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US 6,982,351 B2Granted
Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor
AssigneeCellgate, Inc.
InventorsBenjamin Frydman, Aldonia L. Valasinas, Andrei V. Blokhin, Aparajita Sarkar, Hirak S. Basu, Venodhar K. Reddy, Laurence J. Marton, Yu Wang
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Abstract
Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
Claims11
A compound of the formula:
- E-NH-B-A-B-NH-B-A-B-NH-B-A-B-NH(-B-A-B-NH)x-E
- wherein A is independently selected from the group consisting of a single bond, C2-C6 alkyl, C2-C6 hydroxyalkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C6 cycloalkyl, C3-C6 cycloaryl, and C3-C6 cycloalkenyl;
- B is independently selected from the group consisting of a single bond, C1-C6 alkyl, C1-C6 hydroxyalkyl, and C2-C6 alkenyl;
- E is independently selected from the group consisting of H, C1-C6 alkyl, C1-C6 hydroxyalkyl, C2-C6 alkenyl, and C2-C6 alkynyl;
- and
- x is an integer from 1 to 16;
- with the proviso that at least one A moiety is cyclopropyl, and that each -B-A-B- subunit contains at least two carbon atoms;
- and all salts and stereoisomers thereof.
5 more elements
Dependencies are inferred from the claim text.