Estrogenic compounds as anti-angiogenic agents
AssigneeChildren's Medical Center Corporation
InventorsRobert J. D'Amato, Moses J. Folkman
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Abstract
The application discloses methods of treating mammalian diseases characterized by undesirable angiogenesis by administering estradiol derivatives including those comprising colchicine or combretastatin A-4 structural motifs of the general formulae found below in a dosage sufficient to inhibit cell mitosis. The application discloses novel compounds used in the methods.
Claims7
A method for treating a mammalian disease characterized by undesirable angiogenesis, said method comprising administering to a mammal having said undesirable angiogenesis a compound of the formula below, said compound being administered in an amount sufficient to inhibit angiogenesis:
- ##STR6## wherein:
- I. R.sub.a -R.sub.o are defined as follows:
- A) each R.sub.a, R.sub.b, R.sub.c, R.sub.d, R.sub.e, R.sub.f, R.sub.i, R.sub.j, R.sub.k, R.sub.L, R.sub.m, R.sub.o, independently is --R.sub.1, --OR.sub.1, --OCOR.sub.1, --SR.sub.1, --F, --NHR.sub.2, --Br, or --I;
- and R.sub.g is --R.sub.1, --OR.sub.1, --OCOR.sub.1, --SR.sub.1, --F, --NHR.sub.2, --Br, --I, or --C.tbd.CH;
- or
- B) each R.sub.a, R.sub.b, R.sub.c, R.sub.f, R.sub.k, R.sub.L, R.sub.o, independently is --R.sub.1, --OR.sub.1, --OCOR.sub.1, --SR.sub.1, --F, --NHR.sub.2, --Br, or --I;
- and each R.sub.d, R.sub.e, R.sub.i, R.sub.j, R.sub.m, independently is .dbd.O, --R.sub.1, --OR.sub.1, --OCOR.sub.1, --SR.sub.1, --F, NHR.sub.2, --Br or --I;
- and R.sub.g is .dbd.O, --R.sub.1, --OR.sub.1, --OCOR.sub.1, --SR.sub.1, --F, --NHR.sub.2, --Br, --I, or --C.tbd.CH;
- and
- II. Z' is defined as follows:
- Z' is X, where X is ##STR7## and III. Z" is defined as follows:
- Z" is Y, where Y is ##STR8## where n is 0-6;
- and IV. provided that when each R.sub.b, R.sub.c, R.sub.d, R.sub.e, R.sub.i, R.sub.j, R.sub.k, R.sub.L, R.sub.m and R.sub.o is H;
- R.sub.f is --CH.sub.3 ;
- R.sub.g is --OH;
- Z' is >COH;
- and
- Z" is >CH2;
- then R.sub.a is not --H;
- where, in each formula set forth above, each R.sub.1 and R.sub.2 independently is --H, or an alkyl, alkenyl or alkynl group of up to 6 carbons.
Dependencies are inferred from the claim text.