NAPHTHYL AND DIHYDRONAPHTHYL INTERMEDIATES, COMPOUNDS, COMPOSITIONS, AND METHODS.

摘要

The present invention provides compounds of formula (I), wherein R1 is -H, -OH, -O(C1-C4 alkyl), -OCO6H5, -OCO(C1-C6 alkyl), or -OSO2(C4-C6 alkyl); R2 is C1-C6 alkyl or C5-C7 cycloalkyl which is optionally substituted with 1 to 3 substituents selected from the group consisting of C1-C4 alkyl, C1-C4 alkoxy, hydroxy, amino, nitro, and halo; X is -CH(OH)- or -CH2-; M is -CH2CH2- or -CH=CH-; n is 2 or 3; and R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidinyl, 4-morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Also provided are methods of using the compounds of the present invention for the treatment of various medical indications associated with post-menopausal syndrome, uterine fibroid disease, endometriosis, and aortal smooth muscle cell profiferation. The present invention further provides pharmaceutical compositions of compounds of formula (I), as well as intermediate compounds for the preparation thereof.