Treating estrogen deficiency associated disorders, e.g. menopausal problems, osteoporosis, neoplasia or neurodegenerative disease, using new or known ent-steroids having bone-selective estrogenic activity

摘要

The use of ent-steroids (I) for treating estrogen deficiency-associated diseases and states in females or males is new. Most compounds (I) are new. The use of ent-steroids of formula (I) is claimed for treating estrogen deficiency-associated diseases and states in females or males. R1 = H, OR12 or OSO2R13; R12 = H or 1-5C hydrocarbyl (optionally containing a C-C double or triple bond); R13 = NR14R15; R14, R15 = H, 1-5C alkyl or COR16; or NR14R15 = pyrrolidone, piperidino, homopiperidino or morpholino; R16 = 1-12C hydrocarbyl (optionally containing a C-C double or triple bond), 3-7C cycloalkyl, aryl or a combination of these moieties; R2 = OR12, OSO2R13 or OCOR16; R3-R5, R8, R9 = H, halo, OR12, OSO2R13 or R16; R6 = beta -H and R7 = H; or R6 + R7 = alpha - or beta -CH2; R10 = H2, dihalo, (H, halo), CR17R18, (H, OR12), H, OSO2R13), (R12, OCOR16), (R12, OH) or O; R17, R18 = H or halo; R11 = H, Me or Et; one or more double bond(s) may be present in the 6(7), 7(8), 8(9), 9(11), 11(12), 8(14), 14(15), 15(16) and/or 16(17) position(s). Independent claims are included for: (a) (I) as new compounds, with the exception of ent-estradiol, ent-estradiol-3-acetate, ent-estradiol-17-acetate, ent-estradiol-dicetate, ent-estrone, ent-estrone acetate, ent-estradiol-3-benzoate, ent-17 alpha -ethinyl-estra-1,3,5(10)-triene-3,17-diol, ent-17 alpha -ethinyl-estra-1,3,5(10)-triene-3,17-diyl diacetate, ent-3-hydroxy-estra-1,3,5(10),7-tetraen-17-one, ent-3-hydroxy-estra-1,3,5(10),6,8-pentaen-17-one and ent-16 beta -3-methoxy-estra-1,3,5(10)-trien-17-one; and (b) the use of the (8 alpha , 9 beta , 10 alpha , 13 alpha , 14 beta )-gonane partial structure as a component of the total structure of compounds showing dissociation towards estrogenic action in the bones relative to that on the uterus.