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PYRAZOLE-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES FOR USE IN THE TREATMENT OF CANCER AND AUTOIMMUNE DISORDERS

申请公布号:WO2006134318(A1)

申请号:WO2006GB02071

申请日期:2006.06.06

申请公布日期:2006.12.21

申请人:
VERNALIS R & D LIMITED;WALMSLEY, DAVID, LEE;DRYSDALE, MARTIN, JAMES;NORTHFIELD, CHRISTOPHER, JOHN;FROMONT, CHRISTOPHE

发明人:WALMSLEY, DAVID, LEE;DRYSDALE, MARTIN, JAMES;NORTHFIELD, CHRISTOPHER, JOHN;FROMONT, CHRISTOPHE

分类号:C07D401/14;A61K31/4184;A61P35/00;A61P37/00;C07D403/04;C07D405/04;C07D451/04;C07D453/02;C07D487/04

主分类号:C07D401/14

摘要:<p>Compounds of formula (I) are inhibitors of PDK1 and CHK1 activity, and of use in the treatment of cancer and autoimmune disorders (I) : wherein R&lt;SUB&gt;2&lt;/SUB&gt; is a radical of formula R&lt;SUB&gt;7&lt;/SUB&gt;-(CH&lt;SUB&gt;2&lt;/SUB&gt;)&lt;SUB&gt;n-&lt;/SUB&gt;, or a radical of formula -Alk-N(-R&lt;SUB&gt;8&lt;/SUB&gt;)-R&lt;SUB&gt;9&lt;/SUB&gt; wherein n is 0, 1 , 2 or 3 and AIk is C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt; alkylene; R&lt;SUB&gt;7&lt;/SUB&gt; is (i) a heterocyclic ring of 5 or 6 ring atoms coupled via a ring carbon wherein the sole heteroatom is nitrogen, optionally substituted by C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt; alkyl or aryl C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;6&lt;/SUB&gt; alkyl, (ii) 1-aza-bicyclo[2.2.2] oct-3-yl, or (iii) 8-methyl-8-aza-bicyclo[3.2.1] oct-3-yl; R&lt;SUB&gt;8&lt;/SUB&gt; and R&lt;SUB&gt;9&lt;/SUB&gt; are independently selected from hydrogen or C&lt;SUB&gt;1&lt;/SUB&gt;-C&lt;SUB&gt;3&lt;/SUB&gt; alkyl; and the remaining substituents are as defined in the claims.</p>

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