Heterocyclyl-condensed benzoylguanidines, their production...

Details Heterocyclyl-condensed benzoylguanidines, their production... Heterocyclyl-condensed benzoylguanidines, their production...

C - Chemistry, Metallurgy

07

D

C07D 333/64 (2006.01) A61K 31/38 (2006.01) A61K 31/425 (2006.01) A61K 31/54 (2006.01) C07D 277/64 (2006.01) C07D 279/16 (2006.01) C07D 327/02 (2006.01) C07D 333/54 (2006.01) C07D 333/62 (2006.01) C07D 333/66 (2006.01) C07D 333/68 (2006.01) C07D 335/06 (2006.01) C07D 339/08 (2006.01) C07D 495/10 (2006.01)

Patent

CA 2241143

Cyclic sulphones of formula (I) are disclosed, in which: R1 and R2 each independently of one another stand for H, A, CF3, CH2F, CHF2, C2F5, Hal, OH, OA, NH2, NHA, NA2, NO2 or CN; X stands for CR4R5, C=Z, O, S, NH, NA or NR3; Y stands for CR6R7, C=Z, O, NH, NA, or NR3; Z stands for O, S, NH, NA, NOH, NOA, CH2, CHA or CA2; R4, R5, R6 and R7 each independently of one another stand for H, A, R3, Hal, OH, OA, SH, SA, NH2, NHA or NA2, or alternatively, R5 and R6 or R7 and R8 can together represent a bond, only one such bond being present in each molecule; R4 and R5 together can also stand for O-(CH2)2-O or O-(CH2)3-O; R8 and R9 each independently of one another stand for H or A; A stands for alkyl with 1-6 C atoms; Hal stands for F, Cl, Br or I; and R3 stands for phenyl or benzyl which is unsubstituted or single-, double- or triple- substituted by A, OA, NH2, NHA, NA2, F, Cl, Br and/or CF3; and n is 0 or 1. Also disclosed are the physiologically tolerable salts of these compounds. These compounds and their salts have anti-arrhythmic properties and act as inhibitors of the cellular Na+/H+-antiporter.

Sulfones cycliques de formule (I), dans laquelle R?1¿ et R?2¿ désignent chacun, indépendamment l'un de l'autre, H, A, CF¿3?, CH¿2?F, CHF¿2?, C¿2?F¿5?, Hal, OH, OA, NH¿2?, NHA, NA¿2?, NO¿2? ou CN; X désigne CR?4¿R?5¿, C=Z, O, S, NH, NA ou NR?3¿; Y désigne CR?6¿R?7¿, C=Z, O, NH, NA, ou NR?3¿; Z désigne O, S, NH, NA, NOH, NOA, CH¿2?, CHA ou CA¿2?; R?4¿, R?5¿, R?6¿ et R?7¿ désignent chacun, indépendamment l'un de l'autre, H, A, R?3¿, Hal, OH, OA, SH, SA, NH¿2?, NHA ou NA¿2?, ou encore, en variante, R?5¿ et R?6¿ ou R?7¿ et R?8¿ peuvent représenter conjointement une liaison, une seule liaison de ce genre pouvant toutefois être présente, au maximum, dans chaque molécule; R?4¿ et R?5¿ répresentent conjointement, également, O-(CH¿2?)¿2?-O ou O-(CH¿2?)¿3?-O; R?8¿ et R?9¿ désignent chacun, indépendamment l'un de l'autre, H ou A; A est un alkyle de 1 à 6 C atomes de carbone, Hal désigne F, Cl, Br ou I; et R?3¿ désigne un phényle ou un benzyle non substitué ou mono-, bi ou tri-substitué par A, OA, NH¿2?, NHA, NA¿2?, F, Cl, Br et/ou CF¿3?; n est également 0 ou 1. L'invention concerne également les sels physiologiquement tolérables de ces composés. Lesdits composés et leurs sels présentent des propriétés antiarythmiques et agissent comme inhibiteurs de l'antiport cellulaire Na+/H+.

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