The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Jun. 11, 1996

Filed:

Oct. 25, 1994
Applicant:
Inventors:

Samuel J Danishefsky, New Haven, CT (US);

Lawrence B Snyder, New York, NY (US);

Assignee:
Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ; A61K / ;
U.S. Cl.
CPC ...
546 48 ; 536 174 ;
Abstract

Substituted analogues of camptothecin possessing cytotoxic activity towards cancer cells, of the general structure: ##STR1## wherein E is H, CO.sub.2 R, CONH.sub.2, CONHR, CONR.sub.2, or CN; R.sup.0 and R.sup.1 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.2, R.sup.3 and R.sup.4 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl, hydroxyalkyl or aryl group; R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are independently the same or different and are H, or a linear or branched alkyl, linear or branched alkylaryl or aryl group, or an alkoxy, aryloxy, hydroxyalkyl, C-glycal, nitro, cyano or aminoalkoxy group, or CO.sub.2 R, Cl, F, Br, I, SR.sup.10, NR.sup.11 R.sup.12 or OR.sup.13 ; R is H, an alkyl, aryl, alkylaryl or hydroxyalkyl group; R.sup.10, R.sup.11 and R.sup.12 are independently the same or different and are H, an alkyl, aryl, alkylaryl or acyl group; R.sup.13 is glycosyl; and n is 0 or 1. Also provided are compositions comprising the analogues and methods of treating tumors as well as methods for preparing the analogues.


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