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    • 8. 发明授权
    • Compounds useful as motilin agonists and method
    • 可用作胃动素激动剂和方法的化合物
    • US07262195B2
    • 2007-08-28
    • US10940240
    • 2004-09-14
    • James J. LiHannguang J. ChaoJoseph A. TinoWilliam R. Ewing
    • James J. LiHannguang J. ChaoJoseph A. TinoWilliam R. Ewing
    • A61K31/50C07D237/00C07D487/00
    • C07D471/20A61K31/495A61K31/50
    • Compounds are provided which are useful in treating disorders of gastrointestinal motility and which have the structure or a pharmaceutically acceptable salt thereof, a prodrug ester thereof, and all stereoisomers thereof, wherein R1 and R2 are the same or different and are independently selected from hydrogen, alkyl, aryl, cycloalkyl, alkenyl, alkynyl, arylalkyl, heteroaryl, heteroarylalkyl or heterocycloalkyl; Z is selected from —CON(R4)R4a, —CO2R4, —SO2N(R4)R4a, —SO2R4, CN, and R4 and R4a are the same or different and are independently selected from hydrogen, alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl or R4 and R4a can be joined together to form a heterocycle. R4b is selected from hydrogen, halogen, hydroxyl, CN, OCF3, CF3, CONH2, SONH2, SO2CH3, NHCOCH3 or NHCO2CH3; and Q is a substituted bicyclic heterocycle. A method for using such compounds for treating disorders of gastrointestinal motility is also provided.
    • 提供了可用于治疗胃肠蠕动障碍并且具有其结构或其药学上可接受的盐,其前药酯及其所有立体异构体的化合物,其中R 1和R 2 独立地选自氢,烷基,芳基,环烷基,烯基,炔基,芳基烷基,杂芳基,杂芳基烷基或杂环烷基; Z选自-CON(R 4 S)R 4a,-CO 2 R 4,-SO 3, N 2(R 4)R 4a,-SO 2 R 4,CN R 4a和R 4a相同或不同并且独立地选自氢,烷基,环烷基,芳基,芳基烷基,杂芳基或杂芳基烷基或R 1, 4和R 4a可以连接在一起形成杂环。 R 4b选自氢,卤素,羟基,CN,OCF 3,CF 3,CONH 2, SO 2 H 2,CH 2 CH 3,NHCOCH 3或NHCO 2 CH 3, SUB> 3 Q是取代的双环杂环。 还提供了使用这些化合物治疗胃肠蠕动障碍的方法。