-
公开(公告)号：US10166226B2
公开(公告)日：2019-01-01
申请号：US15882038
申请日：2018-01-29
发明人： John Andrew Christopher , Miles Stuart Congreve , Sarah Joanne Bucknell , Francesca Deflorian , Mark Pickworth , Jonathan Stephen Mason
IPC分类号： C07D401/14 , A61K31/4709
摘要： The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
-
公开(公告)号：US09975890B2
公开(公告)日：2018-05-22
申请号：US15595107
申请日：2017-05-15
发明人： Giles Albert Brown , Julie Elaine Cansfield , Miles Stuart Congreve , Mark Pickworth , Benjamin Gerald Tehan
IPC分类号： C07D401/04 , C07D451/04 , C07D401/08
CPC分类号： C07D451/04 , A61K31/439 , A61K31/4439 , C07B59/002 , C07B2200/05 , C07D401/04 , C07D401/08
摘要： This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.
-
公开(公告)号：US20180086814A1
公开(公告)日：2018-03-29
申请号：US15716302
申请日：2017-09-26
发明人： Richard Henderson , Christopher Gordon Tate , Francesca Magnani , Maria Josefa Serrano-Vega , Yoko Shibata , Antony Johannes Warne , Malcolm Peter Weir
IPC分类号： C07K14/72 , C12N15/10 , G01N33/566
CPC分类号： C07K14/723 , C12N15/1034 , G01N33/566 , G01N2333/726
摘要： The invention relates to mutant G-protein coupled receptors with increased conformational stability, and methods of use thereof. In some aspects, polynucleotides encoding the mutant G-protein coupled receptors are provided. In some aspects, host cells comprising the polynucleotides are provided. In some aspects, the invention relates to crystallized forms of the mutant G-protein coupled receptors, and methods of preparing the same.
-
公开(公告)号：US09907805B2
公开(公告)日：2018-03-06
申请号：US15436224
申请日：2017-02-17
IPC分类号： A61K31/55 , A61K31/4545
CPC分类号： A61K31/55 , A61K31/4545 , C07D211/06 , C07D401/04 , C07D401/14
摘要： This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
-
公开(公告)号：US09758506B2
公开(公告)日：2017-09-12
申请号：US15227325
申请日：2016-08-03
IPC分类号： C07D401/04 , C07D401/08 , A61K31/451 , A61K31/4523
CPC分类号： C07D401/04 , A61K31/451 , A61K31/4523 , C07D401/08
摘要： This invention relates to compounds that are agonists of the muscarinic M1 receptor and/or M4 receptor and which are useful in the treatment of muscarinic M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds include those according to formula (1a) or a salt thereof, wherein p, q, r, s, Q, R3 and R4 are as defined herein.
-
公开(公告)号：US09688660B2
公开(公告)日：2017-06-27
申请号：US15336893
申请日：2016-10-28
发明人： John Andrew Christopher , Miles Stuart Congreve , Sarah Joanne Bucknell , Francesca Deflorian , Mark Pickworth , Jonathan Stephen Mason
IPC分类号： C07D401/14 , A61K31/4709
CPC分类号： A61K31/4709 , C07D401/14
摘要： The disclosures herein relate to novel compounds of formula wherein Ar1 and R1 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.
-
公开(公告)号：US09573929B2
公开(公告)日：2017-02-21
申请号：US14941328
申请日：2015-11-13
IPC分类号： A61K31/55 , C07D401/04 , C07D211/06 , C07D401/14
CPC分类号： A61K31/55 , A61K31/4545 , C07D211/06 , C07D401/04 , C07D401/14
摘要： This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula I, where n is 1 or 2; p is 0, 1 or 2; q is 0, 1 or 2; and R1-R6 are as defined herein.
