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Heterocyclic boronic acid compounds
专利权人:
SINO-MED INTERNATIONAL ALLIANCE; INC.
发明人:
CAMPBELL, DAVID,WINN, DAVID
申请号:
ES04810839
公开号:
ES2524916T3
申请日:
2004.11.12
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Compound of formula (I): ** Formula ** which includes its cyclic isomers having the formula ** Formula ** its stereoisomers, its solvates, its hydrates and its pharmaceutically acceptable salts, in which: n is 1; X is CH2; Z is H; R1 and R2 independently or together are -OH; a hydroxyl bearing a protecting group of boronic acid; or a group that can be hydrolyzed to a hydroxyl group in an aqueous solution at physiological pH or in biological liquids; R3 and R4 are hydrogen and R5 is: ** Formula ** in which R20 is hydrogen, (C1-8) alkyl, (C1-6) alkylcarbonyl, dialkyl (C1-6) aminocarbonyl, cycloalkyl (C3-8) carbonyl; benzyl, benzoyl, (C 1-6) alkyl oxycarbonyl, aralkyloxycarbonyl, pyridinyl, pyrimidinyl, phenyl, thiazolyl substituted phenyl, phenylaminocarbonyl, alkylsulfonyl or phenylsulfonyl; wherein the benzyl, benzoyl, pyridinyl, pyrimidinyl, phenyl, phenylaminocarbonyl, alkylsulfonyl and phenylsulfonyl groups are optionally monosubstituted or independently disubstituted with R12; R12 is halogen, trifluoromethyl, cyano, nitro, (C1-6) alkyl, alkoxy (C1-6), cycloalkyl, carboxy, acetamido, hydroxy, hydroxyalkyl (C1-6), hydroxymethyl, trifluoromethoxy, sulfamoyl, carbamoyl, sulfonamido, alkylsulfonyl , phenylsulfonyl, aryl, or heteroaryl; wherein the aryl and heteroaryl groups are optionally monosubstituted or independently plurisubstituted with R7; R7 is halogen, (C1-10) alkyl, (C1-10) alkoxy, (C1-10) alkyl, amino, dialkyl (C1-10) amino, benzyl, benzyloxy, hydroxyalkyl (C1-6), hydroxymethyl, nitro, trifluoromethyl , trifluoromethoxy, trifluoromethylthio, N-hydroxyamino, cyano, carboxy, acetamido, hydroxy, sulfamoyl, sulfonamido, carbamoylCompuesto de fórmula (I):**Fórmula** que incluye sus isómeros cíclicos que presentan la fórmula**Fórmula** sus estereoisómeros, sus solvatos, sus hidratos y sus sales farmacéuticamente aceptables, en la que: n es 1; X es CH2; Z es H; R1 y R2 independiente o conjuntamente son -OH; un hidroxilo portador de un grupo protector de ácido 20
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