Welwyn Garden City, United Kingdom
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Patent
Heptares Therapeutics | Date: 2016-08-03

This invention relates to compounds that are agonists of the muscarinic M_(1 )receptor and/or M_(4 )receptor and which are useful in the treatment of muscarinic M_(1)/M_(4 )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, R^(3 )and R^(4 )are as defined herein.


Grant
Agency: GTR | Branch: Innovate UK | Program: | Phase: Collaborative Research & Development | Award Amount: 1.50M | Year: 2015

Congenital Hyperinsulinism is a rare neonatal disease presenting severe hypoglycaemia associated with poor clinical outcomes and long-term neurodisability. The support of the Technology Strategy Board will enable Heptares, in collaboration with the University of Manchester and Great Ormond Street Hospital, to carry out the pre-clinical development of a novel safe, effective and orally available treatment for Congenital Hyperinsulinsm. A succesful outcome will provide a clinically ready molecule with anticipated additional benefits in other areas associated with intractable hypoglycaemia; including neonatal hypoglycaemia, hypoglycaemia occurring as a consequence of gastric bypass surgery and insulinoma-associated hypoglycaemia. .


Patent
Heptares Therapeutics | Date: 2016-01-13

The disclosures herein relate to novel compounds of formula wherein W, X and Y_(1), Y_(2), Y_(3 )and Y_(4 )are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.


Patent
Heptares Therapeutics | Date: 2016-01-06

A method of producing a conformational specific binding partner of a GPCR, the method comprising: a) providing a mutant GPCR of a parent GPCR, wherein the mutant GPCR has increased stability in a particular conformation relative to the parent GPCR; b) providing a test compound; c) determining whether the test compound binds to the mutant GPCR when residing in a particular conformation; and d) isolating a test compound that binds to the mutant GPCR when residing in the particular formation. Methods of producing GPCRs with increased stability relative to a parent GPCR are also disclosed.


Patent
Heptares Therapeutics | Date: 2015-12-21

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 A_(1)-A_(2b )or, particularly, the A_(2a )receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy^(1 )or Het^(A); Cy^(1 )represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy^(1 )group is optionally substituted by one or more R^(4a )substituents; Het^(A )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 Cy^(2 )or Het^(B); Cy^(2 )represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy^(2 )group is optionally substituted by one or more R^(4c )substituents; Het^(B )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 Het^(a )group is optionally substituted by one or more R^(4d )substituents


Patent
Heptares Therapeutics | Date: 2014-07-02

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 A_(1)-A_(2b )or, particularly, the A_(2a )receptor wherein the compound of formula A1 has the structure, wherein, A represents Cy^(1 )or Het^(A); Cy^(1 )represents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cy^(1 )group is optionally substituted by one or more R^(4a )substituents; Het^(A )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 Cy^(2 )or Het^(B); Cy^(2 )represents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cy^(2 )group is optionally substituted by one or more R^(4c )substituents; Het^(B )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 Het^(B )group is optionally substituted by one or more R^(4d )substituents.


Patent
Heptares Therapeutics | Date: 2015-08-26

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.


Patent
Heptares Therapeutics | Date: 2015-11-13

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 R_(1)-R_(6 )are as defined herein.


Patent
Heptares Therapeutics | Date: 2016-01-15

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 R_(1)-R_(5), X_(1), X_(2 )and p are as defined herein.


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^(1), R^(2), R^(3 )and R^(4 )are as defined herein.

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