BLAAUW, Richard Hendrik,LEENDERS, Ruben Gerardus George,STERK, Geert Jan,HERMKENS, Pedro Harold Han
申请号：
ES13759838
公开号：
ES2622190T3
申请日:
2013.07.12
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A compound of general formula (I): ** Formula ** in which - L is a linker comprising 1 to 10 optionally substituted skeleton atoms, selected from carbon, nitrogen and oxygen； and - R1 and R2 are each independently selected from hydrogen and C1-C6 alkyl, or R1 and R2 are linked together to form a second linker between the amide nitrogen atom and the cationic nitrogen atom, or R1 is attached to a skeleton atom of linker L in a cyclic structure and / or R2 is attached to a skeleton atom of linker L in a cyclic structure； and - R3 is selected from hydrogen and C1-C6 alkyl, wherein the alkyl moiety may be substituted with one or more halogen atoms or (halo) alkoxy moieties, or R3 is absent when the cationic nitrogen atom is part of a imine residue； and - R4 is selected from hydrogen and C1-C6 alkyl, wherein the alkyl moiety may be substituted with one or more halogen atoms or (halo) alkoxy moieties； and - X- is a pharmaceutically acceptable anion, in which the compound is not: (i) the compound of formula (I), in which L>； = - (CH2) 3- (L3), R1>； = H, R2>； = H, R3>； = H, R4>； = H and X>； = Cl； (ii) the compound of formula (I), wherein L>； = - (CH2) 2-CHR1'-CH2-NH- (CH2) 4-, R1-R1 '>； = - (CH2) 2- (L1 ), R2>； = H, R3>； = - (CH2) 2-CH3, R4>； = H and X>； = Cl； (iii) the compound of formula (I), in which L>； = - (CH2) 3- (L3), R1>； = H, R2>； = H, R3>； = H, R4>； = H； X>； = TFA, which is in the S configuration in position 2； (iv) 1- [2- (6-amino-4-methyl-2-pyridinyl) ethyl] -4 - [(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-) hydrochloride 2H- [1] - benzopyran-2-yl) carbonyl] -piperazine； (v) 1- [4- (2-Amino-6-pyridinyl) -3-butynyl] -4 - [(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H hydrochloride) - [1] - benzopyran-2-yl) carbonyl] -piperazine； or (vi) N- [4- (6-amino-4-methyl-2-pyridinyl) butyl] -6-hydroxy-2,5,7,8-tetramethyl-2-chromanocarboxamide fumarate.Un compuesto de fórmula general (I):**Fórmula** en la que - L es un ligador que compren
