abstract |
The present invention relates to novel benzopyran ER-β agonist compounds, pharmaceutical compositions thereof, and use of these compounds to treat a ER-β mediated disease such as nocturia, obstructive uropathy, benign prostatic hypertrophy, obesity, dementia, hypertension, incontinence, colon cancer, prostate cancer, infertility, depression, leukemia, inflammatory bowel disease, and arthritis. Formula (I), wherein G is -O-, -S(O)n, -CF2-, -C(O)-, -CR1H- or -CR2(OH)-; R is halo, (C1-C4)alkyl or R3-(CH2)m-; R1 is F, hydroxyl, cyano, trifluoromethyl, (C1-C4)alkyl, (C2-C4)alkenyl, (C2-C4)alkynyl, (C1-C4)alkoxy, (C1-C4)alkylcarbonyloxy or benzyl; R2 is trifluoromethyl or (C1-C4)alkyl; R3 is cyano, hydroxyl, (C2-C4)alkenyl, (C1-C4)alkoxy or (C1-C4)alkoxycarbonyl; n is 0, 1 or 2; and m is 0, 1 or 2; and pharmaceutically acceptable salts thereof. |