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6-SUBSTITUTED ESTRADIOL DERIVATIVES AND METHODS OF USE
专利权人:
LLC;Endece
发明人:
YARGER, James G.
申请号:
AU2016238850
公开号:
AU2016238850A1
申请日:
2016.10.05
申请国别(地区):
AU
年份:
2016
代理人:
摘要:
#$%^&*AU2016238850A120161020.pdf#####Abstract Disclosed are compounds of the formula: Y R, R4 R2 X wherein R1 , R2 , R3 and R4 are independently hydrogen, CI-C, alkyl, halo, a sulfate, a glucuronide, -OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N(CH2),; a phosphate group, and a phosphinate group; R, is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1 -Cg alkyl, halogen, a sulfate, a glucoronide, -SO2NH-, -COOH, -CN, -CH 2 CN-, -NHCN-, -CHO, =CHOCH3 , -COO salt, -OSO 2 alkyl, -NH 2 , and -NHCO (CH2),; R1 2 is selected from the group consisting of H, a C1-C6 alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of Ci-C2 alkyl, C2-C1 2 alkenyl, C2 -C1 2 alkynyl, halogen, a glucoronide, -NH2, SO 2NH 2 , -COOH, -CN, -CH 2CN, -NHCN, -CHO, -COOsalt, -OSO 2 alkyl, -SH, -SCH 3 , -CH [ (CH2)nCH3] COOCH 3 , - (CH2)mCOOCH3, - (CH2) m-O-CH 3 , - (CH2 ) m-0- (CH2) nCH 3 , (CH 2 ) m-S-CH3, - (CH2 ) -S(CH2 ) nCH3 , - (CH2),-NH- (CH 2 )nCH, -C 2 -Cs alkenyl-O- (CH 2 ) CH 3 , C2 -C 8 alkenyl-S- (CH2)nCH 3 , -C 2 -Cs alkenyl-N- (CH 2 )nCH 3 , -C2-OC alkynyl-O- (CH 2 ) nCH 3 , -C 2 -C8 alkynyl-S- (CM 2 )nCH 3 , -C 2 -Cs alkynyl-N- (CH2)nCH3, - (CH2)mOH, - (CH 2 )m-O-NH 2 , - (CH2)m-S-NH2, -NH (CH 2 ) mCH3, -NH (CH 2 ) mOCH3, -NH (CH 2 ) mCHOH-COOH, -N (CH3) 2, - (CH 2 ) m (NH) CH 2OH, -NHCOOH, - (CH 2 ) NHCOOH, -N0 2 , -SCN, -SO 2 alkyl, -B(OH)2, -(CH 2 )m N(CH 3)-S02-NH3 , -CN2)nmNNSO 2NH2 , - NHC(=S)CH, and -NHNH ; and Y is selected from hydrogen. =0, -OCO(Rg) and -OH; wherein m is an integer between 0-20, n is an integer between 0-8, the symbol represents either a single or a double bond capable of forming a keto group at position 3 or 17; and theA^^svymbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical iso
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