JP2013526843A5 - - Google Patents
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- 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
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- 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 (https=) | 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)
| Country | Link |
|---|---|
| US (3) | US20130059851A1 (https=) |
| EP (1) | EP2545187B1 (https=) |
| JP (1) | JP5985401B2 (https=) |
| KR (1) | KR20120139767A (https=) |
| CN (1) | CN103038364A (https=) |
| AU (1) | AU2011224410B2 (https=) |
| BR (1) | BR112012022801B8 (https=) |
| CA (1) | CA2791247C (https=) |
| EA (1) | EA030276B1 (https=) |
| ES (1) | ES2714875T3 (https=) |
| MX (1) | MX343368B (https=) |
| WO (1) | WO2011112678A1 (https=) |
Families Citing this family (40)
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| US7723477B2 (en) | 2005-10-31 | 2010-05-25 | Oncomed Pharmaceuticals, Inc. | Compositions and methods for inhibiting Wnt-dependent solid tumor cell growth |
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| 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 |
| CA2794674A1 (en) | 2010-04-01 | 2011-10-06 | Oncomed Pharmaceuticals, Inc. | Frizzled-binding agents and uses thereof |
| 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 |
| US10202643B2 (en) | 2011-10-31 | 2019-02-12 | University Of Utah Research Foundation | Genetic alterations in glioma |
| JP2015502958A (ja) * | 2011-12-09 | 2015-01-29 | 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 | がんの処置のための併用療法 |
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| 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 |
| EP3478674B1 (en) | 2016-06-30 | 2020-05-13 | Gilead Sciences, Inc. | 4,6-diaminoquinazolines as cot modulators and methods of use thereof |
| US12158399B2 (en) | 2016-08-05 | 2024-12-03 | 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 |
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| EP3703742A4 (en) * | 2017-11-02 | 2022-03-09 | 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 |
| WO2020097398A1 (en) | 2018-11-07 | 2020-05-14 | Dana-Farber Cancer Institute, Inc. | Benzothiazole derivatives and 7-aza-benzothiazole 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 |
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| TWI770527B (zh) | 2019-06-14 | 2022-07-11 | 美商基利科學股份有限公司 | Cot 調節劑及其使用方法 |
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-
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- 2011-03-09 CN CN2011800231091A patent/CN103038364A/zh active Pending
- 2011-03-09 BR BR112012022801A patent/BR112012022801B8/pt not_active IP Right Cessation
- 2011-03-09 MX MX2012010420A patent/MX343368B/es active IP Right Grant
- 2011-03-09 KR KR1020127025801A patent/KR20120139767A/ko not_active Abandoned
- 2011-03-09 EP EP11709278.3A patent/EP2545187B1/en active Active
- 2011-03-09 US US13/583,056 patent/US20130059851A1/en not_active Abandoned
- 2011-03-09 WO PCT/US2011/027689 patent/WO2011112678A1/en not_active Ceased
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- 2011-03-09 EA EA201290883A patent/EA030276B1/ru not_active IP Right Cessation
- 2011-03-09 AU AU2011224410A patent/AU2011224410B2/en not_active Ceased
- 2011-03-09 JP JP2012557201A patent/JP5985401B2/ja active Active
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