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    METHODS, CELLS AND SYSTEMS FOR INCORPORATING NON-CANONICAL AMINO ACIDS INTO PROTEINS
    2.
    发明申请
    METHODS, CELLS AND SYSTEMS FOR INCORPORATING NON-CANONICAL AMINO ACIDS INTO PROTEINS 有权
    将非经典氨基酸掺入蛋白质的方法，细胞和系统

    公开(公告)号：US20120237971A1

    公开(公告)日：2012-09-20

    申请号：US13353106

    申请日：2012-01-18

    申请人： Ying Huang ,  Wenshe Liu ,  Ying Huang

    发明人： Ying Huang ,  Wenshe Liu ,  Ying Huang

    IPC分类号： C12P21/00 ,  C12N1/21 ,  C12N15/63 ,  C12N1/00

    CPC分类号： C12N15/67

    摘要： The present disclosure pertains to methods of incorporating one or more non-canonical amino acids into a protein during a translation of the protein in bacterial cells. The present disclosure also pertains to methods of incorporating one or more non-canonical amino acids into a protein during an in vitro translation of the protein. In additional embodiments, the present disclosure pertains to isolated bacterial cells and in vitro translation systems (e.g., cell-free extract systems) for incorporating one or more non-canonical amino acids into a protein during a translation of the protein.

    摘要翻译： 本公开涉及在蛋白质在细菌细胞中翻译期间将一种或多种非标准氨基酸掺入蛋白质的方法。 本公开还涉及在体外翻译蛋白质期间将一种或多种非标准氨基酸掺入蛋白质的方法。 在另外的实施方案中，本公开涉及在翻译蛋白质期间将一种或多种非标准氨基酸掺入到蛋白质中的分离的细菌细胞和体外翻译系统（例如，无细胞提取系统）。

    PREPARATION AND USE OF COMPOUNDS AS PROTEASE INHIBITORS
    7.
    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
    8.
    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。