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Title:
STEREOSELECTIVE PROCESS AND CRYSTALLINE FORMS OF A CAMPTOTHECIN
Document Type and Number:
WIPO Patent Application WO2006067092
Kind Code:
A3
Abstract:
A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]- camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.

Inventors:
CARMINATI PAOLO (IT)
TINTI MARIA ORNELLA (IT)
MARZI MAURO (IT)
GIORGI FABRIZIO (IT)
CABRI WALTER (IT)
ALPEGIANI MARCO (IT)
VERGANI DOMENICO (IT)
GHETTI PAOLO (IT)
Application Number:
PCT/EP2005/056849
Publication Date:
November 02, 2006
Filing Date:
December 16, 2005
Export Citation:
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Assignee:
SIGMA TAU IND FARMACEUTI (IT)
CARMINATI PAOLO (IT)
TINTI MARIA ORNELLA (IT)
MARZI MAURO (IT)
GIORGI FABRIZIO (IT)
CABRI WALTER (IT)
ALPEGIANI MARCO (IT)
VERGANI DOMENICO (IT)
GHETTI PAOLO (IT)
International Classes:
C07D491/22
Domestic Patent References:
WO2003074527A12003-09-12
Foreign References:
EP1044977A12000-10-18
Other References:
DALLAVALLE S ET AL: "Novel 7-Oxyiminomethyl Derivatives of Camptothecin with Potent in Vitro and in Vivo Antitumor Activity", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 44, no. 20, 9 May 2001 (2001-05-09), pages 3264 - 3274, XP002307863, ISSN: 0022-2623
CAIRA M R: "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY, SPRINGER, BERLIN, DE, vol. 198, 1998, pages 163 - 208, XP001156954, ISSN: 0340-1022
ROSSI ET AL.: "structural studies on ST1481...", ACTA CRYST., vol. a61, August 2005 (2005-08-01), pages C275, XP002388924
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