发明名称 6,7-Epoxy paclitaxels.
摘要 <p>The present invention provides paclitaxel derivatives of formula I &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="51" wi="93" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" /&gt;&lt;/Chemistry&gt; in which &lt;DefinitionList id="dla01"&gt;&lt;DefinedTerm&gt;R¹ is&lt;/DefinedTerm&gt;&lt;DefinitionDescription&gt;-COR&lt;Sup&gt;z&lt;/Sup&gt;, in which R&lt;Sup&gt;z&lt;/Sup&gt; is RR&lt;Sup&gt;o&lt;/Sup&gt;N-, RHN-, RO- or R;&lt;/DefinitionDescription&gt;&lt;DefinedTerm&gt;R² is&lt;/DefinedTerm&gt;&lt;DefinitionDescription&gt;C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₃₋₆ cycloalkyl, or a radical of the formula -W-R&lt;Sup&gt;x&lt;/Sup&gt; in which W is a bond, C₂₋₆ alkenediyl, or -(CH₂)&lt;Sub&gt;t&lt;/Sub&gt;-, in which t is one to six; and R&lt;Sup&gt;x&lt;/Sup&gt; is naphthyl, phenyl, or heteroaryl, and furthermore R&lt;Sup&gt;x&lt;/Sup&gt; can be optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups;&lt;/DefinitionDescription&gt;&lt;DefinedTerm&gt;R and R&lt;Sup&gt;o&lt;/Sup&gt; are&lt;/DefinedTerm&gt;&lt;DefinitionDescription&gt;independently C₁₋₆ alkyl, C₂₋₆ alkenyl, C₃₋₆ cycloalkyl, C₂₋₆ alkynyl, or phenyl, optionally substituted with one to three same or different C₁₋₆ alkyl, C₁₋₆ alkoxy, halogen or -CF₃ groups.&lt;/DefinitionDescription&gt;&lt;/DefinitionList&gt;&lt;!-- EPO &lt;DP n="55"&gt; --&gt;</p><p>Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.</p>
申请公布号 EP0671399(A1) 申请公布日期 1995.09.13
申请号 EP19950103435 申请日期 1995.03.09
申请人 BRISTOL-MYERS SQUIBB COMPANY 发明人 ROTH, GREGORY
分类号 A61K31/335;A61P35/00;C07D493/08;(IPC1-7):C07D493/08;C07D305/14 主分类号 A61K31/335
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