发明名称 N-Benzyl-Indoles, processes for their preparation and pharmaceutical compositions containing them.
摘要 <p>A compound of the formula &lt;CHEM&gt; in which R&lt;1&gt; is hydrogen, halo, C1-4 alkyl, C1-4 alkoxy, nitrile, optionally protected carboxy, optionally protected tetrazolyl, trihalomethyl, hydroxy-C1-4 alkyl, aldehydo,- CH2Z, -CH=CH-Z or -CH2CH2Z where Z is optionally protected carboxy or optionally protected tetrazolyl; R&lt;2&gt; is halo, nitrile, an optionally protected acid group or -CONR&lt;7&gt;R&lt;8&gt; where R&lt;7&gt; and R&lt;8&gt; are each hydrogen or C1-4 alkyl, R&lt;3&gt; and R&lt;4&gt; are each hydrogen, C1-4 alkyl, optionally substituted phenyl, or C1-4 alkyl substituted by -CONR&lt;7&gt;R&lt;8&gt; or an optionally protected acid group; R&lt;5&gt; is &lt;CHEM&gt; &lt;CHEM&gt; where W is -CH=CH-, -CH=N-, -N=CH-, -O- or -S-, R&lt;9&gt; is hydrogen, halo, C1-4 alkyl, C1-4 alkoxy or trihalomethyl, and R&lt;1&gt;&lt;0&gt; is hydrogen, C1-4 alkyl, C2-6 alkenyl, C3-6 cycloalkyl or C1-4 alkyl-C3-6 cycloalkyl; R&lt;6&gt; is hydrogen or C1-4 alkyl; X is -O-(CH2)nCR&lt;1&gt;&lt;1&gt;CR&lt;1&gt;&lt;2&gt;-, -CR&lt;1&gt;&lt;1&gt;R&lt;1&gt;&lt;2&gt;-, -CR&lt;1&gt;&lt;1&gt;R&lt;1&gt;&lt;2&gt;.(CH2)n.CR&lt;1&gt;&lt;3&gt;R&lt;1&gt;&lt;4&gt;- or -CR&lt;1&gt;&lt;1&gt;=CR&lt;1&gt;&lt;2&gt;- where R&lt;1&gt;&lt;1&gt;, R&lt;1&gt;&lt;2&gt;, R&lt;1&gt;&lt;3&gt; and R&lt;1&gt;&lt;4&gt; are each hydrogen or C1-4 alkyl, and n is 0, 1 or 2; and Y is -O-CR&lt;1&gt;&lt;5&gt;R&lt;1&gt;&lt;6&gt;-, -CR&lt;1&gt;&lt;5&gt;=CR&lt;1&gt;&lt;6&gt;- or -CR&lt;1&gt;&lt;5&gt; R&lt;1&gt;&lt;6&gt;.CR&lt;1&gt;&lt;7&gt;R&lt;1&gt;&lt;8&gt;- where R&lt;1&gt;&lt;5&gt;, R&lt;1&gt;&lt;6&gt;, R&lt;1&gt;&lt;7&gt; and R&lt;1&gt;&lt;8&gt; are each hydrogen or C1-4 alkyl; or a salt thereof. The compounds in unprotected form are active as leukotriene antagonists.</p>
申请公布号 EP0469833(A1) 申请公布日期 1992.02.05
申请号 EP19910306940 申请日期 1991.07.29
申请人 LILLY INDUSTRIES LIMITED 发明人 GILMORE, JEREMY;TODD, ALEC
分类号 A61K31/40;A61K31/33;A61K31/403;A61K31/404;A61K31/423;A61K31/425;A61K31/427;A61K31/428;A61K31/44;A61K31/4427;A61K31/4439;A61K31/4709;A61K31/498;A61K31/517;A61P9/00;A61P9/10;A61P11/06;A61P29/00;A61P37/08;A61P43/00;C07D209/32;C07D401/10;C07D401/12;C07D401/14;C07D403/10;C07D403/12;C07D403/14;C07D413/10;C07D413/12;C07D413/14;C07D417/10;C07D417/12;C07D417/14 主分类号 A61K31/40
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