JP2010509348A5 - - Google Patents
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- Publication number
- JP2010509348A5 JP2010509348A5 JP2009536401A JP2009536401A JP2010509348A5 JP 2010509348 A5 JP2010509348 A5 JP 2010509348A5 JP 2009536401 A JP2009536401 A JP 2009536401A JP 2009536401 A JP2009536401 A JP 2009536401A JP 2010509348 A5 JP2010509348 A5 JP 2010509348A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- alkyl
- aryl
- pyrrolo
- pyrazol
- 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
Links
- 125000003710 aryl alkyl group Chemical group 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 6
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 239000002254 cytotoxic agent Substances 0.000 claims 3
- 229940127089 cytotoxic agent Drugs 0.000 claims 3
- 231100000599 cytotoxic agent Toxicity 0.000 claims 3
- 229940127084 other anti-cancer agent Drugs 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000002837 carbocyclic group Chemical group 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 2
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- ZBXZVCHTUDQACV-SVZXGPMESA-N 2-(5-cyclopropyl-1H-pyrazol-3-yl)-4-[(1S)-1-(4-fluorophenyl)ethyl]imino-1,3-dihydropyrrolo[2,1-f][1,2,4]triazin-2-amine Chemical compound C1(CC1)C1=CC(=NN1)C1(NN2C(C(=N1)N[C@@H](C)C1=CC=C(C=C1)F)=CC=C2)N ZBXZVCHTUDQACV-SVZXGPMESA-N 0.000 claims 1
- OCCJHZHENPEDFR-RSXQAXDFSA-N 2-(5-cyclopropyl-1H-pyrazol-3-yl)-4-[(2S)-hexan-2-yl]imino-1,3-dihydropyrrolo[2,1-f][1,2,4]triazin-2-amine Chemical compound C1(CC1)C1=CC(=NN1)C1(NN2C(C(=N1)N[C@H](CCCC)C)=CC=C2)N OCCJHZHENPEDFR-RSXQAXDFSA-N 0.000 claims 1
- ZEZLDJMDTSNDCV-UHFFFAOYSA-N 4-(1-benzylpyrrolidin-3-yl)-2-N-(5-methyl-1H-pyrazol-3-yl)-1H-pyrrolo[2,1-f][1,2,4]triazine-2,4-diamine Chemical compound C(C1=CC=CC=C1)N1CC(CC1)C1(N=C(NN2C1=CC=C2)NC1=NNC(=C1)C)N ZEZLDJMDTSNDCV-UHFFFAOYSA-N 0.000 claims 1
- BIWTUOGNDCABCF-CRIUFTBBSA-N 4-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[(1R)-1-phenylethyl]imino-1,3-dihydropyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical compound C1(CC1)C1=NNC(=C1)C1(N=C(NN2C1=CC=C2)N[C@H](C)C1=CC=CC=C1)N BIWTUOGNDCABCF-CRIUFTBBSA-N 0.000 claims 1
- BIWTUOGNDCABCF-SZQRVLIRSA-N 4-(5-cyclopropyl-1H-pyrazol-3-yl)-2-[(1S)-1-phenylethyl]imino-1,3-dihydropyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical compound C1(CC1)C1=NNC(=C1)C1(N=C(NN2C1=CC=C2)N[C@@H](C)C1=CC=CC=C1)N BIWTUOGNDCABCF-SZQRVLIRSA-N 0.000 claims 1
- DCPZKPHHGRFVHE-UHFFFAOYSA-N 4-(cyclohexylmethyl)-2-N-(5-cyclopropyl-1H-pyrazol-3-yl)-1H-pyrrolo[2,1-f][1,2,4]triazine-2,4-diamine Chemical compound C1(CCCCC1)CC1(N=C(NN2C1=CC=C2)NC1=NNC(=C1)C1CC1)N DCPZKPHHGRFVHE-UHFFFAOYSA-N 0.000 claims 1
- IWPKATVNAZDFDY-RSXQAXDFSA-N 4-[(1S)-1-(4-fluorophenyl)ethyl]-2-N-(5-methyl-1H-pyrazol-3-yl)-1H-pyrrolo[2,1-f][1,2,4]triazine-2,4-diamine Chemical compound FC1=CC=C(C=C1)[C@H](C)C1(N=C(NN2C1=CC=C2)NC1=NNC(=C1)C)N IWPKATVNAZDFDY-RSXQAXDFSA-N 0.000 claims 1
- CBROBSJYCBORRW-SZQRVLIRSA-N 4-[(1S)-1-cyclohexylethyl]-2-N-(5-cyclopropyl-1H-pyrazol-3-yl)-1H-pyrrolo[2,1-f][1,2,4]triazine-2,4-diamine Chemical compound C1(CCCCC1)[C@H](C)C1(N=C(NN2C1=CC=C2)NC1=NNC(=C1)C1CC1)N CBROBSJYCBORRW-SZQRVLIRSA-N 0.000 claims 1
- LBJHNFDNNGZHLB-UHFFFAOYSA-N 4-cycloheptyl-2-N-(5-cyclopropyl-1H-pyrazol-3-yl)-1H-pyrrolo[2,1-f][1,2,4]triazine-2,4-diamine Chemical compound C1(CCCCCC1)C1(N=C(NN2C1=CC=C2)NC1=NNC(=C1)C1CC1)N LBJHNFDNNGZHLB-UHFFFAOYSA-N 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 101100335081 Mus musculus Flt3 gene Proteins 0.000 claims 1
- 101150111783 NTRK1 gene Proteins 0.000 claims 1
- 101150117329 NTRK3 gene Proteins 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 101150056950 Ntrk2 gene Proteins 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 claims 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 claims 1
- 201000002510 thyroid cancer Diseases 0.000 claims 1
