JP2003522163A5 - - Google Patents
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- JP2003522163A5 JP2003522163A5 JP2001557854A JP2001557854A JP2003522163A5 JP 2003522163 A5 JP2003522163 A5 JP 2003522163A5 JP 2001557854 A JP2001557854 A JP 2001557854A JP 2001557854 A JP2001557854 A JP 2001557854A JP 2003522163 A5 JP2003522163 A5 JP 2003522163A5
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- JP
- Japan
- Prior art keywords
- group
- aliphatic
- compound
- cancer
- kinase
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000001931 aliphatic group Chemical group 0.000 description 28
- 150000001875 compounds Chemical class 0.000 description 28
- 125000003118 aryl group Chemical group 0.000 description 13
- 229910052739 hydrogen Inorganic materials 0.000 description 12
- 239000001257 hydrogen Substances 0.000 description 12
- 150000001721 carbon Chemical group 0.000 description 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 11
- 125000001072 heteroaryl group Chemical group 0.000 description 10
- -1 CONR 2 Inorganic materials 0.000 description 9
- 239000000203 mixture Substances 0.000 description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 8
- 125000001424 substituent group Chemical group 0.000 description 8
- 125000000217 alkyl group Chemical group 0.000 description 7
- 201000010099 disease Diseases 0.000 description 7
- 125000000623 heterocyclic group Chemical group 0.000 description 7
- 206010028980 Neoplasm Diseases 0.000 description 6
- 102000001253 Protein Kinase Human genes 0.000 description 6
- 108060006633 protein kinase Proteins 0.000 description 6
- 201000011510 cancer Diseases 0.000 description 5
- 239000003814 drug Substances 0.000 description 5
- 229910052736 halogen Inorganic materials 0.000 description 5
- 150000002367 halogens Chemical class 0.000 description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 5
- 102000007665 Extracellular Signal-Regulated MAP Kinases Human genes 0.000 description 4
- 108010007457 Extracellular Signal-Regulated MAP Kinases Proteins 0.000 description 4
- 108091007911 GSKs Proteins 0.000 description 4
- 102000004103 Glycogen Synthase Kinases Human genes 0.000 description 4
- 102000015617 Janus Kinases Human genes 0.000 description 4
- 108010024121 Janus Kinases Proteins 0.000 description 4
- 108091008611 Protein Kinase B Proteins 0.000 description 4
- 102100033810 RAC-alpha serine/threonine-protein kinase Human genes 0.000 description 4
- 125000004423 acyloxy group Chemical group 0.000 description 4
- 125000006615 aromatic heterocyclic group Chemical group 0.000 description 4
- 125000003710 aryl alkyl group Chemical group 0.000 description 4
- 229910052799 carbon Inorganic materials 0.000 description 4
- 208000035475 disorder Diseases 0.000 description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 description 4
- 125000004415 heterocyclylalkyl group Chemical group 0.000 description 4
- 229910052757 nitrogen Inorganic materials 0.000 description 4
- 150000003839 salts Chemical class 0.000 description 4
- 206010003210 Arteriosclerosis Diseases 0.000 description 3
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 3
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- 206010019280 Heart failures Diseases 0.000 description 3
- 108010055717 JNK Mitogen-Activated Protein Kinases Proteins 0.000 description 3
- 102100037808 Mitogen-activated protein kinase 8 Human genes 0.000 description 3
- 108010053099 Vascular Endothelial Growth Factor Receptor-2 Proteins 0.000 description 3
- 102100033177 Vascular endothelial growth factor receptor 2 Human genes 0.000 description 3
- 208000011775 arteriosclerosis disease Diseases 0.000 description 3
