发明名称 Pyridine derivatives.
摘要 <p>Compounds of formula (1):- &lt;Chemistry id="chema01" num="0001"&gt;&lt;Image id="ia01" he="32" wi="28" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;and pharmaceutically acceptable salts thereof, where &lt;UnorderedLists id="ula01" listStyle="none"&gt;&lt;ListItem&gt;R&lt;Sup&gt;1&lt;/Sup&gt; and R&lt;Sup&gt;2&lt;/Sup&gt; are the same or different and are C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl or with the nitrogen atom to which they are attached form a pyrrolidino or piperidino group;&lt;/ListItem&gt;&lt;ListItem&gt;R&lt;Sup&gt;3&lt;/Sup&gt; is C&lt;Sub&gt;1-4&lt;/Sub&gt; alkylene;&lt;/ListItem&gt;&lt;ListItem&gt;W is a group -XYCH&lt;Sub&gt;2&lt;/Sub&gt;CH&lt;Sub&gt;2&lt;/Sub&gt;NHR&lt;Sup&gt;4&lt;/Sup&gt; in which&lt;/ListItem&gt;&lt;ListItem&gt;Y is methylene or sulphur:&lt;/ListItem&gt;&lt;ListItem&gt;X is methylene or oxygen, provided that it is methylene when Y is sulphur, and&lt;/ListItem&gt;&lt;ListItem&gt;R&lt;Sup&gt;4&lt;/Sup&gt; is a group of formula (2):-&lt;/ListItem&gt;&lt;/UnorderedLists&gt;&lt;Chemistry id="chema02" num="0002"&gt;&lt;Image id="ia02" he="25" wi="32" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;where &lt;UnorderedLists id="ula02" listStyle="none"&gt;&lt;ListItem&gt;R&lt;Sup&gt;5&lt;/Sup&gt; is NCN, NNO&lt;Sub&gt;2&lt;/Sub&gt;, NH or CHNO&lt;Sub&gt;2&lt;/Sub&gt; and R&lt;Sup&gt;6&lt;/Sup&gt; is hydrogen, hydroxy, amino, C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl, C&lt;Sub&gt;2-4&lt;/Sub&gt; alkynyl; or R&lt;Sup&gt;4&lt;/Sup&gt; is a group of formula (3):-&lt;/ListItem&gt;&lt;/UnorderedLists&gt;&lt;Chemistry id="chema03" num="0003"&gt;&lt;Image id="ia03" he="27" wi="50" file="IMGA0003.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;where &lt;UnorderedLists id="ula03" listStyle="none"&gt;&lt;ListItem&gt;R&lt;Sup&gt;7&lt;/Sup&gt; is a covalent bond or methylene or ethane-1, 2-diyl optionally substituted with one C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl group or a &lt;!-- EPO &lt;DP n="2"&gt; --&gt;second C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl group or a phenyl (C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl) group, or a group of formula (4):- &lt;Chemistry id="chema04" num="0004"&gt;&lt;Image id="ia04" he="27" wi="48" file="IMGA0004.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;&lt;/ListItem&gt;&lt;/UnorderedLists&gt;where &lt;UnorderedLists id="ula04" listStyle="none"&gt;&lt;ListItem&gt;R&lt;Sup&gt;8&lt;/Sup&gt; is hydrogen; C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl, optionally substituted phenyl or phenyl (C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl), (the substituents being one or more C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl or C&lt;Sub&gt;1-6&lt;/Sub&gt; alkoxy groups or halogen atoms or a methylenedioxo group), or optionally substituted furanyl- or thienyl- or pyridyl(C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl) (the substituents being one or more C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl or C&lt;Sub&gt;1-6&lt;/Sub&gt; alkoxy groups); and R&lt;Sup&gt;9&lt;/Sup&gt; is hydrogen, C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl or benzyl,&lt;/ListItem&gt;&lt;ListItem&gt;or W is Y&lt;Sup&gt;1&lt;/Sup&gt;R&lt;Sup&gt;10&lt;/Sup&gt; where&lt;/ListItem&gt;&lt;ListItem&gt;Y&lt;Sup&gt;1&lt;/Sup&gt; is (CH&lt;Sub&gt;2&lt;/Sub&gt;), where a is from 3 to 6 or (CH&lt;Sub&gt;2&lt;/Sub&gt;)&lt;Sub&gt;b&lt;/Sub&gt;S(CH&lt;Sub&gt;2&lt;/Sub&gt;)&lt;Sub&gt;d&lt;/Sub&gt; where b and d are the same or different and are from 1 to 3 or O(CH&lt;Sub&gt;2&lt;/Sub&gt;)&lt;Sub&gt;f&lt;/Sub&gt; where f is from 2 to 5 and&lt;/ListItem&gt;&lt;ListItem&gt;R&lt;Sup&gt;10&lt;/Sup&gt; is a group of formula (5):- &lt;Chemistry id="chema05" num="0005"&gt;&lt;Image id="ia05" he="23" wi="33" file="IMGA0005.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;&lt;/ListItem&gt;&lt;/UnorderedLists&gt;where &lt;UnorderedLists id="ula05" listStyle="none"&gt;&lt;ListItem&gt;R" is cyano, carbamoyl, ureido, hydroxy, C&lt;Sub&gt;1-6&lt;/Sub&gt; alkoxy, C&lt;Sub&gt;1-6&lt;/Sub&gt; alkanoyl, C&lt;Sub&gt;1-6&lt;/Sub&gt; alkanoylamino, arylsulphamoyl, aralkanoyl, carboxymethyl or a group of formula (6):- &lt;Chemistry id="chema06" num="0006"&gt;&lt;Image id="ia06" he="14" wi="19" file="IMGA0006.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /&gt;&lt;/Chemistry&gt;&lt;/ListItem&gt;&lt;/UnorderedLists&gt;where &lt;UnorderedLists id="ula06" listStyle="none"&gt;&lt;ListItem&gt;R" is C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl, haloC&lt;Sub&gt;1-6&lt;/Sub&gt;alkyl, optionally substituted phenyl, amino, mono or di(C&lt;Sub&gt;1-6&lt;/Sub&gt;)alkanoylamino, arylamino or arylalkanoylamino;&lt;/ListItem&gt;&lt;ListItem&gt;R&lt;Sup&gt;12&lt;/Sup&gt; is hydrogen C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl C&lt;Sub&gt;2-6&lt;/Sub&gt; alkanoyl, C&lt;Sub&gt;2-6&lt;/Sub&gt; alkenyl, C&lt;Sub&gt;2-6&lt;/Sub&gt; alkynyl, cyano; or&lt;/ListItem&gt;&lt;ListItem&gt;R&lt;Sup&gt;10&lt;/Sup&gt; is a group of formula -CONHR&lt;Sup&gt;14&lt;/Sup&gt; where R&lt;Sup&gt;14&lt;/Sup&gt; is hydrogen, C&lt;Sub&gt;1-6&lt;/Sub&gt; alkyl, hydroxy or sulfamoyl.&lt;/ListItem&gt;&lt;/UnorderedLists&gt;</p>
申请公布号 EP0089153(A2) 申请公布日期 1983.09.21
申请号 EP19830301160 申请日期 1983.03.04
申请人 SMITH KLINE & FRENCH LABORATORIES LIMITED 发明人 COOPER, DAVID GWYN;SACH, GEORGE SIDNEY
分类号 C07D213/32;C07D213/58;C07D401/12;(IPC1-7):07D213/38;07D213/32;61K31/445;07D213/58;07D401/06;07D401/12;61K31/44 主分类号 C07D213/32
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