发明名称 SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY
摘要 <p>The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR&lt;SUP&gt;5&lt;/SUP&gt;; J&lt;SUP&gt;1&lt;/SUP&gt;-J&lt;SUP&gt;2&lt;/SUP&gt; is N=C(R&lt;SUP&gt;6&lt;/SUP&gt;), (R&lt;SUP&gt;7&lt;/SUP&gt;)C=N, (R&lt;SUP&gt;8&lt;/SUP&gt;)N- C(O), (R&lt;SUP&gt;8&lt;/SUP&gt;)&lt;SUB&gt;2&lt;/SUB&gt;C-C(O), N=N or (R&lt;SUP&gt;7&lt;/SUP&gt;)C=C(R&lt;SUP&gt;6&lt;/SUP&gt;); Q&lt;SUP&gt;3&lt;/SUP&gt; is a bond or a saturated C&lt;SUB&gt;1-3&lt;/SUB&gt; hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt;, CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R&lt;SUP&gt;1a&lt;/SUP&gt; and R&lt;SUP&gt;1b&lt;/SUP&gt; are the same or different and each is hydrogen or a substituent R&lt;SUP&gt;10&lt;/SUP&gt;; or R&lt;SUP&gt;1a&lt;/SUP&gt; and R&lt;SUP&gt;1b&lt;/SUP&gt; together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R&lt;SUP&gt;10&lt;/SUP&gt;; and R&lt;SUP&gt;2&lt;/SUP&gt;, R&lt;SUP&gt;3&lt;/SUP&gt;, R&lt;SUP&gt;4&lt;/SUP&gt;, R&lt;SUP&gt;5&lt;/SUP&gt;, R&lt;SUP&gt;7&lt;/SUP&gt;, R&lt;SUP&gt;6&lt;/SUP&gt;, R&lt;SUP&gt;8&lt;/SUP&gt;, and R&lt;SUP&gt;10&lt;/SUP&gt; are as defined in the claims.</p>
申请公布号 WO2008075109(A1) 申请公布日期 2008.06.26
申请号 WO2007GB50776 申请日期 2007.12.20
申请人 ASTEX THERAPEUTICS LIMITED;THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL;CANCER RESEARCH TECHNOLOGY LIMITED;ASTRAZENECA AB;WOODHEAD, STEVEN, JOHN;FREDERICKSON, MARTYN;HAMLETT, CHRISTOPHER;WOODHEAD, ANDREW, JAMES;VERDONK, MARINUS, LEENDERT;SORE, HANNAH, FIONA;WALKER, DAVID, WINTER;BLURTON, PETER;COLLINS, IAN;CHEUNG, KWAI, MING;CALDWELL, JOHN;DA FONSECA MCHARDY, TATIANA, FARIA;LUKE, RICHARD, WILLIAM, ARTHUR;MATUSIAK, ZBIGNIEW, STANLEY;LEACH, ANDREW;MORRIS, JEFFREY, JAMES 发明人 WOODHEAD, STEVEN, JOHN;FREDERICKSON, MARTYN;HAMLETT, CHRISTOPHER;WOODHEAD, ANDREW, JAMES;VERDONK, MARINUS, LEENDERT;SORE, HANNAH, FIONA;WALKER, DAVID, WINTER;BLURTON, PETER;COLLINS, IAN;CHEUNG, KWAI, MING;CALDWELL, JOHN;DA FONSECA MCHARDY, TATIANA, FARIA;LUKE, RICHARD, WILLIAM, ARTHUR;MATUSIAK, ZBIGNIEW, STANLEY;LEACH, ANDREW;MORRIS, JEFFREY, JAMES
分类号 C07D471/04;A61K31/437;A61K31/52;A61P35/00;C07D473/34;C07D487/04;C07D519/00 主分类号 C07D471/04
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