Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators
    21.
    发明授权
    Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators 有权
    取代的喹喔啉型桥接哌啶化合物作为ORL-1调节剂

    公开(公告)号:US08476271B2

    公开(公告)日:2013-07-02

    申请号:US13010632

    申请日:2011-01-20

    IPC分类号: A61K31/495

    摘要: Compounds of Formula (I): where R1, R2, R5, a, and b are disclosed herein, and pharmaceutically acceptable derivatives thereof (a “Substituted-Quinoxaline-Type Bridged-Piperidine Compound”), compositions comprising an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Bridged-Piperidine Compound.

    摘要翻译: 式(I)的化合物:其中R 1,R 2,R 5,a和b在此公开,及其药学上可接受的衍生物(“取代的喹喔啉型桥连哌啶化合物”),包含有效量的取代 - 喹喔啉型桥连哌啶化合物,以及治疗或预防诸如疼痛的病症的方法,包括向有需要的动物施用有效量的取代的喹喔啉型桥连哌啶化合物。

    Benzenesulfonamide compounds and the use thereof
    24.
    发明授权
    Benzenesulfonamide compounds and the use thereof 有权
    苯磺酰胺化合物及其用途

    公开(公告)号:US08765736B2

    公开(公告)日:2014-07-01

    申请号:US12599608

    申请日:2008-09-26

    CPC分类号: C07D211/58 C07D401/04

    摘要: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1, R2, R3, Z and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

    摘要翻译: 本发明涉及式(I)的氮杂环丁烷基,吡咯烷基,哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐,前药或溶剂化物,其中R1,R2,R3,Z和q如说明书所述定义。 本发明还涉及使用式I化合物来治疗对阻断钙通道,特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。

    PROLINE ANALOGS AS LIGANDS FOR CANNABINOID RECEPTORS
    26.
    发明申请
    PROLINE ANALOGS AS LIGANDS FOR CANNABINOID RECEPTORS 有权
    作为CANNABINOID受体配体的精氨酸模拟物

    公开(公告)号:US20090291947A1

    公开(公告)日:2009-11-26

    申请号:US12350450

    申请日:2009-01-08

    摘要: The present invention relates to Proline Analog Compounds that are ligands for cannabinoid receptors, compositions comprising a Proline Analog Compound and a pharmaceutically-acceptable carrier, methods of making such Proline Analog Compounds, and methods for treating or preventing a Condition comprising administering an effective amount of a Proline Analog Compound to an animal in need thereof.

    摘要翻译: 本发明涉及作为大麻素受体配体的脯氨酸类似物化合物,包含脯氨酸类似物化合物和药学上可接受的载体的组合物,制备此类脯氨酸类似物的方法,以及用于治疗或预防病症的方法,包括给予有效量的 脯氨酸类似物化合物给有需要的动物。

    Benzenesulfonamide compounds and the use thereof
    27.
    发明授权
    Benzenesulfonamide compounds and the use thereof 有权
    苯磺酰胺化合物及其用途

    公开(公告)号:US08937181B2

    公开(公告)日:2015-01-20

    申请号:US12296788

    申请日:2007-04-13

    摘要: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

    摘要翻译: 本发明涉及式(I)的氮杂环丁烷基,吡咯烷基,哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐,前药或溶剂化物,其中R1-R3,Z,p和q如说明书所述定义。 本发明还涉及使用式(I)化合物来治疗,预防或改善对阻断钙通道,特别是N型钙通道的病症。 本发明的化合物特别适用于治疗疼痛。

    Proline analogs as ligands for cannabinoid receptors
    28.
    发明授权
    Proline analogs as ligands for cannabinoid receptors 有权
    脯氨酸类似物作为大麻素受体的配体

    公开(公告)号:US08084612B2

    公开(公告)日:2011-12-27

    申请号:US12350450

    申请日:2009-01-08

    IPC分类号: C07D409/12

    摘要: The invention relates to compounds of Formulae I(a) to XI and pharmaceutically acceptable salts and solvates thereof (Proline Analog Compounds), that are useful, e.g., as ligands for cannabinoid receptors, as compositions comprising a Proline Analog Compound and a pharmaceutically acceptable carrier, in methods of making such Proline Analog Compounds, and in methods for treating or preventing a Condition, such as pain, nausea, vomiting and an eating disorder, comprising administering an effective amount of a Proline Analog Compound to an animal in need thereof.

    摘要翻译: 本发明涉及式I(a)至XI的化合物及其药学上可接受的盐和溶剂合物(脯氨酸类似物化合物),其可用作例如大麻素受体的配体,作为包含脯氨酸类似物化合物和药学上可接受的载体的组合物 ,在制备这种脯氨酸类似物化合物的方法中,以及用于治疗或预防诸如疼痛,恶心,呕吐和进食障碍的病症的方法中,包括向有需要的动物施用有效量的脯氨酸类似物化合物。

    AMIDE COMPOUNDS AND THE USE THEREOF
    30.
    发明申请
    AMIDE COMPOUNDS AND THE USE THEREOF 审中-公开
    AMIDE化合物及其用途

    公开(公告)号:US20110190300A1

    公开(公告)日:2011-08-04

    申请号:US12602392

    申请日:2008-05-30

    摘要: The invention relates to amide compounds of Formula I: (I) and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl, etc.; R1 and R2 are each independently hydrogen, halogen, cyano, optionally substituted lower alky, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heterocyclyl etc. R3 and R4 are hydrogen, each optionally substituted lower alkyl, cycloalkyl, aryl or heterocyclyl etc.; X is ═O, optionally substituted lower alkyl, halogen, cyano, nitro etc., n is 0-5, m is 1 or 2 and p is 0-2. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

    摘要翻译: 本发明涉及式I的酰胺化合物:(I)及其药学上可接受的盐,前药和溶剂合物,其中:Y是CO或SOm; Z各自为任选取代的低级烷基,低级烯基,环烷基,芳基,杂环基等; R 1和R 2各自独立地为氢,卤素,氰基,任选取代的低级烷基,任选取代的环烷基,任选取代的芳基或任选取代的杂环基等。R 3和R 4是氢,各自任选取代的低级烷基,环烷基,芳基或杂环基等; X是= 0,任意取代的低级烷基,卤素,氰基,硝基等,n为0-5,m为1或2,p为0-2。 本发明还涉及使用式I的化合物来治疗,预防或改善对阻断钙通道,特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。