| 摘要 |
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. |
| 主权项 |
1. A compound of formula (I)whereinX 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 substituent selected from (C1-3)alkyl and cyano; andthe 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 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, (C3-6)cycloalkyl, (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 (C1-3)alkyl; di-substituted with (C1-3)alkyl; 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 heteroatoms selected from nitrogen, wherein said fused 5- or 6-membered aromatic ring independently is optionally further mono- or di-substituted wherein the substituents are independently selected from (C1-3)alkyl, (C3-6)cycloalkyl, (C1)fluoroalkyl, or cyano; or R1 represents methyl, or halogen; and (R4)n represents one substituent selected from (C1-3)fluoroalkoxy which is attached to the phenyl/pyridinyl ring in ortho or meta-position to the point of attachment of the —CH2—CO—NH— group;Y represents a ring carbon or a ring nitrogen atom; andR2 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. |
