| 摘要 |
The invention comprises 3-aminopyrazoles substituted in the 5-position by an unsubstituted or lower alkyl- or lower alkoxy-substituted pyridyl-(4) or quinolyl-(4) group and optionally substituted in the 4-position by a lower alkyl, phenyl, lower alkyl-phenyl, lower alkoxy-phenyl, halophenyl or trifluoromethyl group or a halogen atom and in the 2-position by an aliphatic hydrocarbon group which may be substituted by a free or substituted hydroxyl, mercapto or amino group as hereinafter defined or by a cycloaliphatic or cycloaliphatic-aliphatic hydrocarbon group each of which may be substituted by an alkyl group, or by an aromatic or araliphatic group or a saturated or unsaturated heterocyclic or heterocyclic-aliphatic group each of which may be substituted by a lower alkyl or lower alkoxy group or a halogen atom (the word "lower" referring to groups containing at most 7 carbon atoms); and their N-acylates; and salts and quaternary ammonium derivatives of these compounds. Substituted hydroxyl, mercapto and amino groups are lower alkoxy, alkylmercapto, or mono- or di-alkylamino or -cycloalkylamino groups, and alkyleneimino, oxaalkyleneimino, azaalkyleneimino or thiaalkyleneimino groups, including the N-hydroxyethyl-piperazino group. Heterocyclic groups referred to are pyridyl and N-alkyl-piperidyl groups. N-Acyl compounds may be mono-or di-acyl and may be derived from carbonic acid or its derivatives (e.g. carbamic acids) or from lower aliphatic, alicyclic, aromatic or heterocyclic acids. The aminopyrazoles may be prepared by reacting a hydrazine containing at least 3 hydrogen atoms with a pyridyl- or quinolyl-(4) ketone that contains in the alpha position at least one hydrogen atom and a nitrile group, e.g. a 4-(a -cyanoalkanoyl)-pyridine. The amino-pyrazoles may be acylated by conventional methods. Resulting 4-unsubstituted pyrazoles may be 4-halogenated. Many detailed examples are given and a list of salt-forming organic and inorganic acids is also provided. 4-(a -Cyano-alkanoyl)-pyridines and quinolines are prepared from pyridine-(4) or quinoline-(4) carboxylic acid esters and alkyl cyanides. The compounds of the invention are stated to possess anti-inflammatory, anti-pyretic, analgesic and anti-allergic properties. The 2-piperidyl-(4) compounds, e.g. 2-(N-methylpiperidyl-(4)- 3-amino- 5-pyridyl-(4)-pyrazole, are also stated to possess hypotensive properties. They may be made up into pharmaceutical preparations, e.g. tablets, dragees, capsules, solutions, suspensions or emulsions, with suitable carriers. The preparations may also contain preserving, stabilising, wetting or emulsifying agents, salts for regulating the osmotic pressure or buffers.
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