摘要翻译： 本发明涉及作为毒蕈碱M1受体的激动剂并可用于治疗毒蕈碱M1受体介导的疾病的化合物。 还提供含有化合物的药物组合物和化合物的治疗用途。 所提供的化合物为式I，其中n为1或2; p为0,1或2; q是0,1或2; 和R 1 -R 6如本文所定义。
-
公开(公告)号：US20160052991A1
公开(公告)日：2016-02-25
申请号：US14836820
申请日：2015-08-26
申请人： Richard Henderson , Christopher Gordon Tate , Francesca Magnani , Maria Josefa Serrano-Vega , Yoko Shibata , Antony Johannes Warne , Malcolm Peter Weir
发明人： Richard Henderson , Christopher Gordon Tate , Francesca Magnani , Maria Josefa Serrano-Vega , Yoko Shibata , Antony Johannes Warne , Malcolm Peter Weir
IPC分类号： C07K14/72
CPC分类号： C07K14/723 , C12N15/1034 , G01N33/566 , G01N2333/726
摘要： The invention relates to mutant G-protein coupled receptors with increased conformational stability, and methods of use thereof. In some aspects, polynucleotides encoding the mutant G-protein coupled receptors are provided. In some aspects, host cells comprising the polynucleotides are provided. In some aspects, the invention relates to crystallized forms of the mutant G-protein coupled receptors, and methods of preparing the same.
摘要翻译： 本发明涉及具有增加的构象稳定性的突变型G蛋白偶联受体及其使用方法。 在一些方面，提供了编码突变型G蛋白偶联受体的多核苷酸。 在一些方面，提供了包含多核苷酸的宿主细胞。 在一些方面，本发明涉及突变型G蛋白偶联受体的结晶形式及其制备方法。
-
公开(公告)号：US09266857B2
公开(公告)日：2016-02-23
申请号：US14428927
申请日：2013-09-18
发明人： Giles Albert Brown , Julie Elaine Cansfield , Miles Stuart Congreve , Mark Pickworth , Benjamin Gerald Tehan
IPC分类号： C07D211/06 , C07D295/00 , C07D401/04
CPC分类号： C07D451/04 , A61K31/439 , A61K31/4439 , C07B59/002 , C07B2200/05 , C07D401/04 , C07D401/08
摘要： This invention relates to compounds (Formula (1)) that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where R1-R5, X1, X2 and p are as defined herein.
摘要翻译： 本发明涉及作为毒蕈碱M1受体的激动剂并可用于治疗毒蕈碱M1受体介导的疾病的化合物（式（1））。 还提供含有化合物的药物组合物和化合物的治疗用途。 所提供的化合物具有下式：其中R1-R5，X1，X2和p如本文所定义。
-
公开(公告)号：US09081020B2
公开(公告)日：2015-07-14
申请号：US12866594
申请日：2009-02-05
IPC分类号： G01N33/74 , G01N33/68 , G01N33/53 , C07K14/705
CPC分类号： G01N33/74 , C07K14/70571 , G01N33/6872 , G01N2333/726
摘要： A method for selecting a membrane protein with increased stability, the method comprising: a) providing one or more mutants of a parent membrane protein in a membrane-containing composition, wherein the one or more mutants are exposed to an amount of a membrane destabilizing agent which is effective to destabilize the parent membrane protein in-situ, b) determining whether the or each mutant membrane protein has increased stability with respect to its structure and/or a biological activity compared to the stability of the parent membrane protein with respect to its structure and/or the same biological activity, and c) selecting the one or more mutants which have increased stability compared to the stability of the parent membrane protein.
摘要翻译： 一种用于选择具有增加的稳定性的膜蛋白的方法，所述方法包括：a）在含膜组合物中提供一种或多种亲本膜蛋白的突变体，其中所述一种或多种突变体暴露于一定量的膜去稳定剂 其有效地原位破坏亲本膜蛋白质，b）与相对于其亲本膜蛋白的稳定性相比，确定该突变膜蛋白或每个突变膜蛋白是否相对于其结构和/或生物活性具有增加的稳定性 结构和/或相同的生物活性，以及c）选择与亲本膜蛋白的稳定性相比具有增加的稳定性的一种或多种突变体。
-
-
-
-
-
-
-
-
-
搜索结果
122 条记录 (耗时 0.051 秒)
