Aminopiperidines, their production and the pharmaceutical compositions incorporating them
First Claim
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1. Aryl alkyl piperidines of the formula I ##STR29## in which R1 is a hydrogen or a lower alkyl radical,R is an alkylene chain having from 2 to 4 carbon atoms which may be substituted with one or more lower alkyl radicals,X is a grouping ##STR30## in which R2 is hydrogen, a lower alkyl carbonyl residue, a lower alkenyl radical or a lower alkyl radical;
- Ac is an acyl residue from an alkyl carboxylic acid having up to 10 carbon atoms;
R4, R5 and R6 which are the same or different represent a hydrogen, a halogen, a lower alkyl radical, a lower alkoxy or a lower alkylene dioxy;
and Ar is an unsubstituted phenyl or substituted phenyl radical of the formula ##STR31## wherein D is a halogen, a lower alkyl radical, a lower alkenyl radical, a lower alkoxy, a lower alkenyloxy, a lower alkynyloxy, a lower alkylthio, a hydroxy carbonyl, a lower alkoxy carbonyl, a nitro group, an amino, a lower alkyl amino, a dilower alkyl amino, a lower acylamino, a sulphonamido, a lower alkyl amino sulphonyl, a dilower alkyl amino sulphonyl, a lower alkyl sulphonyl, an amino carbonyl, a cyano, a trifluoromethyl or a lower alkylene dioxyand m is O or an integer from 1 to 5, inclusive.
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Abstract
This invention relates to 4-aminopiperidines and more precisely to 4-aminopiperidines the nitrogen atom of the piperidine ring is substituted with an aryl lower alkyl side-chain.
This invention also relates to processes for producing the same.
This invention further extends to pharmaceutical compositions and to the method of using the same.
23 Citations
25 Claims
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1. Aryl alkyl piperidines of the formula I ##STR29## in which R1 is a hydrogen or a lower alkyl radical,
R is an alkylene chain having from 2 to 4 carbon atoms which may be substituted with one or more lower alkyl radicals, X is a grouping ##STR30## in which R2 is hydrogen, a lower alkyl carbonyl residue, a lower alkenyl radical or a lower alkyl radical; -
Ac is an acyl residue from an alkyl carboxylic acid having up to 10 carbon atoms; R4, R5 and R6 which are the same or different represent a hydrogen, a halogen, a lower alkyl radical, a lower alkoxy or a lower alkylene dioxy; and Ar is an unsubstituted phenyl or substituted phenyl radical of the formula ##STR31## wherein D is a halogen, a lower alkyl radical, a lower alkenyl radical, a lower alkoxy, a lower alkenyloxy, a lower alkynyloxy, a lower alkylthio, a hydroxy carbonyl, a lower alkoxy carbonyl, a nitro group, an amino, a lower alkyl amino, a dilower alkyl amino, a lower acylamino, a sulphonamido, a lower alkyl amino sulphonyl, a dilower alkyl amino sulphonyl, a lower alkyl sulphonyl, an amino carbonyl, a cyano, a trifluoromethyl or a lower alkylene dioxy and m is O or an integer from 1 to 5, inclusive. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25)
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Specification
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Current AssigneeScience Union et CIE
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Original AssigneeScience Union et CIE
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InventorsVincent, Michel, Remond, Georges, Laubie, Michel
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Primary Examiner(s)Milestone, Norma S.
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Application NumberUS05/948,536Time in Patent Office839 DaysField of Search424/267, 546/224US Class Current514/329CPC Class CodesA61P 9/12 AntihypertensivesC07C 321/00 Thiols, sulfides, hydropoly...C07D 211/58 attached in position 4C07D 333/34 Sulfur atoms
