JP2013526843A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013526843A5 JP2013526843A5 JP2012557201A JP2012557201A JP2013526843A5 JP 2013526843 A5 JP2013526843 A5 JP 2013526843A5 JP 2012557201 A JP2012557201 A JP 2012557201A JP 2012557201 A JP2012557201 A JP 2012557201A JP 2013526843 A5 JP2013526843 A5 JP 2013526843A5
- Authority
- JP
- Japan
- Prior art keywords
- inhibitor
- cancer
- raf
- subject
- phosphorylation
- 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
- 239000003112 inhibitor Substances 0.000 claims 29
- 238000000034 method Methods 0.000 claims 21
- 108090000623 proteins and genes Proteins 0.000 claims 18
- 206010028980 Neoplasm Diseases 0.000 claims 17
- 201000011510 cancer Diseases 0.000 claims 17
- 102100026907 Mitogen-activated protein kinase kinase kinase 8 Human genes 0.000 claims 16
- 102100033479 RAF proto-oncogene serine/threonine-protein kinase Human genes 0.000 claims 13
- 239000000126 substance Substances 0.000 claims 13
- 108091000080 Phosphotransferase Proteins 0.000 claims 12
- 210000004027 cell Anatomy 0.000 claims 12
- 102000020233 phosphotransferase Human genes 0.000 claims 12
- 108020004999 messenger RNA Proteins 0.000 claims 9
- 230000026731 phosphorylation Effects 0.000 claims 9
- 238000006366 phosphorylation reaction Methods 0.000 claims 9
- 235000018102 proteins Nutrition 0.000 claims 9
- 102000004169 proteins and genes Human genes 0.000 claims 9
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims 8
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims 8
- 230000035772 mutation Effects 0.000 claims 8
- 229940079593 drug Drugs 0.000 claims 7
- 239000003814 drug Substances 0.000 claims 7
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 6
- 102100029375 Crk-like protein Human genes 0.000 claims 5
- 101000919315 Homo sapiens Crk-like protein Proteins 0.000 claims 5
- 101001055091 Homo sapiens Mitogen-activated protein kinase kinase kinase 8 Proteins 0.000 claims 5
- 101150010110 Map3k8 gene Proteins 0.000 claims 5
- 238000004113 cell culture Methods 0.000 claims 5
- 210000004748 cultured cell Anatomy 0.000 claims 5
- 201000001441 melanoma Diseases 0.000 claims 5
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 4
- 229940124647 MEK inhibitor Drugs 0.000 claims 4
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 4
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 238000002648 combination therapy Methods 0.000 claims 4
- 108020004707 nucleic acids Proteins 0.000 claims 4
- 102000039446 nucleic acids Human genes 0.000 claims 4
- 150000007523 nucleic acids Chemical class 0.000 claims 4
- 235000001014 amino acid Nutrition 0.000 claims 3
- 150000001413 amino acids Chemical group 0.000 claims 3
- MLSAQOINCGAULQ-QFMPWRQOSA-N (E)-SB-590885 Chemical compound C1=CC(OCCN(C)C)=CC=C1C1=NC(C=2C=CN=CC=2)=C(C=2C=C3CCC(/C3=CC=2)=N\O)N1 MLSAQOINCGAULQ-QFMPWRQOSA-N 0.000 claims 2
- YABJJWZLRMPFSI-UHFFFAOYSA-N 1-methyl-5-[[2-[5-(trifluoromethyl)-1H-imidazol-2-yl]-4-pyridinyl]oxy]-N-[4-(trifluoromethyl)phenyl]-2-benzimidazolamine Chemical group N=1C2=CC(OC=3C=C(N=CC=3)C=3NC(=CN=3)C(F)(F)F)=CC=C2N(C)C=1NC1=CC=C(C(F)(F)F)C=C1 YABJJWZLRMPFSI-UHFFFAOYSA-N 0.000 claims 2
- PYEFPDQFAZNXLI-UHFFFAOYSA-N 3-(dimethylamino)-N-[3-[[(4-hydroxyphenyl)-oxomethyl]amino]-4-methylphenyl]benzamide Chemical compound CN(C)C1=CC=CC(C(=O)NC=2C=C(NC(=O)C=3C=CC(O)=CC=3)C(C)=CC=2)=C1 PYEFPDQFAZNXLI-UHFFFAOYSA-N 0.000 claims 2
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 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
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 208000032612 Glial tumor Diseases 0.000 claims 2
