T-type calcium channel blockers

Details T-type calcium channel blockers T-type calcium channel blockers

A - Human Necessities

61

K

A61K 31/675 (2006.01) A61P 7/10 (2006.01) A61P 9/04 (2006.01) A61P 9/06 (2006.01) A61P 9/10 (2006.01) A61P 13/12 (2006.01) C07F 9/59 (2006.01) C07F 9/6509 (2006.01) C07F 9/6571 (2006.01)

Patent

CA 2520628

T-Type calcium channel blockers consisting of optically active 1,4- dihydropyridines represented by the general formula (1), pharmaceutically acceptable salts thereof, or solvates of both: (1) wherein R1 and R2 are each independently C1-6 alkyl, or R1 and R2 are united to form -CR5R6-CR7R8-, - CR5R6-CR7R8-CR9R10-, -CR5R6-CR7R8-CR9R10-CR11R12-, or the like; X1 and X2 are each independently O or NR13; Ar is optionally substituted phenyl or the like; Ra and Rb are each independently C1-6 alkyl, -L2-NR16R17, CH2O-L2-NR16R17, CN, -L2-N(CH2CH2)2NR16, NR16R17, or the like; Y is C1-20 alkyl, -L3-NR18R19, (2) (3) (4) (5) or (6) and * represents R-configuration.

La présente invention se rapporte à des agents bloquant les canaux calciques de type T, constitués de 1,4-dihydropyridines optiquement actives représentées par la formule générale (1), à des sels pharmaceutiquement acceptables de ces agents bloquants ou à des solvates de ces agents ou de leurs sels. Dans la formule (1), R?1¿ et R?2¿ sont chacun indépendamment alkyle C¿1-6?, ou R?1¿ et R?2¿ sont unis de manière à former -CR?5¿R?6¿-CR?7¿R?8¿-CR?9¿R?10¿-, -CR?5¿R?6¿-CR?7¿R?8¿-CR?9¿R?10¿-CR?11¿R?12¿- ou analogue ; X?1¿ et X?2¿ sont chacun indépendamment O ou NR?13 ¿; Ar est phényle éventuellement substitué ou analogue ;? ¿R?a¿ et R?b¿ sont chacun indépendamment alkyle C¿1-6?, -L?2¿-NR?16¿R?17¿, CH¿2?O-L?2¿-NR?16¿R?17¿, CN, -L?2¿-N(CH¿2?CH¿2?)¿2?NR?16¿, NR?16¿R?17¿, ou analogue ; Y est alkyle C¿1-20?, -L?3¿-NR?18¿R?19¿, formules (2), (3), (4), (5) ou (6) et * représente une configuration -R.

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