885595-75-5Relevant academic research and scientific papers
PHARMACEUTICAL COMPOUNDS
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, (2008/06/13)
Compounds of the formula (I), and salts, solvates, tautomers and N-oxide thereof; wherein TG is selected from groups (1) and (2): wherein the asterisk (*) represents the point of attachment of the group E to the group X; Rla is an optionally substituted aryl or heteroaryl group; Rlb is hydrogen or a group Rla; X is an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 are heteroatoms selected from O, N and S; and A, E, R2, R3, R4, Q1 and Q2 are as defined in the claims; provided that when E is aryl or heteroaryl, then Q2 is other than a bond; and further provided that the moiety (a) is other than a group (BG1) or (BG2); wherein (BGl) and (BG2) are each optionally substituted; T is N or CRZ; J1-J2 is selected from N=C(RZ), (RZ)C=N, (RZ)N-C(O), (RZ)2C-C(O), N=N and (RZ)C=C(R6); J4 -J3 is a group N=C(RZ) or a group (RZ)N-CO; and RZ is hydrogen or a substituent. The compounds of the formula (I) have PKA and PKB kinase inhibiting activity and are useful in the treatment of cancers.
Rapid evolution of 6-phenylpurine inhibitors of protein kinase B through structure-based design
Donald, Alastair,McHardy, Tatiana,Rowlands, Martin G.,Hunter, Lisa-Jane K.,Davies, Thomas G.,Berdini, Valerio,Boyle, Robert G.,Aherne, G. Wynne,Garrett, Michelle D.,Collins, Ian
, p. 2289 - 2292 (2008/02/03)
6-Phenylpurines were identified as novel, ATP-competitive inhibitors of protein kinase B (PKB/Akt) from a fragment-based screen and were rapidly progressed to potent compounds using iterative protein-ligand crystallography with a PKA-PKB chimeric protein.
HETEROCYCLIC CONTAINING AMINES AS KINASE B INHIBITORS
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, (2010/11/25)
The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof; for use as a PKB kinase inhibitor or PKA kinase inhibitor. In formula (I), A is a saturated hydrocarbon linker group; E is a monocyclic or bicyclic carbo