- 206010018338 Glioma Diseases 0.000 claims 2
- 101000967216 Homo sapiens Eosinophil cationic protein Proteins 0.000 claims 2
- 101001026852 Homo sapiens Protein kinase C epsilon type Proteins 0.000 claims 2
- 101000971400 Homo sapiens Protein kinase C eta type Proteins 0.000 claims 2
- 101000712530 Homo sapiens RAF proto-oncogene serine/threonine-protein kinase Proteins 0.000 claims 2
- 101000927796 Homo sapiens Rho guanine nucleotide exchange factor 7 Proteins 0.000 claims 2
- 101000987315 Homo sapiens Serine/threonine-protein kinase PAK 3 Proteins 0.000 claims 2
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 101150048267 PAK3 gene Proteins 0.000 claims 2
- -1 PD334581 Chemical compound 0.000 claims 2
- YZDJQTHVDDOVHR-UHFFFAOYSA-N PLX-4720 Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(Cl)=CN=C3NC=2)=C1F YZDJQTHVDDOVHR-UHFFFAOYSA-N 0.000 claims 2
- 101150010978 PRKCE gene Proteins 0.000 claims 2
- 101150062385 Prkch gene Proteins 0.000 claims 2
- 102100037339 Protein kinase C epsilon type Human genes 0.000 claims 2
- 102100021556 Protein kinase C eta type Human genes 0.000 claims 2
- 102100027911 Serine/threonine-protein kinase PAK 3 Human genes 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 230000014509 gene expression Effects 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000011932 ovarian sarcoma Diseases 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- 229960003787 sorafenib Drugs 0.000 claims 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims 2
- 229960003862 vemurafenib Drugs 0.000 claims 2
- LFTHSVHVSCMOQP-UHFFFAOYSA-N 6-methoxy-7-(3-morpholin-4-ylpropoxy)-4-(4-phenoxyanilino)quinoline-3-carbonitrile Chemical compound N#CC1=CN=C2C=C(OCCCN3CCOCC3)C(OC)=CC2=C1NC(C=C1)=CC=C1OC1=CC=CC=C1 LFTHSVHVSCMOQP-UHFFFAOYSA-N 0.000 claims 1
- DEZZLWQELQORIU-RELWKKBWSA-N GDC-0879 Chemical compound N=1N(CCO)C=C(C=2C=C3CCC(/C3=CC=2)=N\O)C=1C1=CC=NC=C1 DEZZLWQELQORIU-RELWKKBWSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- 101710141955 RAF proto-oncogene serine/threonine-protein kinase Proteins 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 238000012258 culturing Methods 0.000 claims 1
- 230000001747 exhibiting effect Effects 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 1
- VLCMRTMCMQJSKM-UHFFFAOYSA-N phenyl-[4-phenyl-8-(trifluoromethyl)quinolin-3-yl]methanone Chemical compound C=1C=CC=CC=1C(=O)C1=CN=C2C(C(F)(F)F)=CC=CC2=C1C1=CC=CC=C1 VLCMRTMCMQJSKM-UHFFFAOYSA-N 0.000 claims 1
- 230000001177 retroviral effect Effects 0.000 claims 1
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
- 230000035899 viability Effects 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US31219310P | 2010-03-09 | 2010-03-09 | |
| US61/312,193 | 2010-03-09 | ||
| US31251910P | 2010-03-10 | 2010-03-10 | |
| US61/312,519 | 2010-03-10 | ||
| US32602110P | 2010-04-20 | 2010-04-20 | |
| US61/326,021 | 2010-04-20 | ||
| US41556910P | 2010-11-19 | 2010-11-19 | |
| US61/415,569 | 2010-11-19 | ||
| PCT/US2011/027689 WO2011112678A1 (en) | 2010-03-09 | 2011-03-09 | Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013526843A JP2013526843A (ja) | 2013-06-27 |
| JP2013526843A5 true JP2013526843A5 (cg-RX-API-DMAC10.html) | 2014-04-24 |
| JP5985401B2 JP5985401B2 (ja) | 2016-09-06 |
Family
ID=43837946
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012557201A Active JP5985401B2 (ja) | 2010-03-09 | 2011-03-09 | 第一の癌療法に対する耐性を現に有するか、または、そのような耐性を生じる患者において癌を診断および治療する方法 |
Country Status (12)
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7723477B2 (en) | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
