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80 条记录 (耗时 0.043 秒)

    Neuropeptide Y Y5 receptor antagonists
    53.
    发明授权
    Neuropeptide Y Y5 receptor antagonists 失效
    神经肽Y Y5受体拮抗剂

    公开(公告)号：US07157472B2

    公开(公告)日：2007-01-02

    申请号：US10609638

    申请日：2003-06-30

    申请人： Andrew W. Stamford ,  Yusheng Wu

    发明人： Andrew W. Stamford ,  Yusheng Wu

    IPC分类号： A61K31/454 ,  C07D401/12

    CPC分类号： C07D401/12

    摘要： The present invention discloses compounds which, are receptor antagonists for NPY Y5 as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such NPY Y5 receptor antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

    摘要翻译： 本发明公开了作为NPY Y5的受体拮抗剂的化合物以及这些化合物的制备方法。 在另一个实施方案中，本发明公开了包含这种NPY Y5受体拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

    Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors
    56.
    发明授权
    Derivatives of phosphinic acid useful as endothelin converting enzyme inhibitors 失效
    次膦酸的衍生物可用作内皮素转化酶抑制剂

    公开(公告)号：US5476847A

    公开(公告)日：1995-12-19

    申请号：US267630

    申请日：1994-06-29

    申请人： Brian A. McKittrick ,  Michael F. Czarniecki ,  Samuel Chackalamannil ,  Shin Chung ,  Shawn DeFrees ,  Andrew W. Stamford

    发明人： Brian A. McKittrick ,  Michael F. Czarniecki ,  Samuel Chackalamannil ,  Shin Chung ,  Shawn DeFrees ,  Andrew W. Stamford

    IPC分类号： A61K31/66 ,  A61P1/00 ,  A61P3/08 ,  A61P9/00 ,  A61P9/06 ,  A61P9/08 ,  A61P9/10 ,  A61P9/12 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P35/00 ,  A61P43/00 ,  C07F9/30 ,  C07F9/572 ,  C07F9/6558 ,  A61K31/405 ,  C07D209/14 ,  C07F9/36

    CPC分类号： C07F9/65583 ,  C07F9/303 ,  C07F9/5728

    摘要： Phosphinic acid derivatives of the structural formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R.sub.1 and R.sub.2 form a cycloalkyl ring of 3-8 members and R.sub.3 and R.sub.4 are as defined; or R.sub.3 and R.sub.4 form a cycloalkyl ring of 3-7 members and R.sub.1 and R.sub.2 are as defined; or R.sub.1 and R.sub.2 together, and R.sub.3 and R.sub.4 together, each form a cycloalkyl ring;R.sub.5 is --OR.sub.9 or --NHR.sub.9, wherein R.sub.9 is hydrogen or alkyl;n is 0 or 1;A.sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A.sub.1 and R.sub.5 together form a radical of an .alpha.-aminoacyl derivative; andR.sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or --A.sub.2 --R.sub.7, wherein A.sub.2 is a divalent .alpha.-aminoacyl radical, and R.sub.7 is a substituent on the .alpha.-amino atom selected from H, R.sub.8 OCO--, R.sub.8 SO.sub.2 -- and R.sub.8 NHCO--, wherein R.sub.8 is aryl, arylmethyl or (C.sub.1 -C.sub.8)alkyl;are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R.sup.3 and R.sup.4 form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.

    摘要翻译： 结构式为“IMAGE”的次膦酸衍生物或其药学上可接受的盐，其中R为H，烷基或烷酰氧基亚甲基; R 1，R 2，R 3和R 4是H，烷基，烯基，链烯基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，羟基烷基，羧基烷基，硫代烷基，烷氧基硫代烷基，氨基烷基，烷基氨基烷基，环烷基取代的烷基或杂环烷基。 或R 1和R 2形成3-8成员的环烷基环，并且R 3和R 4如所定义; 或R 3和R 4形成3-7成员的环烷基环，并且R 1和R 2如所定义; 或R 1和R 2一起，并且R 3和R 4一起形成环烷基环; R5是-OR9或-NHR9，其中R9是氢或烷基; n为0或1; A1是对氨基苯甲酰基或对氨基苯磺酰基，或者A1和R5一起形成α-氨基酰基衍生物的基团; R6为苯基甲氧基羰基，芳基羰基，杂芳基羰基或-A2-R7，其中A2为二价α-氨基酰基，R7为选自H，R8OCO-，R8SO2-和R8NHCO-的α-氨基原子上的取代基，其中R8 是芳基，芳甲基或（C1-C8）烷基; 被公开用作内皮素转化酶抑制剂; 还公开了一种其中R3和R4形成环烷基环的新化合物，以及包含所述新化合物的药物组合物。

    Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
    59.
    发明授权
    Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use 有权
    二氢化二氮杂二恶烷化合物作为抑制剂，组合物及其用途

    公开(公告)号：US08563543B2

    公开(公告)日：2013-10-22

    申请号：US13392955

    申请日：2010-10-06

    申请人： Jack D. Scott ,  Andrew W. Stamford ,  Eric J. Gilbert ,  Jared N. Cumming ,  Ulrich Iserloh ,  Lingyan Wang ,  Wei Li

    发明人： Jack D. Scott ,  Andrew W. Stamford ,  Eric J. Gilbert ,  Jared N. Cumming ,  Ulrich Iserloh ,  Lingyan Wang ,  Wei Li

    IPC分类号： A61K31/54

    CPC分类号： C07D417/04 ,  C07D285/18 ,  C07D417/10

    摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.

    摘要翻译： 在其许多实施方案中，本发明提供某些亚氨基二嗪二氧化物化合物，包括式（a）化合物，并且包括其互变异构体，溶剂化物，前药，酯和氘代，以及所述化合物，互变异构体，溶剂合物，前药，酯， 氘代，其中R1，R2，R3，R4，R5，R9，环A，环B，环C，m，n，p，q，-L1-，-L2，L3-和L4- 独立选择和如本文所定义。 本发明的化合物令人惊奇地和有利地提高了溶液的稳定性。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。

    Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use
    60.
    发明授权
    Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions, and their use 有权
    五氟硫基亚氨基杂环化合物作为BACE-1抑制剂，组合物及其应用

    公开(公告)号：US08557826B2

    公开(公告)日：2013-10-15

    申请号：US13390856

    申请日：2010-10-06

    申请人： Andrew W. Stamford ,  Jared N Cumming

    发明人： Andrew W. Stamford ,  Jared N Cumming

    IPC分类号： A01N43/54 ,  C07D239/42 ,  C07D401/04

    CPC分类号： C07D239/22 ,  C07D409/04

    摘要： In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (I): and tautomers thereof, and solvates, prodrugs, esters, and deuterates of said compounds and said tautomers, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R1, R2, R3, R4, R5, R9, R11, ring A, ring B, m, n, p, q, r, -L1-, L2-, and L3- is selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.

    摘要翻译： 在其许多实施方案中，本发明提供某些五氟硫亚氨基杂环化合物，包括式（I）化合物及其互变异构体，以及所述化合物和所述互变异构体的溶剂合物，前药，酯和氘代，以及所述化合物的药学上可接受的盐， 互变异构体，溶剂化物，前药，酯和氘代，其中R1，R2，R3，R4，R5，R9，R11，环A，环B，m，n，p，q，r，-L1-， 和L3-是独立选择的，如本文所定义。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。