University of California

Mgi Pharma, Inc.

Trevor C McMorris

Michael J Kelner

Raymond Taetle

John R Donaubauer

The present invention provides illudin analogs of the general formula (I): 

Illudin analogs useful as antitumor agents

Acylfulvene analogs, which inhibit tumor growth, especially solid tumor growth, and which have an adequate therapeutic index to be effective for in vivo treatment are provided herein. The compounds described herein are useful as anti-neoplastic agents, i.e., to inhibit tumor cell growth in vitro or in vivo, in mammalian hosts, such as humans or animals, e.g., domestic animals, and are effective against solid tumors, hematologic malignancies and multi-drug resistant cancers/tumors. The present compounds can be used alone or they can be used in combination with one or more anti-cancer or anti-tumor agents.

Illudin analogs useful as anticancer agents

The present invention provides compounds of the general formula I: wherein R, R, R, R, R, and Rhave any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Antitumor agents

The present invention provides compounds of general formula I or II: wherein R, R, R, R, R, R, and Rhave any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.

The present invention provides illudin analogs of the general formula (I):

The present invention provides compounds of general formula I or II:wherein R, R, R, R, R, R, and Rhave any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.

The present invention provides illudin analogs of the general formula I:wherein R, R, R, R, R, and Rhave any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Total synthesis of antitumor acylfulvenes

The present invention provides illudin analogs of the general formula I:

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La Jolla, CA, United States of America

Trevor C McMorris