JP2015513901A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2015513901A5 JP2015513901A5 JP2015503230A JP2015503230A JP2015513901A5 JP 2015513901 A5 JP2015513901 A5 JP 2015513901A5 JP 2015503230 A JP2015503230 A JP 2015503230A JP 2015503230 A JP2015503230 A JP 2015503230A JP 2015513901 A5 JP2015513901 A5 JP 2015513901A5
- Authority
- JP
- Japan
- Prior art keywords
- raf
- cancer
- polypeptide
- inhibitor
- nucleic acid
- 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
- 101710141955 RAF proto-oncogene serine/threonine-protein kinase Proteins 0.000 claims 25
- 229920001184 polypeptide Polymers 0.000 claims 25
- 102000004196 processed proteins & peptides Human genes 0.000 claims 25
- 108090000765 processed proteins & peptides Proteins 0.000 claims 25
- 238000000034 method Methods 0.000 claims 16
- 102000039446 nucleic acids Human genes 0.000 claims 16
- 108020004707 nucleic acids Proteins 0.000 claims 16
- 150000007523 nucleic acids Chemical class 0.000 claims 16
- 239000003112 inhibitor Substances 0.000 claims 15
- 102100025093 Zinc fingers and homeoboxes protein 2 Human genes 0.000 claims 14
- 206010028980 Neoplasm Diseases 0.000 claims 13
- 201000011510 cancer Diseases 0.000 claims 12
- 125000003275 alpha amino acid group Chemical group 0.000 claims 11
- 238000006467 substitution reaction Methods 0.000 claims 10
- -1 pyrimidin-2-ylamino Chemical group 0.000 claims 8
- 150000001413 amino acids Chemical class 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 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 6
- 229960003862 vemurafenib Drugs 0.000 claims 6
- 229940124647 MEK inhibitor Drugs 0.000 claims 5
- 125000000539 amino acid group Chemical group 0.000 claims 5
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 5
- 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 4
- 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 4
- GFMMXOIFOQCCGU-UHFFFAOYSA-N 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide Chemical group C=1C=C(I)C=C(Cl)C=1NC1=C(F)C(F)=CC=C1C(=O)NOCC1CC1 GFMMXOIFOQCCGU-UHFFFAOYSA-N 0.000 claims 4
- 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 4
- 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 4
- 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 4
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 4
- 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 4
- 201000001441 melanoma Diseases 0.000 claims 4
- RUZLIIJDZBWWSA-INIZCTEOSA-N methyl 2-[[(1s)-1-(7-methyl-2-morpholin-4-yl-4-oxopyrido[1,2-a]pyrimidin-9-yl)ethyl]amino]benzoate Chemical group COC(=O)C1=CC=CC=C1N[C@@H](C)C1=CC(C)=CN2C(=O)C=C(N3CCOCC3)N=C12 RUZLIIJDZBWWSA-INIZCTEOSA-N 0.000 claims 4
- 239000002773 nucleotide Substances 0.000 claims 4
- 125000003729 nucleotide group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 229960003787 sorafenib Drugs 0.000 claims 4
- HHVIBTZHLRERCL-UHFFFAOYSA-N sulfonyldimethane Chemical compound CS(C)(=O)=O HHVIBTZHLRERCL-UHFFFAOYSA-N 0.000 claims 4
- KNTZCGBYFGEMFR-UHFFFAOYSA-N (propan-2-ylazaniumyl)formate Chemical compound CC(C)NC(O)=O KNTZCGBYFGEMFR-UHFFFAOYSA-N 0.000 claims 3
- 230000035772 mutation Effects 0.000 claims 3
- QFWCYNPOPKQOKV-UHFFFAOYSA-N 2-(2-amino-3-methoxyphenyl)chromen-4-one Chemical compound COC1=CC=CC(C=2OC3=CC=CC=C3C(=O)C=2)=C1N QFWCYNPOPKQOKV-UHFFFAOYSA-N 0.000 claims 2
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 2
- XXSSGBYXSKOLAM-UHFFFAOYSA-N 5-bromo-n-(2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodoanilino)benzamide Chemical compound OCC(O)CONC(=O)C1=CC(Br)=C(F)C(F)=C1NC1=CC=C(I)C=C1F XXSSGBYXSKOLAM-UHFFFAOYSA-N 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 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
- 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
- 102000018471 Proto-Oncogene Proteins B-raf Human genes 0.000 claims 2
- 108010091528 Proto-Oncogene Proteins B-raf Proteins 0.000 claims 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 2
- 125000003368 amide group Chemical group 0.000 claims 2
- 230000001419 dependent effect Effects 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 239000013604 expression vector Substances 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 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 2
- 208000011932 ovarian sarcoma Diseases 0.000 claims 2
- 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 2