- 150000002431 hydrogen Chemical class 0.000 description 3
- 238000000034 method Methods 0.000 description 3
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- 229940124597 therapeutic agent Drugs 0.000 description 3
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- 201000001320 Atherosclerosis Diseases 0.000 description 2
- 102000003989 Aurora kinases Human genes 0.000 description 2
- 108090000433 Aurora kinases Proteins 0.000 description 2
- 208000020084 Bone disease Diseases 0.000 description 2
- 208000006029 Cardiomegaly Diseases 0.000 description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 2
- 208000035473 Communicable disease Diseases 0.000 description 2
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- 208000029462 Immunodeficiency disease Diseases 0.000 description 2
- 206010061218 Inflammation Diseases 0.000 description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 2
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- 108090000190 Thrombin Proteins 0.000 description 2
- 125000001118 alkylidene group Chemical group 0.000 description 2
- 230000000172 allergic effect Effects 0.000 description 2
- 208000010668 atopic eczema Diseases 0.000 description 2
- 210000004027 cell Anatomy 0.000 description 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 230000001066 destructive effect Effects 0.000 description 2
- 206010012601 diabetes mellitus Diseases 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 210000004907 gland Anatomy 0.000 description 2
- 230000004054 inflammatory process Effects 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 230000002062 proliferating effect Effects 0.000 description 2
- 210000000664 rectum Anatomy 0.000 description 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 2
- 229960004072 thrombin Drugs 0.000 description 2
- 230000003612 virological effect Effects 0.000 description 2
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 description 1
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 description 1
- 208000023275 Autoimmune disease Diseases 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 239000004215 Carbon black (E152) Substances 0.000 description 1
- 206010007572 Cardiac hypertrophy Diseases 0.000 description 1
- 206010008342 Cervix carcinoma Diseases 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 description 1
- 206010019842 Hepatomegaly Diseases 0.000 description 1
- 208000017604 Hodgkin disease Diseases 0.000 description 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 description 1
- 206010020880 Hypertrophy Diseases 0.000 description 1
- 208000008839 Kidney Neoplasms Diseases 0.000 description 1
- 206010023825 Laryngeal cancer Diseases 0.000 description 1
- 208000018501 Lymphatic disease Diseases 0.000 description 1
- 206010029260 Neuroblastoma Diseases 0.000 description 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 208000009565 Pharyngeal Neoplasms Diseases 0.000 description 1
- 206010060862 Prostate cancer Diseases 0.000 description 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 1
- 206010038389 Renal cancer Diseases 0.000 description 1
- 206010039491 Sarcoma Diseases 0.000 description 1
- 201000010208 Seminoma Diseases 0.000 description 1
- 208000005718 Stomach Neoplasms Diseases 0.000 description 1
- 208000006011 Stroke Diseases 0.000 description 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 description 1
- 230000006044 T cell activation Effects 0.000 description 1
- 208000024313 Testicular Neoplasms Diseases 0.000 description 1
- 206010057644 Testis cancer Diseases 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 208000008385 Urogenital Neoplasms Diseases 0.000 description 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 description 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 description 1
