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111 条记录 (耗时 0.051 秒)

    Aspartyl protease inhibitors
    62.
    发明申请
    Aspartyl protease inhibitors 有权
    天冬氨酰蛋白酶抑制剂

    公开(公告)号：US20060287294A1

    公开(公告)日：2006-12-21

    申请号：US11451195

    申请日：2006-06-12

    申请人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Tao Guo ,  Thuy Le

    发明人： Zhaoning Zhu ,  Brian McKittrick ,  Andrew Stamford ,  Tao Guo ,  Thuy Le

    IPC分类号： A61K31/554 ,  A61K31/553 ,  A61K31/551 ,  C07D285/36 ,  C07D243/10 ,  C07D223/14

    CPC分类号： C07D471/10 ,  C07D239/70 ,  C07D487/10 ,  C07D491/10 ,  C07D495/10

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein U, W, A, R, R1, R2, R6a and R7, 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或溶剂合物，其中U，W，A，R，R 1，R 2， R 6a和R 7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m 1激动剂或m 2 H 2拮抗剂组合治疗认知或神经变性疾病的方法。

    Gamma secretase modulators
    66.
    发明授权
    Gamma secretase modulators 有权

    公开(公告)号：US09598437B2

    公开(公告)日：2017-03-21

    申请号：US15101224

    申请日：2014-12-02

    申请人： Mihir B. Mandal ,  Zhaoning Zhu

    发明人： Mihir B. Mandal ,  Zhaoning Zhu

    IPC分类号： C07D498/04

    CPC分类号： C07D498/04

    摘要： Disclosed herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.

    Gamma secretase modulators
    67.
    发明授权
    Gamma secretase modulators 有权
    伽玛分泌酶调节剂

    公开(公告)号：US09096582B2

    公开(公告)日：2015-08-04

    申请号：US14354992

    申请日：2012-10-26

    申请人： William Greenlee ,  Dmitri Pissarnitski ,  Zhiqiang Zhao ,  Zhaoning Zhu

    发明人： William Greenlee ,  Dmitri Pissarnitski ,  Zhiqiang Zhao ,  Zhaoning Zhu

    IPC分类号： C07D413/10

    CPC分类号： C07D413/10 ,  C07D413/14

    摘要： Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and use of the compounds in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.

    摘要翻译： 本文公开了式（I）的化合物及其药学上可接受的盐，其中每个取代基被给出如说明书和权利要求书中所阐述的定义。 还公开了含有式（I）化合物的药物组合物和该化合物在治疗神经变性疾病或病症如阿尔茨海默病中的用途。

    PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS
    68.
    发明申请
    PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS 审中-公开
    化合物作为蛋白酶抑制剂的制备和使用

    公开(公告)号：US20140206715A1

    公开(公告)日：2014-07-24

    申请号：US14226338

    申请日：2014-03-26

    申请人： Andrew W. Stamford ,  Guoqing Li ,  William Greenlee ,  Zhaoning Zhu ,  Brian McKittrick ,  Robert Mazzola ,  Ying Huang ,  Tao Guo ,  Thuy X.E. Le ,  Gang Qian ,  Yuefei Shao

    发明人： Andrew W. Stamford ,  Guoqing Li ,  William Greenlee ,  Zhaoning Zhu ,  Brian McKittrick ,  Robert Mazzola ,  Ying Huang ,  Tao Guo ,  Thuy X.E. Le ,  Gang Qian ,  Yuefei Shao

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04 ,  C07D209/44 ,  C07D487/04

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.

    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或溶剂合物，其中Q是键或-N（R 5） - ; T是键，-O - ， - C（O） - ; S，-N（R 5） - 或-C（R 6'R 7'）; U是键或-C（R6）（R7）-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个，优选0至2个杂原子的3至9元环烷基，环烯基，杂环基，杂环烯基，芳基和杂芳基环，其独立地选自O，S， N和-N（R） - ，其中当环A是环烷基，环烯基，杂环基或杂环烯基时，环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。 并且R，R 1，R 2，R 3，R 4，R 5，R 6，R 6，R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和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。

    Substituted isoindolines as aspartyl protease inhibitors
    69.
    发明授权
    Substituted isoindolines as aspartyl protease inhibitors 有权
    取代的异吲哚啉作为天冬氨酰蛋白酶抑制剂

    公开(公告)号：US08722708B2

    公开(公告)日：2014-05-13

    申请号：US11451065

    申请日：2006-06-12

    申请人： Andrew Stamford ,  Guoqing Li ,  William Greenlee ,  Zhaoning Zhu ,  Brian McKittrick ,  Robert Mazzola ,  Ying Huang ,  Tao Guo ,  Thuy X. H. Le ,  Gang Qian ,  Yuefei Shao

    发明人： Andrew Stamford ,  Guoqing Li ,  William Greenlee ,  Zhaoning Zhu ,  Brian McKittrick ,  Robert Mazzola ,  Ying Huang ,  Tao Guo ,  Thuy X. H. Le ,  Gang Qian ,  Yuefei Shao

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61K31/4035 ,  A61K31/4406 ,  C07D487/14 ,  A61K31/437 ,  A61P25/28 ,  A61P9/00 ,  A61P31/14

    CPC分类号： C07D471/04 ,  C07D209/44 ,  C07D487/04

    摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein Q is a bond or —N(R5)—; T is a bond, —O—, —C(O)—; S, —N(R5)—, or —C(R6′R7′); U is a bond or —C(R6)(R7)— Y is C or N; Z is C or N; ring A, including variables Y and Z, is a three to nine membered cycloalkyl, cycloalkenyl, heterocyclyl, heterocyclenyl, aryl, and heteroaryl ring having 0 to 4, preferably 0 to 2, heteroatoms independently selected from the group consisting of O, S, N and —N(R)—, wherein ring A is unsubstituted or substituted with 1 to 5 independently selected R1 moieties and/or oxo when ring A is cycloalkyl, cycloalkenyl, heterocyclyl or heterocyclenyl; and R, R1, R2, R3, R4, R5, R6, R6, R7 and R7′ are as defined in the specification; pharmaceutical compositions comprising the compounds of formula I and the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases.

    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或溶剂合物，其中Q是键或-N（R 5） - ; T是键，-O - ， - C（O） - ; S，-N（R 5） - 或-C（R 6'R 7'）; U是键或-C（R6）（R7）-Y是C或N; Z是C或N; 环A包括变量Y和Z是具有0至4个，优选0至2个杂原子的3至9元环烷基，环烯基，杂环基，杂环烯基，芳基和杂芳基环，其独立地选自O，S， N和-N（R） - ，其中当环A是环烷基，环烯基，杂环基或杂环烯基时，环A是未取代的或被1至5个独立选择的R 1部分和/或氧代取代。 并且R，R 1，R 2，R 3，R 4，R 5，R 6，R 6，R 7和R 7'如本说明书中所定义; 包含式I化合物的药物组合物和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。