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Substituted estradiol derivatives in position 6 for use in the remielination of nerve axons
专利权人:
LLC;Endece
发明人:
YARGER, James G.,NYE, Steve
申请号:
ES12761491
公开号:
ES2561536T3
申请日:
2012.03.21
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A derivative of estradiol substituted in position 6 of the formula: ** Formula ** in which ring "a" is selected from the group consisting of ** Formula ** 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; R11 is selected from the group consisting of H, C1-C6 alkyl, halogen, a sulfate, a glucuronide, -SO2NH2, -COOH, -CN, -CH2CN -, - NHCN-, -CHO,>; = CHOCH3, salt -CO, -OSO2alkyl, -NH2, and -NHCO (CH2) n; X is selected from the group consisting of C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, halogen, glucuronide, -NH2, -SO2NH2, -COOH, -CN, -CH2CN, -NHCN, -CHO, salt - COO, -OSO2alkyl, -SH, -SCH3, -CH [(CH2) nCH3] COOCH3, - (CH2) mCOOCH3, - (CH2) mO-CH3, - (CH2) mO- (CH2) nCH3, (CH2) mS -CH3, - (CH2) mS- (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-NH2, - (CH2) mO-NH2, - (CH2) mS-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; Y is selected from hydrogen,>; = O, -OCO (C1-C20 alkyl) and -OH; and Z is H or methyl; in which m is an integer between 0 and 20, n is an integer between 0 and 8, the symbol - - - - represents a single or double bond capable of forming a keto group in position 3 and / or 17; and the symbol represents any type of link with indifference to stereochemistry; and enantiomers, other stereochemical isomers, hydrates, solvates, tautomers and pharmaceutically acceptable salts of said compounds, for use in the prevention of demyelination and / or intensification of the remyelination of an axon of a nerve cell
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