Selective androgen receptor modulators and methods of use thereof

摘要

Selective androgen receptor modulator propanamide derivatives (I) are new. Selective androgen receptor modulator propanamide derivatives of formula (I) are new. X : O, CH 2, NH, Se, PR or NR; Z : NO 2, CN, COR, COOH or CONHR; Y : I, CF 3, Br, Cl or SnR 3; Q : alkyl, H, NR 2, NHCOCH 3, NHCOCF 3, NHCOR, NHCONHR, NHCCOR, OCONHR, CONHR, NHCSCH 3, NHCSCF 3, NHCSR, NHSO 2CH 3, NHSO 2R, OR, COR, OCOR, OSO 2R, SO 2R or SR; or Q : a fused ring of formula (i)-(iii); R : alkyl, aryl, 1-4C (halo)alkyl, phenyl, halo, alkenyl or OH; R 1 : CH 3, CF 3, CH 2CH 3or CF 2CF 3; and T : OH, OR, NHCOCH 3or NHCOR. Independent claims are included for: (1) a method of modulating spermatogenesis comprising administration of (I); (2) a method of hormone therapy comprising administration of (I); (3) a method of treating hormone related conditions comprising administration of (I); and (4) a method of treating prostate cancer comprising administration of (I). [Image] [Image] ACTIVITY : Cytostatic. MECHANISM OF ACTION : Androgen receptor modulator. In vitroactivity of the selective androgen receptor modulator compounds (I) was determined. N-[4-nitro-3-trifluoromethyl)-phenyl]-(2S)-3-[4-(acetylamino)-phenoxy]-2-hydroxy-2-methylpropanamide (Ia) bound to the androgen receptor with a K ivalue of 7.5 nM.