发明名称 Phenylalkyl-2,3-dihydrobenzofurans and analogs useful as anti-inflammatory agents.
摘要 <p>Compounds of formula (I): &lt;CHEM&gt; and pharmaceutically acceptable salts thererof are disclosed wherein m is 1 to 4; n is 2 or 3; r is 1 to 3; A is, e.g., phenyl substituted with (R&lt;1&gt;)q wherein q is an integer of 1 to 5 and when there are more than one R&lt;1&gt;, R&lt;1&gt; can be the same or different from each other and is hydrogen; halo; loweralkoxy; lower alkenoyl; haloloweralkyl; cyano; hydroxyloweralkyl; or hydroxy; and R, R&lt;2&gt; and R&lt;3&gt; independently are R&lt;1&gt;. Those compounds are prepared by (1) nucleophilic substitution involving an appropriately substituted 2,3-dihydrobenzofuranol (or 2,3-dihydrobenzopyranol) and a cinnamylhalide followed by reduction; or (2) by Wittig reaction involving a halomethyl derivative of 2,3-dihydrobenzofuran (or 2,3,-dihydrobenzopyran and an aryl or a heteroaryl aldehyde followed by reduction. These compounds were found to be potent antiinflammatory agents. </p>
申请公布号 EP0199235(A2) 申请公布日期 1986.10.29
申请号 EP19860105073 申请日期 1986.04.14
申请人 MERCK & CO. INC. 发明人 CHANG, MICHAEL N.;THOMPSON, KATHRYN L.;BOULTON, DAVID A.
分类号 A61K31/34;A61K31/343;A61K31/35;A61K31/352;A61K31/415;A61P29/00;C07D307/78;C07D307/79;C07D307/80;C07D307/82;C07D307/84;C07D311/04;C07D311/58;C07D311/66;C07D333/00;C07D405/06;C07D409/06;(IPC1-7):C07D307/79;A61K31/335 主分类号 A61K31/34
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