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公开(公告)号：US11834407B2
公开(公告)日：2023-12-05
申请号：US17306390
申请日：2021-05-03
IPC分类号： A61K31/015 , C07C211/35 , C07D207/14 , C07D209/96 , C07D213/57 , C07D243/08 , C07D271/06 , C07D295/205 , C07D401/08 , C07D403/04 , C07D409/08 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
CPC分类号： C07D207/14 , C07D209/96 , C07D213/57 , C07D243/08 , C07D271/06 , C07D295/205 , C07D401/08 , C07D403/04 , C07D409/08 , C07D413/04 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10
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.-
公开(公告)号：US20230021177A1
公开(公告)日：2023-01-19
申请号：US17239137
申请日：2021-04-23
发明人： Miles Stuart Congreve , Stephen Philippe Andrews , Jonathan Stephen Mason , Christine Mary Richardson , Giles Albert Brown
IPC分类号： C07D401/04 , A61K31/506 , A61K31/5355 , A61K31/4427 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/10 , C07D413/04 , C07D417/12 , C07D487/04 , C07D253/07 , C07D413/14 , A61K31/53 , A61K31/5377 , A61K31/5386 , C07D417/04 , C07D417/14
摘要： According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more hetermatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.
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公开(公告)号：US20220251110A1
公开(公告)日：2022-08-11
申请号：US17617851
申请日：2020-06-12
发明人： Giles Albert Brown , Miles Stuart Congreve , Stephen Paul Watson , Julie Cansfield , Michael Alistair O'Brien , Francesca Deflorian , Gregory R. Ott , Nigel Alan Swain , Andrew David Cansfield
IPC分类号： C07D498/22
摘要： The disclosures herein relate to novel compounds of Formula (1a): and salts thereof, wherein W, Z, L, R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with CGRP receptors.
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公开(公告)号：US11352342B2
公开(公告)日：2022-06-07
申请号：US16999806
申请日：2020-08-21
发明人： Giles Albert Brown , Julie Elaine Cansfield , Miles Stuart Congreve , Benjamin Gerald Tehan , Barry John Teobald
IPC分类号： C07D403/04 , C07D401/14 , C07D401/08 , C07D403/14 , C07D417/14 , C07D491/107 , C07D498/08 , A61P25/28 , A61P25/02 , A61P25/18 , C07D413/14 , C07D451/02 , C07D451/14
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 (1) wherein X1; X2; R1 and R4 are as defined herein.
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公开(公告)号：US11324738B2
公开(公告)日：2022-05-10
申请号：US16728762
申请日：2019-12-27
发明人： Giles Albert Brown , Miles Stuart Congreve , Mark Pickworth , Mark David Rackham , Benjamin Gerald Tehan
IPC分类号： A61P25/14 , A61P25/28 , C07D401/14 , C07D413/14 , 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 n, p, Q, R1, R2, R3, R9 and R4 are as defined herein.
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公开(公告)号：US20210353637A1
公开(公告)日：2021-11-18
申请号：US17226523
申请日：2021-04-09
IPC分类号： A61K31/55 , C07D401/04 , C07D211/06 , C07D401/14 , A61K31/4545
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.
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公开(公告)号：US10988455B2
公开(公告)日：2021-04-27
申请号：US16161409
申请日：2018-10-16
发明人： Miles Stuart Congreve , Stephen Philippe Andrews , Jonathan Stephen Mason , Christine Mary Richardson , Giles Albert Brown
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D253/07 , A61K31/4427 , A61K31/53 , A61P35/00 , C07D417/04 , C07D417/14 , C07D405/04 , C07D413/04 , C07D413/14 , A61K31/506 , A61K31/5355 , C07D401/12 , C07D403/12 , C07D405/10 , C07D417/12 , C07D487/04 , A61K31/5377 , A61K31/5386
摘要： According to the invention there is provided a compound of formula A1 which may be useful in the treatment of a condition or disorder ameliorated by the inhibition of the A1-A2b or, particularly, the A2a receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy1 or HetA; Cy1 represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy1 group is optionally substituted by one or more R4a substituents; HetA represents a 5- to 14-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one, two or three rings and which HetA group is optionally substituted by one or more R4b substituents; B represents a Cy2 or HetB; Cy2 represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy2 group is optionally substituted by one or more R4c substituents; HetB represents a 3- to 10-membered heterocyclic group that may be aromatic, fully saturated or partially unsaturated, and which contains one or more heteroatoms selected from O, S and N, which heterocyclic group may comprise one or two rings and which HetB group is optionally substituted by one or more R4d substituents.
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公开(公告)号：US10981889B2
公开(公告)日：2021-04-20
申请号：US16780155
申请日：2020-02-03
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：US10689368B2
公开(公告)日：2020-06-23
申请号：US16459179
申请日：2019-07-01
发明人： Giles Albert Brown , Julie Elaine Cansfield , Miles Stuart Congreve , Michael Alistair O'Brien , Mark Pickworth , Mark David Rackham , Benjamin Gerald Tehan , Barry John Teobald
IPC分类号： A61K31/4545 , A61K31/454 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/107
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, R1, R2, R3 and R4 are as defined herein.
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公开(公告)号：US20190276437A1
公开(公告)日：2019-09-12
申请号：US16411821
申请日：2019-05-14
发明人： Giles Albert Brown , Julie Elaine Cansfield , Miles Stuart Congreve , Benjamin Gerald Tehan , Barry John Teobald
IPC分类号： C07D403/04 , C07D451/14 , C07D451/02 , A61P25/02 , A61P25/18 , C07D413/14 , C07D401/14 , C07D498/08 , C07D491/107 , C07D417/14 , C07D403/14 , C07D401/08 , A61P25/28
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 (1) wherein X1; X2; R1 and R4 are as defined herein.
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