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New glutaminyl cyclase inhibitors
专利权人:
PROBIODRUG AG
发明人:
THORMANN, MICHAEL,ALMSTETTER, MICHAEL,TREML, ANDREAS,HEISER, ULRICH,BUCHHOLZ, MIRKO
申请号:
ES07822338
公开号:
ES2468546T3
申请日:
2007.11.08
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula (I), or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R1 represents 3-imidazol-1-yl propyl or 1H-benzimidazolyl; R2 represents C1-8 alkyl, which may be optionally substituted with hydroxy; C3-10 cycloalkyl or C5-10 cycloalkenyl of which anyone can be optionally substituted with C1-4 alkyl; phenyl; naphthyl; -phenyl-heterocyclyl, in which heterocyclyl is a 5 or 6 membered ring containing 1 or 2 heteroatoms selected from N, S and O; (2-methyl) - (4-pyrrolidin-1-yl) -phenyl; (3-methyl) - (4-pyrrolidin-1-yl) -phenyl; H; heteroaryl, wherein heteroaryl is a 5 to 10 membered monocyclic or bicyclic ring containing 1, 2 or 3 heteroatoms selected from N, S and O; wherein the phenyl, naphthyl and heteroaryl groups may be optionally substituted with one or more substituents selected from C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 haloalkyl, -thiomethyl, -SO2Me, OMe, cycloalkyl C3-6, -SO2-C3-6 cycloalkyl, C2-4 alkenyloxy, C2-4- alkynyloxy, COMe, C1-4 alkoxy (C1-4 alkyl) -, nitro, fluoro, chloro, bromo, cyano, hydroxy, oxo, -C (O) OH, -C (O) OMe, -NH2, -NHMe, dimethylamino-, -C (O) N (C1-4 alkyl) 2, -C (O) NH2 and -C (O ) NH (C1-4 alkyl); or heterocyclyl, wherein heterocyclyl is a 5- or 6-membered ring containing 1 or 2 heteroatoms selected from N, S and O, which may be optionally substituted with one or more substituents selected from C 1-6 alkyl, hydroxy and oxo.Un compuesto de fórmula (I), o una sal, solvato o polimorfo farmacéuticamente aceptable del mismo, incluyendo todos los tautómeros y estereoisómeros del mismo, en la que R1 representa 3-imidazol-1-il propilo o 1H-bencimidazolilo; R2 representa alquilo C1-8, que puede estar opcionalmente sustituido con hidroxi; cicloalquilo C3-10 o cicloalquenilo C5-10 de los que cualquiera puede estar opcionalmente sustituido con alquilo C1-4 ; fenilo; naftilo; -fenil-heterociclilo, en la que heterociclilo es un anillo de 5 o 6 miembro
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