| EP2331136B1 (en) | 2008-09-26 | 2018-01-10 | OncoMed Pharmaceuticals, Inc. | Frizzled-binding agents and uses thereof |
| TWI535445B (zh) | 2010-01-12 | 2016-06-01 | 安可美德藥物股份有限公司 | Ｗｎｔ拮抗劑及治療和篩選方法 |
| CN102971337B (zh) | 2010-04-01 | 2016-09-21 | 昂考梅德药品有限公司 | 卷曲蛋白结合药剂及其应用 |
| US20140296248A1 (en) * | 2011-04-04 | 2014-10-02 | Stichting het Nederlands Kanker Instiuut-Antoni van Leeuwenhoek ziekenhuis | Methods and compositions for predicting resistance to anticancer treatment |
| WO2013067050A1 (en) * | 2011-10-31 | 2013-05-10 | University Of Utah Research Foundation | Genetic alterations in glioblastoma |
| WO2013086260A2 (en) * | 2011-12-09 | 2013-06-13 | Oncomed Pharmaceuticals, Inc. | Combination therapy for treatment of cancer |
| TR201808010T4 (tr) | 2012-03-28 | 2018-06-21 | Dana Farber Cancer Inst Inc | RAF inhibitörlerine direnç veren C-RAF mutantları. |
| DK2884979T3 (da) | 2012-08-17 | 2019-09-02 | Hoffmann La Roche | Kombinationsbehandlinger mod melanom omfattende indgivelse af cobimetinib og vemurafenib |
| JP2015536933A (ja) | 2012-10-23 | 2015-12-24 | オンコメッド ファーマシューティカルズ インコーポレイテッド | Ｗｎｔ経路結合剤を用いて神経内分泌腫瘍を処置する方法 |
| CN105073195A (zh) | 2013-02-04 | 2015-11-18 | 昂科梅德制药有限公司 | 使用Wnt途径抑制剂进行治疗的方法及对该治疗的监测 |
| US9168300B2 (en) | 2013-03-14 | 2015-10-27 | Oncomed Pharmaceuticals, Inc. | MET-binding agents and uses thereof |
| US10968484B2 (en) | 2013-03-15 | 2021-04-06 | The Broad Institute, Inc. | Methods of identifying responses to map kinase inhibition therapy |
| WO2014204261A1 (ko) * | 2013-06-21 | 2014-12-24 | 사회복지법인 삼성생명공익재단 | Tpl2의 발현억제제 또는 활성억제제를 유효성분으로 포함하는 신세포암의 예방 또는 치료용 약학적 조성물 |
| WO2016041932A1 (en) * | 2014-09-17 | 2016-03-24 | Institut Curie | Map3k8 as a marker for selecting a patient affected with an ovarian cancer for a treatment with a mek inhibitor |
| KR20160129609A (ko) | 2015-04-30 | 2016-11-09 | 삼성전자주식회사 | Ｂｒａｆ 저해제를 포함하는 세포 또는 개체의 노화를 감소시키기 위한 조성물 및 그의 용도 |
| ES2734713T3 (es) | 2015-07-06 | 2019-12-11 | Gilead Sciences Inc | Moduladores Cot y métodos de utilización de los mismos |
| MX2017017124A (es) | 2015-07-06 | 2018-03-09 | Gilead Sciences Inc | 6-amino-quinolin-3-carbonitrilos como moduladores de cancer osaka tiroides (cot). |
| GB201520178D0 (en) * | 2015-11-16 | 2015-12-30 | Univ London Queen Mary | Method |
| CN105695616A (zh) * | 2016-04-22 | 2016-06-22 | 王冬国 | 诊断甲状腺癌的分析标志物及其应用 |
| JP6776378B2 (ja) | 2016-06-30 | 2020-10-28 | ギリアード サイエンシーズ， インコーポレイテッド | Ｃｏｔモジュレーターとしての４，６−ジアミノキナゾリン類およびその使用方法 |
| WO2018027223A1 (en) * | 2016-08-05 | 2018-02-08 | Duke University | Camkk2 inhibitor compositions and methods of using the same |
| KR20190103156A (ko) | 2016-12-20 | 2019-09-04 | 에테하 취리히 | 암에서 비-유전적 약물 내성 프로그램을 표적으로 하는 약물의 동정 |
| US10793901B2 (en) * | 2016-12-28 | 2020-10-06 | Roche Molecular Systems, Inc. | Reversibly protected nucleotide reagents with high thermal stability |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2019090020A1 (en) * | 2017-11-02 | 2019-05-09 | University Of Georgia Research Foundation, Inc. | Methods and compositions related to increased rotavirus production |
| CN108872438B (zh) * | 2018-08-06 | 2021-01-15 | 杭州迪相实业有限公司 | 一种外泌体中肺癌标志物gk5快速检测试剂盒 |
| EP3876939A4 (en) | 2018-11-07 | 2022-08-10 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole derivatives as janus kinase 2 inhibitors and uses thereof |
| US12509455B2 (en) | 2018-11-07 | 2025-12-30 | Dana-Farber Cancer Institute, Inc. | Imidazopyridine derivatives and aza-imidazopyridine derivatives as Janus kinase 2 inhibitors and uses thereof |
| WO2020097396A1 (en) * | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzimidazole derivatives and aza-benzimidazole derivatives as janus kinase 2 inhibitors and uses thereof |
