JP6389529B2 - 癌の治療のためのＲＡＦ阻害剤としての１−（５−ｔｅｒｔ−ブチル−２−アリール−ピラゾール−３−イル）−３−［２−フルオロ−４−［３−オキソ−４Ｈ−ピリド［２，３−ｂ］ピラジン−８−イル）オキシ］フェニル］尿素誘導体 - Google Patents
癌の治療のためのＲＡＦ阻害剤としての１−（５−ｔｅｒｔ−ブチル−２−アリール−ピラゾール−３−イル）−３−［２−フルオロ−４−［３−オキソ−４Ｈ−ピリド［２，３−ｂ］ピラジン−８−イル）オキシ］フェニル］尿素誘導体 Download PDFInfo
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- JP6389529B2 JP6389529B2 JP2016554928A JP2016554928A JP6389529B2 JP 6389529 B2 JP6389529 B2 JP 6389529B2 JP 2016554928 A JP2016554928 A JP 2016554928A JP 2016554928 A JP2016554928 A JP 2016554928A JP 6389529 B2 JP6389529 B2 JP 6389529B2
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- CMVWUUGCHTXFDO-UHFFFAOYSA-N Cc1ccnc(N2)c1N=CC2=O Chemical compound Cc1ccnc(N2)c1N=CC2=O CMVWUUGCHTXFDO-UHFFFAOYSA-N 0.000 description 2
- MXZMACXOMZKYHJ-UHFFFAOYSA-N CC(C)(C)C(CC#N)=O Chemical compound CC(C)(C)C(CC#N)=O MXZMACXOMZKYHJ-UHFFFAOYSA-N 0.000 description 1
- 0 CC(C)(C)OC(Nc(ccc(Oc1c(*)c(N)ncc1)c1)c1F)=O Chemical compound CC(C)(C)OC(Nc(ccc(Oc1c(*)c(N)ncc1)c1)c1F)=O 0.000 description 1
- LYDSVUNKBRBKNB-UHFFFAOYSA-N CC(C)(C)OC(Nc(ccc(Oc1ccnc(N2)c1N=CC2=O)c1)c1F)=O Chemical compound CC(C)(C)OC(Nc(ccc(Oc1ccnc(N2)c1N=CC2=O)c1)c1F)=O LYDSVUNKBRBKNB-UHFFFAOYSA-N 0.000 description 1
- FAOLXHKERQXRDG-UHFFFAOYSA-N CC(C)(C)OC(Nc(ccc(Oc1ccnc(N=C2)c1NC2=O)c1)c1F)=O Chemical compound CC(C)(C)OC(Nc(ccc(Oc1ccnc(N=C2)c1NC2=O)c1)c1F)=O FAOLXHKERQXRDG-UHFFFAOYSA-N 0.000 description 1
- CGOZYYXGKRKZRR-UHFFFAOYSA-N CC(C)(C)c(cc1C(O)=O)n[n]1-c1cc(F)ccc1 Chemical compound CC(C)(C)c(cc1C(O)=O)n[n]1-c1cc(F)ccc1 CGOZYYXGKRKZRR-UHFFFAOYSA-N 0.000 description 1
- QOVGZKZWSXKFGS-UHFFFAOYSA-N CC(C)(C)c(cc1C(O)=O)n[n]1-c1cc(OC)ccc1 Chemical compound CC(C)(C)c(cc1C(O)=O)n[n]1-c1cc(OC)ccc1 QOVGZKZWSXKFGS-UHFFFAOYSA-N 0.000 description 1
- NGHFJTIJKWYHAD-UHFFFAOYSA-N CC(C)(C)c(cc1NC(Nc(ccc(Oc2ccnc(C3NC33)c2N=CC3=O)c2)c2F)=O)n[n]1-c1cccc(F)c1 Chemical compound CC(C)(C)c(cc1NC(Nc(ccc(Oc2ccnc(C3NC33)c2N=CC3=O)c2)c2F)=O)n[n]1-c1cccc(F)c1 NGHFJTIJKWYHAD-UHFFFAOYSA-N 0.000 description 1
- FQXUZMBHYALYGP-UHFFFAOYSA-N CC(C)(C)c(cc1NC(Oc2ccccc2)=O)n[n]1-c1cc(F)ccc1 Chemical compound CC(C)(C)c(cc1NC(Oc2ccccc2)=O)n[n]1-c1cc(F)ccc1 FQXUZMBHYALYGP-UHFFFAOYSA-N 0.000 description 1
- WRSYDCVUFQRYLC-UHFFFAOYSA-N C[NH+]([N](C)(C)I)[O-] Chemical compound C[NH+]([N](C)(C)I)[O-] WRSYDCVUFQRYLC-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/04—Artificial tears; Irrigation solutions
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- A—HUMAN NECESSITIES
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
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- Ophthalmology & Optometry (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Cardiology (AREA)
- Communicable Diseases (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Virology (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Otolaryngology (AREA)
- Immunology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB1320729.5A GB201320729D0 (en) | 2013-11-25 | 2013-11-25 | Therapeutic compounds and their use |
| GB1320729.5 | 2013-11-25 | ||
| PCT/GB2014/053490 WO2015075483A1 (en) | 2013-11-25 | 2014-11-25 | 1 -(5-tert-butyl-2-aryl-pyrazol-3-yl)-3-[2-fluoro-4-[(3-oxo-4h-pyrido[2, 3-b]pyrazin-8-yl)oxy]phenyl]urea derivatives as raf inhibitors for the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016538345A JP2016538345A (ja) | 2016-12-08 |
| JP2016538345A5 JP2016538345A5 (enExample) | 2017-12-28 |
