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US 4,133,814 AGranted
2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
AssigneeEli Lilly and Company
InventorsC. David Jones, Tulio Suarez
Life of this patent
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Abstract
Derivatives of 2-phenyl-3-aroylbenzothiophenes and 2-phenyl-3-aroylbenzothiophene-1-oxides are useful as antifertility agents. Certain of these compounds also are useful in suppressing the growth of mammary tumors.
Claims10
A compound of the formula ##STR57## in which R is hydroxyl;
- R.sub.1 is hydrogen, hydroxyl, C.sub.1 -C.sub.5 alkoxy, or ##STR58## R.sub.2 is hydrogen;
- and R.sub.3 and R.sub.4 independently are C.sub.1 -C.sub.4 alkyl, or R.sub.3 and R.sub.4 taken together with the nitrogen to which they are bonded constitute a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, or morpholino;
- and pharmaceutically acceptable non-toxic acid addition salts of those compounds in which R.sub.1 is ##STR59##
A compound of the formula ##STR60## in which R is hydrogen, hydroxyl, or C.sub.1 -C.sub.5 alkoxy;
- R.sub.1 is hydrogen, C.sub.1 -C.sub.5 acyloxy, C.sub.1 -C.sub.5 alkoxycarbonyloxy, benzoyloxy, adamantoyloxy, chloro, bromo, or ##STR61## R.sub.2 is hydroxyl;
- and R.sub.3 and R.sub.4 independently are C.sub.1 -C.sub.4 alkyl, or R.sub.3 and R.sub.4 taken together with the nitrogen to which they are bonded constitute a heterocyclic ring selected from the group consisting of pyrrolidino, piperidino, hexamethyleneimino, or morpholino;
- and pharmaceutically acceptable non-toxic acid addition salts of those compounds in which R.sub.1 is ##STR62##
A compound of the formula ##STR63## in which R is hydroxyl;
- R.sub.1 is hydroxyl;
- and R.sub.2 is C.sub.1 -C.sub.5 alkoxy.
A compound of the formula ##STR64## in which R is hydrogen, hydroxyl, or C.sub.1 -C.sub.5 alkoxy;
- R.sub.1 is hydroxyl;
- and R.sub.2 is ##STR65## in which R.sub.3 and R.sub.4 taken together with the nitrogen to which they are bonded constitute a pyrrolidino ring;
- and pharmaceutically acceptable non-toxic acid addition salts of such compounds.
Dependencies are inferred from the claim text.