US 6,982,351 B2
Cycloalkyl substituted polyamines for cancer therapy and methods of synthesis therefor
Benjamin Frydman, Madison, Wis. (US); Aldonia L. Valasinas, Madison, Wis. (US); Andrei V. Blokhin, Fitchburg, Wis. (US); Aparajita Sarkar, Madison, Wis. (US); Hirak S. Basu, Madison, Wis. (US); Venodhar K. Reddy, Madison, Wis. (US); Laurence J. Marton, Palo Alto, Calif. (US); and Yu Wang, Madison, Wis. (US)
Assigned to CellGate, Inc., Redwood City, Calif. (US)
Filed on Dec. 06, 2002, as Appl. No. 10/313,530.
Claims priority of provisional application 60/339205, filed on Dec. 07, 2001.
Prior Publication US 2003/0195377 A1, Oct. 16, 2003
Int. Cl. C07C 211/17 (2006.01)
U.S. Cl. 564—453 11 Claims
 
1. 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.