发明名称 SULFASALAZINE ANALOGUES AS NF-KB INHIBITORS
摘要 <p>Use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for use as a Nuclear Factor-kB (NF-kB) inhibitor formula (I), wherein: A has the following structure; formula (i) Z is -COOH5 -P(O)(OH)&lt;SUB&gt;2&lt;/SUB&gt; or -SO&lt;SUB&gt;2&lt;/SUB&gt;OH ; each R&lt;SUP&gt;1&lt;/SUP&gt; is the same or different and is halogen, hydroxy, C&lt;SUB&gt;1-6&lt;/SUB&gt; alkyl, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkenyl, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkynyl, C&lt;SUB&gt;1-6&lt;/SUB&gt; alkoxy, C&lt;SUB&gt;1-6&lt;/SUB&gt; alkylthio, thio, amino, mono(C&lt;SUB&gt;1-6&lt;/SUB&gt; alkyl)amino, di(C&lt;SUB&gt;1-6&lt;/SUB&gt; alkyl)amino, nitro, cyano or -CO&lt;SUB&gt;2&lt;/SUB&gt;R&lt;SUP&gt;/&lt;/SUP&gt;, wherein R&lt;SUP&gt;/&lt;/SUP&gt; represents hydrogen or C&lt;SUB&gt;1-6&lt;/SUB&gt; alkyl; n is 0, 1, 2 or 3; R&lt;SUP&gt;2&lt;/SUP&gt; is hydrogen, C&lt;SUB&gt;1-6&lt;/SUB&gt; alkyl, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkenyl or C&lt;SUB&gt;2-6&lt;/SUB&gt; alkynyl; Y is a linking group; and X is C&lt;SUB&gt;1-6&lt;/SUB&gt; alkyl, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkenyl, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkynyl, aryl, heteroaryl, carbocyclyl, heterocyclyl, -M-aryl, -M-heteroaryl, -M-carbocyclyl or -M-heterocyclyl, wherein M is C&lt;SUB&gt;1-6&lt;/SUB&gt; alkylene, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkenylene, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkynylene, -Q-Het-Q'- or -Q-Het- wherein Q and Q' are the same or different and are C&lt;SUB&gt;1-6&lt;/SUB&gt; alkylene, C&lt;SUB&gt;2-6&lt;/SUB&gt; alkenylene or C&lt;SUB&gt;2-6&lt;/SUB&gt; alkynylene and Het is selected from -NR&lt;SUP&gt;/&lt;/SUP&gt;-, -O-, -S-, -SO&lt;SUB&gt;2&lt;/SUB&gt;-, -SO-, -C(O)-O-, -OC(O), -CO-, -C(O)-NR&lt;SUP&gt;/&lt;/SUP&gt;- or -NR&lt;SUP&gt;/&lt;/SUP&gt;-C(O)- wherein R&lt;SUP&gt;/&lt;/SUP&gt; is as defined above, provided that: when n is 0, Z is -COOH, R&lt;SUP&gt;2&lt;/SUP&gt; is hydrogen and Y is -N=N-, X is other than 2-pyridyl.</p>
申请公布号 WO2006072783(A1) 申请公布日期 2006.07.13
申请号 WO2006GB00018 申请日期 2006.01.05
申请人 UNIVERSITY OF SOUTHAMPTON;PACKHAM, GRAHAM, KEITH;GANESAN, ARASU;MANN, DEREK, A.;OAKLEY, FIONA;NATARAJAN, SRINIVASAN 发明人 PACKHAM, GRAHAM, KEITH;GANESAN, ARASU;MANN, DEREK, A.;OAKLEY, FIONA;NATARAJAN, SRINIVASAN
分类号 A61K31/192;A61K31/63;A61P9/10;A61P29/00;A61P31/00;A61P35/00 主分类号 A61K31/192
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