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    SUBSTITUTED TETRAHYDROPYRAN SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF
    3.
    发明申请
    SUBSTITUTED TETRAHYDROPYRAN SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF 有权
    取代四氢呋喃螺旋吡咯烷酮和哌啶酮，其制备和治疗用途

    公开(公告)号：US20120238757A1

    公开(公告)日：2012-09-20

    申请号：US13483503

    申请日：2012-05-30

    申请人： Zhongli GAO ,  Ryan HARTUNG ,  David STEFANY

    发明人： Zhongli GAO ,  Ryan HARTUNG ,  David STEFANY

    IPC分类号： C07D491/107

    CPC分类号： C07D491/107

    摘要： The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.

    摘要翻译： 本公开涉及一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺：其中R 1，R 2，m，n和p如本文所述。 更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。 另外，公开了制备取代的N-苯基 - 联吡咯烷甲酰胺和中间体的方法。

    SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF
    5.
    发明申请
    SUBSTITUTED PIPERIDINE SPIRO PYRROLIDINONE AND PIPERIDINONE, PREPARATION AND THERAPEUTIC USE THEREOF 有权
    替代哌啶螺吡喃吡咯烷酮和哌啶酮，其制备和治疗用途

    公开(公告)号：US20120258979A1

    公开(公告)日：2012-10-11

    申请号：US13527147

    申请日：2012-06-19

    申请人： Zhongli GAO ,  Daniel HALL ,  Ryan HARTUNG

    发明人： Zhongli GAO ,  Daniel HALL ,  Ryan HARTUNG

    IPC分类号： A61K31/438 ,  A61P3/04 ,  A61P25/24 ,  A61P25/22 ,  A61P25/00 ,  A61P25/28

    CPC分类号： C07D471/10

    摘要： The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefor are disclosed.

    摘要翻译： 本公开涉及一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺。 其中R1，R2，R3，m，n和p如本文所述。 更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。 另外，公开了制备取代的N-苯基 - 联吡咯烷甲酰胺及其中间体的方法。

    2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF
    7.
    发明申请
    2-ALKYL-6-CYCLOAMINO-3-(PYRIDIN-4-YL)IMIDAZO[1,2-B]-PYRIDAZINE DERIVATIVES, PREPARATION THEREOF, AND THERAPEUTIC APPLICATION THEREOF 审中-公开
    2-氨基-6-环丙氨基-3-（吡啶-4-基）咪唑并[1,2-B] - 吡啶衍生物，其制备方法及其治疗应用

    公开(公告)号：US20110312934A1

    公开(公告)日：2011-12-22

    申请号：US13058665

    申请日：2009-08-12

    申请人： Antonio Almario Garcia ,  Philippe Burnier ,  Sylvain Cote-Des Combes ,  Jean-François Gibert ,  Christophe Pacaud ,  Frédéric Puech ,  Yulin Chiang ,  Larry Davis ,  Zhongli Gao ,  Qiuxia Zhao

    发明人： Antonio Almario Garcia ,  Philippe Burnier ,  Sylvain Cote-Des Combes ,  Jean-François Gibert ,  Christophe Pacaud ,  Frédéric Puech ,  Yulin Chiang ,  Larry Davis ,  Zhongli Gao ,  Qiuxia Zhao

    IPC分类号： A61K31/551 ,  C07D498/10 ,  C07D471/08 ,  A61P25/30 ,  A61K31/5386 ,  A61P35/00 ,  A61P25/00 ,  C07D487/04 ,  A61K31/5025

