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Taiazole or oxazole derivatives which are useful in treatment of cardiovascular and related diseases

机译:泰唑或恶唑衍生物,可用于治疗心血管疾病和相关疾病

摘要

A compound of formula (I) and pharmaceutically acceptable salts, solvates and hydrolysable esters thereofWhereinR1 and R2 are independently H or C1-3 alkyl or R1 and R2 which are bonded to the same carbon atom may together with the carbon atom to which they are bonded form a 3-5 membered cycloalkyl ring;X1 represents O or S;Each R3, R4, R8 and R9 independently represents H, halogen, -CH3 and -OCH3;R5 represents H or C1-6 alkyl or R4 and R5 together form a 3-6 membered cycloalkyl ring.X2 represents NH, NCH3 or O;One of Y and Z is N, and the other is O or S;R6 represents phenyl or pyridyl (wherein the N is in position 2 or 3) and is optionally substituted by one or more halogen, CF3, C1-6 straight or branched alkyl (optionally substituted by halogen), with the provision that when R6 is pyridyl, the N is unsubstituted.R7 represents C1-6alkyl, (optionally substituted by one or more halogens), -C0-8alkyl-5 membered heteroaryl, C0-6alkyl-(O)n-phenyl, wherein n is 0 or 1, with the proviso that when R1 and R2 are methyl, R8 and R9are H, R5 is H, then R7 cannot be CH3 or CF3.
机译:式(I)的化合物及其药学上可接受的盐,溶剂化物和可水解酯,其中R 1和R 2独立地为与相同碳键合的H或C 1-3烷基或R 1和R 2。原子可与它们所键合的碳原子一起形成3-5元环烷基环; X 1表示O或S;每个R 3,R 4,R 8和R 9独立地表示H ,卤素,-CH 3和-OCH 3; R 5代表H或C 1-6烷基或R 4和R 5一起形成3-6元环烷基环。X2代表NH,NCH 3或O; Y和Z为N,另一个为O或S; R 6代表苯基或吡啶基(其中N位于2或3位),并任选地被一个或多个卤素,CF 3,C1-6直链或支链烷基(任选地被卤素取代),条件是当R 6是吡啶基时,N是未被取代的。R7代表C 1-6烷基(任选地被一个或多个卤素取代),-C 0-8烷基- 5元杂芳基,C 6-6烷基-(O)n-苯基,其中n为0或1,条件是当R 1和R 2为甲基时,R 8和R 9为H,R 5为H,则R 7不能为CH 3或CF 3 。

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