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<SUP>5</SUP>; J<SUP>1</SUP>-J<SUP>2</SUP> is N=C(R<SUP>6</SUP>), (R<SUP>7</SUP>)C=N, (R<SUP>8</SUP>)N- C(O), (R<SUP>8</SUP>)<SUB>2</SUB>C-C(O), N=N or (R<SUP>7</SUP>)C=C(R<SUP>6</SUP>); Q<SUP>3</SUP> is a bond or a saturated C<SUB>1-3</SUB> hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR<SUP>2</SUP>R<SUP>3</SUP>, 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<SUP>1a</SUP> and R<SUP>1b</SUP> are the same or different and each is hydrogen or a substituent R<SUP>10</SUP>; or R<SUP>1a</SUP> and R<SUP>1b</SUP> 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<SUP>10</SUP>; and R<SUP>2</SUP>, R<SUP>3</SUP>, R<SUP>4</SUP>, R<SUP>5</SUP>, R<SUP>7</SUP>, R<SUP>6</SUP>, R<SUP>8</SUP>, and R<SUP>10</SUP> are as defined in the claims.</p> |
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 |