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    Macrocyclic heterocyclic aspartyl protease inhibitors
    41.
    发明申请
    Macrocyclic heterocyclic aspartyl protease inhibitors 有权
    大环杂环天门冬酰胺蛋白酶抑制剂

    公开(公告)号：US20060281729A1

    公开(公告)日：2006-12-14

    申请号：US11451064

    申请日：2006-06-12

    申请人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes Voigt

    发明人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes Voigt

    IPC分类号： A61K31/4188 ,  C07D487/02

    CPC分类号： C07D487/08

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂化物或酯，其中U，W，X，L，Y，M，Z，c，d，e，f，g， s，t，R 1，R 2，R 7，R 8，R 9， R 10，R 11，R 12，R 13，R 14， R 15，R 16，R 17和R 18如本说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m 1激动剂或m 2 N拮抗剂组合治疗认知或神经变性疾病的方法。

    Macrocyclic Heterocyclic Aspartyl Protease Inhibitors
    42.
    发明申请
    Macrocyclic Heterocyclic Aspartyl Protease Inhibitors 有权
    大环杂环天门冬酰胺蛋白酶抑制剂

    公开(公告)号：US20100063121A1

    公开(公告)日：2010-03-11

    申请号：US12620291

    申请日：2009-11-17

    申请人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes H. Voigt

    发明人： Ulrich Iserloh ,  Zhaoning Zhu ,  Andrew Stamford ,  Johannes H. Voigt

    IPC分类号： A61K31/4188 ,  C07D487/08

    CPC分类号： C07D487/08

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt, solvate or ester thereof, wherein U, W, X, L, Y, M, Z, c, d, e, f, g, h, s, t, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17 and R18 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases. Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic m1 agonist or m2 antagonist.

    摘要翻译： 公开了式I化合物或其立体异构体，互变异构体或其药学上可接受的盐，溶剂化物或酯，其中U，W，X，L，Y，M，Z，c，d，e，f，g， s，t，R1，R2，R7，R8，R9，R10，R11，R12，R13，R14，R15，R16，R17和R18如说明书中所定义; 以及包含式I化合物的药物组合物。还公开了抑制天冬氨酰蛋白酶的方法，特别是治疗心血管疾病，认知和神经变性疾病的方法。 还公开了使用式I化合物与胆碱酯酶抑制剂或毒蕈碱m1激动剂或m2拮抗剂组合治疗认知或神经变性疾病的方法。

    Cyclic amine bace-1 inhibitors having a heterocyclic substituent
    43.
    发明授权
    Cyclic amine bace-1 inhibitors having a heterocyclic substituent 有权
    具有杂环取代基的环胺类bace-1抑制剂

    公开(公告)号：US07910590B2

    公开(公告)日：2011-03-22

    申请号：US12490884

    申请日：2009-06-24

    申请人： Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Jianping Pan

    发明人： Ying Huang ,  Guoqing Li ,  Ulrich Iserloh ,  Andrew Stamford ,  Corey Strickland ,  Johannes H. Voigt ,  Jianping Pan

    IPC分类号： A61K31/496 ,  A61K31/506

    CPC分类号： C04B35/632 ,  C07D207/277 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

    摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is X is —O—, —C(R 14)2— or —N(R)—; Z is —C(R14)2— or —N(R)—; t is 0, 1, 2 or 3; each R and R2 is independently H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, alkenyl or alkynyl; each R14 is H, alkyl, alkenyl, alkynyl, halo, —CN, haloalkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, heterocycloalkyl, arylalkyl, heteroarylalkyl, heterocycloalkylalkyl, —OR35, —N(R24)(R25) or —SR35; R41 is alkyl, cycloalkyl, —SO2(alkyl), —C(O)-alkyl, —C(O)-cycloalkyl or -alkyl-NH—C(O)CH3; and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I and methods of treating cognitive or neurodegenerative diseases with compounds of formula I.Also disclosed are pharmaceutical compositions and methods of treatment comprising compounds of formula I in combination with other agents useful in treating cognitive or neurodegenerative diseases.

    摘要翻译： 公开了下式的新化合物或其药学上可接受的盐或溶剂合物，其中R 1是X是-O - ， - C（R 14）2 - 或-N（R） - ; Z是-C（R 14）2 - 或-N（R） - ; t为0,1,2或3; 每个R和R 2独立地为H，烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，烯基或炔基; 每个R 14是H，烷基，烯基，炔基，卤素，-CN，卤代烷基，环烷基，环烷基烷基，芳基，杂芳基，杂环烷基，芳基烷基，杂芳基烷基，杂环烷基烷基，-OR 35，-N（R 24）（R 25）或-SR 35; R41是烷基，环烷基，-SO2（烷基），-C（O） - 烷基，-C（O） - 环烷基或 - 烷基-NH-C（O）CH3; 其余变量如本说明书中所定义。 还公开了包含式I化合物的药物组合物和用式I化合物治疗认知障碍或神经变性疾病的方法。还公开了药物组合物和治疗方法，其包含式I化合物与用于治疗认知或神经变性的其它药剂 疾病

    PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS AND THEIR USE
    44.
    发明申请
    PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS AND THEIR USE 有权
    PENTAFLUOROSULFUR IMINO杂环化合物作为BACE-1抑制剂，组合物及其用途

    公开(公告)号：US20120195881A1

    公开(公告)日：2012-08-02

    申请号：US13391441

    申请日：2010-10-06

    申请人： Ulrich Iserloh ,  Andrew W. Stamford ,  Jared N. Cumming

    发明人： Ulrich Iserloh ,  Andrew W. Stamford ,  Jared N. Cumming

    IPC分类号： A61K39/395 ,  A61K38/00 ,  A61K31/513 ,  C07D405/04 ,  A61P29/00 ,  A61P25/28 ,  A61P25/16 ,  A61P25/00 ,  A61P3/10 ,  A61P31/04 ,  A61K39/00 ,  C07D239/22

    CPC分类号： C07D239/22 ,  C07D405/04

    摘要： In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula (a) have the general structure: (a) wherein each variable 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（a）化合物及其药学上可接受的盐。 式（a）的化合物具有通式结构：（a）其中每个变量是独立选择的，如本文所定义。 还公开了包含一种或多种这样的化合物（单独并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（A＆bgr））蛋白相关的病理学的方法。

    Pentafluorosulfur imino heterocyclic compounds as BACE-1 inhibitors, compositions and their use
    48.
    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，组合物及其用途

    公开(公告)号：US08569310B2

    公开(公告)日：2013-10-29

    申请号：US13391441

    申请日：2010-10-06

    申请人： Ulrich Iserloh ,  Andrew W. Stamford ,  Jared N Cumming

    发明人： Ulrich Iserloh ,  Andrew W. Stamford ,  Jared N Cumming

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

    CPC分类号： C07D239/22 ,  C07D405/04

    摘要： In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula (a) have the general structure: (a) wherein each variable 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（a）化合物及其药学上可接受的盐。 式（a）的化合物具有通式结构：（a）其中每个变量是独立选择的，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。

    Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
    50.
    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。