- 0 *c1cc(Nc(nc2N*)n[n]3c2ccc3)n[n]1 Chemical compound *c1cc(Nc(nc2N*)n[n]3c2ccc3)n[n]1 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US86417506P | 2006-11-03 | 2006-11-03 | |
| US60/864,175 | 2006-11-03 | ||
| PCT/US2007/083436 WO2008057994A2 (en) | 2006-11-03 | 2007-11-02 | Pyrrolotriazine kinase inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010509348A JP2010509348A (ja) | 2010-03-25 |
| JP2010509348A5 true JP2010509348A5 (enExample) | 2011-07-14 |
| JP5180967B2 JP5180967B2 (ja) | 2013-04-10 |
Family
ID=39365255
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009536401A Expired - Fee Related JP5180967B2 (ja) | 2006-11-03 | 2007-11-02 | ピロロトリアジンキナーゼ阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US7982033B2 (enExample) |
| EP (1) | EP2081936B1 (enExample) |
| JP (1) | JP5180967B2 (enExample) |
| CN (1) | CN101535312B (enExample) |
| NO (1) | NO20091374L (enExample) |
| WO (1) | WO2008057994A2 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101511835B (zh) * | 2006-07-07 | 2013-11-27 | 布里斯托尔-迈尔斯斯奎布公司 | 吡咯并三嗪激酶抑制剂 |
| US8268998B2 (en) * | 2006-11-03 | 2012-09-18 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP2300013B2 (en) | 2008-05-21 | 2024-11-13 | Takeda Pharmaceutical Company Limited | Phosphorous derivatives as kinase inhibitors |
| EP2344504B1 (en) * | 2008-10-08 | 2014-06-04 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP2376491B1 (en) | 2008-12-19 | 2015-03-04 | Cephalon, Inc. | Pyrrolotriazines as alk and jak2 inhibitors |
| JP5093527B2 (ja) * | 2010-02-10 | 2012-12-12 | 日本電気株式会社 | 複合光導波路、波長可変フィルタ、波長可変レーザ、および光集積回路 |
| AU2011295440B2 (en) * | 2010-08-27 | 2015-06-11 | Merck Patent Gmbh | Triazolopyrazine derivatives |
| CN103848833B (zh) * | 2012-11-28 | 2016-08-31 | 上海希迈医药科技有限公司 | 吡咯并三嗪类衍生物、其制备方法及其在医药上的应用 |
| US9840517B2 (en) | 2013-09-18 | 2017-12-12 | Beijing Hanmi Pharmaceutical Co., Ltd. | Compound inhibiting activities of BTK and/or JAK3 kinases |
| CN104974163B (zh) * | 2014-04-14 | 2017-11-07 | 广东东阳光药业有限公司 | 取代的杂芳基化合物及其组合物和用途 |
| FR3025717A1 (fr) * | 2014-09-16 | 2016-03-18 | Univ Lille Sciences Tech | Utilisation conjointe d'un inhibiteur de trka et d'un inhibiteur de epha2 pour une utilisation dans le traitement de cancers |
| WO2016190847A1 (en) * | 2015-05-26 | 2016-12-01 | Calitor Sciences, Llc | Substituted heteroaryl compounds and methods of use |
| WO2017004134A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ303660B6 (cs) * | 1999-05-21 | 2013-02-13 | Bristol-Myers Squibb Company | Pyrrolotriazin a farmaceutický prostredek s jeho obsahem |
| US6982265B1 (en) | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| US6670357B2 (en) * | 2000-11-17 | 2003-12-30 | Bristol-Myers Squibb Company | Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors |
| KR100847605B1 (ko) | 2000-11-17 | 2008-07-21 | 브리스톨-마이어스스퀴브컴파니 | ｐ38 키나제 관련 질병의 치료 방법 및 키나제 억제제로서유용한 피롤로트리아진 화합물 |
| EP1497019B1 (en) * | 2002-04-23 | 2015-05-20 | Bristol-Myers Squibb Company | Pyrrolo-triazine aniline compounds useful as kinase inhibitors |
| WO2004013145A1 (en) * | 2002-08-02 | 2004-02-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| CA2425123C (en) * | 2003-01-16 | 2010-09-21 | Decoma International Inc. | Lightweight composite tailgate |
| US7531539B2 (en) * | 2006-08-09 | 2009-05-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| ES2393410T3 (es) * | 2006-08-09 | 2012-12-21 | Bristol-Myers Squibb Company | Pirrolotriazinas inhibidoras de quinasas |
| EP2134716A1 (en) | 2007-04-18 | 2009-12-23 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
-
2007
- 2007-11-02 CN CN2007800405379A patent/CN101535312B/zh not_active Expired - Fee Related
- 2007-11-02 JP JP2009536401A patent/JP5180967B2/ja not_active Expired - Fee Related
- 2007-11-02 EP EP07844826.3A patent/EP2081936B1/en active Active
- 2007-11-02 WO PCT/US2007/083436 patent/WO2008057994A2/en not_active Ceased
- 2007-11-02 US US12/447,751 patent/US7982033B2/en active Active
-
2009
- 2009-04-03 NO NO20091374A patent/NO20091374L/no not_active Application Discontinuation