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    3-heteroaryl (amino or amido)-1-(biphenyl or phenylthiazolyl) carbonylpiperidine derivatives as orexin receptor inhibitors
    4.
    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

    Applicant: Hamed Aissaoui ,  Christoph Boss ,  Markus Gude ,  Ralf Koberstein ,  Thierry Sifferlen

    Inventor： Hamed Aissaoui ,  Christoph Boss ,  Markus Gude ,  Ralf Koberstein ,  Thierry Sifferlen

    IPC: C07D401/12 ,  C07D417/14 ,  C07D513/04 ,  A61K31/506

    CPC classification number: C07D401/12 ,  C07D417/14 ,  C07D513/04

    Abstract: 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.

    Abstract translation: 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
    7.
    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

    Applicant: Hamed Aissaoui ,  Christoph Boss ,  Markus Gude ,  Ralf Koberstein ,  Thierry Sifferlen

    Inventor： Hamed Aissaoui ,  Christoph Boss ,  Markus Gude ,  Ralf Koberstein ,  Thierry Sifferlen

    IPC: A61K31/506 ,  C07D239/28 ,  C07D417/04 ,  A61K31/445 ,  A61P25/30 ,  A61P25/32

    CPC classification number: C07D401/12 ,  C07D417/14 ,  C07D513/04

    Abstract: 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.

    Abstract translation: 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。

    3-UREIDOISOQUINOLIN-8-YL DERIVATIVES
    9.
    发明申请
    3-UREIDOISOQUINOLIN-8-YL DERIVATIVES 有权
    3-UREIDOISOQUINOLIN-8-YL衍生物

    公开(公告)号：US20140038961A1

    公开(公告)日：2014-02-06

    申请号：US14009093

    申请日：2012-03-28

    Applicant: Markus Gude ,  Christian Hubschwerlen ,  Philippe Panchaud

    Inventor： Markus Gude ,  Christian Hubschwerlen ,  Philippe Panchaud

    IPC: C07D217/22 ,  C07D401/14 ,  C07D401/04 ,  C07D401/12

    CPC classification number: C07D217/22 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14

    Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-oxopyrrolidin-2-yl, 2,5-dioxopyrrolidin-1-yl, 2-oxoimidazolidin-1-yl, 4-(tert-butoxycarbonyl)piperazin-1-yl, 4-(aminomethyl)cyclohexyl or heteroaryl; R4 is H or methyl; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.

    Abstract translation: 本发明涉及式I的3-脲基异喹啉-8-基衍生物，其中R 1是烷基，卤代烷基或环丙基; R 2是H，卤素，哒嗪-4-基，嘧啶-5-基或任选取代的吡啶-3-基，吡啶-4-基或苯基; R3是烷基，炔基，氨基烷基，氨甲酰基烷基，甲基氨基甲酰基烷基，烷氧基，卤代烷氧基，炔氧基，（4-羟基丁-2-炔-1-基）氧基，（4-氨基丁-2-炔-1-基）氧基，二甲基氨基烷氧基， 氨基甲酰基烷氧基，烷基氨基，环烷基，环烷基烷基，环烷基烷氧基，羟基烷基，羟基烷氧基，烷氧基烷基，烷氧基烷氧基，羧基烷基，羧基烷氧基，烷氧基羰基烷氧基，芳基，杂芳基，苄基，苄氧基，2-氰基乙氧基，2,3-二羟基丙氧基，3,4-二羟基丁氧基， ，-CH 2 CH 2 R b， - （CH 2）n C（O）O-R d， - （CH 2）n N（R c）C（O）O-R d，-O-（CH 2）n N（R c） - （CH 2）n -R e或-O-（CH 2）n -R e; R a是氰基，乙酰氨基或N，N-二甲基氨基; Rb是氰基或氨基甲酰基; Rc是H或甲基; Rd为烷基; Re是吡咯烷-1-基，哌啶-1-基，哌啶-3-基，吗啉-1-基，2-氧代吡咯烷-1-基，5-氧代吡咯烷-2-基，2,5-二氧代吡咯烷-1-基， 哌啶-1-基，4-（氨基甲基）环己基或杂芳基; R4是H或甲基; 和这些化合物的盐。 这些化合物可用于预防或治疗细菌感染。

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