Abstract Gem-Dichlorocyclopropanes (Analog II derivatives) which demonstrate antiproliferative activity toward MCF-7 cells, in vitro and are generally not reversed by estradiol or having intrinsic estrogenicity (except the hydroxyphenyl derivative Compound 30). In general the cyclopropane compounds have the formula: <IMAGE> or any pharmaceutically acceptable salt thereof. X is selected from a group consisting of hydrogen and halogen atoms. The group R1 may be a hydrogen atom, an alkyl group, an acyl group, or an arylalkyl group. The group R2 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The group R3 may be a hydrogen atom, an alkyl group, a cycloalkyl group, a substituted aryl group or an unsubstituted aryl group. The group R4 may be a hydrogen atom, an unsubstituted aryl group or a substituted aryl group. The R4 is absent when R3 is a cycloalkyl group having a first position carbon and a terminal position carbon bonded to the same carbon of the cyclopropane. Further, no more than any two of R2, R3 and R4 has an aryl group.
A cyclopropane compound having the formula: ##STR23## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 2
Dependent Claim
62 words
A cyclopropane compound having the formula: ##STR23## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 3
Dependent Claim
10 words
The compound of claim 1 in which X is chlorine.
Claim 4
Dependent Claim
78 words
A composition of matter comprising a compound having the formula: ##STR24## or any pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound, in which: X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 5
Dependent Claim
78 words
A composition of matter comprising a compound having the formula: ##STR24## or any pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound, in which: X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane wherein the R 4 group is absent.
Claim 6
Independent Claim
76 words
A method of increasing uterine growth in a mammal comprising administering to the mammal an effective amount of one or more of the compounds having the formula: ##STR25## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane.
Claim 7
Independent Claim
76 words
A method of increasing uterine growth in a mammal comprising administering to the mammal an effective amount of one or more of the compounds having the formula: ##STR25## or any pharmaceutically acceptable salt thereof, in which X is a halogen atom; R 1 is a hydrogen; R 2 is a hydroxyphenyl; and R 3 is a cyclopentyl group having the first position carbon and the fifth position carbon bonded to the same carbon of the cyclopropane.
Claim 8
Dependent Claim
10 words
The method of claim 4 in which X is chlorine.
Claim 9
Dependent Claim
21 words
The method of claim 4 wherein the compound further comprises a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound.