Invention Grant
- Patent Title: Substituted pyridazines for the treatment of pain
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Application No.: US15000531Application Date: 2016-01-19
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Publication No.: US10016420B2Publication Date: 2018-07-10
- Inventor: Karl Richard Gibson , Dafydd Rhys Owen
- Applicant: INHIBITAXIN LIMITED
- Applicant Address: GB Sandwich Kent
- Assignee: INHIBITAXIN LIMITED
- Current Assignee: INHIBITAXIN LIMITED
- Current Assignee Address: GB Sandwich Kent
- Agent Dennis A. Bennett
- Main IPC: A61K31/50
- IPC: A61K31/50 ; C07D237/24 ; C07D403/12 ; C07D237/20 ; C07D413/12 ; A61K31/501 ; C07D401/14 ; C07D413/14 ; A61K45/06

Abstract:
The invention provides compounds of formula I, wherein: R1 represents a cyclic group selected from phenyl, heteroaryl1, heterocyclyl1 and C3-6 cycloalkyl; wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C1-6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C1-6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl1a and heterocyclyl1a; and wherein each cyclic group is optionally fused to a 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 heterocyclyl1 and heterocyclyl1a may additionally be substituted with ═O; X represents a bond or C1-6 alkylene (which may be straight or branched); R2 represents H or C1-6 alkyl; R3 represents H or C1-6 alkyl; Y represents a bond or C1-6 alkylene (which may be straight or branched, and optionally substituted with OH or CF3); R4 represents a cyclic group selected from phenyl, heteroaryl4, heterocyclyl4 and C3-6 cycloalkyl; wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C1-6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C1-6 alkyl substituted with phenyl, C1-6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl4a and heterocyclyl4a; 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 heterocyclyl4 and heterocyclyl4a may additionally be substituted with ═O; heteroaryl1, heteroaryl1a, heteroaryl4 and heteroaryl4a independently represent a 5- or 6-membered heteroaryl group containing from 1 to 3 heteroatoms (selected from N, O and S); and heterocyclyl1, heterocyclyl1a, heterocyclyl4 and heterocyclyl4a 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. The compounds are useful as pharmaceuticals, particularly in the treatment of fibrotic diseases, cancer and pain.
Public/Granted literature
- US20160287584A1 SUBSTITUTED PYRIDAZINES FOR THE TREATMENT OF PAIN Public/Granted day:2016-10-06
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