CN107835811A - 苯胺嘧啶衍生物及其用途 - Google Patents
苯胺嘧啶衍生物及其用途 Download PDFInfo
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- CN107835811A CN107835811A CN201680041201.3A CN201680041201A CN107835811A CN 107835811 A CN107835811 A CN 107835811A CN 201680041201 A CN201680041201 A CN 201680041201A CN 107835811 A CN107835811 A CN 107835811A
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- methyl
- amino
- compound
- pyrimidine
- imidazoles
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- 125000001493 tyrosinyl group Chemical group [H]OC1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- LSGOVYNHVSXFFJ-UHFFFAOYSA-N vanadate(3-) Chemical compound [O-][V]([O-])([O-])=O LSGOVYNHVSXFFJ-UHFFFAOYSA-N 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 238000010792 warming Methods 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000000080 wetting agent Substances 0.000 description 1
Classifications
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
本公开涉及作为EGFR抑制剂的苯胺嘧啶衍生物或其药学上可接受的盐，具体涉及式（Ⅰ）所示化合物或其药学上可接受的盐、其药物组合物、及其用于治疗EGFR介导的疾病的方法和用途。
Description
PCT国内申请，说明书已公开。
Claims (12)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201510419018X | 2015-07-16 | ||
| CN201510419018 | 2015-07-16 | ||
| PCT/CN2016/090149 WO2017008761A1 (zh) | 2015-07-16 | 2016-07-15 | 苯胺嘧啶衍生物及其用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN107835811A true CN107835811A (zh) | 2018-03-23 |
| CN107835811B CN107835811B (zh) | 2019-11-08 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680041201.3A Active CN107835811B (zh) | 2015-07-16 | 2016-07-15 | 苯胺嘧啶衍生物及其用途 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US10329277B2 (zh) |
| EP (1) | EP3323817B1 (zh) |
| JP (1) | JP6970081B2 (zh) |
| KR (1) | KR102666414B1 (zh) |
| CN (1) | CN107835811B (zh) |
| AU (1) | AU2016292450B2 (zh) |
| CA (1) | CA2992317A1 (zh) |
| RU (1) | RU2734849C2 (zh) |
| TW (1) | TWI739753B (zh) |
| WO (1) | WO2017008761A1 (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114026090A (zh) * | 2019-07-04 | 2022-02-08 | 微境生物医药科技(上海)有限公司 | 一类抑制egfr激酶的化合物及其制备方法和用途 |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK3205650T3 (da) * | 2014-10-11 | 2021-09-13 | Shanghai Hansoh Biomedical Co Ltd | Egfr-hæmmer og fremstilling og anvendelse deraf |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技（上海）有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| JP2019501222A (ja) | 2016-01-07 | 2019-01-17 | シーエス ファーマテック リミテッド | Ｅｇｆｒチロシンキナーゼの臨床的に重要な変異体の選択的阻害薬 |
| CN107540661A (zh) * | 2016-06-24 | 2018-01-05 | 正大天晴药业集团股份有限公司 | 作为egfr抑制剂的苯胺嘧啶化合物的结晶 |
| SI3943491T1 (sl) | 2019-03-19 | 2025-08-29 | Voronoi Inc. | Heteroarilni derivat, postopek za njegovo proizvodnjo in farmacevtski sestavek, ki ga obsega kot učinkovito komponento |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| JP2022526713A (ja) | 2019-03-21 | 2022-05-26 | オンクセオ | がんの処置のための、キナーゼ阻害剤と組み合わせたＤｂａｉｔ分子 |
| US12523663B2 (en) | 2019-06-04 | 2026-01-13 | Inserm (Institut National De La Santé Et De La Rescherche Médicale) | Use of CD9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
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| WO2011140338A1 (en) * | 2010-05-05 | 2011-11-10 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| CN103702990A (zh) * | 2011-07-27 | 2014-04-02 | 阿斯利康(瑞典)有限公司 | 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症 |
