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<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>); A is an optionally substituted saturated C<SUB>1-7 </SUB>hydrocarbon linker group having a maximum chain length of 5 atoms extending between R<SUP>1</SUP> and NR<SUP>2</SUP>R<SUP>3</SUP> and a maximum chain length of 4 atoms extending between E and NR<SUP>2</SUP>R<SUP>3</SUP>, 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<SUB>2</SUB>, O, S or NH and G is a C<SUB>1-4 </SUB>alkylene chain wherein one of the carbon atoms is optionally replaced by O, S or NH; R<SUP>1</SUP> is hydrogen or an aryl or heteroaryl group; R<SUP>2</SUP> and R<SUP>3</SUP> are each hydrogen, optionally substituted C<SUB>1-4 </SUB>hydrocarbyl or optionally substituted C<SUB>1-4 </SUB>acyl; or NR<SUP>2</SUP>R<SUP>3</SUP> forms an imidazole group or a saturated monocyclic heterocyclic group having 4-7 ring members; or NR<SUP>2</SUP>R<SUP>3</SUP> and A together form a saturated monocyclic heterocyclic group having 4-7 ring members which is optionally substituted by C<SUB>1-4</SUB>alkyl; or NR<SUP>2</SUP>R<SUP>3</SUP> and the adjacent carbon atom of linker group A together form a cyano group; or R<SUP>1</SUP>, A and NR<SUP>2</SUP>R<SUP>3</SUP> together form a cyano group; and R<SUP>4</SUP>, R<SUP>5</SUP>, R<SUP>6</SUP>, R<SUP>7</SUP> and R<SUP>8</SUP> are each independently selected from hydrogen and various substituents as defined in the claims.</p> |
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 |