发明名称 ORTHO- CONDENSED PYRIDINE AND PYRIMIDINE DERIVATIVES (E. G. PURINES) AS PROTEIN KINASES INHIBITORS
摘要 <p>The invention provides a compound for use in the prophylaxis or treatment of a disease state or condition mediated by protein kinase B, the compound having the formula (I): or salts, solvates, tautomers or N-oxides thereof, wherein T is N or 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;); A is an optionally substituted saturated C&lt;SUB&gt;1-7 &lt;/SUB&gt;hydrocarbon linker group having a maximum chain length of 5 atoms extending between R&lt;SUP&gt;1&lt;/SUP&gt; and NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt; and a maximum chain length of 4 atoms extending between E and NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt;, one of the carbon atoms in the linker group being optionally replaced by oxygen or nitrogen; E is a monocyclic or bicyclic carbocyclic or heterocyclic group or an acyclic group X-G wherein X is CH&lt;SUB&gt;2&lt;/SUB&gt;, O, S or NH and G is a C&lt;SUB&gt;1-4 &lt;/SUB&gt;alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R&lt;SUP&gt;1&lt;/SUP&gt; is hydrogen or an aryl or heteroaryl group; R&lt;SUP&gt;2&lt;/SUP&gt; and R&lt;SUP&gt;3&lt;/SUP&gt; are each hydrogen, optionally substituted C&lt;SUB&gt;1-4 &lt;/SUB&gt;hydrocarbyl or optionally substituted C&lt;SUB&gt;1-4 &lt;/SUB&gt;acyl; or NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt; forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt; and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C&lt;SUB&gt;1-4&lt;/SUB&gt;alkyl; or NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt; and the adjacent carbon atom of linker group A together form a cyano group; or R&lt;SUP&gt;1&lt;/SUP&gt;, A and NR&lt;SUP&gt;2&lt;/SUP&gt;R&lt;SUP&gt;3&lt;/SUP&gt; together form a cyano group; and R&lt;SUP&gt;4&lt;/SUP&gt;, R&lt;SUP&gt;5&lt;/SUP&gt;, R&lt;SUP&gt;6&lt;/SUP&gt;, R&lt;SUP&gt;7&lt;/SUP&gt; and R&lt;SUP&gt;8&lt;/SUP&gt; are each independently selected from hydrogen and various substituents as defined in the claims.</p>
申请公布号 WO2006046023(A1) 申请公布日期 2006.05.04
申请号 WO2005GB04115 申请日期 2005.10.25
申请人 ASTEX THERAPEUTICS LIMITED;PITAL THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOS;CANCER RESEARCH TECHNOLOGY LIMITED;BERDINI, VALERIO;BOYLE, ROBERT, GEORGE;SAXTY, GORDON;VERDONK, MARINUS, LEENDERT;WOODHEAD, STEVEN, JOHN;WYATT, PAUL, GRAHAM;SORE, HANNAH, FIONA;CALDWELL, JOHN;COLLINS, IAN;DA FONSECA, TATIANA, FARIA;DONALD, ALASTAIR 发明人 BERDINI, VALERIO;BOYLE, ROBERT, GEORGE;SAXTY, GORDON;VERDONK, MARINUS, LEENDERT;WOODHEAD, STEVEN, JOHN;WYATT, PAUL, GRAHAM;SORE, HANNAH, FIONA;CALDWELL, JOHN;COLLINS, IAN;DA FONSECA, TATIANA, FARIA;DONALD, ALASTAIR
分类号 A61K31/52;A61K31/437;A61K31/519;C07D471/04;C07D473/00;C07D473/34;C07D487/04 主分类号 A61K31/52
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