利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

52 条记录 (耗时 0.029 秒)

    3-(pyridinyl-piperazin-1-yl)-phenylethyl amides as potassium channel openers
    2.
    发明授权
    3-(pyridinyl-piperazin-1-yl)-phenylethyl amides as potassium channel openers 有权
    3-（吡啶基 - 哌嗪-1-基） - 苯基乙酰胺作为钾通道开放剂

    公开(公告)号：US07087609B2

    公开(公告)日：2006-08-08

    申请号：US10719188

    申请日：2003-11-21

    申请人： Yong-Jin Wu ,  Li-Qiang Sun ,  Jie Chen

    发明人： Yong-Jin Wu ,  Li-Qiang Sun ,  Jie Chen

    IPC分类号： A61K31/496 ,  C07D401/04 ,  C07D401/14 ,  C07D409/14

    CPC分类号： C07D409/12 ,  C07D213/74 ,  C07D401/12

    摘要： The present invention provides piperazinyl phenylethyl amides and related derivatives having the general Formula I 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.

    摘要翻译： 本发明提供具有通式I的哌嗪基苯乙基酰胺和相关衍生物，其中R 1，R 2，R 3，R 3， 4，R 5，R 6，A和B如说明书中所定义，或其无毒的药学上可接受的盐，溶剂合物或水合物，其为开放剂 或KCNQ钾通道的激活剂。 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。

    1-aryl-2-hydroxyethyl amides as potassium channel openers
    4.
    发明授权
    1-aryl-2-hydroxyethyl amides as potassium channel openers 有权
    1-芳基-2-羟乙基酰胺作为钾通道开放剂

    公开(公告)号：US07045551B2

    公开(公告)日：2006-05-16

    申请号：US10719465

    申请日：2003-11-21

    申请人： Yong-Jin Wu ,  Li-Qiang Sun ,  Huan He ,  Alexandre L'Heureux

    发明人： Yong-Jin Wu ,  Li-Qiang Sun ,  Huan He ,  Alexandre L'Heureux

    IPC分类号： A61K31/165 ,  A61K31/34 ,  A61K31/535 ,  C07D265/30 ,  C07D307/78

    CPC分类号： C07D295/135 ,  C07C233/19 ,  C07C233/22 ,  C07C233/60 ,  C07C233/73 ,  C07C2601/08 ,  C07C2601/14 ,  C07D213/40 ,  C07D307/54 ,  C07D333/24

    摘要： The present invention provides novel aryl hydroxyethyl amides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, R7 and A 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 aryl hydroxyethyl 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.

    摘要翻译： 本发明提供了具有通式I的新型芳基羟乙基酰胺和相关衍生物，其中R 1，R 2，R 3，R 3， R 4，R 5，R 6，R 7和A如说明书中所定义，或无毒的药学上可接受的 盐，溶剂合物或水合物，它们是KCNQ钾通道的开放剂或活化剂。 本发明还提供包含所述芳基羟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的方法。

    Cinnamide derivatives as KCNQ potassium channel modulators
    5.
    发明授权
    Cinnamide derivatives as KCNQ potassium channel modulators 有权
    桂酰胺衍生物作为KCNQ钾通道调节剂

    公开(公告)号：US06831080B2

    公开(公告)日：2004-12-14

    申请号：US10160582

    申请日：2002-05-31

    申请人： Yong-Jin Wu ,  Li-Quang Sun ,  Jie Chen ,  Huan He ,  Alexandre L'Heureux ,  Pierre Dextraze ,  Jean-Paul Daris ,  Gene G. Kinney ,  Steven I. Dworetzky ,  Piyasena Hewawasam

    发明人： Yong-Jin Wu ,  Li-Quang Sun ,  Jie Chen ,  Huan He ,  Alexandre L'Heureux ,  Pierre Dextraze ,  Jean-Paul Daris ,  Gene G. Kinney ,  Steven I. Dworetzky ,  Piyasena Hewawasam

