Estrogenic compounds as anti-mitotic agents
First Claim
Patent Images
1. A compound of the formula:
- ##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;
A) Z'"'"' is X, where X is ##STR7## or B) Z'"'"' is ##STR8## where Rn is --R1, --OR1, --SR1, --F, --NHR2, --Br or --I; and
X'"'"' is X, as defined above;
or X'"'"' is >
C═
O; and
III. Z" is defined as follows;
A) Z" is Y, where Y is ##STR9## B) Z" is ##STR10## where Rp is --R1, OR1, --SR1, --F, --NHR2, --Br or --I and Y is defined as in III(A);
IV. provided that when each Rb, Rc, Rk, RL, and Rm is --H, and each Rd, Re, and Rj is --H2 ;
Rf is --CH3 ;
Rg is --OH;
or ##STR11## Ri is --H, --OH, or ═
O;
Ro is --H or --Br;
Z'"'"' is >
COH; and
Z" is >
CH2 or >
CHOH;
thenRa is not --F, --Br, --OH or --H; and
V. provided that when each Rb, Rc, and Rk, RL, is --H, and each Rd, Re, Ri, and Rm is --H2 ;
Rf is --CH3 ;
Rg is --OH; and
Z" is >
CH2 ;
thenZ'"'"' is not >
COCH3 ; and
each Ra, Ro independently is not --OCH3 or --H; and
VI. provided that when each Rc, Rk, RL, and Ro is --H, and each Re, Rj, and Rm is --H2 ;
Ra is --H or --OCH3,Rb is --H or --CH3,Rd is --OH;
Rf is --CH3 ;
Rg is ═
O;
Ri is --OH, ═
O or --C.tbd.CH; and
Z" is >
CH2 ;
thenZ'"'"' is not >
COH;
##STR12## or --H; and
VII. provided that when each Rb, Rc, Rk, RL, and Ro is --H, and each Rd, Re, Ri, Rj, and Rm is --H2 ;
Ra is --OCH3 ;
Rf is --CH3 ;
Rg is --OH; and
Z" is >
CH2 ;
thenZ'"'"' is not >
COH; and
VIII. provided that when each Ra, Rb, Rc, Rk, RL, and Ro is --H, and each Rd, Re, Ri, Rj, and Rm is --H2 ;
Rf is --CH3 ;
Rg is ═
O; and
Z" is >
CH2 ;
thenZ'"'"' is not >
COH;
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 abnormal cell mitosis 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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Citations
3 Claims
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1. A compound of the formula:
- ##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; A) Z'"'"' is X, where X is ##STR7## or B) Z'"'"' is ##STR8## where Rn is --R1, --OR1, --SR1, --F, --NHR2, --Br or --I; and
X'"'"' is X, as defined above;
or X'"'"' is >
C═
O; andIII. Z" is defined as follows; A) Z" is Y, where Y is ##STR9## B) Z" is ##STR10## where Rp is --R1, OR1, --SR1, --F, --NHR2, --Br or --I and Y is defined as in III(A); IV. provided that when each Rb, Rc, Rk, RL, and Rm is --H, and each Rd, Re, and Rj is --H2 ; Rf is --CH3 ; Rg is --OH;
or ##STR11## Ri is --H, --OH, or ═
O;
Ro is --H or --Br;Z'"'"' is >
COH; andZ" is >
CH2 or >
CHOH;
thenRa is not --F, --Br, --OH or --H; and V. provided that when each Rb, Rc, and Rk, RL, is --H, and each Rd, Re, Ri, and Rm is --H2 ; Rf is --CH3 ; Rg is --OH; and Z" is >
CH2 ;
thenZ'"'"' is not >
COCH3 ; andeach Ra, Ro independently is not --OCH3 or --H; and VI. provided that when each Rc, Rk, RL, and Ro is --H, and each Re, Rj, and Rm is --H2 ; Ra is --H or --OCH3, Rb is --H or --CH3, Rd is --OH; Rf is --CH3 ; Rg is ═
O;Ri is --OH, ═
O or --C.tbd.CH; andZ" is >
CH2 ;
thenZ'"'"' is not >
COH;
##STR12## or --H; and
VII. provided that when each Rb, Rc, Rk, RL, and Ro is --H, and each Rd, Re, Ri, Rj, and Rm is --H2 ;Ra is --OCH3 ; Rf is --CH3 ; Rg is --OH; and Z" is >
CH2 ;
thenZ'"'"' is not >
COH; andVIII. provided that when each Ra, Rb, Rc, Rk, RL, and Ro is --H, and each Rd, Re, Ri, Rj, and Rm is --H2 ; Rf is --CH3 ; Rg is ═
O; andZ" is >
CH2 ;
thenZ'"'"' is not >
COH;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)
- ##STR6## wherein;
Specification