Welwyn Garden City, United Kingdom
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.


Patent
Heptares Therapeutics | Date: 2015-03-19

This invention relates to compounds that are agonists of the muscarinic M_(1 )receptor and which are useful in the treatment of muscarinic M_(1 )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, X^(1), X^(2), R^(1), R^(2 )R^(3 )and R^(4 )are as defined herein.


Patent
Heptares Therapeutics | Date: 2016-10-28

The disclosures herein relate to novel compounds of formula wherein Ar^(1 )and R_(1 )are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.


Patent
Heptares Therapeutics | Date: 2017-01-18

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: 2016-10-28

The disclosures herein relate to novel compounds of formula wherein R^(1), R^(2 )and R^(3 )are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.


Patent
Heptares Therapeutics | Date: 2016-10-28

The disclosures herein relate to novel compounds of formula wherein R^(1), R^(2), R^(3 )and R^(4 )are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.


Patent
Heptares Therapeutics | Date: 2016-06-29

A method for producing a mutant G-protein coupled receptor (GPCR) with increased stability relative to a parent GPCR, the method comprising making one or more mutations in the amino acid sequence that defines a Class 1 parent GPCR, wherein (i) the one or more mutations are located within a window of i plus or minus 5 residues, where i is the position of amino acid residue 3.55 in the parent GPCR, and/or (ii) the one or more mutations are located within a window of i minus 2 to i residues, where i is the position of amino acid residue 5.63 in the parent GPCR, and/or (iii) the one or more mutations are located within a window of i minus 4 to i plus 1 residues, where i is the position of amino acid residue 7.42 in the parent GPCR, to provide one or more mutants of the parent GPCR with increased stability.


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: 2016-01-06

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: 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.

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