- 125000005160 aryl oxy alkyl group Chemical group 0.000 description 1
- 125000004429 atom Chemical group 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 239000002876 beta blocker Substances 0.000 description 1
- 229940097320 beta blocking agent Drugs 0.000 description 1
- 201000009036 biliary tract cancer Diseases 0.000 description 1
- 208000020790 biliary tract neoplasm Diseases 0.000 description 1
- 239000012472 biological sample Substances 0.000 description 1
- 201000004571 bone carcinoma Diseases 0.000 description 1
- 208000015322 bone marrow disease Diseases 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 208000025188 carcinoma of pharynx Diseases 0.000 description 1
- 201000007455 central nervous system cancer Diseases 0.000 description 1
- 208000015114 central nervous system disease Diseases 0.000 description 1
- 201000010881 cervical cancer Diseases 0.000 description 1
- 239000000544 cholinesterase inhibitor Substances 0.000 description 1
- 210000001072 colon Anatomy 0.000 description 1
- 239000002934 diuretic Substances 0.000 description 1
- 229940030606 diuretics Drugs 0.000 description 1
- 230000003511 endothelial effect Effects 0.000 description 1
- 201000004101 esophageal cancer Diseases 0.000 description 1
- 208000021045 exocrine pancreatic carcinoma Diseases 0.000 description 1
- 230000003325 follicular Effects 0.000 description 1
- 206010017758 gastric cancer Diseases 0.000 description 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 description 1
- 125000005114 heteroarylalkoxy group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 description 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 description 1
- 208000026278 immune system disease Diseases 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 201000010982 kidney cancer Diseases 0.000 description 1
- 208000003849 large cell carcinoma Diseases 0.000 description 1
- 210000002429 large intestine Anatomy 0.000 description 1
- 206010023841 laryngeal neoplasm Diseases 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 210000004185 liver Anatomy 0.000 description 1
- 201000007270 liver cancer Diseases 0.000 description 1
- 208000019423 liver disease Diseases 0.000 description 1
- 208000014018 liver neoplasm Diseases 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 201000005249 lung adenocarcinoma Diseases 0.000 description 1
- 208000018555 lymphatic system disease Diseases 0.000 description 1
- 201000001441 melanoma Diseases 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 150000002823 nitrates Chemical class 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 208000008443 pancreatic carcinoma Diseases 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 210000003800 pharynx Anatomy 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 239000000523 sample Substances 0.000 description 1
- 229920006395 saturated elastomer Polymers 0.000 description 1
- 208000000649 small cell carcinoma Diseases 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- 206010041823 squamous cell carcinoma Diseases 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 125000003107 substituted aryl group Chemical group 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 239000011593 sulfur Substances 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- 201000003120 testicular cancer Diseases 0.000 description 1
- 210000001685 thyroid gland Anatomy 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
- 208000037964 urogenital cancer Diseases 0.000 description 1
- 230000002792 vascular Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US18050600P | 2000-02-05 | 2000-02-05 | |
