| ASTEX THERAPEUTICS LIMITED Patent applications |
| Patent application number | Title | Published |
|---|
| 20120101064 | IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES - The invention provides compounds of the formula (I): | 04-26-2012 |
| 20120041000 | IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY - The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 02-16-2012 |
| 20120035171 | BICYCLIC HETEROCYCLYL DERIVATIVES AS FGFR KINASE INHIBITORS FOR THERAPEUTIC USE - The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 02-09-2012 |
| 20120035153 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 02-09-2012 |
| 20120035152 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 02-09-2012 |
| 20110274616 | 4-(2,6-DICHLORO-BENZOYLAMINO)-1H-PYRAZOLE-3-CARBOXYLIC ACID PIPERIDIN-4-YLAMIDE ACID ADDITION SALTS AS KINASE INHIBITORS - The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. | 11-10-2011 |
| 20110269808 | COMPOSITIONS COMPRISING (S)-2-AMINO-1-(4-CHLOROPHENYL)-1-[4-(1H-PYRAZOL-4-YL)-PHENYL]-ETHANOL AS MODULATOR OF PROTEIN KINASES - The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)-1-[4-( | 11-03-2011 |
| 20110224203 | BENZIMIDAZOLE DERIVATIVES AND THEIR USE AS PROTEIN KINASE INHIBITORS - The invention provides compounds of the formula (I): | 09-15-2011 |
| 20110159111 | PHARMACEUTICAL COMBINATIONS - The invention provides combinations of an ancillary compound of the formula (0): and a compound of the formula (I′): Also provided are crystalline forms of the constituent compounds, methods for making them and their uses in treating cancers. | 06-30-2011 |
| 20110144080 | PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS - The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R | 06-16-2011 |
| 20110105501 | PHARMACEUTICAL COMBINATIONS - The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): | 05-05-2011 |
| 20110002879 | Combinations of Pyrazole Kinase Inhibitors - The invention provides a combination comprising a cytotoxic compound, a signalling inhibitor, an ancillary agent, or two or more further anti-cancer agents, and a compound having the formula (Ib): | 01-06-2011 |
| 20100331296 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 12-30-2010 |
| 20100286113 | BICYCLIC HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS - The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R | 11-11-2010 |
| 20100210617 | Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors - The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y | 08-19-2010 |
| 20100166699 | PHARMACEUTICAL COMBINATIONS COMPRISING PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS - The invention provides a combination comprising an ancillary compound (e.g. one, two or more ancillary compounds) and a compound of the formula (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R | 07-01-2010 |
| 20100160324 | PYRAZOLE DERIVATIVES AS THAT MODULATE THE ACTIVITY OF CDK, GSK AND AURORA KINASES - The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R | 06-24-2010 |
| 20100152184 | PHARMACEUTICAL COMPOUNDS - The invention provides a compound for use in medicine, the compound being a compound of the formula (VI | 06-17-2010 |
| 20100130464 | PHARMACEUTICAL COMPOUNDS - The invention provides compounds of the formula (I) having ROCK kinase and/or protein kinase p70S6K inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R1 and NR | 05-27-2010 |
| 20100120798 | SUBSTITUTED PIPERIDINES CONTAINING A HETEROARYLAMIDE OR HETEROARYLPHENYL MOIETY - The invention provides compounds of the formula (I) having PKA and PKB kinase inhibiting compounds of the formula (I): GP 1 J T 2 J N 4 R N H (I) or salts, solvates, tautomers or N-oxides thereof, wherein (1) GP is a group GP1: HET 2a a Q G (HNCO)f 7 (R)x N * (GP1) (2) GP is a group GP2: 10 (R)r O 2a a QG (CH2)w N V H N * (GP2) wherein HET is a monocyclic or bicyclic heterocyclic group containing up to 4 heteroatom ring members; the ring V is a monocyclic or bicyclic heteroaryl group of 5 to 10 ring members; and J1, J2, R4, R7, R10, Q2a, Ga, x, w and f are as defined in the claims | 05-13-2010 |
| 20100120761 | Bicyclic Heterocyclic Compounds as FGFR Inhibitors - The invention relates to new bicyclic heterocyclic derivative compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 05-13-2010 |
| 20100113551 | COMPOSITIONS COMPRISING (S)-2-AMINO-1-(4-CHLOROPHENYL)-1-[4-(1H-PYRAZOL-4-YL)-PHENYL]-ETHANOL AS MODULATOR OF PROTEIN KINASES - The invention provides a composition comprising (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, wherein the composition is either substantially free of (R) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol or the composition contains a mixture of the (S) and (R) enantiomers in which the (S) enantiomer predominates. Also provided are processes for the preparation of the (S) 2-amino-1-(4-chloro-phenyl)-1-[4-(1H-pyrazol-4-yl)-phenyl]-ethanol, novel process intermediates and methods for making the novel process intermediates. | 05-06-2010 |
