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    3-(PYRIDINYL-PIPERAZIN-1-YL)-PHENYLETHYL AMIDES AS POTASSIUM CHANNEL OPENERS
    2.
    发明申请
    3-(PYRIDINYL-PIPERAZIN-1-YL)-PHENYLETHYL AMIDES AS POTASSIUM CHANNEL OPENERS 审中-公开
    3-（吡啶基 - 哌嗪-1-基） - 苯基乙烯酰胺作为磷酸盐通道开放剂

    公开(公告)号：WO2004047745A2

    公开(公告)日：2004-06-10

    申请号：PCT/US2003/037350

    申请日：2003-11-21

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： WU, Yong-Jin ,  SUN, Li-Qiang ,  CHEN, Jie

    IPC: A61K

    CPC classification number: C07D409/12 ,  C07D213/74 ,  C07D401/12

    Abstract: The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I [INSERT CHEMICAL STRUCTURE] wherein R1, R2, R3, R4, R5, R6, A and B are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said piperazinyl phenylethyl amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain, and anxiety.

    Abstract translation: 本发明提供具有通式I [INSERT CHEMICAL STRUCTURE]的哌嗪基苯乙基酰胺和相关衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，A和B如说明书中所定义，或无毒的药学上可接受的盐， 其是KCNQ钾通道的开放剂或活化剂的溶剂化物或水合物。 本发明还提供了包含所述哌嗪基苯乙基酰胺的药物组合物和治疗对KCNQ钾通道开放活性敏感的疾病如偏头痛或偏头痛发作，双相情感障碍，癫痫，急性和慢性疼痛和焦虑症的方法。

    HOMOPIPERDININE DERIVATIVES AS NK-1 ANTAGONISTS
    5.
    发明申请
    HOMOPIPERDININE DERIVATIVES AS NK-1 ANTAGONISTS 审中-公开

    公开(公告)号：WO2006014703A3

    公开(公告)日：2006-02-09

    申请号：PCT/US2005/025688

    申请日：2005-07-20

    Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  WU, Yong-Jin ,  HE, Huan

    Inventor： WU, Yong-Jin ,  HE, Huan

    IPC: A61P25/00 ,  A61K31/55 ,  C07D223/04

    Abstract: The present disclosure relates to chemical compounds and their use in human therapy. In a specific embodiment, compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds (I) useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

    CYCLOPENTYLAMINE AND CYCLOHEXYLAMINE DERIVATIVES AS NK-1/SSRI ANTAGONISTS
    6.
    发明申请
    CYCLOPENTYLAMINE AND CYCLOHEXYLAMINE DERIVATIVES AS NK-1/SSRI ANTAGONISTS 审中-公开
    作为NK-1 / SSRI拮抗剂的环丙胺和环己基胺衍生物

    公开(公告)号：WO2006014664A2

    公开(公告)日：2006-02-09

    申请号：PCT/US2005/025630

    申请日：2005-07-20

    Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  WU, Yong-Jin ,  HE, Huan

    Inventor： WU, Yong-Jin ,  HE, Huan

    IPC: A61K31/55 ,  A61K31/495 ,  A61K31/445 ,  A61K31/40

    CPC classification number: C07C217/52 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14

    Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.

    Abstract translation: 本公开涉及化学化合物及其在人类治疗中的用途。 本公开的具体实施方案涉及式（I）的化合物; 或其异构体，药学上可接受的盐或溶剂合物或包含所述化合物的药学上可接受的制剂可用于治疗或预防由速激肽介导的病症和/或选择性抑制5-羟色胺再摄取转运蛋白。 该化合物作为双重NK-1拮抗剂和选择性5-羟色胺再摄取抑制剂。

    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    7.
    发明申请
    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION 审中-公开
    用于还原β-淀粉酶生产的化合物

    公开(公告)号：WO2012162334A1

    公开(公告)日：2012-11-29

    申请号：PCT/US2012/039037

    申请日：2012-05-23

    Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  WU, Yong-Jin

    Inventor： WU, Yong-Jin

    IPC: C07D513/04 ,  A61K31/542 ,  A61P25/28

    CPC classification number: C07D513/04

    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are independently hydrogen, C 1 -C 6 alkyl or C 1 -C 6 cycloalkyl; Y and Z are independently a C 6 -C 10 - aryl group or a 5-10 membered heterocyclic group, wherein each Y and Z group can be optionally substituted with from 0-3 substituents selected from halogen, amino, C 1-4 alkylamino, C 1-4 dialkylamino, haloC 1-4 alkyl, OH, CN, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, and C 2 -C 4 alkynyl; L is either a bond or is -NHCO-; L and Z together can be absent; and m is 1, 2 or 3.

