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Pyrroloquinoline derivatives as 5-HT6 antagonists, method of preparation and use thereof
专利权人:
UNIWERSYTET JAGIELLONSKI;INSTYTUT FARMAKOLOGII POLSKIEJ AKADEMII NAUK;CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE;UNIVERSITE DE MONTPELLIER
发明人:
ZAJDEL, Pawel,GRYCHOWSKA, Katarzyna,LAMATY, Frederic,COLACINO, Evelina,BANTREIL, Xavier,MARTINEZ, Jean,PAWLOWSKI, Maciej,SATALA, Grzegorz,BOJARSKI, Andrzej J.,PARTYKA, Anna,KOS, Tomasz,POPIK, Piotr,SU
申请号:
ES13759883
公开号:
ES2674476T3
申请日:
2013.07.25
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of the general formula (XIV): ** Formula ** or a tautomer, stereoisomer, N-oxide, isotopically labeled analogue, or a pharmacologically acceptable salt, hydrate or solvate of any of the foregoing, in which: - R1 , R2 independently represent hydrogen, an unsubstituted (C1-C3) alkyl group, a (C1-C3) alkyl group substituted with one or more halogen atoms, a (C1-C3) alkoxy group, or independently a group selected from: cyano, nitro, amino, hydroxyl; - T represents CO, CH2, substituted (C1-C2) alkyl group, SO, SO2; - Ar represents unsubstituted aryl (5-6 members), biaryl (8-10 members), heteroaryl (5-6 members), heteroaryl (8-10 members) that has 1-3 heteroatoms independently selected from the group consisting of N, O, S, optionally substituted with one or more substituents selected from (C1-C3) alkyl group, a (C1-C3) alkyl group substituted with one or more halogen atoms, (C1-C3) alkoxy group , (C2-C4) alkenyl, halogen, nitro, hydroxyl, cyano, amino, alkylamino, carboxamide; - R3 represents a substituent selected from the group of substituted or unsubstituted cyclic or linear amines consisting of structures XV-XVIII: ** Formula ** in which: - A represents NH, O, CH2, NR5; - B represents NH, O, NR4; - R4 represents hydrogen atom or (C1-C3) alkyl group; - R5 represents (C1-C3) alkyl or benzyl group; - R6 represents (C1-C3) alkyl group; - n is selected from 0, 1, 2; - m is selected from 0, 1, 2; - l is selected from 1 and 2.Un compuesto de la fórmula general (XIV):**Fórmula** o un tautómero, estereoisómero, N-óxido, análogo marcado isotópicamente, o una sal, hidrato o solvato farmacológicamente aceptable de cualquiera de los anteriores, en la que: - R1, R2 representan independientemente hidrógeno, un grupo alquilo (C1-C3) no sustituido, un grupo alquilo (C1- C3) sustituido con uno o más átomos de halógeno, un grupo alcoxilo (C1-C3), o independientemente un grupo seleccionado de: ciano, nitro, amino, hidroxilo; - T representa CO, CH2, grupo alquilo (C1-C2) sustit
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