Estrogenic compounds as anti-angiogenic agents
First Claim
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1. 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. Ra -Ro are defined as follows;
A) each Ra, Rb, Rc, Rd, Re, Rf, Ri, Rj, Rk, RL, Rm, Ro, independently is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, or --I; and
Rg is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, --I, or --C.tbd.CH;
orB) each Ra, Rb, Rc, Rf, Rk, RL, Ro, independently is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, or --I; and
each Rd, Re, Ri, Rj, Rm, independently is ═
O, --R1, --OR1, --OCOR1, --SR1, --F, NHR2, --Br or --I; and
Rg is ═
O, --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --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 Rb, Rc, Rd, Re, Ri, Rj, Rk, RL, Rm and Ro is H;
Rf is --CH3 ;
Rg is --OH;
Z'"'"' is >
COH; and
Z" is >
CH2;
then Ra is not --H;
where, in each formula set forth above, each R1 and R2 independently is --H, or an alkyl, alkenyl or alkynl group of up to 6 carbons.
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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.
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7 Claims
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1. 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. Ra -Ro are defined as follows;A) each Ra, Rb, Rc, Rd, Re, Rf, Ri, Rj, Rk, RL, Rm, Ro, independently is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, or --I; and
Rg is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, --I, or --C.tbd.CH;
orB) each Ra, Rb, Rc, Rf, Rk, RL, Ro, independently is --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, or --I; and
each Rd, Re, Ri, Rj, Rm, independently is ═
O, --R1, --OR1, --OCOR1, --SR1, --F, NHR2, --Br or --I; and
Rg is ═
O, --R1, --OR1, --OCOR1, --SR1, --F, --NHR2, --Br, --I, or --C.tbd.CH; andII. 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 Rb, Rc, Rd, Re, Ri, Rj, Rk, RL, Rm and Ro is H;Rf is --CH3 ; Rg is --OH; Z'"'"' is >
COH; andZ" is >
CH2;then Ra is not --H; where, in each formula set forth above, each R1 and R2 independently is --H, or an alkyl, alkenyl or alkynl group of up to 6 carbons. - View Dependent Claims (2, 3, 4, 5, 6, 7)
- ##STR6## wherein;
Specification