C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) A61K 31/437 (2006.01) A61K 31/443 (2006.01) A61K 31/4433 (2006.01) A61P 9/10 (2006.01) A61P 9/12 (2006.01) C07D 405/12 (2006.01)
Patent
CA 2622082
Compounds of the general formula (I) or its salt or a compound in which one or more atoms are replaced by their stable, nonradio-active isotopes, in particular its pharmaceutically acceptable salt; in which X is -CH2-; R1 is a mono- to tetrasubstituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R2 is C1-6alkyl or C3-6cycloalkyl; R3 is independently of one another H, C1-6alkyl, C1-6alkoxycarbonyl or C1-6alkanoyl; R4 is C2-6alkenyl, C1-6alkyl, unsubstituted or substituted aryl- C1-6alkyl or C3-8cycloalkyl; R5 is -Lm-R6; L is C1-6alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n = 0, 1 or 2; m = 0 or 1; R6 is a radical composed of 2 cyclic systems selected from bicyclo[x.y.z]alkyl, spiro[o.p]alkyl, mono- or bioxabicyclo[x.y.z]alkyl or mono- or bioxaspiro[o.p]alkyl, all of which may be substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy- C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino, or if m = 0: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6alkoxy- C1-6alkyl, hydroxy- C1-6alkyl or dialkylamino, or if m = 1: is also saturated C3-8heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1- 3 substituents selected from C1-6alkyl, C1-6alkoxy, cyano, halogen, C1-6- alkoxy-C1-6alkyl, hydroxy-C1-6alkyl or dialkylamino; have renin- inhibiting properties and can be used as medicines for the treatment of hypertension.
Selon l'invention, des composés de formule générale (I) ou leurs sels ou composés, dans lesquels un ou plusieurs atomes sont remplacés par leurs isotopes stables, non radioactifs, notamment, par leur sel acceptable pharmaceutiquement et dans lesquels les significations des substituants R1, R2, R3, R4, R5 et X sont telles qu'indiquées dans la revendication 1, présentent des propriétés de ré-inhibition et peuvent être utilisés comme des médicaments.
Behnke Dirk
Herold Peter
Jelakovic Stjepan
Mah Robert
Marti Christiane
Fetherstonhaugh & Co.
Speedel Experimenta Ag
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