CN112236422A - 喹唑啉类化合物作为egfr三突变抑制剂及其应用 - Google Patents
喹唑啉类化合物作为egfr三突变抑制剂及其应用 Download PDFInfo
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- CN112236422A CN112236422A CN201980025718.7A CN201980025718A CN112236422A CN 112236422 A CN112236422 A CN 112236422A CN 201980025718 A CN201980025718 A CN 201980025718A CN 112236422 A CN112236422 A CN 112236422A
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Classifications
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
- A61K31/495—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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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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
- A61K31/535—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
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- 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
- C07D403/14—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 three or more hetero rings
-
- 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
- C07D413/12—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 linked by a chain containing hetero atoms as chain links
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- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
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- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
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Abstract
涉及喹唑啉类化合物作为EGFR三突变抑制剂及其应用。具体而言,公开了下式(I)所示化合物、含有下式(I)化合物的药物组合物及所述化合物在治疗EGFR介导的相关疾病以及制备治疗EGFR介导的相关疾病的药物中的用途。
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 |
---|---|---|---|
CN201810332709.XA CN110372666B (zh) | 2018-04-13 | 2018-04-13 | 喹唑啉类化合物作为egfr三突变抑制剂及其应用 |
CN201810332709X | 2018-04-13 | ||
PCT/CN2019/082498 WO2019196938A1 (zh) | 2018-04-13 | 2019-04-12 | 喹唑啉类化合物作为egfr三突变抑制剂及其应用 |
Publications (2)
Publication Number | Publication Date |
---|---|
CN112236422A true CN112236422A (zh) | 2021-01-15 |
CN112236422B CN112236422B (zh) | 2023-05-16 |
Family
ID=68163006
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
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CN201810332709.XA Active CN110372666B (zh) | 2018-04-13 | 2018-04-13 | 喹唑啉类化合物作为egfr三突变抑制剂及其应用 |
CN201980025718.7A Active CN112236422B (zh) | 2018-04-13 | 2019-04-12 | 喹唑啉类化合物作为egfr三突变抑制剂及其应用 |
Family Applications Before (1)
Application Number | Title | Priority Date | Filing Date |
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CN201810332709.XA Active CN110372666B (zh) | 2018-04-13 | 2018-04-13 | 喹唑啉类化合物作为egfr三突变抑制剂及其应用 |
Country Status (6)
Country | Link |
---|---|
US (1) | US20210155604A1 (zh) |
EP (1) | EP3778586A4 (zh) |
JP (1) | JP2021521215A (zh) |
KR (1) | KR20210003807A (zh) |
CN (2) | CN110372666B (zh) |
WO (1) | WO2019196938A1 (zh) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN112778217B (zh) * | 2019-11-08 | 2024-01-26 | 沈阳化工研究院有限公司 | 一种喹唑啉类化合物及其应用 |
KR102267662B1 (ko) * | 2019-11-19 | 2021-06-22 | 한국화학연구원 | 벤즈아미드 유도체, 이의 제조방법 및 이를 유효성분으로 함유하는 암의 예방 또는 치료용 약학적 조성물 |
Citations (5)
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CN1391562A (zh) * | 1999-09-21 | 2003-01-15 | 阿斯特拉曾尼卡有限公司 | 用作药物的喹唑啉衍生物 |
