C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) A61K 31/435 (2006.01) C07D 211/58 (2006.01) C07D 211/74 (2006.01) C07D 401/14 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 471/04 (2006.01)
Patent
CA 2075684
1-Acylpiperidine compound of the formula I Image in which R1 is an optionally substituted aralkyl, aryloxyalkyl, heteroaralkyl, aroyl, heteroaroyl, cycloalkylcarbonyl, aralkanoyl, heteroarylalkanoyl, aralkoxycarbonyl or arylcarbamoyl radical or the acyl radical of an .alpha.-amino acid which is optionally N-substituted by lower alkanoyl or carbamoyl-lower-alkanoyl, R2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X2 is alkylene, carbonyl or a direct linkage, and X3 is carbonyl, oxo-lower- alkylene, oxo(aza)-lower-alkylene or an alkylene radical which is optionally substituted by phenyl, hydroxymethyl, optionally esterified or amidated carboxyl or, in higher than the a position, by hydroxyl, and its salts have substance-P-antagonistic properties and can be used as pharmaceutically active substances in pharmaceuticals for the treatment of disorders in whose development substance P plays an essential part.
Ofner Silvio
Schilling Walter
Veenstra Siem J.
Ag Ciba-Geigy
Fetherstonhaugh & Co.
Novartis Ag
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