Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1997-03-05
1999-08-10
Kight, John
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142315, 514255, 514311, 514312, 514330, 544 60, 544129, 544360, 546192, 546196, 546204, 546208, 546209, 546212, 546213, 546216, 546219, 546220, 5462784, 5462787, A61K 3154, A61K 3143, C07D41760, C07D21108
Patent
active
059359510
DESCRIPTION:
BRIEF SUMMARY
The invention relates to novel 1-acyl-4-aliphatylaminopiperidine compounds of the formula I ##STR2## in which R.sub.1 is a benzoyl, naphthoyl or cycloalkanoyl radical which is unsubstituted or substituted by lower alkyl, lower alkoxy, halogen and/or trifluoromethyl; unsubstituted or substituted by lower alkyl, lower alkoxy, halogen, nitro, cyano and/or trifluoromethyl; alkylene; or alkyl or a radical of the formula --(CH.sub.2).sub.n --(.dbd.O)--R.sub.5 (Ia); and R.sub.4 is hydrogen, lower alkyl or a radical of the formula --(CH.sub.2).sub.n --C(.dbd.O)--R.sub.5 (Ia); lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxearbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene, (ii) hydroxyl, cycloalkoxy, lower alkoxy or lower alkoxy which is substituted by lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylamino-alkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene, or (iii) amino or amino substituted by lower alkyl, cycloalkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene; group or a free or etherified hydorowcymethylene group; and n-4-yl!acetamide; process for the preparation of the compounds according to the invention, pharmaceutical preparations containing these, and their use as pharmaceutical active ingredients.
Cycloalkyl and radicals derived therefrom have, for example, 3 to 8, in particular 5 to 7, primarily 5 or 6, ring members and are, for example, cyclopentyl, cyclohexyl or cycloheptyl.
Alkyl which is substituted by halogen, lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa-, or thia-lower alkylene is, for example, haloalkyl, in particular halo-lower alkyl, lower alkoxyalkyl, in particular lower alkoxy-lower alkyl, aminoalkyl, in particular amino-lower alkyl, mono- or di-lower alkylaminoalkyl, in particular mono- or di-lower alkylamino-lower alkyl, lower alkanoylaminoalkyl, in particular lower alkanoylamino-lower alkyl, lower alkoxycarbonylaminoalkyl, in particular lower alkoxycarbonylamino-lower alkyl, pyrrolidinoalkyl, in particular pyrrolidino-lower alkyl, piperidinoalkyl, in particular piperidino-lower alkyl, free or N'-lower alkylated or N'-lower alkanoylated piperazinoalkyl, in particular the corresponding piperazino-lower alkyl, morpholino alkyl, in particular morpholino-lower alkyl, or free or S-oxidized thiomorpholinoalkyl, in particular the corresponding thiomorpholino-lower alkyl.
Amino substituted by lower alkyl, (3- to 8-membered) cycloalkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene is, for example, mono- or di-lower alkylamino, (3- to 8-membered) cycloalkylamino, amino-lower alkylamino, mono- or di-lower alkylamino-lower alkylamino, lower alkanoylamino, lower-alkoxycarbonylamino, pyrrolidino, piperidino, free or N'-lower alkylated or N'-lower alkanoylated piperazino, morpholino or free or S-oxidized thiomorpholino.
Lower alkoxy which is substituted by lower alkoxy, amino or amino substituted by lower alkyl, amino-lower alkyl, mono- or di-lower alkylaminoalkyl, lower alkanoyl, lower alkoxycarbonyl or lower alkylene or aza-, oxa- or thia-lower alkylene is, for example, lower alkoxy-lower alkoxy, amino-lower alkoxy, mono- or di-lower alkylamino-lower alkoxy, lower alkanoylamino-lower alkoxy, lower alkoxycarbonylamino-lower alkoxy, pyrrolidino-lower alkoxy, piperidino-lower alkoxy, free or N'-lower alkylated or N'-lower alkanoylated piperazino-lower alkoxy, morpholino-lower alkoxy, or free or S-oxidized thiomorpholino-lower alkoxy.
Alkyl is, for example, straight-chain or branched C.sub.1 -C.sub.14 -alkyl, in particular C.sub.1 -C.sub.10 -alkyl, preferably lower alkyl.
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REFERENCES:
patent: 5310743 (1994-05-01), Schilling et al.
patent: 5459270 (1995-10-01), Williams et al.
Schilling et al. Chemical abstract vol. 119 No. 271005 "Prep of 1-acylpiperdation and their use as substance of P Antagonists" 1993.
Ofner Silvio
Veenstra Siem Jacob
Covington Raymond
Ferraro Gregory D.
Kight John
Novartis Finance Corporation
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