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DÉRIVÉS SUBSTITUÉS EN POSITION 6 DE L'ESTRADIOL ET PROCÉDÉS D'UTILISATION
专利权人:
Endece; LLC
发明人:
申请号:
EP10834033.2
公开号:
EP2507253A2
申请日:
2010.11.30
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
Disclosed are compounds of the formula: wherein R1, R2, R3 and R4 are independently hydrogen, C1-C6 alkyl, halo, a sulfate, a glucuronide, —OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, —N(CH2)n; a phosphate group, and a phosphinate group; R9 is hydrogen, halogen or alkyl; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucoronide, —SO2NH2, —COOH, —CN, —CH2CN—, —NHCN—, —CHO, ═CHOCH3, —COO salt, —OSO2alkyl, —NH2, and —NHCO(CH2)n; R12 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 C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, a glucoronide, —NH2, —SO2NH2, —COOH, —CN, —CH2CN, —NHCN, —CHO, —COOsalt, —OSO2alkyl, —SH, —SCH3, —CH[(CH2)nCH2]COOCH2, —(CH2)mCOOCH3, —(CH2)m—O—CH3, —(CH2)m—O—(CH2)nCH3, (CH2)m—S—CH3, —(CH2)m—S—(CH2)nCH3, —(CH2)m—NH—(CH2)nCH3, —C2-C8 alkenyl-O—(CH2)nCH3, —C2-C8 alkenyl-S—(CH2)nCH3, —C2-C8 alkenyl-N—(CH2)nCH3, —C2-C8 alkynyl-O—(CH2)nCH3, —C2-C8 alkynyl-S—(CH2)nCH3, —C2-C8 alkynyl-N—(CH2)nCH3, —(CH2)m—OH, —(CH2)m—O—NH2, —(CH2)m—S—NH2, —NH(CH2)mCH3, —NH(CH2)mOCH3, —NH(CH2)mCHOH—COOH, —N(CH3)2, —(CH2)m(NH)CH2OH, —NHCOOH, —(CH2)mNHCOOH, —NO2, —SCN, —SO2alkyl, —B(OH)2, —(CH2)m N(CH3)—SO2—NH3, —(CH2)m—NH—SO2—NH2, —NHC(═S)CH3, and —NHNH2; and Y is selected from hydrogen, ═O, —OCO(R6) and —OH; wherein m is an integer between 0-20, n is a
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