Patent ID: 6559181
Filing Date: 2003-05-06
Classification: A61P,C07C,C07D

Abstract:
A method to treat endometrial carcinoma, prostate cancer, or prostate hyperplasia comprising administering to a patient in need of such treatment an effective dose of a 3,4-Diphenyl-bicyclo[4.3.0]nonyl compound of formula I in whichR1 is optionally substituted C1-C20 alkanoyl, optionally substituted C1-C20 alkyl, optionally substituted C7-C20 aralkyl, optionally substituted C7-C15 aroyl, a group PG1 or a hydrogen atom, R2 is optionally substituted C1-C20 alkanoyl, optionally substituted C1-C20 alkyl, optionally substituted C7-C20 aralkyl, optionally substituted C7-C15 aroyl, a group PG2 or a hydrogen atom, PG1 and PG2 are the same or different and each is a protective group PG, â€ƒgroup (hydroxy=&agr; or; &bgr; epoxy=&agr; or &bgr;), X is a bond, an oxygen atom, a sulfur atom, SO or SO2, E is a straight-chain or branched-chain alkylene, alkenylene or alkynylene group with up to 15 carbon atoms, Y is F, Cl, Br, I, a substituent R4, an optionally substituted aryl or heteroaryl radical, or an NR4aR4bâ€”, SO2NR4aR4bâ€”, NR4a(CH2)pâ€”Qâ€”Gâ€”, NR5(CHR6â€”CHR7)â€”(CH2)tâ€”Qâ€”Gâ€”, SO2NR4a(CH2)pâ€”Qâ€”G, Oâ€”Gâ€”, Sâ€”Gâ€”, SOâ€”Gâ€”, or SO2â€”G group, R4 is a hydrogen atom, optionally substituted C1-C20 alkyl, partially or completely fluorinated C1-C20 alkyl, optionally substituted C1-C20 alkanoyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted C7-C20 aralkyl, or optionally substituted C7-C15 aroyl, Q is an oxygen atom, a sulfur atom, SO or SO2 G is â€”(CH2)nâ€”R3, n is 0 to 10, p is 1 to 10, t is 0, 1 or 2 R3 is hydrogen, a straight-chain or branched-chain alkyl, alkenyl or alkynyl group with up to 10 carbon atoms, a straight-chain or branched-chain, partially or completely fluorinated alkyl or alkenyl group with up to 10 carbon atoms, an optionally substituted C4-C8 cycloalkyl group, an optionally substituted aryl group, an optionally substituted C7-C20 aralkyl group or, if n>0, a hydroxy group or a halogen atom, R4a and R4b are the same or different and are R4 or together are a C3-C15 alkylene group, which can be straight-chain or branched, R5 is a hydrogen atom or a C1-5 alkyl group, R6 and R7 each is a hydrogen atom, or R5 and R6 together are an alkylene group â€”(CH2)dâ€” with d=2, 3, 4 or 5 and R7 is a hydrogen atom, or R5 and R7 together are an alkylene group â€”(CH2)eâ€” with e=2, 3 or 4 and R6 is a hydrogen atom, and Z is hydrogen, halogen, OH, N3, NH2, CO2H, CO2â€”(C1-C20)-alkyl, C1-C20 alkoxy, â€”NO2, â€”CN or C1-C20 acyloxy.