| WO2020176693A2 (en) * | 2019-02-26 | 2020-09-03 | Cell Response, Inc. | Methods for treating map3k8 positive cancers |
| TWI915558B (zh) | 2019-06-14 | 2026-02-21 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
| CA3156828A1 (en) | 2019-10-03 | 2021-04-08 | Dana-Farber Cancer Institute, Inc. | Tricyclic kinase inhibitors and uses thereof |
| CN110862968A (zh) * | 2019-10-30 | 2020-03-06 | 中国农业科学院兰州兽医研究所 | Map3k8基因敲除pk-15细胞系的构建方法及其应用 |
| CA3175541A1 (en) | 2020-03-30 | 2021-10-07 | Gilead Sciences, Inc. | Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound |
| EP4126862B1 (en) | 2020-04-02 | 2025-05-21 | Gilead Sciences, Inc. | Process for preparing a cot inhibitor compound |
| TW202204350A (zh) | 2020-05-06 | 2022-02-01 | 美商雅捷可斯治療公司 | 作為ｊａｋ２抑制劑之６－雜芳基氧基苯并咪唑及氮雜苯并咪唑 |
| EP4267574B1 (en) | 2020-12-23 | 2025-04-23 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| US12173039B1 (en) | 2021-01-08 | 2024-12-24 | Washington University | TPL2 inhibiting agents, uses thereof, and detection of TPL2 |
| CA3234638A1 (en) | 2021-11-09 | 2023-05-19 | Ajax Therapeutics, Inc. | 6-heteroaryloxy benzimidazoles and azabenzimidazoles as jak2 inhibitors |
| US12162881B2 (en) | 2021-11-09 | 2024-12-10 | Ajax Therapeutics, Inc. | Forms and compositions of inhibitors of JAK2 |
Family Cites Families (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR8108820A (pt) | 1980-09-24 | 1982-08-24 | Cetus Corp | Processo e sonda de diagnostico |
| EP0084796B1 (en) | 1982-01-22 | 1990-05-02 | Cetus Corporation | Hla typing method and cdna probes used therein |
| US4683202A (en) | 1985-03-28 | 1987-07-28 | Cetus Corporation | Process for amplifying nucleic acid sequences |
| CA1284931C (en) | 1986-03-13 | 1991-06-18 | Henry A. Erlich | Process for detecting specific nucleotide variations and genetic polymorphisms present in nucleic acids |
| CA1338457C (en) | 1986-08-22 | 1996-07-16 | Henry A. Erlich | Purified thermostable enzyme |
| EP0266032A1 (en) | 1986-08-29 | 1988-05-04 | Beecham Group Plc | Modified fibrinolytic enzyme |
| US7705215B1 (en) | 1990-04-17 | 2010-04-27 | Dekalb Genetics Corporation | Methods and compositions for the production of stably transformed, fertile monocot plants and cells thereof |
| FR2650840B1 (fr) | 1989-08-11 | 1991-11-29 | Bertin & Cie | Procede rapide de detection et/ou d'identification d'une seule base sur une sequence d'acide nucleique, et ses applications |
| US6004744A (en) | 1991-03-05 | 1999-12-21 | Molecular Tool, Inc. | Method for determining nucleotide identity through extension of immobilized primer |
| GB9222888D0 (en) | 1992-10-30 | 1992-12-16 | British Tech Group | Tomography |
| AT404556B (de) | 1995-11-23 | 1998-12-28 | Pharma Consult Gmbh | Einrichtung zum dichten verschliessen eines glas- oder kunststoffbehälters zur aufnahme flüssiger pharmazeutischer produkte |
| GB2323845A (en) | 1997-03-31 | 1998-10-07 | Merck & Co Inc | MEK inhibiting lactones |
| US6310060B1 (en) | 1998-06-24 | 2001-10-30 | Warner-Lambert Company | 2-(4-bromo or 4-iodo phenylamino) benzoic acid derivatives and their use as MEK inhibitors |
| ES2229515T3 (es) | 1997-07-01 | 2005-04-16 | Warner-Lambert Company Llc | Derivados 4-bromo o 4-yodo del acido fenilamino benzhidroxamico y su uso como inhibidores de la mek. |
| ATE344791T1 (de) | 1997-07-01 | 2006-11-15 | Warner Lambert Co | 2-(4-brom or 4-iod phenylamino)benzoesäurederivate und ihre anwendung als mek-inhibitoren |
| US6506798B1 (en) | 1997-07-01 | 2003-01-14 | Warner-Lambert Company | 4-Arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective MEK inhibitors |
