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6-substituted estradiol derivatives and methods of use
专利权人:
LLC;ENDECE INC.;ENDECE
发明人:
YARGER, JAMES G.
申请号:
AU2010324632
公开号:
AU2010324632A1
申请日:
2010.11.30
申请国别(地区):
AU
年份:
2012
代理人:
摘要:
Disclosed are compounds of the formula (I): where in R, R, R and R are independent l y hydrogen, C -C alkyl, halo, a sulfate, a glucuronide, -OH, a bulky group, aryl, cycloalkyl, heteroaryl, heterocycloalkyl, N ( CH ) ; a phosphate group, and a phosphinate group; R is hydrogen, halogen or alkyl; R11 i s selected from the group consisting of H, C -C alkyl, halogen, a sulfate, a glucoronide, - SONH, -COOH, -CN, -CHCN-, -NHCN-, -CHO, =CHOCH, -COO salt, -0S0alkyl, -NH, and -NHCO ( CH ) n; R is selected from the group consisting o f H, a C -C alkyl, a sulfate, a glucoronide, a bulky group, aryl, cycloalkyl, heteroaryl and heterocycloalkyl; X i s selected from the group consisting of C -C alkyl, C -C alkenyl, C -C alkynyl, halogen, a glucoronide, -NH, - SONH, -COOH, -CN, -CHCN, -NHCN, -CHO, -COOsalt, -0S0alkyl, - SH, - SCH, -CH [ ( CH ) CH ] COOCH, - ( CH ) mCOOCH, - ( CH U-O-CH, - ( CH ) m-0- ( CH ) CH, ( CH) - S -CH, - ( CH U- S - ( CH )CH, - ( CH ) -NH- ( CH ) CH, -C -C alkenyl -0- ( CH ) CH, - C -C alkenyl - S - ( CH ) CH, -C -Calkenyl -N- ( CH ) CH, -C -C alkynyl -O- ( CH ) CH, -C -C alkynyl - S - ( CH ) CH, -C-C alkynyl -N- ( CH ) CH, - ( CH U-OH, - ( CH ) -O-NH, - ( CH) - S -NH, -NH ( CH ) CH, -NH ( CH ) OCH, -NH ( CH ) CHOH-COOH, -N ( CH ), - ( CH ) (NH ) CHOH, -NHCOOH, - ( CH ) NHCOOH, -NO, - SCN, - S0alkyl, -B ( OH ) , - ( CH ) N ( CH ) - SO-NH, - ( CH ) -NH- SO -NH,-NHC ( = S) CH, and -NHNH; and Y is selected from hydrogen, =0, -OCO(R) 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 the Λ/WV symbol represents any type of bond regardless of the stereochemistry; and the respective enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds. The compounds are useful in the treatment of various types of cancer.
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