Aroyl-piperazine derivatives, their preparation and their use as tachykinin antagonists

A compound of the formula

• 9
• wherein
• Y is bond or lower alkylene,
• R1 is aryl which may have substituent(s),
• R2 is aryl or indolyl, each of which may have substituent(s),
• R3 is hydrogen or lower alkyl,
• R4 is pyridyl(lower)alkylamino(lower)alkynyl;
• N-(lower alkyl)-N-[pyridyl(lower)alkyl]amino-(lower)alkyl;
• hydroxy(lower)alkoxy(lower)alkyl;
• lower alkanoyl(lower)alkoxy(lower)alkyl;
• phenyl(lower)alkyl which has hydroxy(lower)alkyl or morpholinyl(lower)alkyl;
• ar(lower)alkoxycarbonyl;
• (2-pyridyl)(lower)alkyl which may have 1 to 3 substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkoxycarbonyl, mono(or di or tri)halo(lqwer)alkyl and halogen;
• (3-pyridyl)propyl which may have lower alkoxy or amino;
• (3-pyridyl)butyl which may have lower alkoxy or amino;
• pyridyl(lower)alkenyl which may have lower alkoxy or amino;
• (2-pyridyl)(lower)alkynyl which may have 1 to 3 substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, lower alkoxycarbonyl, mono(or di or tri)halo(lower)alkyl and halogen;
• (3-pyridyl)(lower)alkynyl which may have lower alkoxy or amino;
• pyridyl, thiazolyl, imidazolyl or pyrazolyl, each of which may have substituent(s);
• imidazolyl(lower)alkyl which may have 1 or 2 substituent(s) selected from the group consisting of lower alkyl, lower alkynyl, ar(lower)alkyl, pyridyl(lower)alkyl, mono(or di or tri)halo(lower)alkyl and halogen;
• pyrazolyl(lower)alkyl which may have hydroxy(lower)alkyl, carboxy(lower)alkyl, lower alkoxycarbonyl(lower)alkyl, morpholinyl(lower)alkyl or morpholinylcarbonyl(lower)alkyl;
• thiazolyl(lower)alkyl which may have lower alkyl;
• piperidyl(lower)alkyl which may have hydroxy(lower)alkyl or lower alkoxy;
• morpholinyl(lower)alkyl which has 1 or 2 substituent(s) selected from the group consisting of ethyl, hydroxy(lower)alkyl, halo(lower)alkyl and lower alkoxy(lower)alkyl;
• morpholinyl(lower)alkyl which has lower alkyl and lower alkoxy(lower)alkyl;
• (3,5-dimethylmorpholino)(lower)alkyl;
• morpholino(lower)alkenyl which may have lower alkyl or lower alkoxy(lower)alkyl;
• (2- or 3-morpholinyl)(lower)alkenyl which may have lower alkoxycarbonyl;
• pyrrolidinyl(lower)alkynyl which may have lower alkoxy(lower)alkyl;
• morpholinyl(lower)alkynyl which may have 1 or 2 substituent(s) selected from the group consisting of ethyl, propyl, isopropyl, isobutyl, spirocyclo(lower)alkyl, lower alkoxy(lower)alkyl, hydroxy(lower)alkyl, carboxy(lower)alkyl, di(lower alkyl)carbamoyl, lower alkoxycarbonyl and halo(lower)alkyl;
• morpholinyl(lower)alkynyl which has methyl and lower alkoxy;
• (dimethylmorpholino)(lower)alkynyl;
• homomorpholinyl(lower)alkynyl which have halogen;
• (morpholinylamino)propyl which may have lower alkanoyl;
• thiomorpholinyl(lower)alkynyl which may have substituent(s);
• homomorpholinylamino(lower)alkyl;
• thiomorpholinylamino(lower)alkyl;
• or
• saturated heterocyclicimino(lower)alkyl, saturated heterocyclicaminocarbonyl(lower)alkyl or saturated heterocyclic(lower)alkoxy(lower)alkyl, each of which may have substituent(s),
• provided that when
• R4 is 2-[N-methyl-N-(3-pyridylmethyl)amino]ethyl,
• 3-(3-pyridyl)propyl,
• 3-(3-pyridyl)-2-propynyl,
• 4-[(2-methoxymethyl)pyrrolidino]-2-butynyl,
• 4-thiomorpholino-2-butynyl,
• 3-(morphlinoamino)propyl,
• 4-morpholino-2-butenyl,
• 4-morpholino-2-butynyl, or
• 4-(3,3-dimethylmorpholino)-2-butynyl, then
• R1 is not 3,5-bis(trifluoromethyl)phenyl, and a salt thereof.