| US6821963B2 (en) | 1997-07-01 | 2004-11-23 | Warner-Lambert Company | 4-Bromo or 4-iodo phenylamino benzhydroxamic acid derivatives and their use as MEK inhibitors |
| KR20010099877A (ko) | 1998-12-22 | 2001-11-09 | 로즈 암스트롱, 크리스틴 에이. 트러트웨인 | 배합물 화학요법 |
| US20040171632A1 (en) | 1998-12-22 | 2004-09-02 | Gowan Richard Carleton | Combination chemotherapy |
| JP2002534515A (ja) | 1999-01-13 | 2002-10-15 | ワーナー−ランバート・カンパニー | １−複素環置換されたジアリールアミン |
| JP2000212157A (ja) | 1999-01-13 | 2000-08-02 | Warner Lambert Co | ジアリ―ルアミン |
| CA2349832A1 (en) | 1999-01-13 | 2000-07-20 | Warner-Lambert Company | Benzenesulfonamide derivatives and their use as mek inhibitors |
| JP2000204075A (ja) | 1999-01-13 | 2000-07-25 | Warner Lambert Co | ジアリ―ルアミン |
| ID30439A (id) | 1999-01-13 | 2001-12-06 | Warner Lambert Co | Benzoheterosiklus dan penggunaannya sebagai penghambat mek |
| JP2000204077A (ja) | 1999-01-13 | 2000-07-25 | Warner Lambert Co | ジアリ―ルアミン |
| CA2348236A1 (en) | 1999-01-13 | 2000-07-20 | Stephen Douglas Barrett | 4-arylamino, 4-aryloxy, and 4-arylthio diarylamines and derivatives thereof as selective mek inhibitors |
| JP2000204079A (ja) | 1999-01-13 | 2000-07-25 | Warner Lambert Co | ジアリ―ルアミン |
| AU2482800A (en) | 1999-01-13 | 2000-08-01 | Warner-Lambert Company | Sulphohydroxamic acids and sulphohydroxamates and their use as mek inhibitors |
| AU7349801A (en) | 2000-07-19 | 2002-01-30 | Warner Lambert Co | Oxygenated esters of 4-iodo phenylamino benzhydroxamic acids |
| EP1438295B1 (en) | 2001-10-23 | 2012-08-15 | Merck Serono SA | Azole derivatives and pharmaceutical compositions containing them |
| AU2002365899B2 (en) | 2001-12-04 | 2007-09-13 | Onyx Pharmaceuticals, Inc. | RAF-MEK-ERK pathway inhibitors to treat cancer |
| WO2003047583A1 (en) | 2001-12-05 | 2003-06-12 | Astrazeneca Ab | Pharmaceutical compositions comprising benzofuranyl substituted 3-cyanoquinoline derivatives and their use for the treatment of solid tumours |
| AU2002347360A1 (en) | 2001-12-05 | 2003-06-17 | Astrazeneca Ab | Pharmaceutical compositions comprising benzofuranyl substituted 3-cyanoquinoline derivatives and their use for the treatment of solid tumours |
| BR0307060A (pt) | 2002-01-23 | 2004-10-26 | Warner Lambert Co | ésteres hidroxamato do ácido n-(fenil 4-substituìdo)-antranìlico |
| DOP2003000556A (es) | 2002-01-23 | 2003-10-31 | Warner Lambert Co | Esteres hidroxamato de acido n-(4-fenil-sustituido)-antranilico. |
| WO2003077855A2 (en) | 2002-03-13 | 2003-09-25 | Array Biopharma, Inc | N3 alkylated benzimidazole derivatives as mek inhibitors |
| US6989451B2 (en) | 2002-06-04 | 2006-01-24 | Valeant Research & Development | Heterocyclic compounds and uses thereof |
| SI1509230T1 (sl) * | 2002-06-05 | 2007-06-30 | Cedars Sinai Medical Center | Gefitinib (iressa) za zdravljenje raka |
| EP1545529A4 (en) | 2002-09-30 | 2010-03-03 | Bristol Myers Squibb Co | NEW TYROSINE KINASE HEMMER |
| US20060270643A1 (en) | 2002-10-31 | 2006-11-30 | Chawnshang Chang | Hyfroxyflutamide induced pathways related to androgen receptor negative prostate cancer cells |
| GB0225579D0 (en) | 2002-11-02 | 2002-12-11 | Astrazeneca Ab | Chemical compounds |
| AU2003291268A1 (en) | 2002-11-12 | 2004-06-03 | Mercury Therapeutics, Inc. | Xanthene compounds for cancer chemotherapy |
| US20050004186A1 (en) | 2002-12-20 | 2005-01-06 | Pfizer Inc | MEK inhibiting compounds |
| KR20050108383A (ko) | 2003-03-11 | 2005-11-16 | 노파르티스 아게 | 이소퀴놀린 유도체의 암 및 ｍａｐ 키나제 관련 질병의치료를 위한 용도 |