WO2004013091A2 (en) * | 2002-08-01 | 2004-02-12 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | 4-anilido substituted quinazolines and use thereof as inhibitors of epidermal growth factor receptor kinases |
CN101248059A (zh) * | 2005-04-27 | 2008-08-20 | 安姆根有限公司 | 作为蛋白激酶抑制剂的取代的酰胺衍生物 |
CN104230826A (zh) * | 2013-06-08 | 2014-12-24 | 复旦大学 | 2-氟代喹唑啉环类化合物及其制备方法和药用用途 |
CN107849034A (zh) * | 2015-06-30 | 2018-03-27 | 达纳-法伯癌症研究所公司 | Egfr抑制剂及其使用方法 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5538325A (en) * | 1978-09-11 | 1980-03-17 | Sankyo Co Ltd | 4-anilinoquinazoline derivative and its preparation |
WO2000020402A1 (en) * | 1998-10-01 | 2000-04-13 | Astrazeneca Ab | Chemical compounds |
US20030149045A1 (en) * | 1999-08-20 | 2003-08-07 | Fatih M Uckun | Therapeutic compounds |
TW200505452A (en) * | 2003-06-17 | 2005-02-16 | Astrazeneca Ab | Chemical compounds |
WO2010068951A1 (en) * | 2008-12-12 | 2010-06-17 | Fox Chase Cancer Center | Combination therapy based on src and aurora kinase inhibition for the treatment of cancer |
CN102146059A (zh) * | 2010-02-08 | 2011-08-10 | 上海艾力斯医药科技有限公司 | 喹唑啉衍生物、制备方法及其应用 |
CN103965120B (zh) * | 2013-01-25 | 2016-08-17 | 上海医药集团股份有限公司 | 喹啉及喹唑啉衍生物、制备方法、中间体、组合物及应用 |
CN104530063B (zh) * | 2015-01-13 | 2017-01-18 | 北京赛特明强医药科技有限公司 | 喹唑啉并杂环类化合物及其制备方法和作为用于治疗癌症的表皮生长因子受体抑制剂的应用 |
CN107129506B (zh) * | 2016-02-26 | 2019-10-22 | 华东理工大学 | 作为EGFR抑制剂的嘧啶并[4,5-d][1,3]噁嗪-2-酮衍生物及其应用 |
CN105884699B (zh) * | 2016-05-11 | 2019-05-07 | 中国药科大学 | 4-取代苯胺喹唑啉类衍生物及其制备方法和用途 |
-
2018
- 2018-04-13 CN CN201810332709.XA patent/CN110372666B/zh active Active
-
2019
- 2019-04-12 CN CN201980025718.7A patent/CN112236422B/zh active Active
- 2019-04-12 KR KR1020207032817A patent/KR20210003807A/ko unknown
- 2019-04-12 EP EP19785966.3A patent/EP3778586A4/en not_active Withdrawn
- 2019-04-12 JP JP2020556322A patent/JP2021521215A/ja active Pending
- 2019-04-12 US US17/047,002 patent/US20210155604A1/en not_active Abandoned
- 2019-04-12 WO PCT/CN2019/082498 patent/WO2019196938A1/zh unknown
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CN1391562A (zh) * | 1999-09-21 | 2003-01-15 | 阿斯特拉曾尼卡有限公司 | 用作药物的喹唑啉衍生物 |
WO2004013091A2 (en) * | 2002-08-01 | 2004-02-12 | Yissum Research Development Company Of The Hebrew University Of Jerusalem | 4-anilido substituted quinazolines and use thereof as inhibitors of epidermal growth factor receptor kinases |
CN101248059A (zh) * | 2005-04-27 | 2008-08-20 | 安姆根有限公司 | 作为蛋白激酶抑制剂的取代的酰胺衍生物 |
CN104230826A (zh) * | 2013-06-08 | 2014-12-24 | 复旦大学 | 2-氟代喹唑啉环类化合物及其制备方法和药用用途 |
CN107849034A (zh) * | 2015-06-30 | 2018-03-27 | 达纳-法伯癌症研究所公司 | Egfr抑制剂及其使用方法 |
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YU-JING LIU等: ""Recent developments of small molecule EGFR inhibitors based on the quinazoline core scaffolds"", 《ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY》 * |
Also Published As
Publication number | Publication date |
---|---|
CN112236422B (zh) | 2023-05-16 |
CN110372666A (zh) | 2019-10-25 |
EP3778586A4 (en) | 2022-03-16 |
US20210155604A1 (en) | 2021-05-27 |
JP2021521215A (ja) | 2021-08-26 |
KR20210003807A (ko) | 2021-01-12 |
CN110372666B (zh) | 2022-11-08 |
WO2019196938A1 (zh) | 2019-10-17 |
EP3778586A1 (en) | 2021-02-17 |
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