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    Cinnamide derivatives as KCNQ potassium channel modulators
    21.
    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

    Applicant: 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

    Inventor： 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: C07C23720

    CPC classification number: 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

    Abstract: 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.

    Abstract translation: 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。

    Carbamate and carbazate ketolide antibiotics
    22.
    发明授权
    Carbamate and carbazate ketolide antibiotics 失效
    氨基甲酸酯和咔唑酮酮内酯抗生素

    公开(公告)号：US06420343B1

    公开(公告)日：2002-07-16

    申请号：US09399497

    申请日：1999-09-20

    Applicant: Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

    Inventor： Wei-Guo Su ,  Takushi Kaneko ,  Yong-Jin Wu

    IPC: A61K3170

    CPC classification number: C07H17/08

    Abstract: This invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof wherein X1, X2, R2 and R6 are as defined herein. The compounds of formula 1 are antibacterial and antiprotozoal agents that may be used to treat various bacterial and protozoal infections and disorders related to such infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial and protozoal infections by administering 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，前药和溶剂合物，其中X 1，X 2，R 2和R 6如本文所定义。 式1的化合物是可用于治疗各种细菌和原生动物感染的抗细菌剂和抗原虫药，以及与这种感染有关的疾病。 本发明还涉及含有式1化合物的药物组合物和通过施用式1化合物来治疗细菌和原生动物感染的方法。

    Tricyclic 3-keto derivatives of 6-O-methylerthromycin
    24.
    发明授权
    Tricyclic 3-keto derivatives of 6-O-methylerthromycin 失效
    6-O-甲基红霉素的三环3-酮衍生物

    公开(公告)号：US06248719B1

    公开(公告)日：2001-06-19

    申请号：US09485965

    申请日：2000-02-18

    Applicant: Yong-Jin Wu

    Inventor： Yong-Jin Wu

    IPC: A61K3170

    CPC classification number: C07H17/08

    Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts thereof, wherein R1-R7 are as defined herein. The compounds of formula 1 are useful as antibiotic agents. The invention further relates to pharmaceutical compositions and methods of treating bacterial infection using such compounds, and to methods of making 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 7如本文所定义。 式1的化合物可用作抗生素。 本发明还涉及使用这些化合物治疗细菌感染的药物组合物和方法，以及制备式1化合物的方法。

    DIAMINOPROPANE DERIVED MACROCYCLES AS INHIBITORS OF BETA AMYLOID PRODUCTION
    28.
    发明申请
    DIAMINOPROPANE DERIVED MACROCYCLES AS INHIBITORS OF BETA AMYLOID PRODUCTION 有权
    作为淀粉酶生产的抑制剂的二亚胺衍生的大环化合物

    公开(公告)号：US20080194535A1

    公开(公告)日：2008-08-14

    申请号：US12019986

    申请日：2008-01-25

    Applicant: Lawrence R. Marcin ,  Andrew C. Good ,  Yong-Jin Wu ,  Dmitry S. Zuev ,  Richard E. Olson ,  Nenghui Wang

    Inventor： Lawrence R. Marcin ,  Andrew C. Good ,  Yong-Jin Wu ,  Dmitry S. Zuev ,  Richard E. Olson ,  Nenghui Wang

    IPC: A61K31/395 ,  C07D273/02 ,  A61P25/00

    CPC classification number: C07D273/02 ,  C07D413/04 ,  C07D487/04

    Abstract: There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, n, W, X, Y, Z and L as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.

    Abstract translation: 提供一系列式（I）的大环二氨基丙烷或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，m，n，W，X​​，Y，Z和 L，其药物组合物和使用方法。 这些新型化合物通过β-分泌酶抑制淀粉样前体蛋白（APP）的加工，更具体地，抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。

    Homopiperidine derivatives as NK-1 antagonists
    29.
    发明授权
    Homopiperidine derivatives as NK-1 antagonists 有权
    高哌啶衍生物作为NK-1拮抗剂

    公开(公告)号：US07098203B2

    公开(公告)日：2006-08-29

    申请号：US11183691

    申请日：2005-07-18

    Applicant: Yong-Jin Wu ,  Huan He

    Inventor： Yong-Jin Wu ,  Huan He

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

    CPC classification number: 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 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。 在具体实施方案中，式（I）化合物或其异构体，药学上可接受的盐或溶剂合物或药学上可接受的制剂，其包含用于治疗或预防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 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。

    3-(pyridinyl-piperazin-1-yl)-phenylethyl amides as potassium channel openers
    30.
    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

    Applicant: Yong-Jin Wu ,  Li-Qiang Sun ,  Jie Chen

    Inventor： Yong-Jin Wu ,  Li-Qiang Sun ,  Jie Chen

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

    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 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。

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