| WO2005000818A1 (en) | 2003-06-27 | 2005-01-06 | Warner-Lambert Company Llc | 5-substituted-4-`(substituted phenyl)!amino!-2-pyridone deviatives for use as mek inhibitors |
| WO2005007616A1 (en) | 2003-07-23 | 2005-01-27 | Warner-Lambert Company Llc | Diphenylamino ketone derivatives as mek inhibitors |
| US20050049276A1 (en) | 2003-07-23 | 2005-03-03 | Warner-Lambert Company, Llc | Imidazopyridines and triazolopyridines |
| CA2532067C (en) | 2003-07-24 | 2010-12-21 | Stephen Douglas Barrett | N-methyle-substituted benzamidazoles |
| US7144907B2 (en) | 2003-09-03 | 2006-12-05 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| US7538120B2 (en) | 2003-09-03 | 2009-05-26 | Array Biopharma Inc. | Method of treating inflammatory diseases |
| JP4931419B2 (ja) | 2003-09-19 | 2012-05-16 | 中外製薬株式会社 | 新規４−フェニルアミノ−ベンズアルドオキシム誘導体並びにそのｍｅｋ阻害剤としての使用 |
| EP1682126B1 (en) * | 2003-10-16 | 2009-07-01 | Novartis Vaccines and Diagnostics, Inc. | Substituted benzazoles and use thereof as inhibitors of raf kinase |
| US7732616B2 (en) | 2003-11-19 | 2010-06-08 | Array Biopharma Inc. | Dihydropyridine and dihydropyridazine derivatives as inhibitors of MEK and methods of use thereof |
| KR101190912B1 (ko) | 2003-11-19 | 2012-10-12 | 어레이 바이오파마 인크. | Ｍｅｋ의 헤테로시클릭 억제제 및 그의 사용 방법 |
| US7517994B2 (en) | 2003-11-19 | 2009-04-14 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| TW200529846A (en) | 2004-02-20 | 2005-09-16 | Wyeth Corp | 3-quinolinecarbonitrile protein kinase inhibitors |
| KR100883289B1 (ko) | 2004-06-11 | 2009-02-11 | 니뽄 다바코 산교 가부시키가이샤 | 암 치료용5-아미노-2,4,7-트리옥소-3,4,7,8-테트라히드로-2ｈ-피리도[2,3-ｄ]피리미딘 유도체 및 관련 화합물 |
| US7378423B2 (en) | 2004-06-11 | 2008-05-27 | Japan Tobacco Inc. | Pyrimidine compound and medical use thereof |
| MY144232A (en) | 2004-07-26 | 2011-08-15 | Chugai Pharmaceutical Co Ltd | 5-substituted-2-phenylamino benzamides as mek inhibitors |
| CN101006085A (zh) | 2004-08-17 | 2007-07-25 | 霍夫曼-拉罗奇有限公司 | 取代的乙内酰脲类 |
| MX2007001846A (es) | 2004-08-17 | 2007-03-28 | Hoffmann La Roche | Hidantoinas sustituidas. |
| NZ588896A (en) | 2004-08-25 | 2012-05-25 | Targegen Inc | Heterocyclic compounds and methods of use |
| CN101044125A (zh) | 2004-08-25 | 2007-09-26 | 塔尔基公司 | 杂环化合物和应用方法 |
| AU2005278961A1 (en) | 2004-09-01 | 2006-03-09 | Astrazeneca Ab | Quinazolinone derivatives and their use as B-Raf inhibitors |
| JP2006083133A (ja) | 2004-09-17 | 2006-03-30 | Sankyo Co Ltd | スルファミド誘導体医薬組成物 |
| TW200621766A (en) | 2004-09-17 | 2006-07-01 | Hoffmann La Roche | Substituted hydantoins |
| ES2444866T3 (es) | 2004-10-20 | 2014-02-27 | Merck Serono Sa | Derivados de 3-arilamino piridina |
| EP1838675A1 (en) | 2004-11-24 | 2007-10-03 | Laboratoires Serono S.A. | Novel 4-arylamino pyridone derivatives as mek inhibitors for the treatment of hyperproliferative disorders |
| ES2330872T3 (es) | 2004-12-01 | 2009-12-16 | Merck Serono Sa | Derivados de (1,2,4)triazolo(4,3-a)piridina para el tratamiento de enfermedades hiperproliferativas. |
| US7429667B2 (en) | 2005-01-20 | 2008-09-30 | Ardea Biosciences, Inc. | Phenylamino isothiazole carboxamidines as MEK inhibitors |
| TWI441637B (zh) | 2005-05-18 | 2014-06-21 | Array Biopharma Inc | Ｍｅｋ雜環抑制劑及其使用方法 |
| WO2006133417A1 (en) | 2005-06-07 | 2006-12-14 | Valeant Pharmaceuticals International | Phenylamino isothiazole carboxamidines as mek inhibitors |
| MX2008002114A (es) | 2005-07-21 | 2008-04-17 | Ardea Biosciences Inc | Inhibidores de n-(arilamino)-sulfonamida de mek. |
| US8101799B2 (en) | 2005-07-21 | 2012-01-24 | Ardea Biosciences | Derivatives of N-(arylamino) sulfonamides as inhibitors of MEK |
| US20070049591A1 (en) | 2005-08-25 | 2007-03-01 | Kalypsys, Inc. | Inhibitors of MAPK/Erk Kinase |
