Back to results
US 10,246,426 B2Granted
Triazole compounds as T-type calcium channel blockers
AssigneeIdorsia Pharmaceuticals Ltd
InventorsOlivier Bezencon, John Gatfield, Bibia Heidmann, Romain Siegrist, Simon Stamm
Life of this patent
Estimating the term…
Abstract
The invention relates to compounds of formula (I) wherein X, Y, R1, R2, (R4)n, and (R5)m are as defined in the description, and to pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium T-channel blockers.
Claims13
A compound of formula (I)
- wherein
- X represents a ring carbon or a ring nitrogen atom;
- R1 represents
- (C2-6)alkyl;
- (C2-4)alkyl mono-substituted with cyano, or (C1-3)alkoxy;
- (C1-4)fluoroalkyl;
- (C1-3)fluoroalkoxy;
- pentafluoro-sulfanyl;
- (C3-6)cycloalkyl-L1- wherein
- said (C3-6)cycloalkyl optionally contains one ring oxygen atom;
- wherein said (C3-6)cycloalkyl is unsubstituted;
- or mono-substituted with fluoro, (C1-3)alkyl, (C1-3)alkoxy, hydroxy, cyano, or (C1-3)fluoroalkyl;
- or di-substituted with fluoro, or tri-substituted with two fluoro substituents and a (C1-3)alkyl substituent;
- and
- the linker L1 represents a direct bond, (C1-2)alkylene, oxygen, or (C1-2)alkylene-oxy;
- 5- or 6-membered heteroaryl, independently optionally mono-substituted with (C1-3)alkyl;
- —NR11R12, wherein
- R11 and R12 independently represent hydrogen, (C1-3)alkyl, (C2-3)fluoroalkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl mono- or di-substituted with fluoro, (C3-6)cycloalkyl-(C1-3)alkyl, (C1-3)alkoxy-(C2-3)alkyl;
- or R11 and R12, together with the nitrogen atom to which they are attached to, form a 4- to -6 membered ring which is optionally mono- or di-substituted with fluoro;
- a 2-oxo-pyrrolidinyl group;
- or a morpholinyl group;
- and (R4)n represents one or two optional substituents independently selected from (C1-4)alkyl, (C1-4)alkoxy, (C1-3)fluoroalkyl, (C1-3)fluoroalkoxy, halogen, and cyano;
- or R1 together with (R4)n forms a non-aromatic 5- or 6-membered ring which is fused to the phenyl/pyridine ring;
- wherein said 5- or 6-membered ring optionally contains one or two heteroatoms independently selected from oxygen and nitrogen;
- wherein said fused 5- or 6-membered non-aromatic ring independently is optionally further mono-substituted with oxo;
- or di-, tri-, or tetra-substituted wherein one substituent is oxo and the remaining are (C1-3)alkyl;
- or R1 together with (R4)n forms an aromatic 5- or 6-membered ring which is fused to the phenyl/pyridine ring;
- wherein said 5- or 6-membered ring optionally contains one or two nitrogen atoms, wherein said fused 5- or 6-membered aromatic ring independently is optionally further mono- or di-substituted wherein the substituents are independently selected from (C1-4)alkyl, (C3-6)cycloalkyl, (C1)fluoroalkyl, or cyano;
- Y represents a ring carbon or a ring nitrogen atom;
- and
- R2 represents (C1-4)alkyl;
- (C3-6)cycloalkyl;
- (C1-4)alkoxy;
- (C3-6)cycloalkyl-oxy;
- (C1-3)fluoroalkyl;
- (C1-3)fluoroalkoxy;
- (C1-3)alkoxy-(C2-3)alkoxy;
- halogen;
- cyano;
- or —NR21R22, wherein R21 and R22 independently represent hydrogen, or (C1-3)alkyl, or R21 and R22, together with the nitrogen atom to which they are attached to, form a 4- to -6 membered ring optionally mono- or di-substituted with fluoro, or a morpholinyl group;
- and
- (R5)m represents one or two optional substituents independently selected from (C1-4)alkyl;
- (C3-6)cycloalkyl;
- (C1-4)alkoxy;
- halogen;
- cyano;
- (C1-3)fluoroalkyl;
- and (C1-3)fluoroalkoxy;
- or a salt of such a compound.
46 more elements
Dependencies are inferred from the claim text.