- 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 2
- 201000002510 thyroid cancer Diseases 0.000 claims 2
- 150000001408 amides Chemical class 0.000 claims 1
- 238000002648 combination therapy Methods 0.000 claims 1
- OVPLZYJGTGDFNB-UHFFFAOYSA-N propan-2-yl carbamate Chemical compound CC(C)OC(N)=O OVPLZYJGTGDFNB-UHFFFAOYSA-N 0.000 claims 1
- 238000012163 sequencing technique Methods 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261616999P | 2012-03-28 | 2012-03-28 | |
| US61/616,999 | 2012-03-28 | ||
| US201261708372P | 2012-10-01 | 2012-10-01 | |
| US61/708,372 | 2012-10-01 | ||
| PCT/US2013/029513 WO2013148100A1 (en) | 2012-03-28 | 2013-03-07 | C-raf mutants that confer resistance to raf inhibitors |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018048824A Division JP6661685B2 (ja) | 2012-03-28 | 2018-03-16 | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015513901A JP2015513901A (ja) | 2015-05-18 |
| JP2015513901A5 true JP2015513901A5 (enExample) | 2016-04-21 |
| JP6348898B2 JP6348898B2 (ja) | 2018-06-27 |
Family
ID=47892065
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503230A Active JP6348898B2 (ja) | 2012-03-28 | 2013-03-07 | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
| JP2018048824A Active JP6661685B2 (ja) | 2012-03-28 | 2018-03-16 | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
| JP2020019636A Pending JP2020103291A (ja) | 2012-03-28 | 2020-02-07 | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018048824A Active JP6661685B2 (ja) | 2012-03-28 | 2018-03-16 | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
| JP2020019636A Pending JP2020103291A (ja) | 2012-03-28 | 2020-02-07 | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
Country Status (15)
| Country | Link |
|---|---|
| US (6) | US9629839B2 (enExample) |
| EP (3) | EP3333575B1 (enExample) |
| JP (3) | JP6348898B2 (enExample) |
| KR (1) | KR20140139510A (enExample) |
| CN (1) | CN104204806B (enExample) |
| AU (1) | AU2013240483B2 (enExample) |
| BR (1) | BR112014023496A2 (enExample) |
| CA (1) | CA2864169A1 (enExample) |
| EA (1) | EA028135B1 (enExample) |
| ES (3) | ES2673070T3 (enExample) |
| MX (1) | MX351945B (enExample) |
| PL (1) | PL2831589T3 (enExample) |
| PT (1) | PT2831589T (enExample) |
| TR (1) | TR201808010T4 (enExample) |
| WO (1) | WO2013148100A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6348898B2 (ja) * | 2012-03-28 | 2018-06-27 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
| WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| KR102537840B1 (ko) | 2018-07-13 | 2023-05-31 | 삼성전자 주식회사 | 서버 장치 및 다른 장치들의 위치 정보를 수집하는 방법 |
| WO2020163771A1 (en) * | 2019-02-08 | 2020-08-13 | Portage Glasgow Limited | Structure, manufacturing and uses of hoxd12-pde8a cell-penetrating peptides |
| WO2021225980A1 (en) * | 2020-05-04 | 2021-11-11 | Dna-Seq, Inc. | Methods and systems for determination of an effective therapeutic regimen and drug discovery |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5618670A (en) * | 1988-08-26 | 1997-04-08 | The United States Of America As Represented By The Department Of Health & Human Services | Detection method for c-raf-1 genes |
| WO2005009367A2 (en) * | 2003-07-17 | 2005-02-03 | Ambit Biosciences Corporation | Treatment of diseases with kinase inhibitors |
| CA2533803A1 (en) | 2003-07-29 | 2005-02-10 | Bristol-Myers Squibb Company | Biomarkers of cyclin-dependent kinase modulation |
| CN101516376A (zh) * | 2006-09-18 | 2009-08-26 | 贝林格尔.英格海姆国际有限公司 | 用于治疗携带egfr突变的癌症的方法 |
| SI2068880T1 (sl) * | 2006-09-18 | 2012-08-31 | Boehringer Ingelheim Int | Postopek za zdravljenje raka, ki vsebuje mutacije EGFR |
| EP2102362B1 (en) * | 2006-11-16 | 2012-07-04 | Mount Sinai School of Medicine of New York University | Compositions and methods for detecting noonan syndrome |
| WO2010068738A1 (en) | 2008-12-10 | 2010-06-17 | Dana-Farber Cancer Institute, Inc. | Mek mutations conferring resistance to mek inhibitors |
| JO3002B1 (ar) | 2009-08-28 | 2016-09-05 | Irm Llc | مركبات و تركيبات كمثبطات كيناز بروتين |
| AU2011224410B2 (en) * | 2010-03-09 | 2015-05-28 | Dana-Farber Cancer Institute, Inc. | Methods of diagnosing and treating cancer in patients having or developing resistance to a first cancer therapy |
| JP6348898B2 (ja) * | 2012-03-28 | 2018-06-27 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ｒａｆ阻害剤に対する耐性を付与するｃ−ｒａｆ突然変異体 |
-
2013
- 2013-03-07 JP JP2015503230A patent/JP6348898B2/ja active Active