| NZ567140A (en) | 2005-10-07 | 2011-09-30 | Exelixis Inc | Azetidines as MEK inhibitors for the treatment of proliferative diseases |
| WO2007071951A1 (en) | 2005-12-21 | 2007-06-28 | Astrazeneca Ab | Tosylate salt of 6- (4-br0m0-2-chl0r0phenylamin0) -7-fluoro-n- (2-hydroxyethoxy) -3-methyl-3h-benzimi dazole- 5 - carboxamide , mek inhibitor useful in the treatment of cancer |
| US7612212B2 (en) | 2006-02-22 | 2009-11-03 | Hoffmann-La Roche Inc. | Substituted hydantoins |
| JP2009532449A (ja) | 2006-04-05 | 2009-09-10 | アストラゼネカ アクチボラグ | 抗癌活性のある置換キナゾリン |
| US7842836B2 (en) | 2006-04-11 | 2010-11-30 | Ardea Biosciences | N-aryl-N'alkyl sulfamides as MEK inhibitors |
| AU2007237901B2 (en) | 2006-04-18 | 2012-07-05 | Ardea Biosciences, Inc. | Pyridone sulfonamides and pyridone sulfamides as MEK inhibitors |
| EA200802050A1 (ru) | 2006-04-19 | 2009-04-28 | Лаборатуар Сероно Са | Новые гетероарилзамещенные ариламинопиридиновые производные в качестве мек ингибиторов |
| WO2007123939A2 (en) | 2006-04-19 | 2007-11-01 | Laboratoires Serono S.A. | Novel arylamino n-heteraryls as mek inhibitors |
| CA2658725A1 (en) | 2006-08-16 | 2008-02-21 | Exelixis, Inc. | Using pi3k and mek modulators in treatments of cancer |
| WO2008020203A1 (en) | 2006-08-17 | 2008-02-21 | Astrazeneca Ab | Pyridinylquinaz0linamine derivatives and their use as b-raf inhibitors |
| WO2008024724A1 (en) | 2006-08-21 | 2008-02-28 | Genentech, Inc. | Aza-benzothiophenyl compounds and methods of use |
| CA2660546A1 (en) | 2006-08-21 | 2008-02-28 | Genentech, Inc. | Aza-benzofuranyl compounds and methods of use |
| WO2008028141A2 (en) | 2006-08-31 | 2008-03-06 | Array Biopharma Inc. | Raf inhibitor compounds and methods of use thereof |
| EP2113500A1 (en) | 2006-10-31 | 2009-11-04 | Takeda Pharmaceutical Company Limited | MAPK/ERK kinase inhibitors |
| CA2672327A1 (en) | 2006-11-30 | 2008-06-05 | Genentech, Inc. | Aza-indolyl compounds and methods of use |
| WO2008076415A1 (en) | 2006-12-14 | 2008-06-26 | Exelixis, Inc. | Methods of using mek inhibitors |
| WO2008120004A1 (en) | 2007-04-02 | 2008-10-09 | Astrazeneca Ab | Combination of a mek- inhibitor and a b-raf inhibitor for the treatment of cancer |
| WO2009002607A1 (en) * | 2007-05-01 | 2008-12-31 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for identifying transforming and tumor suppressor genes |
| CA2694646C (en) * | 2007-07-30 | 2017-09-05 | Ardea Biosciences, Inc. | Combinations of mek inhibitors and raf kinase inhibitors and uses thereof |
| EP2370568B1 (en) * | 2008-12-10 | 2017-07-19 | Dana-Farber Cancer Institute, Inc. | Mek mutations conferring resistance to mek inhibitors |
| HUE060206T2 (hu) * | 2009-10-16 | 2023-02-28 | Novartis Ag | MEK gátlót és B-Raf gátlót tartalmazó kombináció |
-
2011
- 2011-03-09 EP EP11709278.3A patent/EP2545187B1/en active Active
- 2011-03-09 CN CN2011800231091A patent/CN103038364A/zh active Pending
- 2011-03-09 EA EA201290883A patent/EA030276B1/ru not_active IP Right Cessation
- 2011-03-09 WO PCT/US2011/027689 patent/WO2011112678A1/en not_active Ceased
- 2011-03-09 CA CA2791247A patent/CA2791247C/en not_active Expired - Fee Related
- 2011-03-09 KR KR1020127025801A patent/KR20120139767A/ko not_active Abandoned
- 2011-03-09 JP JP2012557201A patent/JP5985401B2/ja active Active
- 2011-03-09 AU AU2011224410A patent/AU2011224410B2/en not_active Ceased
- 2011-03-09 MX MX2012010420A patent/MX343368B/es active IP Right Grant
- 2011-03-09 US US13/583,056 patent/US20130059851A1/en not_active Abandoned
- 2011-03-09 ES ES11709278T patent/ES2714875T3/es active Active
