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    • 3. 发明申请
    • Thiazole derivatives as a2b antagonists
    • 噻唑衍生物作为a2b拮抗剂
    • US20090233938A1
    • 2009-09-17
    • US10585614
    • 2005-01-20
    • Neil John PressRoger John Taylor
    • Neil John PressRoger John Taylor
    • A61K31/501C07D417/14A61K31/506C07D417/12
    • C07D417/04C07D417/14
    • Compounds of formula (I) in free or salt form, where Ar is phenyl substituted by one or more substituents selected from halogen, cyano and C1-C8-haloalkyl, or naphthyl, R1 is hydrogen, phenyl optionally substituted by one or more substituents selected from halogen, cyano, hydroxy, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-alkoxy-C1-C8 alkyl, carboxy, C1-C8-alkoxycarbonyl and acyloxy, or R1 is a 5- or 6-membered monovalent heterocyclic group, R2 is hydrogen, C1-C8-alkyl, acyl or —CON(R3)R4, R3 and R4 are each independently hydrogen or C1-C8-alkyl, or together with the nitrogen atom to which they are attached denote a 5- or 6-membered heterocyclic group, and Y is a pyrimidinyl or pyridazinyl group, optionally substituted by at least one C1-C8-alkyl, C1-C8-alkoxy, C1-C8-alkylthio, C1-C8-alkyl amino, di(C1-C8-alkyl) amino or acylamino group. The compounds are useful as pharmaceuticals.
    • 游离或盐形式的式(I)化合物,其中Ar为被一个或多个选自卤素,氰基和C 1 -C 8 - 卤代烷基或萘基的取代基取代的苯基,R 1为氢,任选被一个或多个取代基取代的苯基 卤素,氰基,羟基,C 1 -C 8 - 烷基,C 1 -C 8 - 卤代烷基,C 1 -C 8 - 烷氧基,C 1 -C 8 - 烷氧基-C 1 -C 8烷基,羧基,C 1 -C 8烷氧基羰基和酰氧基, 5-或6-元一价杂环基,R 2为氢,C 1 -C 8 - 烷基,酰基或-CON(R 3)R 4,R 3和R 4各自独立地为氢或C 1 -C 8烷基,或与氮原子 它们所连接的表示5或6元杂环基,Y为嘧啶基或哒嗪基,任选被至少一个C 1 -C 8 - 烷基,C 1 -C 8 - 烷氧基,C 1 -C 8 - 烷硫基, C 8 - 烷基氨基,二(C 1 -C 8 - 烷基)氨基或酰氨基。 这些化合物可用作药物。