| US60/180,506 | 2000-02-05 | ||
| US19195600P | 2000-03-24 | 2000-03-24 | |
| US60/191,956 | 2000-03-24 | ||
| US24293500P | 2000-10-24 | 2000-10-24 | |
| US60/242,935 | 2000-10-24 | ||
| PCT/US2001/003911 WO2001057022A2 (en) | 2000-02-05 | 2001-02-05 | Pyrazole compositions useful as inhibitors of erk |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2003522163A JP2003522163A (ja) | 2003-07-22 |
| JP2003522163A5 true JP2003522163A5 (https=) | 2008-03-21 |
| JP4783532B2 JP4783532B2 (ja) | 2011-09-28 |
Family
ID=27391289
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2001557854A Expired - Fee Related JP4783532B2 (ja) | 2000-02-05 | 2001-02-05 | Ｅｒｋのインヒビターとして有用なピラゾール組成物 |
Country Status (19)
| Country | Link |
|---|---|
| US (4) | US6528509B1 (https=) |
| EP (1) | EP1200422A2 (https=) |
| JP (1) | JP4783532B2 (https=) |
| KR (1) | KR20010111298A (https=) |
| CN (1) | CN1362953A (https=) |
| AU (1) | AU782775B2 (https=) |
| BG (1) | BG106054A (https=) |
| BR (1) | BR0104424A (https=) |
| CA (1) | CA2369504C (https=) |
| CZ (1) | CZ20013540A3 (https=) |
| HK (1) | HK1046276A1 (https=) |
| HU (1) | HUP0202332A2 (https=) |
| IL (1) | IL145757A (https=) |
| LT (1) | LT4981B (https=) |
| NO (1) | NO322745B1 (https=) |
| NZ (1) | NZ514583A (https=) |
| SK (1) | SK14082001A3 (https=) |
| TR (1) | TR200103787T1 (https=) |
| WO (1) | WO2001057022A2 (https=) |
Families Citing this family (120)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6207665B1 (en) * | 1997-06-12 | 2001-03-27 | Schering Aktiengesellschaft | Piperazine derivatives and their use as anti-inflammatory agents |
| HUP0202332A2 (en) * | 2000-02-05 | 2002-10-28 | Vertex Pharma | Pyrazole compositions useful as inhibitors of erk |
| US6436915B1 (en) | 2000-04-07 | 2002-08-20 | Kinetek Pharmaceuticals, Inc. | Pyrazole compounds |
| US7074794B2 (en) * | 2000-08-10 | 2006-07-11 | Mitsubishi Pharma Corporation | Proline derivatives and the use thereof as drugs |
| US7473691B2 (en) * | 2000-09-15 | 2009-01-06 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| US6660731B2 (en) * | 2000-09-15 | 2003-12-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| ATE335737T1 (de) | 2000-09-15 | 2006-09-15 | Vertex Pharma | Isoxazole und ihre verwendung als erk-inhibitoren |
| EP1317450B1 (en) | 2000-09-15 | 2006-11-22 | Vertex Pharmaceuticals Incorporated | Pyrazole compounds useful as protein kinase inhibitors |
| AU2001287898A1 (en) | 2000-09-22 | 2002-04-02 | Stephen Garland | Pyrazolopyridines and pyrazolopyridazines as antidiabetics |
| NZ526472A (en) * | 2000-12-21 | 2004-04-30 | Vertex Pharma | Pyrazole compounds useful as protein kinase inhibitors |
| CA2437248A1 (en) * | 2001-02-02 | 2002-08-15 | Takeda Chemical Industries, Ltd. | Jnk inhibitor |
| ATE491701T1 (de) * | 2001-08-03 | 2011-01-15 | Vertex Pharma | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
| DE60226154T2 (de) * | 2001-08-03 | 2009-05-20 | Vertex Pharmaceuticals Inc., Cambridge | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
| RU2332996C2 (ru) | 2001-11-30 | 2008-09-10 | КьюЭлТи Инк. | Производные гидразонпиразола и их применение в качестве лекарственного средства |
| AU2003235798A1 (en) * | 2002-01-10 | 2003-07-24 | F. Hoffmann-La Roche Ag | Use of a gsk-3beta inhibitor in the manufacture of a medicament for increasing bone formation |
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| EP1472245A2 (en) * | 2002-02-06 | 2004-11-03 | Vertex Pharmaceuticals Incorporated | Heteroaryl compounds useful as inhibitors of gsk-3 |
| AU2003218215A1 (en) * | 2002-03-15 | 2003-09-29 | Vertex Pharmaceuticals, Inc. | Azolylaminoazines as inhibitors of protein kinases |
