| abstract |
(57) [Summary] (Modified) [Purpose] With respect to benzothiophene derivatives known to have anti-estrogen activity, by converting the substituent at the 2-position, the anti-estrogen activity is retained and the estrogen activity is weak. Provide an anti-estrogen agent. [Structure] A benzothiophene derivative represented by the general formula (I) or a salt thereof, and a compound of the general formula (II) which is an intermediate for producing the derivative. [In the formulas (I) and (II), R 1 represents H, OH, a lower alkoxy group, an acyloxy group or a (N-substituted) carbamoyloxy group; R 2 represents a halogen atom, a lower alkyl group, or a (substituted) ) Cycloalkyl group, (substituted cycloalkenyl group; R 3 and R 4 are lower alkyl groups, or a heterocyclic group together with the nitrogen atom to which they are bonded; R 11 is hydrogen atom, lower An alkoxy group; A is O, CH 2 ; B represents CO, CH 2 ; n represents 1, 2] [Effect] The compound of the formula (I) has an excellent anti-estrogen action, and is useful for breast cancer, endometrial cancer, mastopathy, etc. It is useful as a therapeutic agent for |