Calcium channel blockers

Details Calcium channel blockers Calcium channel blockers

A - Human Necessities

61

K

A61K 31/495 (2006.01) A61K 31/445 (2006.01) A61K 31/4468 (2006.01) A61K 31/451 (2006.01) A61K 31/4515 (2006.01) A61K 31/454 (2006.01) A61K 31/506 (2006.01) A61K 31/5375 (2006.01) C07D 211/14 (2006.01) C07D 211/16 (2006.01) C07D 211/46 (2006.01) C07D 295/03 (2006.01) C07D 401/04 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2335461

Compounds of formula (1) wherein m is 0, 1 or 2; wherein when m is 0, Z is 0; when m is 1, Z is N, and when m is 2, Z is C; Y is H, OH, NH2, or an organic moiety of 1-20C, optionally additionally containing 1-8 heteroatoms selected from the group consisting of N, P, O, S and halo; each 1 1 and 1 2 is independently 0-5; 1 3 is 0 or 1; each of R1, R2 and R3 is independently alkyl (1-6C), aryl (6-10C) or arylalkyl (7-16C) optionally containing 1-4 heteroatoms selected from the group consisting of halo, N, P, 0, and S or each of R1 and R2 may independently be halo, COOR, CONR2, CF3, CN or NO2, wherein R is H or lower alkyl (1-4C) or alkyl (1-6C); n is 0 or 1; X is a linker, with the proviso that Y is not a tropolone, a coumarin, or an antioxidant containing an aromatic group and with the further proviso that if 1 3 is 0, neither R 1 nor R2 can represent F in the para position; and are useful as calcium channel blockers. Libraries of these compounds can also be used to identify antagonists for other targets.

L'invention porte sur des composés de formule (I) dans laquelle: m est 0, 1 ou 2; quand m est 0, Z est O, quand m est 1, Z est C, et quand m est 2, Z est N; Y est H, OH, NH2 ou un fragment organique 1-20C contenant facultativement 1-8 hétéroatomes sélectionnés parmi N, P, S et halo; chacun des l<1> et l<2> est indépendamment 0-5; l<3> est 0 ou 1; chacun des de R<1>, R<2>, et R<3> est indépendamment alkyle (1-6C), aryle (6-10C) ou arylalkyle (7-16C) et contient facultativement 1-4 hétéroatomes sélectionnés parmi halo, N, P, O et S, ou R<1> et R<2>; peuvent être indépendamment halo, COOR, CONR2, CF3, CN ou NO2, R étant H ou alkyle inférieur (1-4C) ou alkyle (1-6C); n est 0 ou 1; X est un lieur, et cela sous réserve que Y ne soit pas un tropolone, une courmarine, ou un antioxydant contenant un groupe aromatique, et que si l3 est 0, ni R<1> ni R<2> ne puissent représenter F en position para. Lesdits composée peuvent servir de d'inhibiteurs des canaux calciques et pour l'identification d'antagonistes d'autres cibles.

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