    IPC分类号： C07C23720

    CPC分类号： C07D213/40 ,  C07C233/11 ,  C07C235/34 ,  C07D209/08 ,  C07D213/56 ,  C07D215/04 ,  C07D215/12 ,  C07D217/06 ,  C07D239/26 ,  C07D241/12 ,  C07D265/30 ,  C07D265/36 ,  C07D295/135 ,  C07D307/79 ,  C07D311/58 ,  C07D317/58 ,  C07D317/60 ,  C07D319/18 ,  C07D333/24 ,  C07D407/12 ,  C07D491/08

    摘要： There is provided novel cinnamide derivatives of Formula I: wherein R is C1-4 alkyl or trifluoromethyl; R1 is selected from the group consisting of pyridinyl, quinolinyl, thienyl, furanyl, 1,4-benzodioxanyl, 1,3-benzodioxolyl, chromanyl, indanyl, biphenylyl, phenyl and substituted phenyl in which said substituted phenyl is substituted with one or two substituents each independently selected-from the group consisting of halogen, C1-4 alkyl, C1-4 alkoxy, trifluoromethyl, trifluoromethoxy and nitro; R2 and R3 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, and halogen; R4 is selected from the group consisting of di(C1-4 alkyl)amino, trifluoromethoxy and optionally substituted morpholin-4-yl, pyridinyl, pyrimidinyl, piperazinyl, and pyrazinyl with one or two substituents in which said substituent is independently selected from the group consisting of C1-4 alkyl, aminomethyl, hydroxymethyl, chloro or fluoro; R5 is hydrogen, chloro or fluoro; or R4 and R5 taken together are —CH═CH—CH═CH— or —X(CH2)mY— in which X and Y are each independently selected from the group consisting of CH2, (CH2)nN(R9)— and O, wherein m is 1 or 2; n is 0 or 1; and R6, R7, and R8 are each independently selected from hydrogen, chloro and fluoro; and R9 is selected from the group consisting of hydrogen, C1-4 alkyl, hydroxyethyl, C1-4 alkoxyethyl, cyclopropylmethyl, —CO2(C1-4alkyl), and —CH2CH2NR10R11 in which R10 and R11 are each independently hydrogen or C1-4 alkyl, which are openers of the KCNQ potassium channels and are useful in the treatment of disorders which are responsive to the opening of the KCNQ potassium channels.

    摘要翻译： 提供式I的新颖的肉桂酰胺衍生物：其中R是C 1-4烷基或三氟甲基; R 1选自吡啶基，喹啉基，噻吩基，呋喃基，1,4-苯并二恶烷基，1,3-苯并二恶唑基，苯并二氢吡喃基，茚满基，联苯基，苯基和取代的苯基，其中所述取代的苯基被一个 或两个各自独立地选自卤素，C 1-4烷基，C 1-4烷氧基，三氟甲基，三氟甲氧基和硝基的取代基; R 2和R 3各自独立地选自氢，C 1-4烷基和卤素; R 4选自二（C 1-4烷基）氨基，三氟甲氧基和任选取代的吗啉-4-基，吡啶基，嘧啶基，哌嗪基和吡嗪基，其中一个或两个取代基独立地选自所述取代基 由C1-4烷基，氨基甲基，羟甲基，氯或氟组成的基团; R 5是氢，氯或氟; 或R 4和R 5一起为-CH = CH-CH = CH-或-X（CH 2）mY-，其中X和Y各自独立地选自CH 2，（CH 2）n N （R 9） - 和O，其中m为1或2; n为0或1; 和R 6，R 7和R 8各自独立地选自氢，氯和氟; 并且R 9选自氢，C 1-4烷基，羟乙基，C 1-4烷氧基乙基，环丙基甲基，-CO 2（C 1-4烷基）和-CH 2 CH 2 NR 10 R 11， 10>和R 11各自独立地是氢或C 1-4烷基，其是KCNQ钾通道的开放剂，并且可用于治疗对开放KCNQ钾通道有响应的病症。

    Compounds for the reduction of beta-amyloid production
    6.
    发明授权
    Compounds for the reduction of beta-amyloid production 有权
    用于减少β-淀粉样蛋白生成的化合物

