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17 条记录 (耗时 0.08 秒)

    1-aryl-2-hydroxyethyl amides as potassium channel openers
    11.
    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。

    3-Heterocyclic benzylamide derivatives as potassium channel openers
    13.
    发明授权
    3-Heterocyclic benzylamide derivatives as potassium channel openers 有权
    3-杂环苄基酰胺衍生物作为钾通道开放剂

    公开(公告)号：US07135472B2

    公开(公告)日：2006-11-14

    申请号：US10719187

    申请日：2003-11-21

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

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

    IPC分类号： A61K31/50 ,  A61K31/496 ,  C07D213/44 ,  C07D413/00 ,  C07D233/54

    CPC分类号： C07D213/40 ,  C07D213/82 ,  C07D231/12 ,  C07D233/54 ,  C07D249/08 ,  C07D261/08 ,  C07D263/32 ,  C07D277/28 ,  C07D401/12 ,  C07D405/12

    摘要： The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het 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 novel 3-heterocyclic benzylamides 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： 本发明提供新的3-杂环苄基酰胺和具有通式I的相关衍生物，其中R 1，R 2，R 3，R 3， 其中R 4，R 5，R 6，A和H e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，其中 是KCNQ钾通道的开放剂或活化剂。 本发明还提供包含所述新型3-杂环苄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。

    Cinnamide derivatives as KCNQ potassium channel modulators
    15.
    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。

    Preparation of chloromethylpyridine hydrochlorides
    17.
    发明授权
    Preparation of chloromethylpyridine hydrochlorides 失效
    氯甲基吡啶盐酸盐的制备

    公开(公告)号：US5942625A

    公开(公告)日：1999-08-24

    申请号：US187402

    申请日：1998-11-06

    申请人： Yuan Wang ,  Lu Wei Liu ,  Alexandre L'Heureux ,  Olivier Lepage ,  Diane Phelan

    发明人： Yuan Wang ,  Lu Wei Liu ,  Alexandre L'Heureux ,  Olivier Lepage ,  Diane Phelan

    IPC分类号： C07D213/26

    CPC分类号： C07D213/26

    摘要： Chloromethylpyridine hydrochlorides such as 3-chloromethylpyridine hydrochloride, an important pharmaceutical intermediate, are prepared in high yield and high purity by reacting the corresponding pyridyl carbinol with a slight excess of thionyl chloride, in solution in an inert solvent such as toluene. The pyridyl carbinol solution is added to the thionyl chloride gradually and under its surface, to prevent the formation of impurities. The product is recovered by applying vacuum or nitrogen purge to the reaction mixture to assist precipitation, followed by filtration and washing.

    摘要翻译： 氯甲基吡啶盐酸盐如3-氯甲基吡啶盐酸盐，重要的药物中间体，通过在惰性溶剂如甲苯中的溶液中使相应的吡啶基甲醇与稍过量的亚硫酰氯反应，以高产率和高纯度制备。 将吡啶基甲醇溶液逐渐加入到亚硫酰氯的表面，以防止杂质的形成。 通过对反应混合物进行真空或氮气吹扫来回收产物以辅助沉淀，随后过滤和洗涤。