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inhibitors
专利权人:
PROBIODRUG AG
发明人:
ANTJE MEYER,INGEBORG LUES,TORSTEN HOFFMANN,ULRICH HEISER
申请号:
BR112019019553
公开号:
BR112019019553A2
申请日:
2018.04.03
申请国别(地区):
BR
年份:
2020
代理人:
摘要:
the present invention relates to a compound of formula (i): abde (i) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: a is selected from monocyclic heteroaryl and bicyclic, which can be independently substituted by alkyl or amino; b is selected from alkyl, heteroalkyl, alkylamino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups can be independently substituted by alkyl; d is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, in which said aryl, heteroaryl, cycloalkyl and heterocyclyl groups can be independently substituted; and e is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups can be independently substituted. the compounds of formula (i) are glutaminyl cyclase inhibitors (qc, ec 2,3,2,5). qc catalyzes the intramolecular cyclization of n-terminal glutamine residues in pyroglutamic acid (5-oxo-prolyl, pglu *) under ammonia release and the intramolecular cyclization of n-terminal glutamate residues in pyroglutamic acid under water release.a presente invenção refere-se a um composto de fórmula (i): a-b-d-e (i) ou um sal farmaceuticamente aceitável, solvato ou polimorfo do mesmo, incluindo todos os tautômeros e estereoisômeros do mesmo, em que: a é selecionado de heteroarila monocíclica e bicíclica, que pode independentemente ser substituída por alquila ou amino; b é selecionado de alquila, heteroalquila, alquil-amino, arila, heteroarila, cicloalquila, heterociclila e alquileno, em que referidos grupos podem independentemente ser substituídos por alquila; d é selecionado de aril-amino, heteroaril-amino, cicloalquil-amino, heterociclila, heterociclil-amino, ureia, tioamida, tioureia, sulfonamida, sulfoximina e sulfamoíla, em que referidos grupos arila, heteroarila, cicloalquil
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