发明名称 Cholecystokinin antagonist compounds, process for their preparation and pharmaceutical compositions containing them.
摘要 <p>Products of Aspergillus alliaceus fermentation with the formula &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="63" wi="57" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;&lt;Chemistry id="chema02" num="0002"&gt;&lt;Image id="ia02" he="56" wi="62" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;&lt;!-- EPO &lt;DP n="2"&gt; --&gt;or &lt;Chemistry id="chema03" num="0003"&gt;&lt;Image id="ia03" he="52" wi="77" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;and salts and quaternary ammonium salts thereof, wherein X is N or C and R&lt;Sub&gt;1&lt;/Sub&gt;, R&lt;Sub&gt;2&lt;/Sub&gt; and R&lt;Sub&gt;3&lt;/Sub&gt; are H, F, and CH&lt;Sub&gt;3&lt;/Sub&gt;, and R&lt;Sub&gt;4&lt;/Sub&gt; is selected from phenyl, cyclohexyl, cyclopentyl, (CH&lt;Sub&gt;3&lt;/Sub&gt;)&lt;Sub&gt;2&lt;/Sub&gt;CH-CH&lt;Sub&gt;2&lt;/Sub&gt;- , (CF&lt;Sub&gt;3&lt;/Sub&gt;) (CH&lt;Sub&gt;3&lt;/Sub&gt;) CH-CH&lt;Sub&gt;2&lt;/Sub&gt;-. CH&lt;Sub&gt;2&lt;/Sub&gt;=C(CH&lt;Sub&gt;3&lt;/Sub&gt;)CH&lt;Sub&gt;2&lt;/Sub&gt;-, CH&lt;Sub&gt;2&lt;/Sub&gt;=CHCH&lt;Sub&gt;2&lt;/Sub&gt;-, CH&lt;Sub&gt;3&lt;/Sub&gt;-CH&lt;Sub&gt;2&lt;/Sub&gt;-CH&lt;Sub&gt;2&lt;/Sub&gt;-, CH&lt;Sub&gt;3&lt;/Sub&gt;-CH&lt;Sub&gt;2&lt;/Sub&gt;-(CH&lt;Sub&gt;3&lt;/Sub&gt;)CH-, CH&lt;Sub&gt;3&lt;/Sub&gt;-(CH2)&lt;Sub&gt;3&lt;/Sub&gt;-, CH&lt;Sub&gt;3&lt;/Sub&gt;-S-(CH&lt;Sub&gt;2&lt;/Sub&gt;)&lt;Sub&gt;2&lt;/Sub&gt;-, and CH&lt;Sub&gt;3&lt;/Sub&gt;-CH&lt;Sub&gt;2&lt;/Sub&gt;-S-CH&lt;Sub&gt;2&lt;/Sub&gt;- such that R&lt;Sub&gt;1&lt;/Sub&gt; R&lt;Sub&gt;2&lt;/Sub&gt; and R&lt;Sub&gt;3&lt;/Sub&gt; are all H only when R&lt;Sub&gt;4&lt;/Sub&gt; is other than (CH&lt;Sub&gt;3&lt;/Sub&gt;)&lt;Sub&gt;2&lt;/Sub&gt;-CH-CH&lt;Sub&gt;2&lt;/Sub&gt;-, having a cholecystokinin (CCK) antagonist activity, their preparation and use.</p>
申请公布号 EP0192948(A1) 申请公布日期 1986.09.03
申请号 EP19860100637 申请日期 1986.01.18
申请人 MERCK & CO., INC. 发明人 HOUCK, DAVID R.;INAMINE, EDWARD S.;GOETZ, MICHAEL A.
分类号 A61K31/55;A61P1/00;C07D487/04;C07D487/22;C07D519/00;C12P17/18;C12R1/66;(IPC1-7):C07D519/00 主分类号 A61K31/55
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