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    Diaminopropane derived macrocycles as inhibitors of β amyloid production
    31.
    发明授权
    Diaminopropane derived macrocycles as inhibitors of β amyloid production 有权
    二氨基丙烷衍生的大环化合物作为抑制剂 淀粉样蛋白生成

    公开(公告)号：US07772221B2

    公开(公告)日：2010-08-10

    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: C07D403/04 ,  C07D413/04 ,  A61K31/4025 ,  A61P25/28

    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，其中如本文所定义的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。 这些新化合物通过分泌酶抑制淀粉样蛋白前体蛋白（APP）的加工，更具体地，抑制Aβ的生成。 本公开涉及可用于治疗与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。

    Oxime-Containing Acyl Guanidines as Beta-Secretase Inhibitors
    32.
    发明申请
    Oxime-Containing Acyl Guanidines as Beta-Secretase Inhibitors 有权
    含肟的酰基胍作为β-分泌酶抑制剂

    公开(公告)号：US20070232581A1

    公开(公告)日：2007-10-04

    申请号：US11693026

    申请日：2007-03-29

    Applicant: Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

    Inventor： Yong-Jin Wu ,  Samuel Gerritz ,  Shuhao Shi ,  Shirong Zhu

    IPC: A61K31/55 ,  A61K31/445 ,  A61K31/40 ,  A61K31/397 ,  A61K31/396 ,  A61K31/165 ,  C07D211/26 ,  C07D207/30 ,  C07D223/04 ,  C07D203/04

    CPC classification number: C07D209/20 ,  C07C257/20 ,  C07C279/22

    Abstract: There is provided a series of substituted oxime-containing acyl guanidines of Formula (I) or a stereoisomer; or a nontoxic pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, their pharmaceutical compositions and methods of use. These 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: 提供了一系列式（I）的取代的含肟基的酰基胍或立体异构体; 或其无毒的药学上可接受的盐，其中R 1，R 2，R 3，R 4，R R 5，R 6和R 7如本文所定义，其药物组合物和使用方法。 这些化合物通过β-分泌酶抑制淀粉样蛋白前体蛋白（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。

    Cycloalkylamine derivatives as NK-1/SSRI antagonists
    34.
    发明申请
    Cycloalkylamine derivatives as NK-1/SSRI antagonists 有权

    公开(公告)号：US20060019992A1

    公开(公告)日：2006-01-26

    申请号：US11183699

    申请日：2005-07-18

    Applicant: Yong-Jin Wu ,  Huan He

    Inventor： Yong-Jin Wu ,  Huan He

    IPC: C07D211/26 ,  A61K31/445

    CPC classification number: C07D225/02

    Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment relates to compounds of Formula (I) or an isomer, a pharmaceutically acceptable salt or solvate thereof and pharmaceutically acceptable formulations 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.

    Cinnamide derivatives as KCNQ potassium channel modulators
    36.
    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
    37.
    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
    39.
    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。

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