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    • 6. 发明申请
    • AROMATIC 5-MEMBERED HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY
    • 具有TRPV4抑制活性的芳香五聚体杂环衍生物
    • US20150038483A1
    • 2015-02-05
    • US14387387
    • 2013-03-26
    • Shionogi & Co., Ltd.
    • Akira YukimasaNaotake KobayashiKenji TakayaYoshio Hato
    • C07D417/14C07D417/04
    • C07D417/14C07D277/44C07D277/46C07D277/48C07D277/56C07D401/04C07D401/14C07D417/04C07D417/12
    • The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ═C(R4)—, or ═N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, substituted or unsubstituted alkyl, or the like; R4 and R5 are each independently a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like; R6 is a hydrogen atom, halogen, substituted or unsubstituted alkyl, or the like, or a pharmaceutically acceptable salt thereof, or a pharmaceutical composition comprising thereof.
    • 本发明涉及式(I)表示的化合物,其中R 1为氢原子,取代或未取代的烷基,取代或未取代的芳族碳环基等; X是-N(R 3) - , - O-或-S-; Y为≡C(R4) - 或=N-; Z是-N(R 7) - , - O-或-S-; R2是取代或未取代的烷氧基等,或由下式表示的基团: - (CR2aR2b)n-R2c,其中R2a各自独立地为氢原子,卤素等; R2b各自独立地为氢原子,卤素等; 连接到相同碳原子上的R 2a和R 2b可以一起形成氧代,取代或未取代的非芳族碳环等; 与相邻碳原子连接的R2a中的两个和/或与相邻碳原子连接的R2b中的两个可以一起形成键; R2c是取代或未取代的芳族碳环基等; n为1〜3的整数, R 3和R 7各自独立地为氢原子,取代或未取代的烷基等; R 4和R 5各自独立地为氢原子,卤素,取代或未取代的烷基等; R6是氢原子,卤素,取代或未取代的烷基等,或其药学上可接受的盐,或其药物组合物。