OXIME COMPOUNDS AND THE USE THEREOF
    2.
    发明申请
    OXIME COMPOUNDS AND THE USE THEREOF 审中-公开
    OXIME化合物及其用途

    公开(公告)号:US20090298878A1

    公开(公告)日:2009-12-03

    申请号:US12373328

    申请日:2007-07-12

    摘要: The invention relates to oxime compounds of Formula (I) and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein X is hydrogen, optionally substituted aryl, optionally substituted heteroaryl or the like; Y is CO, SO2, CR3R4 or the like; Z is optionally substituted lower alkyl, optionally substituted aryl or the like; W is optionally substituted lower alkylene or optionally substituted lower alkenylene, R3 and R4 are each independently hydrogen, lower alkyl or the like; p is 0, 1, or 2 and q is 0, 1 or 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)的肟化合物及其药学上可接受的盐,前药或溶剂化物,其中X是氢,任选取代的芳基,任选取代的杂芳基等; Y是CO,SO2,CR3R4等; Z是任选取代的低级烷基,任选取代的芳基等; W是任选取代的低级亚烷基或任选取代的低级亚烯基,R 3和R 4各自独立地是氢,低级烷基等; p是0,1或2,q是0,1或2.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有响应的病症,特别是N型 钙通道。 本发明的化合物特别适用于治疗疼痛。

    Substituted-quinoxaline-type bridged-piperidine compounds as ORL-1 modulators
    3.
    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
    6.
    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。

    OXYIMINO COMPOUNDS AND THE USE THEREOF
    8.
    发明申请
    OXYIMINO COMPOUNDS AND THE USE THEREOF 有权
    OXYIMINO化合物及其用途

    公开(公告)号:US20100240703A1

    公开(公告)日:2010-09-23

    申请号:US12602441

    申请日:2008-05-30

    CPC分类号: C07D211/96

    摘要: The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. 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)的氧亚氨基化合物及其药学上可接受的盐,前药和溶剂化物,其中:Y是CO或SOm; Z是氢,每个任选取代的低级烷基,低级烯基,芳基,杂环基等.R 1和R 2各自独立地为氢,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,各X独立地为= 任选取代的低级烷基,氰基,硝基等,m为1或2,p为O,1或2,q为O或1.本发明还涉及式I的用途化合物,以治疗,预防或改善 对钙通道阻断,特别是N型钙通道的阻滞作用。 本发明的化合物特别适用于治疗疼痛。

    Oxyimino compounds and the use thereof
    9.
    发明授权
    Oxyimino compounds and the use thereof 有权
    氧亚氨基化合物及其用途

    公开(公告)号:US08563732B2

    公开(公告)日:2013-10-22

    申请号:US12602441

    申请日:2008-05-30

    IPC分类号: A61K31/44 C07D211/00

    CPC分类号: C07D211/96

    摘要: The invention relates to oxyimino compounds of (Formula I), and pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein: Y is CO or SOm; Z is hydrogen, each optionally substituted lower alkyl, lower alkenyl, aryl, heterocyclyl etc. R1 and R2 are each independently hydrogen, each optionally substituted lower alkyl, lower alkenyl, cycloalkyl, aryl, heterocyclyl etc., each X is independently ═O, optionally substituted lower alkyl, cyano, nitro etc., m is 1 or 2, p is O, 1 or 2 and q is O or 1. 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)的氧亚氨基化合物及其药学上可接受的盐,前药和溶剂化物,其中:Y是CO或SOm; Z是氢,每个任选取代的低级烷基,低级烯基,芳基,杂环基等.R 1和R 2各自独立地为氢,各自为任意取代的低级烷基,低级烯基,环烷基,芳基,杂环基等,各X独立地为= 任选取代的低级烷基,氰基,硝基等,m为1或2,p为O,1或2,q为O或1.本发明还涉及式I的用途化合物,以治疗,预防或改善 对钙通道阻断,特别是N型钙通道的阻滞作用。 本发明的化合物特别适用于治疗疼痛。

    Nitrogen-containing heterocycle derivatives substituted with cyclic group
    10.
    发明授权
    Nitrogen-containing heterocycle derivatives substituted with cyclic group 失效
    用环状基团取代的含氮杂环衍生物

    公开(公告)号:US07935706B2

    公开(公告)日:2011-05-03

    申请号:US12278412

    申请日:2007-02-21

    IPC分类号: A61K31/497

    摘要: It was found out that the nitrogen-containing heterocyclic derivative represented by the formula (I) specifically binds to a receptor of NR1/NR2B, and is used as a NR2B receptor antagonist.A compound represented by: wherein Z is N or CR1, A1 is a nitrogen-containing aromatic monocyclic group which is optionally substituted, a nitrogen-containing aromatic fused cyclic group which is optionally substituted etc., A2 is an aromatic hydrocarbon cyclic group or an aromatic heterocyclic group, each optionally having a substituent, R1, R2, Ra, Rb, Rc and Rd are each independently hydrogen, hydroxy, etc., w is 2 or 3, t is 1 or 2, X is —(CR3R4)m-, —CO(CR3R4)n-, —CONR5(CR3R4)n- etc., m is an integer of 1 to 4, n is an integer of 0 to 4, R3 and R4 are each independently hydrogen, halogen, hydroxy etc., and R5 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt, or a solvate thereof.

    摘要翻译: 发现由式(I)表示的含氮杂环衍生物特异性结合NR1 / NR2B的受体,并用作NR2B受体拮抗剂。 由下式表示的化合物:其中Z为N或CR1,A1为任选取代的含氮芳族单环基团,任选取代的含氮芳族稠合环基等,A2为芳族烃环基或 芳族杂环基,各自任选具有取代基,R 1,R 2,R a,R b,R c和R d各自独立地为氢,羟基等,w为2或3,t为1或2,X为 - (CR 3 R 4)m - ,-CO(CR 3 R 4)n - , - CONR 5(CR 3 R 4)n - 等,m为1〜4的整数,n为0〜4的整数,R 3和R 4各自独立地为氢,卤素,羟基等 R5为氢或低级烷基,或其药学上可接受的盐或溶剂合物。