| AU2003237121A1 (en) * | 2002-04-26 | 2003-11-10 | Vertex Pharmaceuticals Incorporated | Pyrrole derivatives as inhibitors of erk2 and uses thereof |
| MY141867A (en) * | 2002-06-20 | 2010-07-16 | Vertex Pharma | Substituted pyrimidines useful as protein kinase inhibitors |
| US7585866B2 (en) * | 2002-07-31 | 2009-09-08 | Critical Outcome Technologies, Inc. | Protein tyrosine kinase inhibitors |
| DK1532145T3 (da) | 2002-08-02 | 2007-01-15 | Vertex Pharma | Pyrazolpræparater der er anvendelige som inhibitorer af GSK-3 |
| EP1388541A1 (en) * | 2002-08-09 | 2004-02-11 | Centre National De La Recherche Scientifique (Cnrs) | Pyrrolopyrazines as kinase inhibitors |
| AU2003273675A1 (en) * | 2002-10-09 | 2004-05-04 | Wayne R. Danter | Protein tyrosine kinase inhibitors |
| CA2502685A1 (en) * | 2002-10-23 | 2004-05-06 | Exelixis, Inc. | Cdkl1 as modifier of branching morphogenesis and methods of use |
| CN1747949A (zh) * | 2002-12-20 | 2006-03-15 | 法马西亚公司 | 无环吡唑化合物 |
| US20050019366A1 (en) * | 2002-12-31 | 2005-01-27 | Zeldis Jerome B. | Drug-coated stents and methods of use therefor |
| WO2004072029A2 (en) * | 2003-02-06 | 2004-08-26 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridazines useful as inhibitors of protein kinases |
| EP1606019A1 (en) * | 2003-03-07 | 2005-12-21 | The University Court of The University of Aberdeen | Cannabinoid receptor inverse agonists and neutral antagonists as therapeutic agents for the treatment of bone disorders |
| TWI372050B (en) | 2003-07-03 | 2012-09-11 | Astex Therapeutics Ltd | (morpholin-4-ylmethyl-1h-benzimidazol-2-yl)-1h-pyrazoles |
| PL2256106T3 (pl) | 2003-07-22 | 2015-08-31 | Astex Therapeutics Ltd | Związki 3,4-pochodne 1h-pirazolu i ich zastosowanie jako kinazy zależne od cyklin (cdk) i modulatory kinazy syntazy glikogenu-3 (gsk-3) |
| BRPI0413018B8 (pt) | 2003-07-30 | 2021-05-25 | Rigel Pharmaceuticals Inc | composto, e, uso de um composto |
| CA2536470A1 (en) | 2003-08-15 | 2005-02-24 | Vertex Pharmaceuticals Incorporated | Pyrrole compositions useful as inhibitors of c-met |
| DE10354060A1 (de) * | 2003-11-19 | 2005-06-02 | Merck Patent Gmbh | Pyrrolderivate |
| AU2004297235A1 (en) * | 2003-12-04 | 2005-06-23 | Vertex Pharmaceuticals Incorporated | Quinoxalines useful as inhibitors of protein kinases |
| WO2005061519A1 (en) | 2003-12-19 | 2005-07-07 | Takeda San Diego, Inc. | Kinase inhibitors |
| US7488817B2 (en) * | 2004-02-02 | 2009-02-10 | The Trustees Of The University Of Pennsylvania | Metal complex protein kinase inhibitors |
| EP1730134A1 (en) | 2004-03-26 | 2006-12-13 | Vertex Pharmaceuticals Incorporated | Pyridine inhibitors of erk2 and uses thereof |
| WO2005105788A1 (en) * | 2004-04-23 | 2005-11-10 | Takeda San Diego, Inc. | Indole derivatives and use thereof as kinase inhibitors |
| EP1778669A2 (en) | 2004-08-18 | 2007-05-02 | Takeda San Diego, Inc. | Kinase inhibitors |
| FR2876582B1 (fr) * | 2004-10-15 | 2007-01-05 | Centre Nat Rech Scient Cnrse | Utilisation de derives de pyrrolo-pyrazines pour la fabrication de medicaments pour le traitement de la mucoviscidose et de maladies liees a un defaut d'adressage des proteines dans les cellules |
| ATE479687T1 (de) | 2004-10-15 | 2010-09-15 | Takeda Pharmaceutical | Kinaseinhibitoren |
| EP1814883A1 (en) * | 2004-11-22 | 2007-08-08 | Vertex Pharmaceuticals Incorporated | Bicyclic inhibitors or rho kinase |
| EP1833819A1 (en) | 2004-12-30 | 2007-09-19 | Astex Therapeutics Limited | Pyrazole compounds that modulate the activity of cdk, gsk and aurora kinases |
| US20100160324A1 (en) * | 2004-12-30 | 2010-06-24 | Astex Therapeutics Limited | Pyrazole derivatives as that modulate the activity of cdk, gsk and aurora kinases |
