5-AMINO-4-HYDROXY-7- (IMIDAZO [1,2-A] PYRIDIN-6- YLMETHYL)-8-METHYL-NONAMIDE DERIVATIVES AND RELATED COMPOUNDS AS RENIN INHIBITORS FOR THE TREATMENT OF HYPERTENSION

摘要

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 -CH<SUB>2</SUB>-; R<SUP>1</SUP> is a mono- to tetrasubstituted, mono- or bicyclic, unsaturated heterocyclic radical having 1 to 4 nitrogen atoms, R<SUP>2</SUP> is C<SUB>1-6</SUB>alkyl or C<SUB>3-6</SUB>cycloalkyl; R<SUP>3</SUP> is independently of one another H, C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkoxycarbonyl or C<SUB>1-6</SUB>alkanoyl; R<SUP>4</SUP> is C<SUB>2-6</SUB>alkenyl, C<SUB>1-6</SUB>alkyl, unsubstituted or substituted aryl- C<SUB>1-6</SUB>alkyl or C<SUB>3-8</SUB>cycloalkyl; R<SUP>5</SUP> is -L<SUB>m</SUB>-R<SUP>6</SUP>; L is C<SUB>1-6</SUB>alkylene which is optionally substituted by 1-4 halogen, or a linker: formula (II) n = 0, 1 or 2; m = 0 or 1; R<SUP>6</SUP> 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 C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkoxy, cyano, halogen, C<SUB>1-6</SUB>alkoxy- C<SUB>1-6</SUB>alkyl, hydroxy-C<SUB>1-6</SUB>alkyl or dialkylamino, or if m = 0: is also saturated C<SUB>3-8</SUB>heterocyclyl which comprises 1-2 oxygen atoms, substituted by 1-3 substituents selected from C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkoxy, cyano, halogen, C<SUB>1-6</SUB>alkoxy- C<SUB>1-6</SUB>alkyl, hydroxy- C<SUB>1-6</SUB>alkyl or dialkylamino, or if m = 1: is also saturated C<SUB>3-8</SUB>heterocyclyl which comprises 1-2 oxygen atoms, optionally substituted by 1-3 substituents selected from C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkoxy, cyano, halogen, C<SUB>1-6-</SUB>alkoxy-C<SUB>1-6</SUB>alkyl, hydroxy-C<SUB>1-6</SUB>alkyl or dialkylamino; have renin- inhibiting properties and can be used as medicines for the treatment of hypertension.