发明名称 Novel benzodiazepine compounds, their preparation, intermediates employed in their preparation, and pharmaceutical compositions containing them.
摘要 <p>Compounds are described of the formula &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="33" wi="55" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;or an acid addition salt thereof; in which R', R&lt;Sup&gt;2&lt;/Sup&gt;, R&lt;Sup&gt;3&lt;/Sup&gt; and R' independently represent hydrogen, Ci-&lt;Sub&gt;4&lt;/Sub&gt; alkyl, C&lt;Sub&gt;2&lt;/Sub&gt;-&lt;Sub&gt;4&lt;/Sub&gt; alkenyl, C&lt;Sub&gt;3-7&lt;/Sub&gt; cycloalkyl, C&lt;Sub&gt;3&lt;/Sub&gt;-&lt;Sub&gt;7&lt;/Sub&gt; cycloalkyl C&lt;Sub&gt;1-4&lt;/Sub&gt; alkyl, halogen, C&lt;Sub&gt;1-4&lt;/Sub&gt; haloalkyl, Ci-&lt;Sub&gt;4&lt;/Sub&gt; alkanoyl, nitro, amino, C&lt;Sub&gt;2&lt;/Sub&gt;-&lt;Sub&gt;4&lt;/Sub&gt; acylamino, cyano, hydroxyl, C&lt;Sub&gt;1-4&lt;/Sub&gt; alkoxy, C&lt;Sub&gt;1-4&lt;/Sub&gt; alkylthio, C&lt;Sub&gt;1-4&lt;/Sub&gt; haloalkoxy or a group of the formula -SO&lt;Sub&gt;2&lt;/Sub&gt;N(R&lt;Sup&gt;8&lt;/Sup&gt;)&lt;Sub&gt;2&lt;/Sub&gt;, -SO&lt;Sub&gt;2&lt;/Sub&gt;R&lt;Sup&gt;8&lt;/Sup&gt; or -SO&lt;Sub&gt;3&lt;/Sub&gt;R&lt;Sup&gt;8&lt;/Sup&gt; where R&lt;Sup&gt;8&lt;/Sup&gt; is C&lt;Sub&gt;1-4&lt;/Sub&gt; alkyl, C&lt;Sub&gt;1-4&lt;/Sub&gt; haloalkyl or optionally substituted phenyl; in which R' is a group of theformula &lt;Chemistry id="chema02" num="0002"&gt;&lt;Image id="ia02" he="28" wi="42" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;where R&lt;Sup&gt;9&lt;/Sup&gt; is hydrogen, C&lt;Sub&gt;1-4&lt;/Sub&gt; alkyl, C&lt;Sub&gt;3-7&lt;/Sub&gt; cycloalkyl, C&lt;Sub&gt;3-7&lt;/Sub&gt; cycloalkyl Ci-&lt;Sub&gt;4&lt;/Sub&gt; alkyl, C&lt;Sub&gt;1-4&lt;/Sub&gt; haloalkyl, C&lt;Sub&gt;2&lt;/Sub&gt;-&lt;Sub&gt;4&lt;/Sub&gt; alkenyl, C&lt;Sub&gt;1-4&lt;/Sub&gt; alkanoyl, benzyl, cyano or optionally substituted phenyl, where R&lt;Sup&gt;10&lt;/Sup&gt; is hydrogen, C&lt;Sub&gt;1-4&lt;/Sub&gt; alkyl or optionally substituted phenyl and where n is 0 or 1; in which R&lt;Sup&gt;6 &lt;/Sup&gt;is hydrogen, C&lt;Sub&gt;1-10&lt;/Sub&gt; alkyl, C&lt;Sub&gt;3-7&lt;/Sub&gt; cycloalkyl. C&lt;Sub&gt;3&lt;/Sub&gt;-&lt;Sub&gt;7&lt;/Sub&gt; cycloalkyl C&lt;Sub&gt;1-4&lt;/Sub&gt; alkyl, C&lt;Sub&gt;1-4&lt;/Sub&gt; haloalkyl, benzyl, Ci-&lt;Sub&gt;6&lt;/Sub&gt; alkanoyl, C&lt;Sub&gt;1-4&lt;/Sub&gt; carbalkoxy or benzoyl; and in which R' is one of the values of R&lt;Sup&gt;6&lt;/Sup&gt; or halogen, nitro, cyano, amino or C&lt;Sub&gt;1-4&lt;/Sub&gt; acylamino. The compounds are active as pharmaceuticals and particularly in the treatment of disorders of the central nervous system.</p>
申请公布号 EP0027390(A1) 申请公布日期 1981.04.22
申请号 EP19800303649 申请日期 1980.10.15
申请人 LILLY INDUSTRIES LIMITED 发明人 CHAKRABARTI, JIBAN KUMAR;HOTTEN, TERRENCE MICHAEL
分类号 A61P25/20;A61K31/00;A61P1/08;A61P25/18;C07D231/38;C07D487/04;(IPC1-7):07D487/04;61K31/55 主分类号 A61P25/20
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