Pyrazole compounds and their use as T-type calcium channel blockers

摘要

A compound of Formula (I) ** See formula ** in which X represents a ring carbon or ring nitrogen atom; - R1 represents → (C2-6) alkyl; → (C2-4) alkyl monosubstituted with cyano or (C1-3) alkoxy; → fluoroalkyl (C1-4); → fluoroalkoxy (C1-3); → pentafluoro-sulfanyl; → (C3-6) -L1- cycloalkyl in which - said (C3-6) cycloalkyl optionally contains a ring oxygen atom; wherein said cycloalkyl (C3-6) is not substituted or is mono-substituted with fluorine, (C1-3) alkyl, alkoxy (C1-3), hydroxy, cyano or fluoroalkyl (C1-3) or disubstituted with fluorine or trisubstituted with two fluorine substituents and one substituent selected from (C1-3) alkyl and cyano; and - the connector L1 represents a direct bond, alkylene (C1-2), oxygen or alkylene (C1-2) -oxy; → heteroaryl of 5 or 6 elements, independently, optionally monosubstituted with (C1-3) alkyl; → -NR11R12, in which - R11 and R12 independently represent hydrogen, (C1-3) alkyl, fluoroalkyl (C2-3), cycloalkyl (C3-6), cycloalkyl (C3-6) monosubstituted or disubstituted with fluorine, cycloalkyl ( C3-6) - (C1-3) alkyl, (C1-3) alkoxy-(C2-3) alkyl; - or R11 and R12, together with the nitrogen atom to which they are attached, form a ring of 4 to 6 elements optionally monosubstituted or disubstituted with fluorine; a 2-oxo-pyrrolidinyl group or a morpholinyl group; and (R4) n represents one or two optional substituents independently selected from (C1-4) alkyl, C3-6 cycloalkyl, C1-4 alkoxy, C1-3 fluoroalkyl, C1-3 fluoroalkoxy, halogen and cyano; - or R1 together with (R4) n form a non-aromatic ring of 5 or 6 elements that is fused to the phenyl / pyridine ring; wherein said ring of 5 or 6 elements optionally contains one or two heteroatoms independently selected from oxygen and nitrogen; wherein said fused 5 or 6-element non-aromatic ring is, independently, in turn optionally monosubstituted with oxo or (C1-3) alkyl; disubstituted with (C1-3) alkyl; or di-, tri- or tetra-substituted in which one substituent is oxo and the others are (C1-3) alkyl; - or R1 together with (R4) n form an aromatic ring of 5 or 6 elements that is fused to the phenyl / pyridine ring; wherein said ring of 5 or 6 elements optionally contains one or two heteroatoms selected from nitrogen, wherein said aromatic ring of 5 or 6 elements fused is, independently, in turn optionally monosubstituted or disubstituted in which the substituents are independently selected from (C1-3) alkyl, (C3-6) cycloalkyl, (C1) fluoroalkyl or cyano; - or R1 represents methyl or halogen; and (R4) n represents a substituent selected from fluoroalkoxy (C1-3) which is attached to the phenyl / pyridinyl ring in the ortho or meta position by the point of attachment of the group -CH2-CO-NH-; Y represents a carbon atom in the ring or nitrogen in the ring; and R2 represents (C1-4) alkyl, (C3-6) cycloalkyl, (C1-4) alkoxy, (C3-6) cycloalkyl, fluoroalkyl (C1-3), fluoroalkoxy (C1-3), alkoxy (C1 -3) -alkoxy (C2-3), halogen, cyano, or -NR21R22, in which R21 and R22, independently, represent hydrogen or (C1-3) alkyl, or R21 and R22, together with the atom of nitrogen to which they are attached, form a ring of 4 to 6 elements optionally monosubstituted or disubstituted with fluorine 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, fluoroalkyl (C1-3) and fluoroalkoxy (C1 -3); or a salt of such a compound.