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Compounds of 4- (benzoimidazol-2-yl) -thiazole and related aza derivatives
专利权人:
Idorsia Pharmaceuticals Ltd
发明人:
CAROFF, Eva,KELLER, Marcel,KIMMERLIN, Thierry,MEYER, Emmanuel
申请号:
ES13712913
公开号:
ES2632237T3
申请日:
2013.02.01
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (I) ** Formula ** in which ring A represents a benzene, pyridine, or pyrimidine ring; (R1) n represents one or two optional substituents each independently selected from the group consisting of (C1-4) alkyl; (C1-4) alkoxy; fluoroalkyl (C1-3); fluoroalkoxy (C1-3); halogen; cyano; (C3-6) cycloalkyl optionally mono-substituted with hydroxy; (C1-3) alkoxy-(C1-4) alkyl; (C1-3) alkoxy-(C2-4) alkoxy; hydroxy (C1-4) alkyl; hydroxy-C2-4 alkoxy; hydroxy; (C1-4) alkyl sulfonyl; phenyl; 5-membered heteroaryl optionally substituted with (C1-4) alkyl; -CO-C 1-4 alkyl; -CO-C1-4 alkoxy; - (CH2) q-NR6R7, wherein R6 and R7 independently represent hydrogen or (C1-4) alkyl; and q represents the integer 0, 1, or 2; and -L-heterocyclyl, in which -L- represents -O- or - (CH2) r- in which r represents the integer 0, 1, or 2; and the heterocyclyl is independently a 4- to 7-membered monocyclic saturated ring containing one or two heteroatoms independently selected from nitrogen and oxygen, wherein said heterocyclyl is optionally substituted with a substituent independently selected from (C1-4) alkyl, alkoxy ( C1-4), and oxo; R2 represents hydrogen, (C1-4) alkyl, or (C1-3) alkoxy-(C2-4) alkyl; R4 represents hydrogen; and R4 'represents methyl; wherein the carbon atom to which R4 'is attached is in the absolute configuration (R); and R5 represents · aryl, wherein said aryl is unsubstituted, or mono-, di-, or tri-substituted, in which the substituents are independently selected from the group consisting of (C1-4) alkyl; (C1-4) alkoxy; fluoroalkyl (C1-3); fluoroalkoxy (C1-3); halogen; cyano; (C1-3) alkoxy-(C1-4) alkyl; (C1-3) alkoxy-(C2-4) alkoxy; hydroxy; hydroxy (C1-4) alkyl; 5-membered heteroaryl; and heterocyclyl, wherein the heterocyclyl is a 5 to 7 membered monocyclic saturated ring containing one or two nitrogen atoms, wherein said heterocyclyl is optionally substituted on a nitrogen having a free valence with (C1-4) alkyl ; or · 5 or 6 membered heteroaryl, wherein s
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