| JP6389529B2 true JP6389529B2 (ja) | 2018-09-12 |
Family
ID=49918123
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016554928A Active JP6389529B2 (ja) | 2013-11-25 | 2014-11-25 | 癌の治療のためのＲＡＦ阻害剤としての１−（５−ｔｅｒｔ−ブチル−２−アリール−ピラゾール−３−イル）−３−［２−フルオロ−４−［３−オキソ−４Ｈ−ピリド［２，３−ｂ］ピラジン−８−イル）オキシ］フェニル］尿素誘導体 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US9725447B2 (enExample) |
| EP (1) | EP3074396B1 (enExample) |
| JP (1) | JP6389529B2 (enExample) |
| KR (1) | KR102327096B1 (enExample) |
| CN (1) | CN105793260B (enExample) |
| AU (1) | AU2014351571B2 (enExample) |
| BR (1) | BR112016011078B1 (enExample) |
| CA (1) | CA2928009C (enExample) |
| DK (1) | DK3074396T3 (enExample) |
| EA (1) | EA034216B1 (enExample) |
| ES (1) | ES2740325T3 (enExample) |
| GB (1) | GB201320729D0 (enExample) |
| HU (1) | HUE045596T2 (enExample) |
| IL (1) | IL245062B (enExample) |
| MX (1) | MX372942B (enExample) |
| PL (1) | PL3074396T3 (enExample) |
| PT (1) | PT3074396T (enExample) |
| SA (1) | SA516371189B1 (enExample) |
| WO (1) | WO2015075483A1 (enExample) |
Families Citing this family (62)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0821227A2 (pt) | 2007-12-19 | 2015-06-16 | Cancer Rec Tech Ltd | Composto, composição farmacêutica, método para preparar a mesma, uso de um composto, método para tratar uma doença ou distúrbio, para inibir função de raf e para inibir proliferação celular, inibir progressão do ciclo celular, promover apoptose, ou uma combinação de um ou mais dos mesmos |
| EP2531502B1 (en) | 2010-02-01 | 2014-04-02 | Cancer Research Technology Limited | 1-(5-tert-butyl-2-phenyl-2h-pyrazol-3-yl)-3-[2-fluoro-4-(1-methyl-2-oxo-2,3-dihydro-1h-imidazo[4,5-b]pyridin-7-yloxy)-phenyl]-urea and related compounds and their use in therapy |
| GB201320729D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Therapeutic compounds and their use |
| GB201320732D0 (en) | 2013-11-25 | 2014-01-08 | Cancer Rec Tech Ltd | Methods of chemical synthesis |
| IL258521B2 (en) * | 2015-10-08 | 2024-01-01 | Macrogenics Inc | Combination therapy for the treatment of cancer |
| WO2017136741A1 (en) * | 2016-02-05 | 2017-08-10 | Evol Science LLC | Combinations to treat cancer |
| US12042477B2 (en) | 2016-02-23 | 2024-07-23 | Cancer Research Technology Limited | Dietary product devoid of at least two non essential amino acids |
| MX2018012471A (es) | 2016-04-15 | 2019-02-21 | Genentech Inc | Metodos de diagnostico y terapeuticos para el cancer. |
| KR101796684B1 (ko) * | 2016-05-19 | 2017-11-10 | 건국대학교 산학협력단 | 케라틴 8 인산화 억제제를 포함하는 황반변성 예방 또는 치료용 약학 조성물 및 황반변성 치료제의 스크리닝 방법 |
| EP3558955B1 (en) | 2016-12-22 | 2021-08-11 | Amgen Inc. | Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
| WO2018134254A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| CA3051986A1 (en) * | 2017-02-10 | 2018-08-16 | Novartis Ag | 1-(4-amino-5-bromo-6-(1 h-pyrazol-1-yl)pyrimidin-2-yl)-1 h-pyrazol-4-ol and use thereof in the treatment of cancer |
| CN106986860A (zh) * | 2017-05-19 | 2017-07-28 | 南京大学 | 一类含酰胺键的吡唑类抗肿瘤化合物的设计、合成 |
| JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| CN111065414A (zh) * | 2017-08-07 | 2020-04-24 | 埃沃尔科学有限责任公司 | 用以治疗癌症的组合 |
| TW202428305A (zh) | 2017-09-08 | 2024-07-16 | 美商建南德克公司 | 癌症之診斷及治療方法 |
| EP3679040B1 (en) * | 2017-09-08 | 2022-08-03 | Amgen Inc. | Inhibitors of kras g12c and methods of using the same |
| WO2019084030A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HYDROXAMATE COMPOUNDS AND METHODS OF USE |
