Heptares Therapeutics Limited

Nxera Pharma UK Limited

Jonathan Stephen Mason

Miles Stuart Congreve

Giles Albert Brown

Santosh Shripad Kulkarni

Mark Pickworth

John Andrew Christopher

Sarah Joanne Bucknell

Francesca Deflorian

Nigel Alan Swain

Christine Mary Richardson

Stephen Philippe Andrews

Chris De Graaf

Alicia Perez Higueruelo

The disclosures herein relate to novel compounds of formula

CGRP receptor antagonists

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-Aor, particularly, the Areceptor. A process for the preparation of the compound, pharmaceutical compositions comprising the compound, and methods of treatment comprising administration of an effective amount of the compound are also disclosed.

1,2,4-triazine-4-amine derivatives

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-Aor, particularly, the Areceptor wherein the compound of formula A1 has the structure, wherein, A represents Cyor Het; Cyrepresents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents 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 R4substituents; B represents a Cyor Het; Cyrepresents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents 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 Hetgroup is optionally substituted by one or more Rsubstituents. 

The disclosures herein relate to novel compounds of formula wherein R, R, Rand Rare as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

The disclosures herein relate to novel compounds of formula wherein R, Rand Rare as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

The disclosures herein relate to novel compounds of formula wherein Arand Rare as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

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-Aor, particularly, the Areceptor wherein the compound of formula A1 has the structure, wherein, A represents Cyor Het; Cyrepresents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocylic ring system comprising one, two or three rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents 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 Cyor Het; Cyrepresents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents 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 Hetgroup is optionally substituted by one or more Rsubstituents. 

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-Aor, particularly, the Areceptor wherein the compound of formula A1 has the structure, wherein, A represents Cyor Het; Cyrepresents a 5- to 14-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one, two or three rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents 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 Cyor Het; Cyrepresents a 3- to 10-membered aromatic, fully saturated or partially unsaturated carbocyclic ring system comprising one or two rings, which Cygroup is optionally substituted by one or more Rsubstituents; Hetrepresents 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 Hetgroup is optionally substituted by one or more Rsubstituents. 

Growing community of inventors

Walmer, United Kingdom

Jonathan Stephen Mason