US 5,472,962 AGranted

Benzothiophene derivative

AssigneeTeikoku Hormone Mfg. Co., Ltd.

InventorsNaoyuki Koizumi, Shigehiro Takegawa, Shigeki Iwashita, Tomoko Kawachi, Teruaki Matsui, Mamoru Mieda, Hiroo Takahashi, Tomoyuki Saito, Kenyu Shibata

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Abstract

A benzothiophene derivative represented by the formula ##STR1## or a salt thereof has an excellent antiestrogenic activity, and is useful as a therapeutic agent of breast cancer, endometrial cancer, endometriosis, mastopathy, etc. This compound is characterized in that the 2-position (the substituent R.sup.2) of the benzothiophene nucleus is substituted by a halogen atom; a lower alkyl group; or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, acyloxy group or an oxo group.

Claims11

Dependent claims

A benzothiophene derivative represented by the following general formula or a salt thereof ##STR17## wherein R.sup.1 denotes a hydroxyl group, a lower alkoxy group, an acyloxy group or an N,N-di-lower alkyl-substituted or unsubstituted carbamoyloxy group,

R.sup.2 denotes a halogen atom;
a lower alkyl group;
or a cycloalkyl or cycloalkenyl group optionally substituted by a lower alkyl group, a hydroxyl group, an acyloxy group or an oxo group,
R.sup.3 and R.sup.4 each denote a hydrogen atom or a lower alkyl group, or R.sup.3 and R.sup.4 combine with the nitrogen atom to which they bind, to denote a heterocyclic ring which may further contain a hetero atom'selected from O, S and N,
A denotes O or CH.sub.2,
B denotes C.dbd.O or CH.sub.2, and
n denotes 1 or 2.

4 more elements

Dependencies are inferred from the claim text.