6-substituted estradiol derivatives and methods of use

Details 6-substituted estradiol derivatives and methods of use 6-substituted estradiol derivatives and methods of use

C - Chemistry, Metallurgy

07

J

C07J 1/00 (2006.01) A61K 31/56 (2006.01) A61K 31/565 (2006.01) A61K 31/566 (2006.01)

Patent

CA 2726364

wherein R1 and Z are as descpbed above, X is selected from the group consisting of C1 -C6 alkyl, a substituted alkyl, a halogen, a halogenated alkyl, a glucoronide, - NH2, -SO2NH2, COOH, -CN, -CH2CN, -NHCN, -CHO, -COOsalt, -0S02alkyl, -SH, SCH3 -CH (CH2) nCOOCH3, - (CH2) n-O-CH3, -CH2OH, - (CH2) n-O-NH2, NH (CH2) nCH3, NH (CH2) nOCH3, - NH (CH2) nCHOH- COOH, - N (CH3) 2, 10 (CH2)n(NH)CH2OH, -NHCOOH, -(CH2)nNHCOOH, -N02, -SCN, -SO2alkyl, -B (OH) 2, - (CH2) nN (CH3) -S02 NH3, - (CH2) nNH-S02-NH2, -NHC (=S) CH3, and -NHNH2, R3 is selected from the group consisting of H, a C1-C6 alkyl, a substituted alkyl, a halogen, and ahalogenated alkyl, R4 and Y are independently selected from a group consisting of O, -OH, -H, a -C1-C6 alkyl, a substituted alkyl, a halogen, a halogenated alkyl, a sulfate, a glucoronide, a bulky group, a phenyl or a substituted phenyl group, a cyclo- or heterocyclo group, pipepdine, piperazine, morpholine, pypmidine, -NH2, 20 N(CH2)n CH3 etc, and the respective epantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds.

Selon la présente invention, R1 et Z sont comme décrit ci-dessus, X est choisi dans le groupe constitué dun alkyle en C1-C6, un alkyle substitué, un halogène, un alkyle halogéné, un glucoronide, -NH2, -SO2NH2, COOH, -CN, -CH2CN, -NHCN, -CHO, -COO(sel), -OSO2-alkyle, -SH, SCH3-CH(CH2)nCOOCH3, -(CH2)n-O-CH3, -CH2OH, -(CH2)n-O-NH2, NH(CH2)nCH3, NH(CH2)nOCH3, -NH(CH2)nCHOH-COOH, -N(CH3)2, (CH2)n(NH)CH2OH, -NHCOOH, -(CH2)nNHCOOH, -NO2, -SCN, -SO2-alkyle, -B(OH)2, -(CH2)nN(CH3)-SO2NH3, -(CH2)nNH-SO2-NH2, -NHC(=S)CH3, et -NHNH2, R3 est choisi dans le groupe constitué de H, un alkyle en C1-C6, un alkyle substitué, un halogène, et un alkyle halogéné, R4 et Y sont indépendamment choisis dans le groupe constitué de O, -OH, -H, -(alkyle en C1-C6), un alkyle substitué, un halogène, un alkyle halogéné, un sulfate, un glucoronide, un groupe volumineux, un phényle ou un groupe phényle substitué, un groupe cyclo ou hétérocyclo, la pipéridine, la pipérazine, la morpholine, la pyrimidine, -NH2, 20 N(CH2)nCH3, etc., et les énantiomères respectifs, les autres isomères stéréochimiques, les hydrates, les solvates, les tautomères et les sels pharmaceutiquement acceptables desdits composés.

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