation of epothilones, epothilone analogs and derivative, as well as new synthetic methods for producing the intermediates and products.

Methods of making epothilones

Macrolactams are made by feeding aromatic amino acids as replacement starter units to a mutant strain of the geldanamycin-producing microorganismvar.NRRL 3602, wherein the gene cluster encoding enzymes for the biosynthesis of the natural starter unit 3-amino-5-hydroxybenzoic acid has been deleted.

Macrolactams by engineered biosynthesis

Migrastatin and a migrastatin analog can be produced by fermentation ofNRRL 18993 and used in pharmaceutical formulations to treat cancer and/or inhibit metastasis of cancer cells.

Fermentation and purification of migrastatin and analog

This invention relates to compounds of formula (I) and to pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.

Epothilone derivatives and methods for making and using the same

This invention relates to compounds of formula (I)and to pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, W, X, Y, and Ar are as defined herein. Compounds of formula (I) are useful in the treatment of diseases or conditions characterized by cellular hyperproliferation. This invention also relates to means for the preparation of compounds of formula (I); formulations containing compounds of formula (I); and methods for the use of said compounds and formulations in the treatment of a disease or condition characterized by cellular hyperproliferation, including cancer.

Migrastatin and a migrastatin analog can be produced by fermentation of NRRL 18993 and used in pharmaceutical formulations to treat cancer and/or inhibit metastasis of cancer cells.

Epothilone compounds and methods for making and using the same

Fermentation based methods for producing mycolactones allows one to produce large quantities of mycolactones, which can be purified by extraction and chromatography to yield pure preparations of mycolactones A, B, C, and D.

Growing community of inventors

San Bruno, CA, United States of America

John R Carney