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6- 6-SUBSTITUTED ESTRADIOL DERIVATIVES AND METHODS OF USE
专利权人:
엔디씨, 엘엘씨
发明人:
야거, 제임스, 지.
申请号:
KR1020187023922
公开号:
KR1020180095742A
申请日:
2010.11.30
申请国别(地区):
KR
年份:
2018
代理人:
摘要:
Compounds of formula (I) are disclosed: (I) Wherein R 1 , R 2 , R 3 and R 4 are independently selected from the group consisting of hydrogen, C 1 -C 6 alkyl, halo, sulfate, glucuronide, -OH, bulky groups, aryl, cycloalkyl, heteroaryl, heterocyclo alkyl, N (CH 2)n, a phosphate group, and a phosphinate group; R 9 is hydrogen, halogen or alkyl; R 11 is H, C 1 -C 6 alkyl, halogen, sulfate, glucuronide, -SO 2 NH 2 , -COOH, -CN, -CH 2 CN-, -NHCN-, -CHO, = CHOCH 3 , salts selected from -COO, -OSO 2 alkyl, -NH 2, and -NHCO (CH 2)n and the group consisting of; R 12 is selected from the group consisting of H, C 1 -C 6 alkyl, sulfate, glucuronide, bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X is selected from the group consisting of C 1 -C 12 alkyl, C 2 -C 12 alkenyl, C 2 -C 12 alkynyl, halogen, glucuronide, -NH 2 , -SO 2 NH 2 , -COOH, -CN, 2 CN-, -NHCN, -CHO, -COO salt, -OSO 2alkyl, -SH, -SCH 3, -CH [ (CH 2) n CH 3] C00CH 3, - (CH 2) m COOCH 3, - (CH 2) m -O-CH 3, - (CH 2) m -O- (CH 2) n CH 3, - (CH 2) m -S-CH 3, - (CH 2) m -S- ( CH 2) n CH 3, - (CH 2) m -NH- (CH 2) n CH 3, -C 2 -C 8 alkenyl, -O- (CH 2) n CH 3 , -C 2 -C 8 al alkenyl -S- (CH 2) n CH 3 , -C 2 -C 8 alkenyl, -N- (CH 2) n CH 3 , -C 2 -C 8 alkynyl, -O- (CH 2) n CH 3 , -C 2 -C 8 alkynyl, -S- (CH 2) n CH 3 , -C 2 -C 8 alkynyl, -N- (CH 2) n CH 3 , - (CH 2) m -OH, - (CH 2) m -O-NH 2, - (CH 2) m -S-NH 2, -NH (CH 2) m CH 3, -NH (CH 2) m OCH 3, -NH (CH 2) m CHOH- COOH, -N (CH 3) 2 , - (CH 2) m (NH) CH 2 OH, -NHCOOH, - (CH 2) m NHCOOH, -NO 2, -SCN, -SO 2 alkyl, -B (OH ) 2 , - (CH 2 ) m N (CH 3 ) -SO 2 -NH 3 , - (CH 2 ) m -NH-SO 2 -NH 2 , -NHC (═S) CH 3 and -NHNH 2 Selected from the group consisting of; Y is selected from hydrogen, = O, -OCO (R <; 6 >;), and -OH; Wherein m is an integer between 0 and 20, n is an integer between 0 and 8, - - represents a double bond or a single bond capable of forming a keto group at position 3 or 17; The sign indicates any type of bond regardless of the stereochemis
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