| WO2019084026A1 (en) | 2017-10-24 | 2019-05-02 | Genentech, Inc. | (4-HYDROXYPYRROLIDIN-2-YL) -HETEROCYCLIC COMPOUNDS AND METHODS OF USE |
| EP3709991A1 (en) | 2017-11-13 | 2020-09-23 | Greg Hannon | Dietary product |
| US20210008047A1 (en) | 2018-02-13 | 2021-01-14 | Vib Vzw | Targeting minimal residual disease in cancer with rxr antagonists |
| WO2019183523A1 (en) | 2018-03-23 | 2019-09-26 | Genentech, Inc. | Hetero-bifunctional degrader compounds and their use as modulators of targeted ubiquination (vhl) |
| ES2995514T3 (en) | 2018-05-04 | 2025-02-10 | Amgen Inc | Kras g12c inhibitors and methods of using the same |
| AU2019262589B2 (en) | 2018-05-04 | 2022-07-07 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| WO2019211809A1 (en) * | 2018-05-04 | 2019-11-07 | Universidade Do Porto | Chemiluminescent imidazopyrazinone-based photosensitizers with available singlet and triplet excited states |
| MX2020011907A (es) | 2018-05-10 | 2021-01-29 | Amgen Inc | Inhibidores de kras g12c para el tratamiento de cancer. |
| ES2938987T3 (es) | 2018-06-01 | 2023-04-18 | Amgen Inc | Inhibidores de KRAS G12c y métodos de uso de los mismos |
| GB201809295D0 (en) | 2018-06-06 | 2018-07-25 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| CA3100390A1 (en) | 2018-06-12 | 2020-03-12 | Amgen Inc. | Kras g12c inhibitors encompassing piperazine ring and use thereof in the treatment of cancer |
| GB201818649D0 (en) | 2018-11-15 | 2019-01-02 | Univ Sheffield | Compounds |
| GB201818651D0 (en) | 2018-11-15 | 2019-01-02 | Univ Sheffield | Compounds |
| GB201818750D0 (en) | 2018-11-16 | 2019-01-02 | Institute Of Cancer Res Royal Cancer Hospital | Lox inhibitors |
| JP7516029B2 (ja) | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Ｋｒａｓ ｇ１２ｃ阻害剤化合物の重要な中間体の改良合成法 |
| WO2020106640A1 (en) | 2018-11-19 | 2020-05-28 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのｋｒａｓｇ１２ｃ阻害剤及び１種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| CA3128064A1 (en) * | 2019-02-01 | 2020-08-06 | Glaxosmithkline Intellectual Property Development Limited | Combination treatments for cancer comprising belantamab mafodotin and an anti ox40 antibody and uses and methods thereof |
| KR102192576B1 (ko) * | 2019-03-21 | 2020-12-17 | 경북대학교 산학협력단 | 다브라페닙을 유효성분으로 포함하는 알레르기 질환 예방, 치료 또는 개선용 조성물 |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| PH12021552922A1 (en) | 2019-05-21 | 2022-04-04 | Amgen Inc | Solid state forms |
| EP3999057A1 (en) | 2019-07-19 | 2022-05-25 | Anagenesis Biotechnologies Sas | Polyaromatic urea derivatives and their use in the treatment of muscle diseases |
| WO2021142144A1 (en) | 2020-01-10 | 2021-07-15 | Immuneering Corporation | Mek inhibitors and therapeutic uses thereof |
| JP2023530235A (ja) | 2020-06-03 | 2023-07-14 | フェス・セラピューティクス，インコーポレーテッド | 個別化された処置方法のための製剤 |
| JP2023528930A (ja) | 2020-06-04 | 2023-07-06 | フェス・セラピューティクス，インコーポレーテッド | がんを処置する個別化された方法 |
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| CN105793260B (zh) | 2018-04-10 |
| BR112016011078B1 (pt) | 2022-12-06 |
| PL3074396T3 (pl) | 2019-11-29 |
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| EP3074396A1 (en) | 2016-10-05 |
| CA2928009C (en) | 2022-08-30 |
| BR112016011078A8 (pt) | 2020-04-22 |
| KR102327096B1 (ko) | 2021-11-16 |
| MX372942B (es) | 2020-04-03 |
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