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公开(公告)号：US20220213034A1
公开(公告)日：2022-07-07
申请号：US17306390
申请日：2021-05-03
IPC分类号： C07D207/14 , C07D401/08 , C07D403/04 , C07D471/10 , C07D243/08 , C07D409/08 , C07D413/14 , C07D471/04 , C07D487/04 , C07D413/12 , C07D271/06 , C07D413/04 , C07D487/10 , C07D209/96 , C07D295/205 , C07D213/57
摘要： This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
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公开(公告)号：US11339383B2
公开(公告)日：2022-05-24
申请号：US16835431
申请日：2020-03-31
摘要： The invention provides a mutant of a parent heterotrimeric G protein alpha (Gα) subunit, which mutant (i) lacks at least one helix of the helical domain of the parent Gα subunit; (ii) is capable of binding to a GPCR in the absence of a heterotrimeric G protein beta (Gβ) subunit and a heterotrimeric G protein gamma (Gγ) subunit; and (iii) has an amino acid sequence that contains one or more mutations compared to the amino acid sequence of the parent heterotrimeric Gα subunit, which mutations are selected from a deletion, a substitution and an insertion.
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公开(公告)号：US20220056009A1
公开(公告)日：2022-02-24
申请号：US17519486
申请日：2021-11-04
IPC分类号： C07D401/04 , C07D403/04 , C07D239/26
摘要： The disclosures herein relate to novel compounds of formula wherein R1, R2, R3 and R4 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of inflammation, neurological or psychiatric disorders associated with modulating mGlu5 receptor function.
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公开(公告)号：US20210387969A1
公开(公告)日：2021-12-16
申请号：US17311121
申请日：2019-12-09
IPC分类号： C07D403/04 , C07D451/14 , C07D451/04
摘要： This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where X1; X2; R1 and R4 are as defined herein.
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公开(公告)号：US11091456B2
公开(公告)日：2021-08-17
申请号：US16418354
申请日：2019-05-21
IPC分类号： C07D401/04 , C07D401/08 , A61K31/451 , A61K31/4523
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.
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公开(公告)号：US20210179578A1
公开(公告)日：2021-06-17
申请号：US16760807
申请日：2018-11-05
发明人： John Andrew Christopher , Sarah Joanne Bucknell , Miles Stuart Congreve , Benjamin Gerald Tehan , Rebecca Helen Nonoo , Giles Albert Brown , Nigel Alan Swain , Mark Mills
IPC分类号： C07D401/04 , C07D243/04
摘要： The disclosures herein relate to novel compounds of formula (1) and salts thereof, wherein X; Y; R1; R2; R3; R4; R5; R6; R7 and R8 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.
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公开(公告)号：US11034704B2
公开(公告)日：2021-06-15
申请号：US16584185
申请日：2019-09-26
发明人： Miles Stuart Congreve , Giles Albert Brown , Benjamin Gerald Tehan , Mark Pickworth , Julie Elaine Cansfield
IPC分类号： C07D519/00 , C07D471/10 , C07D498/10 , A61K31/438 , A61K31/439
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 where m, p, q, W, Z, Y, X1, X2, R1, R2, R3 and R4 are as defined herein.
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公开(公告)号：US11014880B2
公开(公告)日：2021-05-25
申请号：US16890581
申请日：2020-06-02
IPC分类号： A61K31/015 , C07C211/35 , C07D207/14 , C07D401/08 , C07D403/04 , C07D471/10 , C07D243/08 , C07D409/08 , C07D413/14 , C07D471/04 , C07D487/04 , C07D413/12 , C07D271/06 , C07D413/04 , C07D487/10 , C07D209/96 , C07D295/205 , C07D213/57
摘要： This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
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公开(公告)号：US10759751B2
公开(公告)日：2020-09-01
申请号：US16295364
申请日：2019-03-07
IPC分类号： A61K31/395 , C07D209/96 , C07D207/14 , C07D401/08 , C07D403/04 , C07D471/10 , C07D243/08 , C07D409/08 , C07D413/14 , C07D471/04 , C07D487/04 , C07D413/12 , C07D271/06 , C07D413/04 , C07D487/10 , C07D295/205 , C07D213/57
摘要： This invention relates to compounds that are agonists of the muscarinic M1 receptor or M1 and M4 receptors and which are useful in the treatment of muscarinic M1 or M1/M4 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula wherein Q4, Q5, R5, p, V, Q1, Q2, X1, X2 and W are defined herein.
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公开(公告)号：US10738029B2
公开(公告)日：2020-08-11
申请号：US15749957
申请日：2016-08-03
发明人： Giles Albert Brown , Julie Cansfield , Mark Pickworth , Benjamin Gerald Tehan , Barry John Teobald
IPC分类号： C07D401/14 , A61P25/28 , A61P25/18
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 1 or a salt thereof, wherein q, r, s, Q, R1, R2′, R2″, R3 and R4 are as defined herein.
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