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    COMPOUNDS FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    12.
    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：US20130131049A1

    公开(公告)日：2013-05-23

    申请号：US13478238

    申请日：2012-05-23

    Applicant: Yong-Jin Wu

    Inventor： Yong-Jin Wu

    IPC: C07D513/04

    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。

    Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors
    15.
    发明授权
    Oxime-containing macrocyclic acyl guanidines as β-secretase inhibitors 有权
    含肟的大环酰基鸟嘌呤作为分泌酶抑制剂

    公开(公告)号：US07678784B2

    公开(公告)日：2010-03-16

    申请号：US11940597

    申请日：2007-11-15

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

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

    IPC: C07D267/22 ,  C07D225/04 ,  A61K31/33

    CPC classification number: C07D273/00

    Abstract: There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, n and X 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）的含肟的大环酰基胍或立体异构体; 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，R 4，n和X，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。

    Cycloalkylamine derivatives as NK-1/SSRI antagonists
    16.
    发明授权
    Cycloalkylamine derivatives as NK-1/SSRI antagonists 有权
    环烷基胺衍生物作为NK-1 / SSRI拮抗剂

    公开(公告)号：US07494986B2

    公开(公告)日：2009-02-24

    申请号：US11183699

    申请日：2005-07-18

    Applicant: Yong-Jin Wu ,  Huan He

    Inventor： Yong-Jin Wu ,  Huan He

    IPC: A01N43/00 ,  A61K31/33 ,  C07D225/00 ,  C07D295/00

    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.

    Abstract translation: 本公开涉及化学化合物及其在人类治疗中的用途。 具体实施方案涉及式（I）化合物或其异构体，药学上可接受的盐或溶剂合物和药学上可接受的制剂，其包含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。

    Oxime-containing acyl guanidines as beta-secretase inhibitors
    17.
    发明授权
    Oxime-containing acyl guanidines as beta-secretase inhibitors 有权
    含肟的酰基鸟苷作为β-分泌酶抑制剂

    公开(公告)号：US07390925B2

    公开(公告)日：2008-06-24

    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: C07C233/05 ,  A61K31/65

    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。

    OXIME-CONTAINING MACROCYCLIC ACYL GUANIDINES AS BETA-SECRETASE INHIBITORS
    18.
    发明申请
    OXIME-CONTAINING MACROCYCLIC ACYL GUANIDINES AS BETA-SECRETASE INHIBITORS 有权
    含OXIME的大环酰胺类作为分子抑制剂

    公开(公告)号：US20080139523A1

    公开(公告)日：2008-06-12

    申请号：US11940597

    申请日：2007-11-15

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

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

    IPC: A61K31/395 ,  C07D405/14 ,  A61P25/28

    CPC classification number: C07D273/00

    Abstract: There is provided a series of oxime-containing macrocyclic acyl guanidines of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, R4, n and X 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）的含肟的大环酰基胍或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，R 4，n和X 如本文所定义的，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。

    Novel phenylcarboxyamides as beta-secretase inhibitors
    19.
    发明申请
    Novel phenylcarboxyamides as beta-secretase inhibitors 有权
    新型苯基羧酰胺作为β-分泌酶抑制剂

    公开(公告)号：US20070032470A1

    公开(公告)日：2007-02-08

    申请号：US11494145

    申请日：2006-07-27

    Applicant: Yong-Jin Wu ,  Yunhui Zhang

    Inventor： Yong-Jin Wu ,  Yunhui Zhang

    IPC: A61K31/554 ,  A61K31/55 ,  A61K31/54 ,  A61K31/445 ,  A61K31/425 ,  A61K31/4015

    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，其药物组合物和方法 的使用。 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。

    3-Heterocyclic benzylamide derivatives as potassium channel openers
    20.
    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。

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