Claims for Patent: 8,809,336

Summary for Patent: 8,809,336

Title:	Ortho-condensed pyridine and pyrimidine derivatives (e.g., purines) as protein kinases inhibitors
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 Ror 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 Qis 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:	US14017814
Patent Claims:	2. A method according to wherein NRRis an amino group or a methylamino group.3. A method according to wherein NRRis an amino group.4. A method 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 , NR(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 method according to wherein the nitrogen atom of the piperidine ring is attached to the bicyclic group.6. A method according to wherein Qand Qare attached to different atoms in the group E.7. A method according to wherein Qand the bicyclic group are attached to the group E in a meta or para relative orientation.8. A method according to wherein the compound of formula (I) is in the form of a salt or N-oxide.9. A method according to wherein the disease or condition is selected from a carcinoma of the bladder or breast; colorectal carcinomas; kidney claim 1 , epidermal and liver carcinomas; adenocarcinoma; small cell lung cancer; non-small cell lung carcinomas; carcinomas of the oesophagus claim 1 , gall bladder claim 1 , ovary claim 1 , pancreas claim 1 , stomach claim 1 , cervix claim 1 , endometrium claim 1 , thyroid claim 1 , prostate claim 1 , or skin; leukaemia; acute lymphocytic leukaemia; B-cell lymphoma; T-cell lymphoma; Hodgkin's lymphoma; non-Hodgkin's lymphoma; hairy cell lymphoma; Burkett's lymphoma; acute and chronic myelogenous leukaemias; myelodysplastic syndrome; promyelocytic leukaemia; thyroid follicular cancer; fibrosarcoma; habdomyosarcoma; astrocytoma; neuroblastoma; glioma; schwannoma; melanoma; seminoma; teratocarcinoma; osteosarcoma; xenoderoma pigmentosum; keratoctanthoma; thyroid follicular cancer; and Kaposi's sarcoma.10. A method according to wherein the disease or condition is selected from breast cancer claim 9 , ovarian cancer claim 9 , prostate cancer claim 9 , endometrial cancer and glioma.11. A method according to wherein the disease or condition is selected from breast cancer claim 9 , ovarian cancer claim 9 , colon cancer claim 9 , prostate cancer claim 9 , oesophageal cancer claim 9 , squamous cancer and non-small cell lung carcinomas.12. A method according to wherein the disease or condition is selected from tumours with deletions or inactivating mutations in PTEN or loss of PTEN expression.