    Abstract translation: 包括其药学上可接受的盐的式（I）化合物在本文中阐述：其中R1，R2，R3，R4，R5和R6独立地是氢，C1-C6烷基或C1-C6环烷基; Y和Z独立地为C 6 -C 10 - 芳基或5-10元杂环基，其中每个Y和Z基团可任选被0-3个选自卤素，氨基，C 1-4烷基氨基，C 1-4二烷基氨基 卤代C 1-4烷基，OH，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是键或是-NHCO-; L和Z一起可以不存在; m为1,2或3。

    TRICYCLIC COMPOUNDS AS INHIBITORS FOR THE PRODUCTION OF BETA-AMYLOID
    8.
    发明申请
    TRICYCLIC COMPOUNDS AS INHIBITORS FOR THE PRODUCTION OF BETA-AMYLOID 审中-公开
    作为生产β-淀粉样蛋白的抑制剂的三聚化合物

    公开(公告)号：WO2012162330A1

    公开(公告)日：2012-11-29

    申请号：PCT/US2012/039031

    申请日：2012-05-23

    Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  THOMPSON III, Lorin A. ,  SHI, Jianliang ,  WU, Yong-Jin ,  MARCIN, Lawrence R. ,  RAJAMANI, Ramkumar ,  HIGGINS, Mendi A.

    Inventor： THOMPSON III, Lorin A. ,  SHI, Jianliang ,  WU, Yong-Jin ,  MARCIN, Lawrence R. ,  RAJAMANI, Ramkumar ,  HIGGINS, Mendi A.

    IPC: C07D279/08 ,  C07D417/04 ,  C07D417/12 ,  C07D513/04 ,  A61K31/5415 ,  A61K31/542 ,  A61K31/55 ,  A61P25/28

    CPC classification number: C07D279/08 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D513/04

    Abstract: Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: formula (I), wherein X is selected from the group of CH 2 , O, and NR 2 ; m = 0 or 1; R 1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC 1-4 alkyl, CN, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, and C2-C4 alkynyl; L is a bond, -NHCO-, -NH-, or L and Z together can be absent; Z is a C 6 -C 10 - aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, haloC 1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C 1-4 alkylamino, C 1-4 dialkylamino, haloC 1-4 alkyl, CN, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, and C 2 -C 4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C 1 -C 6 alkyl or cycloalkyl, C 1 -C 6 alkoxy, acetyl, and methanesulfonyl; and R 3 , R 4 and R 5 are independently selected from hydrogen or C 1-4 alkyl.

    Abstract translation: 包括其药学上可接受的盐的式（I）化合物在本文中列出：式（I），其中X选自CH 2，O和NR 2; m = 0或1; 每个实例的R 1选自卤素，羟基，氨基，C 1-4烷基氨基，C 1-4二烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是键，-NHCO-，-NH-或L和Z可以不存在; Z是可以被0-3个选自卤素，卤代C 1-4烷氧基，4-甲氧基苯基，羟基，氨基，C 1 -C 10 - 芳基的取代基取代的C 6 -C 10 - 芳基或5-10元杂环基。 C 1-4烷基氨基，卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; R 2选自氢，苄基，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基，乙酰基和甲磺酰基; 并且R 3，R 4和R 5独立地选自氢或C 1-4烷基。

    PYRIDINYL, PYRIMIDINYL AND PYRAZINYL AMIDES AS POTASSIUM CHANNEL OPENERS
    9.
    发明申请
    PYRIDINYL, PYRIMIDINYL AND PYRAZINYL AMIDES AS POTASSIUM CHANNEL OPENERS 审中-公开
    作为钾通道开放剂的吡啶基，嘧啶基和吡嗪基酰胺

    公开(公告)号：WO2004047739A2

    公开(公告)日：2004-06-10

    申请号：PCT/US2003/037306

    申请日：2003-11-21

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： WU, Yong-Jin ,  SUN, Li-Qiang ,  CHEN, Jie ,  HE, Huan

    IPC: A61K

    CPC classification number: C07D213/74 ,  C07D213/38 ,  C07D213/65 ,  C07D213/68 ,  C07D239/34 ,  C07D405/12 ,  C07D409/12

    Abstract: The present invention provides novel heterocyclic amides and related derivatives having the general Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

    Abstract translation: 本发明提供具有通式（I）的新型杂环酰胺和相关衍生物，其中R 1，R 2，R 4，R 5， 3，R 4，R 5，R 6，A，B和Z如说明书中所定义，或者a 无毒的药学上可接受的盐，溶剂合物或水合物，它们是KCNQ钾通道的开启剂或活化剂。 本发明还提供了包含所述杂环酰胺的药物组合物以及治疗对KCNQ钾通道开放活性敏感的疾病如偏头痛或偏头痛发作，双相性精神障碍，癫痫，急性和慢性疼痛和焦虑的方法。

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