3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors
    5.
    发明授权
    3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors 失效
    (氨基或酰氨基)-1-(联苯基或苯基噻唑基)羰基哌啶衍生物作为食欲素受体抑制剂

    公开(公告)号:US08133901B2

    公开(公告)日:2012-03-13

    申请号:US12517010

    申请日:2007-11-29

    摘要: The invention relates to piperidine compounds of formula (I): wherein X—R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X—R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di- or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di- substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.

    摘要翻译: 本发明涉及式(I)的哌啶化合物:其中X-R 1表示-N(H) - 嘧啶基,其中所述嘧啶基是未取代的或单取代的,其中取代基选自(C 1-4)烷基或卤素,或 X-R1表示-NH-C(O) - 杂环基,其中杂环基选自苯并呋喃基和咪唑并[2,1-b] - 噻唑基,其中所述杂环基是未取代的或独立的单 - ,二 - 或三 - 取代,其中 取代基独立地选自(C 1-4)烷基; A表示苯基或噻唑基,其中苯基或噻唑基未被取代或被(C 1-4)烷基单取代; B表示苯基,其中苯基是未取代的或单取代或二取代的,其中取代基独立地选自(C 1-4)烷基,(C 1-4)烷氧基,三氟甲基,氰基和 卤素; 和其药学上可接受的盐,以及这些化合物的用途用作药物,特别是作为食欲素受体拮抗剂。

    3-HETEROARYL (AMINO OR AMIDO)-1-(BIPHENYL OR PHENYLTHIAZOLYL) CARBONYLPIPERIDINE DERIVATIVES AS OREXIN RECEPTOR INHIBITORS
    8.
    发明申请
    3-HETEROARYL (AMINO OR AMIDO)-1-(BIPHENYL OR PHENYLTHIAZOLYL) CARBONYLPIPERIDINE DERIVATIVES AS OREXIN RECEPTOR INHIBITORS 失效
    作为OREXIN受体抑制剂的3-异丙基(氨基或氨基)-1-(联苯胺或苯基乙酰基)碳二苯胺衍生物

    公开(公告)号:US20100069418A1

    公开(公告)日:2010-03-18

    申请号:US12517010

    申请日:2007-11-29

    摘要: The invention relates to piperidine compounds of formula (I) wherein X-R1 represents —N(H)-pyrimidinyl, wherein said pyrimidinyl is unsubstituted or mono-substituted wherein the substituent is selected from (C1-4)alkyl or halogen, or X-R1 represents —NH—C(O)-heterocyclyl, wherein the heterocyclyl is selected from benzofuranyl and imidazo[2,1-b]-thiazolyl, wherein said heterocyclyl is unsubstituted or independently mono-, di-, or tri-substituted wherein the substituents are independently selected from (C1-4)alkyl; A represents a phenyl- or thiazolyl-group, wherein the phenyl or thiazolyl is unsubstituted or mono-substituted with (C1-4)alkyl; B represents a phenyl-group, wherein the phenyl is unsubstituted or mono-, or di-substituted, wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, trifluoromethyl, cyano and halogen; to pharmaceutically acceptable salts thereof, and to the use of such compounds use as medicaments, especially as orexin receptor antagonists.

    摘要翻译: 本发明涉及式(I)的哌啶化合物,其中X-R 1表示-N(H) - 嘧啶基,其中所述嘧啶基是未取代的或单取代的,其中取代基选自(C 1-4)烷基或卤素,或X -R 1表示-NH-C(O) - 杂环基,其中杂环基选自苯并呋喃基和咪唑并[2,1-b] - 噻唑基,其中所述杂环基是未取代的或独立的单 - ,二 - 或三 - 取代,其中 取代基独立地选自(C 1-4)烷基; A表示苯基或噻唑基,其中苯基或噻唑基未被取代或被(C 1-4)烷基单取代; B表示苯基,其中苯基是未取代的或单取代或二取代的,其中取代基独立地选自(C 1-4)烷基,(C 1-4)烷氧基,三氟甲基,氰基和 卤素; 和其药学上可接受的盐,以及这些化合物的用途用作药物,特别是作为食欲素受体拮抗剂。