Diphenylcyclopropyl analogs as antiestrogenic and antitumor agents
AssigneeThe Board of Regents of the University of Oklahoma
InventorsRobert A. Magarian, Joseph T. Pento, Kwasi S. Avor
Life of this patent
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Abstract
Diphenylcyclopropyl analogs in which one or more of the phenyl rings includes substituents comprising a hydroxy group, a hydrogen atom, an acetate group or a substituted or unsubstituted alkoxy group. The compounds are useful as antiestrogens and antitumor agents.
Claims38
A compound having the formula:
- ##STR9## or any pharmaceutically acceptable salt thereof, in which:
- X is selected from a group consisting of,
- halogen atoms and
- hydrogen atoms;
- R.sub.1 is selected from a group consisting of,
- a hydrogen atom, and
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- R.sub.2 is selected from a group consisting of,
- a hydrogen atom, and
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- with the proviso that R1 and R2 cannot be simultaneously hydrogen.
A composition of matter comprising a compound having the formula:
- ##STR10## or any pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier of sufficient quantity to solubilize the compound, in which:
- X is selected from a group consisting of,
- halogen atoms and
- hydrogen atoms;
- R.sub.1 is selected from a group consisting of,
- a hydrogen atom,
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- R.sub.2 is selected from a group consisting of,
- a hydrogen atom,
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- with the proviso that R1 and R2 cannot be simultaneously hydrogen.
A method of inducing antiestrogenic activity in a mammal in need of such therapy comprising administering to the mammal an antiestrogenically effective amount of one or more compounds having the formula:
- ##STR11## or any pharmaceutically acceptable salt thereof, in which:
- X is selected from a group consisting of,
- halogen atoms and
- hydrogen atoms;
- R.sub.1 is selected from a group consisting of,
- a hydrogen atom,
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- R.sub.2 is selected from a group consisting of,
- a hydrogen atom,
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms, and
- with the proviso that R1 and R2 cannot be simultaneously hydrogen.
A method of inhibiting the development of an estrogen-dependent tumor in a mammal in need of such therapy comprising administering to the mammal an effective amount of one or more compounds having the formula:
- ##STR12## or any pharmaceutically acceptable salt thereof, in which:
- X is selected from a group consisting of,
- halogen atoms and
- hydrogen atoms;
- R.sub.1 is selected from a group consisting of,
- a hydrogen atom,
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- R.sub.2 is selected from a group consisting of,
- a hydrogen atom,
- a substituted alkoxy group in which the substituent of the alkoxy group is selected from a group consisting of,
- an unsubstituted piperazine, and
- a substituted piperazine in which the substituent is an alkyl group containing from 1 to 6 carbon atoms;
- and
- with the proviso that R1 and R2 cannot be simultaneously hydrogen.
Dependencies are inferred from the claim text.