BAGUISI, Alexander,BEEUWKES, Reinier,CASALE, Ralph,KATES, Steven,LADER, Alan
申请号:
ES11793558
公开号:
ES2640474T3
申请日:
2011.11.10
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound represented by Structural Formula (I): ** Formula ** or a pharmaceutically acceptable salt thereof, in which: the enantiomeric excess or diastereomeric excess of the compound or its pharmaceutically acceptable salt is at least 90% ; R is (C1-C18) alkyl, (C6-C18) aryl or (C6-C18) -aryl (C1-C18) alkyl, and is substituted with at least one acid substituent selected from the group consisting of -CO2H, -SO3H , -PO3H2, -OSO3H, -OPO3H2, -B (OH) 2 and -NHOH, wherein the aryl of the aryl (C6-C18) or aryl (C6-C18) -alkyl (C1-C18) is optionally further substituted with one or more substituents selected from the group consisting of hydroxy, halo, (C1-C3) alkyl, haloalkyl (C1-C3), cyano, nitro, alkoxy (C1-C3) and thioalkyl (C1-C3); R 'is hydrogen or (C1-C18) alkyl, wherein (C1-C18) alkyl is optionally substituted with one or more acid substituents selected from the group consisting of -CO2H, -SO3H, -PO3H2, -OSO3H, -OPO3H2 , -B (OH) 2 and -NHOH; and X is absent or is an amino acid, the amino acid being aspartic acid, tyrosine, glutamic acid or alanine, and being oriented to form an amide bond with ** Formula ** provided that the compound of Structural Formula (I) is not N - (R) -lipoyl-glutamylalanine, N- (R) -lipoylaminoethylphosphonic acid or (R) -5- (5- (1,2-dithiolan-3-yl) pentanamide) -2-hydroxybenzoic acid.Un compuesto representado por la Fórmula estructural (I):**Fórmula** o una de sus sales farmacéuticamente aceptables, en el que: el exceso enantiomérico o el exceso diastereomérico del compuesto o de su sal farmacéuticamente aceptable es de al menos el 90 %; R es alquilo (C1-C18), arilo (C6-C18) o aril (C6-C18)-alquilo (C1-C18), y está sustituido con al menos un sustituyente ácido seleccionado del grupo que consiste en -CO2H, -SO3H, -PO3H2, -OSO3H, -OPO3H2, -B(OH)2 y -NHOH, en donde el arilo del arilo (C6-C18) o aril (C6- C18)-alquilo (C1-C18) está opcionalmente sustituido además con uno o más sustituyentes seleccionados del grupo que consiste en hidroxi, halo,