    CPC分类号： C07D487/04 ,  C07D519/00

    摘要： The invention relates to 2-alkyl-6-cycloamino-3-(pyridin-4-yl)imidazo[1,2-b]pyridazine derivatives of the general formula (I) where: R2 is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-4-alkyl, C1-4-alkyloxy-C-M-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl>C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-alkyl, C1-4-fluoroalkyl group; R3 is a hydrogen atom or a substituent selected from halogen atoms and the C1-3 alkyl, —NR4R5, hydroxyl or C1-4 alkyloxy groups; A is a C1-7-alkylene group optionally substituted by one or two Ra groups; B is a C1-7-alkylene group optionally substituted by one or two Rb groups; L is either a nitrogen atom optionally substituted by an Rc or Rd group or a carbon atom substituted by an Re1 group and an Rd group or by two Re2 groups; Rd is a group selected from a hydrogen atom or a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkylthio-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C1-6-fluoroalkyl, hydroxy-C1-6-alkyl group; Rf is a C1-6-alkyl, C3-7-cycloalkyl, C3-7-cycloalkyl-C1-6-alkyl, C1-6-alkyloxy-C1-6-alkyl, C3-7-cycloalkyloxy-C1-4-alkyl, C3-7-cycloalkyl-C1-4-alkyloxy-C1-4-alkyl, hydroxy-C1-6-allyl, C1-6-fluoroalkyl or benzyl group. The invention also relates to a method for preparing same and to the therapeutic application thereof.

    摘要翻译： 本发明涉及通式（I）的2-烷基-6-环氨基-3-（吡啶-4-基）咪唑并[1,2-b]哒嗪衍生物，其中：R2是C1-6烷基，C3 7-环烷基，C 3-7 - 环烷基-C 1-4 - 烷基，C 1-4 - 烷氧基-C1-烷基，C 3-7 - 环烷氧基-C 1-4 - 烷基，C 3-7 - 环烷基-C 1-4 - 烷氧基 C 1-4烷基，羟基-C 1-6 - 烷基，C 1-4 - 氟代烷基; R3是氢原子或选自卤素原子和C1-3烷基，-NR4R5，羟基或C1-4烷氧基的取代基; A是任选被一个或两个R a基团取代的C 1-7 - 亚烷基; B是任选被一个或两个Rb基团取代的C 1-7 - 亚烷基; L是任选被Rc或Rd基团取代的氮原子或被Re 1基团和Rd基团取代的碳原子或两个Re 2基团; Rd是选自氢原子或C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 - 环烷基-C 1-6 - 烷基，C 1-6 - 烷硫基-C 1-6 - 烷基，C 1-6 - 烷氧基-C 1-6 - 烷基，C 1-6 - 氟代烷基，羟基-C 1-6 - 烷基; R f是C 1-6 - 烷基，C 3-7 - 环烷基，C 3-7 - 环烷基-C 1-6 - 烷基，C 1-6 - 烷氧基-C 1-6 - 烷基，C 3-7 - 环烷氧基-C 1-4 - 烷基 C 3-7 - 环烷基-C 1-4 - 烷氧基-C 1-4 - 烷基，羟基-C 1-6 - 烯丙基，C 1-6 - 氟烷基或苄基。 本发明还涉及其制备方法及其治疗应用。

    Substituted tetrahydropyran spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof
    9.
    发明授权
    Substituted tetrahydropyran spiro pyrrolidinone and piperidinone, preparation and therapeutic use thereof 有权
    取代的四氢吡喃螺吡咯烷酮和哌啶酮，其制备和治疗用途

    公开(公告)号：US08383814B2

    公开(公告)日：2013-02-26

    申请号：US13483503

    申请日：2012-05-30

    申请人： Zhongli Gao ,  Ryan Hartung ,  David Stefany

    发明人： Zhongli Gao ,  Ryan Hartung ,  David Stefany

    IPC分类号： C07D491/107 ,  C07D401/04 ,  C07D401/14 ,  C07D401/02

    CPC分类号： C07D491/107

    摘要： The present disclosure relates to a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I): wherein R1, R2, m, n and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, methods of preparation of substituted N-phenyl-bipyrrolidine carboxamides and intermediates therefore are disclosed.

    摘要翻译： 本公开涉及一系列式（I）的取代的N-苯基 - 联吡咯烷甲酰胺：其中R 1，R 2，m，n和p如本文所述。 更具体地，本发明的化合物是H3受体的调节剂，因此可用作药剂，特别是用于治疗和/或预防由H3受体调节的各种疾病，包括与中枢神经系统相关的疾病。 另外，公开了制备取代的N-苯基 - 联吡咯烷甲酰胺和中间体的方法。