JP2015513901A5 - - Google Patents
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- 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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| EP (3) | EP3693741B1 (cg-RX-API-DMAC7.html) |
| JP (3) | JP6348898B2 (cg-RX-API-DMAC7.html) |
| KR (1) | KR20140139510A (cg-RX-API-DMAC7.html) |
| CN (1) | CN104204806B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2013240483B2 (cg-RX-API-DMAC7.html) |
| BR (1) | BR112014023496A2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2864169A1 (cg-RX-API-DMAC7.html) |
| EA (1) | EA028135B1 (cg-RX-API-DMAC7.html) |
| ES (3) | ES2790896T3 (cg-RX-API-DMAC7.html) |
| MX (1) | MX351945B (cg-RX-API-DMAC7.html) |
| PL (1) | PL2831589T3 (cg-RX-API-DMAC7.html) |
| PT (1) | PT2831589T (cg-RX-API-DMAC7.html) |
| TR (1) | TR201808010T4 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2013148100A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BR112014023496A2 (pt) * | 2012-03-28 | 2017-07-18 | Dana Farber Cancer Inst Inc | mutantes c-raf que conferem resistência a inibidores de raf |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | 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 |
| US20060234931A1 (en) | 2003-07-17 | 2006-10-19 | Biggs William H Iii | Treatment of diseases with kinase inhibitors |
| JP2007507204A (ja) | 2003-07-29 | 2007-03-29 | ブリストル−マイヤーズ スクイブ カンパニー | サイクリン依存性キナーゼモデュレーションのバイオマーカー |
| ES2385613T3 (es) | 2006-09-18 | 2012-07-27 | Boehringer Ingelheim International Gmbh | Método para tratar cánceres que portan mutaciones de EGFR |
| 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 |
| EP2102362B1 (en) * | 2006-11-16 | 2012-07-04 | Mount Sinai School of Medicine of New York University | Compositions and methods for detecting noonan syndrome |
| EP2370568B1 (en) | 2008-12-10 | 2017-07-19 | Dana-Farber Cancer Institute, Inc. | Mek mutations conferring resistance to mek inhibitors |
| AR077975A1 (es) | 2009-08-28 | 2011-10-05 | Irm Llc | Derivados de pirazol pirimidina y composiciones como inhibidores de cinasa de proteina |
| JP5985401B2 (ja) | 2010-03-09 | 2016-09-06 | 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 | 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 |
| BR112014023496A2 (pt) * | 2012-03-28 | 2017-07-18 | Dana Farber Cancer Inst Inc | mutantes c-raf que conferem resistência a inibidores de raf |
-
2013
- 2013-03-07 BR BR112014023496A patent/BR112014023496A2/pt not_active IP Right Cessation
- 2013-03-07 AU AU2013240483A patent/AU2013240483B2/en not_active Ceased
- 2013-03-07 EA EA201491780A patent/EA028135B1/ru not_active IP Right Cessation
- 2013-03-07 CN CN201380014747.6A patent/CN104204806B/zh active Active
- 2013-03-07 MX MX2014011686A patent/MX351945B/es active IP Right Grant
- 2013-03-07 EP EP20159381.1A patent/EP3693741B1/en active Active
- 2013-03-07 ES ES18153021T patent/ES2790896T3/es active Active
- 2013-03-07 ES ES13710263.8T patent/ES2673070T3/es active Active
- 2013-03-07 KR KR1020147026716A patent/KR20140139510A/ko not_active Ceased
- 2013-03-07 EP EP13710263.8A patent/EP2831589B1/en active Active
- 2013-03-07 TR TR2018/08010T patent/TR201808010T4/tr unknown
- 2013-03-07 ES ES20159381T patent/ES2908078T3/es active Active
- 2013-03-07 CA CA2864169A patent/CA2864169A1/en not_active Abandoned
- 2013-03-07 US US14/387,735 patent/US9629839B2/en active Active
- 2013-03-07 EP EP18153021.3A patent/EP3333575B1/en active Active
- 2013-03-07 WO PCT/US2013/029513 patent/WO2013148100A1/en not_active Ceased
- 2013-03-07 PT PT137102638T patent/PT2831589T/pt unknown
- 2013-03-07 PL PL13710263T patent/PL2831589T3/pl unknown
- 2013-03-07 JP JP2015503230A patent/JP6348898B2/ja active Active
-
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
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