发明名称 Pyrazolo (3,4-c) and thiazolo (5,4-c) isoquinolines, methods for preparing them, these compounds for use as antiinflammatory, CNS-depressant and anti-anxiety agents and pharmaceutical compositions thereof.
摘要 <p>New tricyclic ortho-fused heterocyclic compounds of formula &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="30" wi="58" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;wherein A is the group R or the group N &lt;Chemistry id="chema02" num="0002"&gt;&lt;Image id="ia02" he="20" wi="66" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;in which R represents hydrogen, (C&lt;Sub&gt;1-4&lt;/Sub&gt;) alkyl, phenyl or tolyl and R, may be (C&lt;Sub&gt;1-4&lt;/Sub&gt;) alkyl, phenyl or tolyl, R&lt;Sub&gt;2&lt;/Sub&gt; is selected from (C&lt;Sub&gt;1-4&lt;/Sub&gt;) alkyl, (C&lt;Sub&gt;2-4&lt;/Sub&gt;) alkanoylmethyl, carbo- (C&lt;Sub&gt;1-3&lt;/Sub&gt;) alkoxymethyl, hydroxy (C&lt;Sub&gt;2-4&lt;/Sub&gt;) alkyl, halo (C&lt;Sub&gt;2&lt;/Sub&gt;.&lt;Sub&gt;4&lt;/Sub&gt;) alkyl and a group &lt;Chemistry id="chema03" num="0003"&gt;&lt;Image id="ia03" he="13" wi="33" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;wherein R&lt;Sub&gt;3&lt;/Sub&gt; is an alkylene group from 2 to 4 carbon atoms and R. and R&lt;Sub&gt;s&lt;/Sub&gt; independently represent hydrogen or (C&lt;Sub&gt;1-4&lt;/Sub&gt;) alkyl or, taken together with the nitrogen atom, a fully hydrogenated 5 or 6 membered heterocyclic radical which may contain a further heteroatom selected from 0, N and S and be optionally substituted by a (C&lt;Sub&gt;1-4&lt;/Sub&gt;) alkyl or phenyl group, or R&lt;Sub&gt;2&lt;/Sub&gt; may represent nil, the dotted lines x and y may represent nil or additional bonds; with the proviso that, when the symbol R&lt;Sub&gt;2&lt;/Sub&gt; linked to the oxygen atom is different from nil, x is an additional bond and y and the other symbol R&lt;Sub&gt;2&lt;/Sub&gt; represent nil; with the further proviso that. when the symbol R&lt;Sub&gt;2&lt;/Sub&gt; linked to the nitrogen atom is different from nil, y is an additional bond and x and the other symbol R&lt;Sub&gt;2&lt;/Sub&gt;, represent nil; and salts therewith of pharmaceutically acceptable acids. The compounds possess antiinflammatory CNS-depressant and anti-anxiety utility.</p>
申请公布号 EP0005745(A1) 申请公布日期 1979.12.12
申请号 EP19790101393 申请日期 1979.05.08
申请人 GRUPPO LEPETIT S.P.A. 发明人 WINTERS, GIORGIO;DI MOLA, NUNZIO
分类号 A61K31/47;A61P25/20;A61P29/00;C07D231/38;C07D471/04;C07D513/04;(IPC1-7):07D471/04;07D513/04;61K31/47 主分类号 A61K31/47
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