TY - PAT
T1 - SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY
AU - Caldwell, John
AU - Da Fonseca McHardy, Tatiana, Faria
AU - Luke, Richard, William, Arthur
AU - Matusiak, Zbigniew, Stanley
AU - Leach, Andrew
AU - Morris, Jeffrey, James
AU - Woodhead, Steven, John
AU - Frederickson, Martyn
AU - Hamlett, Christopher
AU - Woodhead, Andrew, James
AU - Verdonk, Marinus, Leendert
AU - Sore, Hannah, Fiona
AU - Walker, David, Winter
AU - Blurton, Peter
AU - Collins, Ian
AU - Cheung, Kwai, Ming
PY - 2008/6/26
Y1 - 2008/6/26
N2 - 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; J-J is N=C(R), (R)C=N, (R)N- C(O), (R)2C-C(O), N=N or (R)C=C(R); Q is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NRR, 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 and R are the same or different and each is hydrogen or a substituent R; or R and R 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; and R, R, R, R, R, R, R, and R are as defined in the claims.
AB - 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; J-J is N=C(R), (R)C=N, (R)N- C(O), (R)2C-C(O), N=N or (R)C=C(R); Q is a bond or a saturated C1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NRR, 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 and R are the same or different and each is hydrogen or a substituent R; or R and R 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; and R, R, R, R, R, R, R, and R are as defined in the claims.
M3 - Patent
M1 - WO2008075109
ER -