B1-antagonists

摘要

Disclosed are compounds of the formula I;
wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.

主权项

1. A compound of the formula Iwherein
A denotes
a) a bond,b) C1-4-alkylene,c) —N(R2),d) —C(O),e) a saturated 5- or 6-membered aza heterocyclic group orf) a saturated 6- or 7-membered diaza heterocyclic group, Y denotes a C1-6-alkylene group optionally substituted by the group R2, while a methylene group contained therein may additionally be replaced by Y1 and
Y1 denotes —O, —S, —S(O), —N(R2), —N(R2)—C(O), —C(O)—N(R2), —C(O), —CH(aryl) or —S(O)2—, R1 denotes
a) aryl orb) heteroaryl,while the previously mentioned aryl and heteroaryl groups may each be substituted by one, two, three or four groups R1.1 and the groups R1.1 may be identical or different andR1.1 denotes H, F, Cl, Br, I, C1-3-alkyl, F3C, HO, C1-3-alkyl-O or C1-3-alkyl-O—C2-4-alkylene-O—, R2 denotes
a) H orb) C1-3-alkyl, while each methylene group may be substituted by up to two and each methyl group may be substituted by up to three fluorine atoms, R3 denotes
a) a saturated 4- to 7-membered aza heterocyclic group which is selected from among b) a monounsaturated 5- to 7-membered aza heterocyclic group, wherein an olefinic double bond is fused to a group R3.1, orc) a saturated 8- to 10-membered diaza-heterobicyclic group with the proviso that one of A, R4 or R5 is an aza heterocyclic group,andR3.1 denotes phenyl or pyridyl,while the groups R3.1 in the carbon skeleton may additionally be substituted by one, two or three identical or different groups R3.1.1 andR3.1.1 denotes F, Cl, Br, I, H3C or F3C—, R4 denotes
a) a bond,b) C1-3-alkylenec) C3-6-cycloalkylene,d) a saturated 4- to 7-membered aza heterocyclic group,e) a saturated 6- to 7-membered diaza heterocyclic group orf) a saturated 9- to 11-membered diaza-spirocycle, R5 denotes
a) a C1-4-alkyl group substituted by R5.1,b) H2N,c) C1-4-alkyl-NH—d) (C1-4-alkyl)2N ore) a saturated 4- to 6-membered aza heterocyclic group andR5.1 denotes H, (C1-4-alkyl)2N or a saturated 4- to 6-membered aza heterocyclic group,or an enantiomer, diastereomer or salt thereof.