| CN105085489A (zh) * | 2014-11-05 | 2015-11-25 | 上海页岩科技有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| CN106117185A (zh) * | 2015-08-31 | 2016-11-16 | 广州科擎新药开发有限公司 | 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用 |
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| AU770600B2 (en) | 1999-10-07 | 2004-02-26 | Amgen, Inc. | Triazine kinase inhibitors |
| US20030004174A9 (en) * | 2000-02-17 | 2003-01-02 | Armistead David M. | Kinase inhibitors |
| GT200500284A (es) * | 2004-10-15 | 2006-03-27 | Aventis Pharma Inc | Pirimidinas como antagonistas del receptor de prostaglandina d2 |
| WO2011053476A1 (en) * | 2009-11-02 | 2011-05-05 | Abbott Laboratories | Imidazopyridines as a novel scaffold for multi-targeted kinase inhibition |
| RU2012120784A (ru) * | 2009-11-12 | 2013-12-20 | Селвита С.А. | Соединение, способ его получения, фармацевтическая композиция, применение соединения, способ модулирования или регулирования сериновых/треониновых киназ и средство, модулирующее сериновые/треониновые киназы |
| CN104761544B (zh) * | 2014-01-03 | 2019-03-15 | 北京轩义医药科技有限公司 | Egfr酪氨酸激酶的临床重要突变体的选择性抑制剂 |
-
2016
- 2016-07-15 RU RU2018102963A patent/RU2734849C2/ru active
- 2016-07-15 CA CA2992317A patent/CA2992317A1/en active Pending
- 2016-07-15 TW TW105122536A patent/TWI739753B/zh active
- 2016-07-15 US US15/745,329 patent/US10329277B2/en active Active
- 2016-07-15 JP JP2018502096A patent/JP6970081B2/ja active Active
- 2016-07-15 KR KR1020187004698A patent/KR102666414B1/ko active Active
- 2016-07-15 AU AU2016292450A patent/AU2016292450B2/en active Active
- 2016-07-15 CN CN201680041201.3A patent/CN107835811B/zh active Active
- 2016-07-15 EP EP16823908.5A patent/EP3323817B1/en active Active
- 2016-07-15 WO PCT/CN2016/090149 patent/WO2017008761A1/zh not_active Ceased
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2011140338A1 (en) * | 2010-05-05 | 2011-11-10 | Gatekeeper Pharmaceuticals, Inc. | Compounds that modulate egfr activity and methods for treating or preventing conditions therewith |
| CN103702990A (zh) * | 2011-07-27 | 2014-04-02 | 阿斯利康(瑞典)有限公司 | 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症 |
| CN105085489A (zh) * | 2014-11-05 | 2015-11-25 | 上海页岩科技有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| CN106117185A (zh) * | 2015-08-31 | 2016-11-16 | 广州科擎新药开发有限公司 | 2,4‑二含氮基团取代嘧啶类化合物及其制备方法和应用 |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114026090A (zh) * | 2019-07-04 | 2022-02-08 | 微境生物医药科技(上海)有限公司 | 一类抑制egfr激酶的化合物及其制备方法和用途 |
| CN114026090B (zh) * | 2019-07-04 | 2023-01-06 | 微境生物医药科技(上海)有限公司 | 一类抑制egfr激酶的化合物及其制备方法和用途 |
Also Published As
| Publication number | Publication date |
|---|---|
| US20180208581A1 (en) | 2018-07-26 |
| KR102666414B1 (ko) | 2024-05-17 |
| KR20180030190A (ko) | 2018-03-21 |
| HK1250164A1 (zh) | 2018-11-30 |
| JP6970081B2 (ja) | 2021-11-24 |
| TWI739753B (zh) | 2021-09-21 |
| EP3323817B1 (en) | 2022-10-19 |
| TW201703768A (zh) | 2017-02-01 |
| CA2992317A1 (en) | 2017-01-19 |
| AU2016292450B2 (en) | 2021-03-25 |
| JP2018520190A (ja) | 2018-07-26 |
| RU2018102963A (ru) | 2019-08-16 |
| WO2017008761A1 (zh) | 2017-01-19 |
| US10329277B2 (en) | 2019-06-25 |
| EP3323817A4 (en) | 2019-04-10 |
| AU2016292450A1 (en) | 2018-02-15 |
| RU2018102963A3 (zh) | 2019-12-24 |
| EP3323817A1 (en) | 2018-05-23 |
| RU2734849C2 (ru) | 2020-10-23 |
| CN107835811B (zh) | 2019-11-08 |
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