Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-04-04
1996-07-30
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514314, 514318, 514323, 546108, 546194, 546195, 546201, 546205, 546208, 546213, A61K 3147, C07D21512, C07D40900
Patent
active
055411959
ABSTRACT:
1-Acylpiperidine compound of the formula I ##STR1## in which R.sub.1 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, R.sub.2 is cycloalkyl or an optionally substituted aryl or heteroaryl radical, R.sub.3 is hydrogen, alkyl, carbamoyl or an alkanoyl or alkenoyl radical which is optionally substituted by carboxyl or esterified or amidated carboxyl, R.sub.4 is an optionally substituted aryl or optionally partially hydrogenated heteroaryl radical, X.sub.1 is methylene, ethylene, a direct linkage, an optionally ketalised carbonyl group or an optionally etherified hydroxymethylene group, X.sub.2 is alkylene, carbonyl or a direct linkage, and X.sub.3 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 .alpha. 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.
REFERENCES:
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Garret et al.; "Pharmacological Properties of a potent and selective nonpeptide substance P antagonist"; Proc. Natl. Acad Sci. USA vol. 88, 10208-10212, Nov. 1991.
Snider et al.; "A Potent Nonpeptide Antagonist of the Substance P (NK) Receptor"; Science 251, pp. 435-437; Jan. 25, 1991.
McLean et al.; "Activity and Distribution of Binding Sites in Brain of a Nonpeptide Substance P (NK) Receptor Antagonist"; Science 251, pp. 437-439; Jan. 25, 1991.
Chem Abstr. 68: 38700v (1968) of Becker et al.; J. Prakt. Chem. 37 (1-2), 47-58 (1968); Syntheses in the Isoquinoline Series IV.
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Ofner Silvio
Schilling Walter
Veenstra Siem J.
Ciba-Geigy Corporation
Covington Raymond
Fishman Irving M.
Ivy C. Warren
Kaiser Karen G.
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