Title:
ANALOGS OF SALINOSPORAMIDE A
Document Type and Number:
WIPO Patent Application WO2005099687
Kind Code:
A3
Abstract:
Disclosed herein are analogs of Salinosporamide A, having the Formulae Ia - IVa as follows: [insert chemical formula here] Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.
Inventors:
COREY ELIAS J (US)
Application Number:
PCT/US2005/012113
Publication Date:
December 29, 2005
Filing Date:
April 11, 2005
Export Citation:
Assignee:
HARVARD COLLEGE (US)
COREY ELIAS J (US)
COREY ELIAS J (US)
International Classes:
A61K31/407; C07C229/30; C07D263/10; C07D491/044; C07D491/10; C07F7/02; (IPC1-7): C07D491/044; C07C229/30; C07D263/10; C07D491/10; C07F7/02
Domestic Patent References:
| WO2004071382A2 | 2004-08-26 | |||
| WO2005002572A2 | 2005-01-13 | |||
| WO2002094311A1 | 2002-11-28 |
Foreign References:
| US20040138196A1 | 2004-07-15 |
Other References:
COREY E. AND REICHARD G.: "Total Synthesis of Lactacystin", J.AMER.CHEM.SOC., vol. 114, no. 26, December 1992 (1992-12-01), pages 10677 - 10678, XP002062061
COREY E. AND WEI-DONG Z.: "An Efficient Total Synthesis of a New and Highly Active Analog of Lactacystin", TETRAHEDRON LETTERS, vol. 39, no. 41, October 1998 (1998-10-01), pages 7475 - 7478, XP004134329
PANEK J. AND MASSE C.: "Total Synthesis of (+)-Lactacystin", ANGEW. CHEM. INT. ED., vol. 38, no. 8, April 1999 (1999-04-01), pages 1093 - 1095, XP002992366
SOUCY F. ET AL: "A Novel and Efficient Synthesis of a Highly Active Analogue of clasto-Lactacystin Beta-Lactone", vol. 121, no. 43, November 1999 (1999-11-01), pages 9967 - 9976, XP001105956
CRANE S. AND COREY E.: "A Novel Enantioselective Synthetic Route to Omuralide Analogues with the Potential for Species Selectivity in Proteasome Inhibition", vol. 3, no. 9, May 2001 (2001-05-01), pages 1395 - 1397, XP008038134
SARAVANAN P. AND COREY E.: "A Short, Stereocontrolled, and Practical Synthesis of Alpha-Methylomuralide, a Potent Inhibitor of Proteasome Function", J. ORG. CHEM., vol. 68, no. 7, 4 April 2003 (2003-04-04), pages 2760 - 2764, XP002992367
COREY E. AND WEI-DONG Z.: "An Efficient Total Synthesis of a New and Highly Active Analog of Lactacystin", TETRAHEDRON LETTERS, vol. 39, no. 41, October 1998 (1998-10-01), pages 7475 - 7478, XP004134329
PANEK J. AND MASSE C.: "Total Synthesis of (+)-Lactacystin", ANGEW. CHEM. INT. ED., vol. 38, no. 8, April 1999 (1999-04-01), pages 1093 - 1095, XP002992366
SOUCY F. ET AL: "A Novel and Efficient Synthesis of a Highly Active Analogue of clasto-Lactacystin Beta-Lactone", vol. 121, no. 43, November 1999 (1999-11-01), pages 9967 - 9976, XP001105956
CRANE S. AND COREY E.: "A Novel Enantioselective Synthetic Route to Omuralide Analogues with the Potential for Species Selectivity in Proteasome Inhibition", vol. 3, no. 9, May 2001 (2001-05-01), pages 1395 - 1397, XP008038134
SARAVANAN P. AND COREY E.: "A Short, Stereocontrolled, and Practical Synthesis of Alpha-Methylomuralide, a Potent Inhibitor of Proteasome Function", J. ORG. CHEM., vol. 68, no. 7, 4 April 2003 (2003-04-04), pages 2760 - 2764, XP002992367
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