Welwyn Garden City, United Kingdom

Heptares Therapeutics

www.heptares.com
Welwyn Garden City, United Kingdom
SEARCH FILTERS
Time filter
Source Type

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: 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.


Patent
Heptares Therapeutics | Date: 2017-02-17

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.


The present invention provides muscarinic M4 receptor agonists of formula (I) and pharmaceutically acceptable salts thereof, wherein m, n, p, q, R, R^(2 )and R^(3 )are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases such as schizophrenia, Alzheimers disease and various cognitive disorders as well as in the treatment or alleviation of pain.


Patent
Heptares Therapeutics | Date: 2017-01-25

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.


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.


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. .

Loading Heptares Therapeutics collaborators
Loading Heptares Therapeutics collaborators