JP2009513703A5 - - Google Patents
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- JP2009513703A5 JP2009513703A5 JP2008538935A JP2008538935A JP2009513703A5 JP 2009513703 A5 JP2009513703 A5 JP 2009513703A5 JP 2008538935 A JP2008538935 A JP 2008538935A JP 2008538935 A JP2008538935 A JP 2008538935A JP 2009513703 A5 JP2009513703 A5 JP 2009513703A5
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- JP
- Japan
- Prior art keywords
- substituted
- cancer
- group
- alkyl
- unsubstituted
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 25
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 24
- 208000035475 disorder Diseases 0.000 claims 23
- 239000008194 pharmaceutical composition Substances 0.000 claims 21
- 125000000217 alkyl group Chemical group 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 16
- 150000001204 N-oxides Chemical class 0.000 claims 13
- 239000012453 solvate Substances 0.000 claims 13
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 9
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 229910052739 hydrogen Inorganic materials 0.000 claims 8
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 7
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 208000032839 leukemia Diseases 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 4
- 125000004103 aminoalkyl group Chemical group 0.000 claims 4
- 210000001185 bone marrow Anatomy 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 4
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 3
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 2
- 206010005003 Bladder cancer Diseases 0.000 claims 2
- 206010005949 Bone cancer Diseases 0.000 claims 2
- 208000018084 Bone neoplasm Diseases 0.000 claims 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims 2
- 206010017993 Gastrointestinal neoplasms Diseases 0.000 claims 2
- 206010061218 Inflammation Diseases 0.000 claims 2
- 102000042838 JAK family Human genes 0.000 claims 2
- 108091082332 JAK family Proteins 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010025323 Lymphomas Diseases 0.000 claims 2
- 208000002231 Muscle Neoplasms Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 108091000080 Phosphotransferase Proteins 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 208000029742 colonic neoplasm Diseases 0.000 claims 2
- -1 cyano, nitro, amino Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 208000030533 eye disease Diseases 0.000 claims 2
- 230000002496 gastric effect Effects 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 230000004054 inflammatory process Effects 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 201000002077 muscle cancer Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 102000020233 phosphotransferase Human genes 0.000 claims 2
- 208000037244 polycythemia vera Diseases 0.000 claims 2
- 108060006633 protein kinase Proteins 0.000 claims 2
- 208000012201 sexual and gender identity disease Diseases 0.000 claims 2
- 208000015891 sexual disease Diseases 0.000 claims 2
- 201000000849 skin cancer Diseases 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 201000005112 urinary bladder cancer Diseases 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 125000002252 acyl group Chemical group 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 229940124599 anti-inflammatory drug Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 claims 1
- 229940044683 chemotherapy drug Drugs 0.000 claims 1
- 239000013078 crystal Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 239000002955 immunomodulating agent Substances 0.000 claims 1
- 229940121354 immunomodulator Drugs 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000005254 oxyacyl group Chemical group 0.000 claims 1
- 208000003476 primary myelofibrosis Diseases 0.000 claims 1
- 201000007914 proliferative diabetic retinopathy Diseases 0.000 claims 1
- 239000003909 protein kinase inhibitor Substances 0.000 claims 1
