Piperazine derivatives, medicaments containing them, their use, and processes for their preparation

1-pyridyl-piperazine derivs. of formula (I) and their tautomers, stereoisomers and salts are new. Ra = pyridyl; Y1 = CO, CO-CO, Al-CO, CO-Al, SO2-A2, A2-SO2, CO-Al-CO, CO-NR1-CO, CO-NR1-A2, CO-NR1-A2-CO or CO-A2-NR1-CO; R1 = H, 1-5C alkyl, aryl or aryl(1-3C)alkyl; A1 = 1-5C n-alkylene opt. substd. b...

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Hauptverfasser: LINZ, GUENTHER, AUSTEL, VOLKHARD, HIMMELSBACH, FRANK, WEISENBERGER, JOHANNES, PIEPER, HELMUT, GUTH, BRIAN
Format: Patent
Sprache:eng ; fre ; ger
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Zusammenfassung:1-pyridyl-piperazine derivs. of formula (I) and their tautomers, stereoisomers and salts are new. Ra = pyridyl; Y1 = CO, CO-CO, Al-CO, CO-Al, SO2-A2, A2-SO2, CO-Al-CO, CO-NR1-CO, CO-NR1-A2, CO-NR1-A2-CO or CO-A2-NR1-CO; R1 = H, 1-5C alkyl, aryl or aryl(1-3C)alkyl; A1 = 1-5C n-alkylene opt. substd. by a 1-5C alkyl, cyclohexyl(1-3C)alkyl, aryl or aryl(1-3C)alkyl gp. or by an OR1 gp. that is not alpha to a N atom; A2 = 1-4C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl(1-3C)alkyl; Y2 = phenylene, cyclohexylene or pyridine-diyl; a "3-piperidinylene", "4-piperidinylene" or piperazine-1,4-diyl gp. in which 1-2 N-adjacent CH2 gps. are opt. replaced by CO; NR1-B linked to Y1 through NR1 or O-B linked to Y1 through O; B = phenylene cyclohexylene or pyridine-diyl; or a piperidine-diyl gp. which is linked via the 3 or 4 position to NR1 or O and in which 1-2 N-adjacent CH2 gps. are opt. replaced by CO; Y3 = CO, A2-CO (linked via A2 to Y2), CH2-CH(NHR2)-CO, NR2-A3-CO (linked via NR2 to a C atom in Y2), O-A3-CO (linked via O to a C atom in Y2) or CO-A3-CO; A3 = 1-3C n-alkylene opt. monosubstd. by 1-5C alkyl, aryl or aryl(1-3C)alkyl; R2 = H, 1-5C alkyl, aryl(1-3C)alkyl, aryl, 2-6C alkoxycarbonyl, 1-5C alkanoyl, 1-5C alkylsulphonyl, aryl-(1-3C)alkylsulphonyl, arylsulphonyl, aroyl or aryl(2-4C)alkanoyl; E = OH, 1-6C alkoxy, phenyl(1-3C)alkoxy, 3-9C cycloalkoxy, 5-8C cycloalkoxy mono- or disubstd. by 1-3C alkyl, 5-8C cycloalkoxy in which a CH2 gp. in the 3 or 4 position is replaced by O or NR (R = H, 1-3C alkyl, phenyl(1-3C)alkyl, phenyl(2-4C)alkoxycarbonyl or 2-6C alkanoyl) and which is opt. mono- or disubstd. by 1-3C alkyl; 4-7C cycloalkenyloxy, 3-5C alkenyloxy, phenyl(3-5C)alkenyloxy, 3-5C alkynyloxy or phenyl(3-5C)alkynyloxy, provided that no multiple-bonded C atom is bonded to O, (3-8C) cycloalkyl(1-3C)alkoxy, 8-10C bicycloalkoxy opt. mono- or disubstd. by 1-3C alkyl, "1,3-dihydro-3-oxo-1-isobenzfuranyloxy", R5COO-CR3R4-O- or "an alpha -amino group of a natural amino acid or its ester", where the ester is a 1-6C alkyl, 2-6C alkenyl, 5-7C cycloalkyl, phenyl or phenyl(1-3C)alkyl ester; R3 = H, 1-6C alkyl, 3-7C cycloalkyl or phenyl; R4 = H or 1-6C alkyl; R5 = 1-5C alkyl, 1-5C alkoxy, 5-7C cycloalkyl or 5-7C cycloalkoxy; the aryl, phenyl and phenylene gps. are opt. substd. by 1-3C of halogen, alkyl, CF3, NO2, NH2, (di)alkylamino, alkanoylamino, OH, alkoxy, COOH, alkoxycarbonyl, carboxyalkoxy, alkoxycarbonylalkoxy, carbamoyl and (di)alkylcarbamoyl; provided that t