abstract |
The instant invention provides novel benzothiophenencompounds of formula I,n nwherein:n R 1 is -H, -OH,n-O(C 1 -C 4 alkyl), -O-CO-(C 1 -C 6 alkyl),n-O-CO-O(C 1 -C 6 alkyl), -O-CO-Ar where Ar isnphenyl or optionally substituted phenyl, -O-CO-O-Ar where Ar is phenylnor optionally substituted phenyl, orn-OSO 2 -(C 4 -C 6 alkyl); R 2 is -H, -OH, -O(C 1 -C 4 alkyl),n-O-CO-(C 1 -C 6 alkyl),n-O-CO-O(C 1 -C 6 alkyl), -O-CO-Ar where Ar is phenyl ornoptionally substituted phenyl, -O-CO-O-Ar where Ar is phenyl ornoptionally substituted phenyl, -OSO 2 -(C 4 -C 6 nalkyl), -F-, -Cl, or Br; A isn B is -OCH 2 CH 2 NR 3 R 4 ; R 3 and R 4 each are independently C 1 -C 4 alkyl, orncombine to form, with the nitrogen to which they are attached,npiperidinyl, pyrrolidinyl, methylpyrrolidinyl, dimethylpyrrolidinyl, ornhexamethyleneimino; nββββor a pharmaceuticallynacceptable salt or solvate thereof for the inhibition of estrogenndeprivation, postmenopausal symptoms, particularly osteoporosis,ncardiovascular-related pathological conditions including hyperlipidemianand related cardiovascular pathologies, and estrogen-dependent cancer. |