公开(公告)号：US20240254093A1

公开(公告)日：2024-08-01

申请号：US18556178

申请日：2022-04-22

Applicant: Heptares Therapeutics Limited

Inventor： Miles Stuart CONGREVE ,  Nigel Alan SWAIN ,  Giles Albert BROWN ,  Benjamin WHITEHURST ,  Neil John FLANGAN

IPC: C07D257/04 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10

CPC classification number: C07D257/04 ,  C07D401/04 ,  C07D401/10 ,  C07D403/10

Abstract: The disclosures herein relate to novel compounds of formula (1):




and salts and any tautomers thereof, wherein X, R1 and R2 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR35 receptors.

公开(公告)号：US11834407B2

公开(公告)日：2023-12-05

申请号：US17306390

申请日：2021-05-03

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Miles Stuart Congreve ,  Mark Pickworth ,  Benjamin Gerald Tehan

IPC: 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 classification number: 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

Abstract: 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：US20230382949A1

公开(公告)日：2023-11-30

申请号：US18031416

申请日：2021-10-12

Applicant: HEPTARES THERAPEUTICS LIMITED

Inventor： Giles Albert BROWN ,  Miles Stuart CONGREVE ,  Conor SCULLY ,  Rebecca PAUL

IPC: C07K7/08 ,  A61K47/60

CPC classification number: C07K7/08 ,  A61K47/60 ,  A61K38/00

Abstract: The disclosures herein relate to novel compounds of formula (1): and salts thereof, wherein Q, X, AA1, AA2, AA3, AA4, AA5, AA6, AA7, AA8, AA9, AA10, AA11, AA12, AA13, R1 R2 and n are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with Apelin receptors.

公开(公告)号：US20230021177A1

公开(公告)日：2023-01-19

申请号：US17239137

申请日：2021-04-23

Applicant: Heptares Therapeutics Limited

Inventor： Miles Stuart Congreve ,  Stephen Philippe Andrews ,  Jonathan Stephen Mason ,  Christine Mary Richardson ,  Giles Albert Brown

IPC: 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

Abstract: 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.

公开(公告)号：US20220251110A1

公开(公告)日：2022-08-11

申请号：US17617851

申请日：2020-06-12

Applicant: Heptares Therapeutics Limited

Inventor： 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: C07D498/22

Abstract: 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.

公开(公告)号：US11352342B2

公开(公告)日：2022-06-07

申请号：US16999806

申请日：2020-08-21

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Julie Elaine Cansfield ,  Miles Stuart Congreve ,  Benjamin Gerald Tehan ,  Barry John Teobald

IPC: 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

Abstract: 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.

公开(公告)号：US11324738B2

公开(公告)日：2022-05-10

申请号：US16728762

申请日：2019-12-27

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Miles Stuart Congreve ,  Mark Pickworth ,  Mark David Rackham ,  Benjamin Gerald Tehan

IPC: A61P25/14 ,  A61P25/28 ,  C07D401/14 ,  C07D413/14 ,  A61K31/4523

Abstract: 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.

公开(公告)号：US11319312B2

公开(公告)日：2022-05-03

申请号：US17069070

申请日：2020-10-13

Applicant: Heptares Therapeutics Limited

Inventor： Giles Albert Brown ,  Barry John Teobald ,  Benjamin Gerald Tehan

IPC: C07D487/10 ,  C07D498/08 ,  C07D498/10 ,  C07D451/02 ,  C07D451/14 ,  C07D453/06 ,  C07D471/10 ,  C07D413/14 ,  C07D491/08

Abstract: 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; X3; X4; R1 R2 and R4 are as defined herein.

公开(公告)号：US20210353637A1

公开(公告)日：2021-11-18

申请号：US17226523

申请日：2021-04-09

Applicant: Heptares Therapeutics Limited

Inventor： Miles Stuart Congreve ,  Giles Albert Brown ,  Julie Elaine Cansfield ,  Benjamin Gerald Tehan

IPC: A61K31/55 ,  C07D401/04 ,  C07D211/06 ,  C07D401/14 ,  A61K31/4545

Abstract: 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：US10988455B2

公开(公告)日：2021-04-27

申请号：US16161409

申请日：2018-10-16

Applicant: Heptares Therapeutics Limited

Inventor： Miles Stuart Congreve ,  Stephen Philippe Andrews ,  Jonathan Stephen Mason ,  Christine Mary Richardson ,  Giles Albert Brown

IPC: 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

Abstract: 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.