- 2013-03-07 WO PCT/US2013/029513 patent/WO2013148100A1/en not_active Ceased
- 2013-03-07 CA CA2864169A patent/CA2864169A1/en not_active Abandoned
- 2013-03-07 ES ES13710263.8T patent/ES2673070T3/es active Active
- 2013-03-07 PT PT137102638T patent/PT2831589T/pt unknown
- 2013-03-07 ES ES20159381T patent/ES2908078T3/es active Active
- 2013-03-07 BR BR112014023496A patent/BR112014023496A2/pt not_active IP Right Cessation
- 2013-03-07 US US14/387,735 patent/US9629839B2/en active Active
- 2013-03-07 CN CN201380014747.6A patent/CN104204806B/zh active Active
- 2013-03-07 AU AU2013240483A patent/AU2013240483B2/en not_active Ceased
- 2013-03-07 EP EP18153021.3A patent/EP3333575B1/en active Active
- 2013-03-07 EP EP20159381.1A patent/EP3693741B1/en active Active
- 2013-03-07 TR TR2018/08010T patent/TR201808010T4/tr unknown
- 2013-03-07 EP EP13710263.8A patent/EP2831589B1/en active Active
- 2013-03-07 PL PL13710263T patent/PL2831589T3/pl unknown
- 2013-03-07 EA EA201491780A patent/EA028135B1/ru not_active IP Right Cessation
- 2013-03-07 KR KR1020147026716A patent/KR20140139510A/ko not_active Ceased
- 2013-03-07 ES ES18153021T patent/ES2790896T3/es active Active
- 2013-03-07 MX MX2014011686A patent/MX351945B/es active IP Right Grant
-
2017
- 2017-03-29 US US15/472,934 patent/US20170204383A1/en not_active Abandoned
-
2018
- 2018-03-16 JP JP2018048824A patent/JP6661685B2/ja active Active
-
2019
- 2019-01-23 US US16/255,251 patent/US20190142830A1/en not_active Abandoned
-
2020
- 2020-02-07 JP JP2020019636A patent/JP2020103291A/ja active Pending
-
2021
- 2021-08-11 US US17/399,563 patent/US11788151B2/en active Active
-
2023
- 2023-09-11 US US18/464,360 patent/US12146196B2/en active Active
-
2024
- 2024-10-14 US US18/914,634 patent/US20250034652A1/en active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Patel et al. | Clinical responses to selumetinib (AZD6244; ARRY‐142886)‐based combination therapy stratified by gene mutations in patients with metastatic melanoma | |
| Usman et al. | Major molecular signaling pathways in oral cancer associated with therapeutic resistance | |
| JP2015513901A5 (enExample) | ||
| Spagnolo et al. | Upcoming strategies for the treatment of metastatic melanoma | |
| Okayama et al. | NOS2 enhances KRAS‐induced lung carcinogenesis, inflammation and microRNA‐21 expression | |
| JP2017513908A5 (enExample) | ||
| RU2017120287A (ru) | ОТБОР БОЛЬНЫХ РАКОМ ДЛЯ ВВЕДЕНИЯ ИНГИБИТОРОВ СИГНАЛЬНОГО ПУТИ Wnt НА ОСНОВАНИИ СТАТУСА МУТАЦИИ RNF43 | |
| JP2015530080A5 (enExample) | ||
| Ali et al. | PD-1 blockade and CDK4/6 inhibition augment nonoverlapping features of T cell activation in cancer | |
| MX2012009030A (es) | Identificacion de mutacion lkb1 como biomarcador predictivo para sensibilidad a inhibidores de tor cinasa. | |
| Cucurull et al. | Targeting KRAS in lung cancer beyond KRAS G12C inhibitors: the immune regulatory role of KRAS and novel therapeutic strategies | |
| JP2017516458A5 (enExample) | ||
| JP2011505414A5 (enExample) | ||
| EA201401353A1 (ru) | Биомаркеры для определения эффективной ответной реакции на лечение пациентов с гепатоцеллюлярной карциномой (гцк) | |
| Kato et al. | Lactate dehydrogenase and hemolysis in sickle cell disease | |
| Draenert et al. | The prevalence of tooth hypersensitivity following periodontal therapy with special reference to root scaling. A systematic review of the literature. | |
| Mangana et al. | Multicenter, real-life experience with checkpoint inhibitors and targeted therapy agents in advanced melanoma patients in Switzerland | |
| US11136625B2 (en) | Gene expression signatures predictive of subject response to a multi-kinase inhibitor and methods of using the same | |
| Bruckman et al. | Mutational analyses of the BRAF, KRAS, and PIK3CA genes in oral squamous cell carcinoma | |
| JP2014531020A5 (enExample) | ||
| Jakobsen et al. | Review on clinical trials of targeted treatments in malignant mesothelioma | |
| Jing et al. | Down-expression of miR-373 predicts poor prognosis of glioma and could be a potential therapeutic target | |
| Zibelman et al. | Integrating immunotherapy into the management of renal cell carcinoma | |
| Bernardi et al. | Outcome of trimodal therapy in elderly patients with esophageal cancer: prognostic value of the Charlson comorbidity index | |
| Tan et al. | LncRNA SBF2-AS1: A budding star in various cancers |