Claims for Patent: 9,006,430

Summary for Patent: 9,006,430

Title:	Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein
Abstract:	The invention provides a compound for use as a protein kinase B inhibitor, the compound being a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR; J-Jis N═C(R), (R)C═N, (R)N—C(O), (R)C—C(O), N═N or (R)C═C(R); E is a monocyclic carbocyclic or heterocyclic group of 5 or 6 ring members, the heterocyclic group containing up to 3 heteroatoms selected from O, N and S; Qis a bond or a saturated Chydrocarbon linker group, one of the carbon atoms in the linker group being optionally be replaced by an oxygen or nitrogen atom, or an adjacent pair of carbon atoms may be replaced by CONRor NRCO where Ris hydrogen or methyl, or Ris a Calkylene chain linked to R or a carbon atom of Qto form a cyclic moiety; and wherein the carbon atoms of the linker group Qmay optionally bear one or more substituents selected from fluorine and hydroxy; Qis a bond or a saturated hydrocarbon linker group containing from 1 to 3 carbon atoms, wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the linker group may optionally bear one or more substituents selected from fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the G group; and provided that when E is aryl or heteroaryl, then Qis other than a bond; G is hydrogen, NRR, OH or SH provided that when E is aryl or heteroaryl and Qis a bond, then G is hydrogen; Ris hydrogen or an aryl or heteroaryl group, with the proviso that when Ris hydrogen and G is NRR, then Q is a bond; and R, R, R, Rand Rare as defined in the claims.
Inventor(s):	Berdini Valerio, Boyle Robert George, Saxty Gordon, Walker David Winter, Woodhead Steven John, Wyatt Paul Graham, Donald Alastair, Caldwell John, Collins Ian, Da Fonseca Tatiana Faria
Assignee:
Application Number:	US14310475
Patent Claims:	2. A pharmaceutical composition according to wherein Xis NRand Xis ═O.3. A pharmaceutical composition according to wherein NRRis an amino group.4. A pharmaceutical composition according to wherein Ris selected from the group Rconsisting of halogen claim 1 , hydroxy claim 1 , trifluoromethyl claim 1 , cyano claim 1 , amino claim 1 , mono- or di-Calkylamino claim 1 , cyclopropylamino claim 1 , carbocyclic and heterocyclic groups having from 3 to 7 ring members; a group R-Rwherein Ris a bond claim 1 , O claim 1 , CO claim 1 , OC(O) claim 1 , NRC(O) claim 1 , OC(NR) claim 1 , C(O)O claim 1 , C(O)NR claim 1 , S claim 1 , SO claim 1 , SO claim 1 ,NR claim 1 , SONRor NRSO; and Ris selected from hydrogen claim 1 , carbocyclic and heterocyclic groups having from 3 to 7 ring members claim 1 , and a Chydrocarbyl group optionally substituted by one or more substituents selected from hydroxy claim 1 , oxo claim 1 , halogen claim 1 , cyano claim 1 , amino claim 1 , mono- or di-Calkylamino claim 1 , carbocyclic and heterocyclic groups having from 3 to 7 ring members and wherein one or more carbon atoms of the Chydrocarbyl group may optionally be replaced by O claim 1 , S claim 1 , SO claim 1 , SOor NR; provided that Ris not a bond when Ris hydrogen; and Ris selected from hydrogen and Calkyl.5. A pharmaceutical composition according to wherein the nitrogen atom of the piperidine ring is attached to the bicyclic group.6. A pharmaceutical composition according to wherein Qand Qare attached to different atoms in the group E.7. A pharmaceutical composition according to wherein Qand the bicyclic group are attached to the group E in a para relative orientation.8. A pharmaceutical composition according to wherein the compound of formula (I) is in the form of a salt or N-oxide.9. A pharmaceutical composition according to wherein Rand Rare hydrogen.10. A pharmaceutical composition according to wherein Qand Qare attached to different atoms in the group E.11. A pharmaceutical composition according to wherein Xis NRand Xis ═O.12. A pharmaceutical composition according to wherein E is piperidine substituted with 1 substituent Rselected from the group R.13. A pharmaceutical composition according to wherein Xis NRand Xis ═O.14. A pharmaceutical composition according to claim 12 , wherein the group Ris selected from the group R-R.15. A pharmaceutical composition according to in a form suitable for oral or parenteral administration.16. A pharmaceutical composition according to in a form suitable for i.v. administration.17. A pharmaceutical composition according to further comprising one or more pharmaceutically acceptable adjuvants claim 1 , excipients claim 1 , diluents claim 1 , fillers claim 1 , buffers claim 1 , stabilisers claim 1 , preservatives claim 1 , lubricants claim 1 , and/or therapeutic or prophylactic agents.18. A pharmaceutical composition according to in a form suitable for oral or parenteral administration.19. A pharmaceutical composition according to in a form suitable for i.v. administration.20. A pharmaceutical composition according to further comprising one or more pharmaceutically acceptable adjuvants claim 13 , excipients claim 13 , diluents claim 13 , fillers claim 13 , buffers claim 13 , stabilisers claim 13 , preservatives claim 13 , lubricants claim 13 , and/or therapeutic or prophylactic agents.