- 2011-03-09 BR BR112012022801A patent/BR112012022801B8/pt not_active IP Right Cessation
-
2017
- 2017-04-05 US US15/480,126 patent/US11078540B2/en active Active
-
2021
- 2021-06-24 US US17/357,642 patent/US12522872B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Ruscetti et al. | Senescence-induced vascular remodeling creates therapeutic vulnerabilities in pancreas cancer | |
| Zhao et al. | RAS/MAPK activation drives resistance to Smo inhibition, metastasis, and tumor evolution in Shh pathway–dependent tumors | |
| Powell et al. | p53 deficiency linked to B cell translocation gene 2 (BTG2) loss enhances metastatic potential by promoting tumor growth in primary and metastatic sites in patient-derived xenograft (PDX) models of triple-negative breast cancer | |
| Gruosso et al. | MAP3K8/TPL-2/COT is a potential predictive marker for MEK inhibitor treatment in high-grade serous ovarian carcinomas | |
| Sekido | Targeting the Hippo pathway is a new potential therapeutic modality for malignant mesothelioma | |
| Ninomiya et al. | MET or NRAS amplification is an acquired resistance mechanism to the third-generation EGFR inhibitor naquotinib | |
| Chen et al. | TET1 reprograms the epithelial ovarian cancer epigenome and reveals casein kinase 2α as a therapeutic target | |
| Wang et al. | Mitochondrial fragmentation is crucial for c-Myc-driven hepatoblastoma-like liver tumors | |
| Ganesan et al. | Taxane chemotherapy induces stromal injury that leads to breast cancer dormancy escape | |
| Shen et al. | Characterization with KRAS mutant is a critical determinant in immunotherapy and other multiple therapies for non-small cell lung cancer | |
| Lv et al. | Neuropeptide Y1 receptor inhibits cell growth through inactivating mitogen-activated protein kinase signal pathway in human hepatocellular carcinoma | |
| Ning et al. | Bioengineered BERA-Wnt5a siRNA targeting Wnt5a/FZD2 signaling suppresses advanced prostate cancer tumor growth and enhances enzalutamide treatment | |
| Timis et al. | Pathology and molecular biology of melanoma | |
| Pedini et al. | Joint action of miR‐126 and MAPK/PI3K inhibitors against metastatic melanoma | |
| Luo et al. | Targeted degradation of SOS1 exhibits potent anticancer activity and overcomes resistance in KRAS-Mutant tumors and BCR–ABL–Positive leukemia | |
| Mastrodomenico et al. | Personalized systemic therapies in hereditary cancer syndromes | |
| Kwon et al. | Analysis of electric cigarette liquid effect on mouse brain tumor growth through EGFR and ERK activation | |
| Odintsov et al. | Genomic profiling of cardiac angiosarcoma reveals novel targetable KDR variants, recurrent MED12 mutations, and a high burden of germline POT1 alterations | |
| Ji et al. | KRAS/PI3K axis driven GTF3C6 expression and promotes LUAD via FAK pathway | |
| Park et al. | Pembrolizumab and olaparib in homologous-recombination-deficient metastatic pancreatic cancer: the phase 2 POLAR trial | |
| Catalano et al. | Sensitivity and resistance of oncogenic RAS-driven tumors to dual MEK and ERK inhibition | |
| Aytes et al. | Cross-species analysis of genome-wide regulatory networks identifies a synergistic interaction between FOXM1 and CENPF that drives prostate cancer malignancy | |
| Banik et al. | P38 mediates tumor suppression through reduced autophagy and actin cytoskeleton changes in NRAS-mutant melanoma | |
| Ruwali et al. | Clinical management of head and neck cancer cases: role of pharmacogenetics of CYP2 and GSTs | |
| Igawa et al. | Smoking history as a predictor of pemetrexed monotherapy in patients with non-squamous non-small cell lung cancer |