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    Compounds for the reduction of beta-amyloid production
    1.
    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
    2.
    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。

    Phenylcarboxyamides as beta-secretase inhibitors
    5.
    发明授权
    Phenylcarboxyamides as beta-secretase inhibitors 有权
    苯基羧酰胺作为β-分泌酶抑制剂

    公开(公告)号：US07476764B2

    公开(公告)日：2009-01-13

    申请号：US11494145

    申请日：2006-07-27

    Applicant: Yong-Jin Wu ,  Yunhui Zhang

    Inventor： Yong-Jin Wu ,  Yunhui Zhang

    IPC: C07C233/00 ,  A01N37/18

    CPC classification number: C07C251/48 ,  C07C235/42 ,  C07C235/84 ,  C07C311/08 ,  C07C317/44 ,  C07D279/02

    Abstract: There is provided a series of novel phenylcarboxyamides of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, X and Y 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: 提供了一系列式（I）的新型苯基羧酰胺或立体异构体; 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，X和Y，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。

    Cyclopentylamine and cyclohexylamine derivatives as NK-1/SSRI antagonists
    6.
    发明授权
    Cyclopentylamine and cyclohexylamine derivatives as NK-1/SSRI antagonists 有权
    环戊胺和环己胺衍生物作为NK-1 / SSRI拮抗剂

    公开(公告)号：US07276631B2

    公开(公告)日：2007-10-02

    申请号：US11183700

    申请日：2005-07-18

    Applicant: Yong-Jin Wu ,  Huan He

    Inventor： Yong-Jin Wu ,  Huan He

    IPC: C07C243/00 ,  A01N31/00

    CPC classification number: C07C217/52 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14

    Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the 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。 本公开的具体实施方案涉及式（I）的化合物; 或其异构体，药学上可接受的盐或溶剂合物或包含所述化合物的药学上可接受的制剂可用于治疗或预防由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。 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。

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

    公开(公告)号：US06825171B2

    公开(公告)日：2004-11-30

    申请号：US10409016

    申请日：2003-04-08

    Applicant: Yong-Jin Wu

    Inventor： Yong-Jin Wu

    IPC: A61K3170

    CPC classification number: C07H17/08

    Abstract: The invention relates to novel erythromycin derivatives, particularly ones with novel C-13 R13 substitutents, and to pharmaceutically acceptable salts thereof. The compounds of this invention are useful as antibacterial agents and antiprotozoa agents and for other applications (e.g., anticancer, atherosclerosis, gastric motility reduction, etc.) in mammals, including man, as well as in fish and. The invention also relates to pharmaceutical compositions containing such compounds and to methods of treating bacterial protozoa infections by administering such compounds. The invention also relates to methods of preparing such compounds and to intermediates useful in such preparation.

    Abstract translation: 本发明涉及新型红霉素衍生物，特别是具有新型C-13 R 13取代基的红霉素衍生物及其药学上可接受的盐。 本发明的化合物可用作抗菌剂和抗原生动物剂，以及哺乳动物，包括人以及鱼和其他用途（例如抗癌，动脉粥样硬化，胃动力降低等）。 本发明还涉及含有这些化合物的药物组合物以及通过施用这些化合物来治疗细菌原生动物感染的方法。 本发明还涉及制备此类化合物的方法和用于此类制备的中间体。

    13-methyl erythromycin derivatives
    9.
    发明授权
    13-methyl erythromycin derivatives 失效
    13-甲基红霉素衍生物

    公开(公告)号：US06777543B2

    公开(公告)日：2004-08-17

    申请号：US10441347

    申请日：2003-05-19

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

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

    IPC: C07H1708

    CPC classification number: C07H17/08

    Abstract: The invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R17, Rf, A, X, and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1, methods of using the compounds of formula 1 in the treatment of infections and methods of preparing the compounds of formula 1.

    Abstract translation: 本发明涉及下式的化合物及其药学上可接受的盐，前药和溶剂化物，其中R 1，R 2，R 3，R 4，R 5，R 17，R A，X和Y如本文所定义。 本发明还涉及含有式1化合物，使用式1化合物治疗感染的方法和制备式1化合物的方法的药物组合物。

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