- PIPERIDINE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS
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A novel piperidine derivative represented by the formula (I) (I) wherein Ar is a phenyl group optionally having substituent(s), R?1? is a hydrogen atom, a hydrocarbon group optionally having substituent(s), an acyl group or a heterocyclic group optionally having substituent(s), Z is a methylene group optionally having C?1-6#191 alkyl group(s), ring A is a piperidine ring optionally further having substituent(s), and B is a monocyclic aromatic heterocyclic group optionally having substituent(s) (substituents of monocyclic aromatic heterocycle may be bonded to each other to form a ring), or a salt thereof has a superior tachykinin receptor antagonistic action and the like, and is useful as an agent for the prophylaxis or treatment of lower urinary tract disease and the like.
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(2010/11/28)
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- 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
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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.
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