| 20100093748 | SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY - The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I): | 04-15-2010 |
| 20100055094 | PHARMACEUTICAL COMBINATIONS OF 1-CYCLOPROPYL-3- [3-(5-M0RPHOOLIN-4-YL-METHYL-1H-BENZOIMIDAZOL-2-YL)- LH-1-PYRAZOL-4-YL]- UREA - The invention provides combinations of an ancillary compound and a compound which is a salt of 1-cyclopropyl-3-[3-(5-morpholin-4-ylmethyl-1H-benzoimidazol-2-yl)-1H-pyrazol-4-yl]-urea selected from the lactate and citrate salts and mixtures thereof. Also provided are crystalline forms of the salts, methods for making the salts and their uses in treating cancers. The invention further provides combinations of an ancillary compound and a compound of the formula (I) as defined in PCT/GB2004/002824 (WO 2005/002552) or a compound of the formula (I′) | 03-04-2010 |
| 20100022564 | PURINE AND DEAZAPURINE DERIVATIVES AS PHARMACEUTICAL COMPOUNDS - The invention provides a compound of the formula (I) or salts, solvates, tautomers or N-oxides thereof, wherein T is N or CR | 01-28-2010 |
| 20100021420 | COMBINATIONS OF PYRAZOLE DERIVATIVES FOR THE INHIBITION OF CDKS AND GSK'S - A combination comprising (a) a compound of formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is R | 01-28-2010 |
| 20100016340 | PHARMACEUTICAL COMPOUNDS - The invention provides compounds of the formula (I): | 01-21-2010 |
| 20100004243 | PHARMACEUTICAL COMPOUNDS - The invention provides a cyclin dependent kinase (e.g. cdk-4 kinase) inhibitor of the formula (I) or a salt, tautomer, solvate or N-oxide thereof; wherein R | 01-07-2010 |
| 20100004232 | Pharmaceutical Compounds - The use of a compound for the manufacture of a medicament for the prophylaxis or treatment of: A. a disease state or condition mediated by a kinase which is BCR-abl, VEGFR, PDGFR, EGFR, Flt3, JAK (e.g. JAK2 or JAK3), C-abl, PDK1, Chk (e.g. Cbk1 or Chk2), FGFR (e.g. FGFR3), Ret, Eph (e.g. EphB2 or EphB4), or Src (e.g. cSrc); or B. a cancer in which the cancer cells thereof contain a drug resistant kinase mutation which is: (a) a threonine gatekeeper mutation; or (b) a drug-resistant gatekeeper mutation; or (c) an imatinib resistant mutation; or (d) a nilotinib resistant mutation; or (e) a dasatinib resistant mutation; or (f) a T670I mutation in KIT; or (g) a T674I mutation in PDGFR; or (h) T790M mutation in EGFR; or (i) a T315I mutation in abl; or C. a cancer which expresses a mutated molecular target which is a mutated form of BCRabl, c-kit, PDGF, EGF receptor or ErbB2; or D. a disease mediated by a kinase containing a mutation in a region of the protein that binds to or interacts with other cancer agents but does not bind to or interact with the compounds of formula (I) or (I′), for example a mutated kinase selected from c-abl, c-kit, PDGFR including PDGFR-beta and PDGFR-alpha, and ErbB family members such as EGFR (ErbB1), HER2 (ErbB2), ErbB3, and ErbB4, members of the Ephrin receptor family including EphA1, EphA2, EphA3, EphA4, EphA5, EphA8, EphA10, EphB1, EphB2, EphB3, EphB5, EphB6, c-Src and kinases of the JAK family such as TYK2; wherein the compound is a compound of the formula (I or I′): or a salt, solvate, tautomer or N-oxide thereof wherein R | 01-07-2010 |
| 20090318500 | 4-(2, 6-Dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide for the Treatment of Cancer - The invention provides the compound of formula (I) 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide in a substantially crystalline form, therapeutic uses thereof and pharmaceutical compositions containing the crystalline compound. The invention also provides novel pharmaceutical formulations containing 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid (1-methanesulphonyl-piperidin-4-yl)-amide and novel processes for preparing the compound. | 12-24-2009 |
| 20090318430 | MEDICAL USE OF CYCLIN DEPENDENT KINASES INHIBITORS - The invention provides the use of a compound for the manufacture of a medicament for the treatment of pain, wherein the compound is a compound of the formula (0): | 12-24-2009 |
| 20090263398 | PHARMACEUTICAL COMBINATIONS - The invention provides a combination comprising an ancillary compound and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein X is a group R | 10-22-2009 |
| 20090253718 | Pharmaceutical Compounds - The invention provides a compound having the formula (I): | 10-08-2009 |