- 230000012743 protein tagging Effects 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical class [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical group 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US73262905P | 2005-11-01 | 2005-11-01 | |
| US60/732,629 | 2005-11-01 | ||
| US83800306P | 2006-08-15 | 2006-08-15 | |
| US60/838,003 | 2006-08-15 | ||
| PCT/US2006/042044 WO2007053452A1 (en) | 2005-11-01 | 2006-10-26 | Bi-aryl meta-pyrimidine inhibitors of kinases |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012257150A Division JP5814903B2 (ja) | 2005-11-01 | 2012-11-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009513703A JP2009513703A (ja) | 2009-04-02 |
| JP2009513703A5 true JP2009513703A5 (enExample) | 2012-01-05 |
| JP5191391B2 JP5191391B2 (ja) | 2013-05-08 |
Family
ID=38006192
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2008538935A Active JP5191391B2 (ja) | 2005-11-01 | 2006-10-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
| JP2012257150A Active JP5814903B2 (ja) | 2005-11-01 | 2012-11-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012257150A Active JP5814903B2 (ja) | 2005-11-01 | 2012-11-26 | キナーゼのビ−アリールメタ−ピリミジン阻害剤 |
Country Status (25)
| Country | Link |
|---|---|
| US (3) | US7528143B2 (enExample) |
| EP (1) | EP1951684B1 (enExample) |
| JP (2) | JP5191391B2 (enExample) |
| KR (2) | KR101494468B1 (enExample) |
| CN (1) | CN103626742B (enExample) |
| AU (1) | AU2006309013B2 (enExample) |
| BR (3) | BRPI0618179A2 (enExample) |
| CA (1) | CA2628283C (enExample) |
| CY (2) | CY1118330T1 (enExample) |
| DK (1) | DK1951684T3 (enExample) |
| ES (1) | ES2595636T3 (enExample) |
| FI (1) | FIC20210010I1 (enExample) |
| HU (2) | HUE028987T2 (enExample) |
| IL (1) | IL191167A (enExample) |
| LT (2) | LT1951684T (enExample) |
| MX (2) | MX362412B (enExample) |
| MY (1) | MY167260A (enExample) |
| NL (1) | NL301104I2 (enExample) |
| NO (1) | NO342221B1 (enExample) |
| NZ (2) | NZ592990A (enExample) |
| PL (1) | PL1951684T3 (enExample) |
| PT (1) | PT1951684T (enExample) |
| RU (2) | RU2597364C2 (enExample) |
| TW (1) | TWI444368B (enExample) |
| WO (1) | WO2007053452A1 (enExample) |
Families Citing this family (336)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI329105B (en) | 2002-02-01 | 2010-08-21 | Rigel Pharmaceuticals Inc | 2,4-pyrimidinediamine compounds and their uses |
| RS51752B (sr) | 2002-07-29 | 2011-12-31 | Rigel Pharmaceuticals | Metode tretiranja i prevencije autoimunih oboljenja jedinjenjima 2,4-pirimidindiamina |
| US20050282814A1 (en) * | 2002-10-03 | 2005-12-22 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| CA2500727A1 (en) * | 2002-10-03 | 2004-04-15 | Targegen, Inc. | Vasculostatic agents and methods of use thereof |
| HRP20130602T1 (en) | 2003-07-30 | 2013-07-31 | Rigel Pharmaceuticals, Inc. | 2,4-pyrimidinediamine compounds for use in the treatment or prevention of autoimmune diseases |
| NZ551027A (en) * | 2004-04-08 | 2011-01-28 | Targegen Inc | Benzotriazine inhibitors of kinases |
| MX2007002208A (es) | 2004-08-25 | 2007-05-08 | Targegen Inc | Compuestos hetrociclicos y metodos de uso. |
| DE602006010979D1 (de) | 2005-01-19 | 2010-01-21 | Rigel Pharmaceuticals Inc | Prodrugs aus 2,4-pyrimidindiamin-verbindungen und ihre verwendungen |
| CA2608367C (en) | 2005-06-08 | 2014-08-19 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| US20070203161A1 (en) | 2006-02-24 | 2007-08-30 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the jak pathway |
| CA2611720A1 (en) * | 2005-06-08 | 2006-12-14 | Targegen, Inc. | Methods and compositions for the treatment of ocular disorders |
| MX362412B (es) * | 2005-11-01 | 2019-01-15 | Targegen Inc | Inhibidores de biaril meta-pirimidina de cinasas. |
| US8133900B2 (en) * | 2005-11-01 | 2012-03-13 | Targegen, Inc. | Use of bi-aryl meta-pyrimidine inhibitors of kinases |
| US8604042B2 (en) * | 2005-11-01 | 2013-12-10 | Targegen, Inc. | Bi-aryl meta-pyrimidine inhibitors of kinases |
| WO2007056023A2 (en) * | 2005-11-02 | 2007-05-18 | Targegen, Inc. | Thiazole inhibitors targeting resistant kinase mutations |
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