Triphenylethylene derivatives similar to tamoxifen or toremifene derivatives

摘要

A method of preventing conception in a female mammal by administrating a compound of the Formula I. The compound of Formula I is also useful in the treatment of estrogen-stimulated cancer, benign proliferative disorders, Alzheimer's disease, macular degeneration, urinary incontinence or Type II diabetes. Wherein; R1 is -(CH2)nCR5=CR6R7, -(CH2)mC(X)NR8R9 or Formula II; R2 and R3 are independently H, -CH3, OH, OCH3, -OCH2CH3 or -CH(CH3)2; R4 is -CN, -NO2, -CH3, -CH2CH3, -CH2CH2-Y or -Y; R5 and R6 are independently H, -C1-4alkyl, -C2-4alkenyl, -C2-4alkynyl, -X-C1-3alkyl, -X-C2-4alkenyl, -X-C2-4alkynyl or -Y; R7 is -CN, -C1-4alkyl-OH, -C(O)NR10R11, -C(O)NR12R13, -C1-4alkyl-NR10R11, -C(O)R12, -C(O)OR12, -C(O)NR12OR13, -C(O)NHC(O)R12, -C(O)NHCH2R12, -S(O)(O)(OR12), -S(O)(O)(NHCO2R12), PO3R12, -P(O)(NR12R13)(NR12R13), -P(O)(NR12R13)(OR14), -CONR12(CH2)qOCH3, -CONR12(CH2)qNR3R9oxadiazole, substituted with methyl; R8 and R9 are independently hydrogen, -C1-7alkyl, -C3-7cycloalkyl, -O-C1-7alkyl, C1-7alkyl-Y or phenyl; R10 and R11 are independently methyl or ethyl or taken together form a morpholino group bonded via its nitrogen atom; R12, R13 and R14 are independently H, -C1-12alkyl, -C2-12alkenyl, -C2-12alkynyl, -O-C1-12alkyl, -O-C2-12alkenyl, -O-C2-12alkynyl, C3-7cycloalkenyl, -C3-7cycloalkenyl linear and cyclic heteroalkyl, aryl, heteroaryl or -Y; X is oxygen or sulphur; Y is a halogen; n is an integer selected from 0, 1 or 2; m is an integer 1 or 2; p is an integer selected from 1-4; and q is an integer from 1-12.