Benzothiophene compounds and methods of use

摘要

The instant invention provides novel benzothiophene compounds of formula I, <CHEM> wherein: R1 is -H, -OH, -O(C1-C4 alkyl), -O-CO-(C1-C6 alkyl), -O-CO-O(C1-C6 alkyl), -O-CO-Ar where Ar is phenyl or optionally substituted phenyl, -O-CO-O-Ar where Ar is phenyl or optionally substituted phenyl, or -OSO2-(C4-C6 alkyl); R2 is -H, -OH, -O(C1-C4 alkyl), -O-CO-(C1-C6 alkyl), -O-CO-O(C1-C6 alkyl), -O-CO-Ar where Ar is phenyl or optionally substituted phenyl, -O-CO-O-Ar where Ar is phenyl or optionally substituted phenyl, -OSO2-(C4-C6 alkyl), -F-, -Cl, or Br; A is <CHEM> B is -OCH2CH2NR3R4; R3 and R4 each are independently C1-C4 alkyl, or combine to form, with the nitrogen to which they are attached, piperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, or hexamethyleneimino; or a pharmaceutically acceptable salt or solvate thereof for the inhibition of estrogen deprivation, postmenopausal symptoms, particularly osteoporosis, cardiovascular-related pathological conditions including hyperlipidemia and related cardiovascular pathologies, and estrogen-dependent cancer.