The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Mar. 01, 2016
Filed:
Oct. 26, 2012
Inhibitaxin Limited, Sandwich Kent, GB;
Karl Richard Gibson, Kent, GB;
Dafydd Rhys Owen, Cambridge, MA (US);
Inhibitaxin Limited, Sandwich Kent, London, unknown;
Abstract
The invention provides compounds of formula I, (I) wherein: R represents a cyclic group selected from phenyl, heteroaryl, heterocyclyl and C 3-6 cycloalkyl; 10 wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C -6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C -6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl 1a and heterocyclyl 1a; and wherein each cyclic group is optionally fused to a benzene ring or a 5- or 16-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl and heterocyclyl 1a may additionally be substituted with ═O; 20 X represents a bond or C -6 alkylene (which may be straight or branched); R 2 represents H or C -6 alkyl; R 3 represents H or C -6 alkyl; Y represents a bond or C -6 alkylene (which may be straight or branched, and optionally substituted with OH or CF 3); 2 R 4 represents a cyclic group selected from phenyl, heteroaryl 4, heterocyclyl 4 and C 3-6 cycloalkyl; wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C -6 alkyl optionally substituted with 1-3 halogen atoms, TET01063WO 4 phenyl, C -6 alkyl substituted with phenyl, C -6 alkoxy optionally substituted with -3 halogen atoms, cyano, heteroaryl 4a and heterocyclyl 4a; and wherein each cyclic group is optionally fused to benzene ring or a 5- or 6-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl 4 and heterocyclyl 4a may additionally be substituted with ═O; heteroaryl, heteroaryl 1a, heteroaryl 4 and heteroaryl 4a independently represent a 5- or 6-membered heteroaryl group containing from 1 to 3 heteroatoms (selected from N, O and 10 S); and heterocyclyl, heterocyclyl 1a, heterocyclyl 4 and heterocyclyl 4a independently represent a 5- or 6-membered heterocyclyl group containing from 1 to 3 heteroatoms (selected from N, O and S); and pharmaceutically acceptable salts and solvates thereof. 1 The compounds are useful as pharmaceuticals, particularly in the treatment of fibrotic diseases, cancer and pain.