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    3-Heterocyclic benzylamide derivatives as potassium channel openers
    11.
    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

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

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

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

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

    Abstract: 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.

    Abstract translation: 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。

    Compounds for the reduction of beta-amyloid production
    13.
    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

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

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

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

    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: 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.

    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
    16.
    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

    Applicant: Yong-Jin Wu ,  Wei-Guo Su

    Inventor： Yong-Jin Wu ,  Wei-Guo Su

    IPC: C07H1708

    CPC classification number: C07H17/08

    Abstract: 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.

    Abstract translation: 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
    17.
    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

    Applicant: Yong-Jin Wu

    Inventor： Yong-Jin Wu

    IPC: C07H17/08 ,  A61K31/70

    CPC classification number: C07H17/08

    Abstract: 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.

    Abstract translation: 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
    18.
    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

    Applicant: Yong-Jin Wu

    Inventor： Yong-Jin Wu

    IPC: C07D513/04 ,  C07D279/08

    CPC classification number: C07D513/04

    Abstract: 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.

    Abstract translation: 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。

    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    19.
    发明申请
    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION 有权
    用于还原β-淀粉样生成的化合物

    公开(公告)号：US20130131051A1

    公开(公告)日：2013-05-23

    申请号：US13477143

    申请日：2012-05-22

    Applicant: LORIN A. THOMPSON, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

    Inventor： LORIN A. THOMPSON, III ,  Jianliang Shi ,  Yong-Jin Wu ,  Lawrence R. Marcin ,  Ramkumar Rajamani ,  Mendi A. Higgins

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

    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: 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.

    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。

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