| 20090247538 | Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors - 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 | 10-01-2009 |
| 20090215772 | Hydroxybenzamide derivatives and their use as inhibitors of HSP90 - The invention provides compounds of the formula (I): | 08-27-2009 |
| 20090176850 | Novel 2-Amino-Imidazole-4-One Compounds And Their Use In The Manufacture Of A Medicament To Be Used In The Treatment Of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration And Dementia - This invention relates to novel compounds having the structural formula I below and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 07-09-2009 |
| 20090142337 | Pharmaceutical Combinations of Diazole Derivatives for Cancer Treatment - The invention provides a combination comprising (or consisting essentially of) an ancillary compound and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein: R | 06-04-2009 |
| 20090099213 | Ortho-Condensed Pyridine and Pyrimidine Derivatives (e.g., Purines) as Protein Kinases Inhibitors - 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 | 04-16-2009 |
| 20090036435 | Pharmaceutical Compounds - The invention provides a combination of an ancillary agent and a compound having the formula (0): or salts or tautomers or N-oxides or solvates thereof; wherein the ancillary agent is selected from: a monoclonal antibody, an alkylating agent, an anticancer agent, a further CDK inhibitor and a hormone, hormone agonist, hormone antagonist or hormone modulating agent; X is a group R | 02-05-2009 |
| 20090023762 | Substituted 2-Aminopyrimidine-4-Ones, Their Pharmaceutical Compositions And Their Use In The Treatment And/Or Prevention Of Ab-Related Pathologies - This invention relates to novel compounds having the structural formula (I) below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel en compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 01-22-2009 |
| 20090012124 | 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide acid addition salts as kinase inhibitors - The invention provides an acid addition salt of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and crystals thereof, the salt being formed with an acid selected from methanesulphonic acid and acetic acid and mixtures thereof. Also provided are the novel uses of salts of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide, processes for the preparation of 4-(2,6-dichloro-benzoylamino)-1H-pyrazole-3-carboxylic acid piperidin-4-ylamide and its salts and novel chemical intermediates. | 01-08-2009 |
| 20080318985 | Novel 2-Aminopyrimidinone Or 2-Aminopyridinone Derivatives and Their Use -
This invention relates to novel compounds having the structural formula Ia or Ib below: (Ia); (Ib) and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 12-25-2008 |
| 20080312223 | Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases - The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR | 12-18-2008 |
| 20080306069 | Pyrazole Derivatives for the Inhibition of CDK'S and GSK'S - The invention provides compounds of the formula (I), or salts, tautomers, N-oxides or solvates thereof wherein: R1 is selected from: (a) 2,6-dichlorophenyl; (b) 2,6-difluorophenyl; (c) a 2,3,6-trisubstituted phenyl group wherein the substituents for the phenyl group are selected from fluorine, chlorine, methyl and methoxy; (d) a group RO; (e) a group R a; (f) a group RIb; (g) a group RIc; (h) a group RId; and 0) 2,6-difluorophenylamino; wherein R) 0υ, r R>llaa, T Rj HbD, T R) HcC, r R>Iidα, r R>>2zaa, r R>22bD and RJ are as defined in the claims. The compounds have activity as inhibitors of cdk kinase (such as cdk1 or cdk2) and glycogen synthase kinase-3 activity. | 12-11-2008 |
| 20080306054 | Pharmaceutical Compounds - The invention provides a compound for use as an inhibitor of Hsp90, the compound having the formula (I): | 12-11-2008 |
| 20080293718 | Novel 2-Amino-Imidazole-4-One Compounds and Their Use in the Manufacture of a Medicament to Be Used in the Treatment of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration and Dementia - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia. | 11-27-2008 |
| 20080287462 | NEW COMPOUNDS 834 - This invention relates to novel compounds having the structural formula I below: | 11-20-2008 |
| 20080287460 | NEW COMPOUNDS 835 - This invention relates to novel compounds having the structural formula I below: | 11-20-2008 |
| 20080275029 | Compounds for Treating Protein-Kinase Mediated Disorders - The invention provides a compound of the formula (I) or a salt, solvate, tautomer or N-oxide thereof for use in the treatment or prophylaxis of a disease state or condition mediated by protein kinase A and/or protein kinase B; | 11-06-2008 |