| WO2006070202A1 (en) * | 2004-12-30 | 2006-07-06 | Astex Therapeutics Limited | Pyrazole derivatives having kinase modulating activity |
| RU2425677C2 (ru) * | 2005-01-21 | 2011-08-10 | Астекс Терапьютикс Лимитед | Соединения, предназначенные для использования в фармацевтике |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| TW200639163A (en) * | 2005-02-04 | 2006-11-16 | Genentech Inc | RAF inhibitor compounds and methods |
| US20070203161A1 (en) * | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| WO2006133426A2 (en) | 2005-06-08 | 2006-12-14 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| JP2007000061A (ja) * | 2005-06-23 | 2007-01-11 | Sumitomo Chemical Co Ltd | 昆虫由来のｃ−Ｊｕｎアミノ末端リン酸化酵素活性に関わる有害生物の生理状態に変化を与える薬剤 |
| AU2006279376B2 (en) * | 2005-08-18 | 2011-04-14 | Vertex Pharmaceuticals Incoporated | Pyrazine kinase inhibitors |
| US8119655B2 (en) | 2005-10-07 | 2012-02-21 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| EP1954277B1 (en) * | 2005-11-03 | 2017-01-18 | Vertex Pharmaceuticals Incorporated | Aminopyrimidines useful as kinase inhibitors |
| HRP20110892T1 (hr) * | 2005-12-13 | 2011-12-31 | Schering Corporation | Policiklični derivati indazola koji su inhibitori erk |
| US8546404B2 (en) | 2005-12-13 | 2013-10-01 | Merck Sharp & Dohme | Compounds that are ERK inhibitors |
| EP1968579A1 (en) | 2005-12-30 | 2008-09-17 | Astex Therapeutics Limited | Pharmaceutical compounds |
| MX2008010635A (es) | 2006-02-16 | 2008-10-28 | Schering Corp | Derivados de pirrolidina como inhibidores de cinasa regulada por señales extracelulares. |
| CA2642229C (en) | 2006-02-24 | 2015-05-12 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| TW200800203A (en) | 2006-03-08 | 2008-01-01 | Astrazeneca Ab | New use |
| EP2049119A2 (en) | 2006-06-29 | 2009-04-22 | Astex Therapeutics Limited | Pharmaceutical combinations of 1-cyclopropyl-3-[3-(5-morphoolin-4-ylmethyl-1h-benzoimidazol-2-yl)-1h-1-pyrazol-4-yl]-urea |
| SG158147A1 (en) | 2006-10-09 | 2010-01-29 | Takeda Pharmaceutical | Kinase inhibitors |
| EP2223925A1 (en) * | 2006-10-09 | 2010-09-01 | Takeda Pharmaceutical Company Limited | Kinase inhibitors |
| MX2009004807A (es) * | 2006-11-02 | 2009-06-15 | Vertex Pharma | Aminopiridinas y aminopirimidinas utiles como inhibidores de proteina cinasa. |
| NZ577768A (en) * | 2006-12-19 | 2012-01-12 | Vertex Pharma | Aminopyrimidines useful as inhibitors of protein kinases |
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| FR2707295A1 (fr) * | 1993-06-07 | 1995-01-13 | Rhone Poulenc Agrochimie | Fongicides pyrazoles substitués en position 3 par un hétérocycle. |
| JP3734180B2 (ja) * | 1994-12-28 | 2006-01-11 | エーザイ株式会社 | 新規ピラゾール誘導体 |
| GB9608435D0 (en) * | 1996-04-24 | 1996-06-26 | Celltech Therapeutics Ltd | Chemical compounds |
| US6514977B1 (en) * | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| EP0983260A2 (en) * | 1997-05-22 | 2000-03-08 | G.D. Searle & Co. | 3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS |
| AU7726898A (en) * | 1997-05-22 | 1998-12-11 | G.D. Searle & Co. | Pyrazole derivatives as p38 kinase inhibitors |
| HUP0202332A2 (en) * | 2000-02-05 | 2002-10-28 | Vertex Pharma | Pyrazole compositions useful as inhibitors of erk |
-
2001
- 2001-02-05 HU HU0202332A patent/HUP0202332A2/hu unknown
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- 2001-02-05 EP EP01908911A patent/EP1200422A2/en not_active Withdrawn
- 2001-02-05 HK HK02107512.2A patent/HK1046276A1/zh unknown
- 2001-02-05 CN CN01800374A patent/CN1362953A/zh active Pending
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- 2001-02-05 WO PCT/US2001/003911 patent/WO2001057022A2/en not_active Ceased
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