    公开(公告)号：US08604024B2

    公开(公告)日：2013-12-10

    申请号：US13477143

    申请日：2012-05-22

    申请人： Lorin A. Thompson, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

    发明人： Lorin A. Thompson, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

    IPC分类号： C07D279/08 ,  C07D513/04 ,  C07D417/10

    CPC分类号： C07D279/08 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D513/04

    摘要： Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein X is selected from the group of CH2, O, and NR2; m=0 or 1; R1 at each instance is selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is a bond, —NHCO—, —NH—, or L and Z together can be absent; Z is a C6-C10-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, haloC1-4 alkoxy, 4-methoxyphenyl, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; R2 is selected from the group of hydrogen, benzyl, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, acetyl, and methanesulfonyl; and R3, R4 and R5 are independently selected from hydrogen or C1-4alkyl.

    摘要翻译： 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。

    Erythromycin derivatives
    8.
    发明授权
    Erythromycin derivatives 失效
    红霉素衍生物

    公开(公告)号：US06262030B1

    公开(公告)日：2001-07-17

    申请号：US09432500

    申请日：1999-11-02

    申请人： Yong-Jin Wu ,  Wei-Guo Su

    发明人： Yong-Jin Wu ,  Wei-Guo Su

    IPC分类号： C07H1708

    CPC分类号： C07H17/08

    摘要： The invention relates to the compounds of the formula 1 and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula 1, methods of using said compounds of formula 1 in the treatment of infections, and methods of preparing said the compounds of formula 1.

    摘要翻译： 本发明涉及式1的化合物及其药学上可接受的盐，其中R 1，R 2，R 3，X和Y如本文所定义。 本发明还涉及含有式1化合物的药物组合物，使用式1化合物治疗感染的方法，以及制备所述式1化合物的方法。

    9-amino-3-keto erythromycin derivatives
    9.
    发明授权
    9-amino-3-keto erythromycin derivatives 失效
    9-氨基-3-酮红霉素衍生物

    公开(公告)号：US06159945A

    公开(公告)日：2000-12-12

    申请号：US402338

    申请日：1999-10-06

    申请人： Yong-Jin Wu

    发明人： Yong-Jin Wu

    IPC分类号： C07H17/08 ,  A61K31/70

    CPC分类号： C07H17/08

    摘要： The invention relates to compounds of the formula I ##STR1## and to pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I, methods of using said compounds of formula I in the treatment of infections, and methods of preparing said compounds of formula I.

    摘要翻译： PCT No.PCT / IB98 / 01578第 371 1999年10月6日第 102（e）日期1999年10月6日PCT提交1998年10月9日PCT公布。 WO99 /​​ 21866 PCT出版物 日期1999年5月6日本发明涉及式I化合物及其药学上可接受的盐，其中R1，R2，R3，R4和X如本文所定义。 本发明还涉及含有式I化合物的药物组合物，使用式I化合物治疗感染的方法，以及制备所述式I化合物的方法。

    Compounds for the reduction of beta-amyloid production
    10.
    发明授权
    Compounds for the reduction of beta-amyloid production 有权
    用于减少β-淀粉样蛋白生成的化合物

    公开(公告)号：US08598161B2

    公开(公告)日：2013-12-03

    申请号：US13478238

    申请日：2012-05-23

    申请人： Yong-Jin Wu

    发明人： Yong-Jin Wu

    IPC分类号： C07D513/04 ,  C07D279/08

    CPC分类号： C07D513/04

    摘要： Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R1, R2, R3, R4, R5, and R6 are independently hydrogen, C1-C6 alkyl or C1-C6 cycloalkyl; Y and Z are independently a C6-C10-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, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, OH, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is either a bond or is —NHCO—; L and Z together can be absent; and m is 1, 2 or 3.

    摘要翻译： 式（I）化合物，包括其药学上可接受的盐，在此列出：其中R 1，R 2，R 3，R 4，R 5和R 6独立地为氢，C 1 -C 6烷基或C 1 -C 6环烷基; Y和Z独立地是C 6 -C 10 - 芳基或5-10元杂环基，其中每个Y和Z基团可以任选地被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。