CN108779079A - 作为egfr抑制剂的新的氟化喹唑啉衍生物 - Google Patents
作为egfr抑制剂的新的氟化喹唑啉衍生物 Download PDFInfo
- Publication number
- CN108779079A CN108779079A CN201780015324.4A CN201780015324A CN108779079A CN 108779079 A CN108779079 A CN 108779079A CN 201780015324 A CN201780015324 A CN 201780015324A CN 108779079 A CN108779079 A CN 108779079A
- Authority
- CN
- China
- Prior art keywords
- difluoro
- bases
- compound
- methoxy
- quinazoline
- 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.)
- Pending
Links
- 0 C*(CC1)CCC1(F)F Chemical compound C*(CC1)CCC1(F)F 0.000 description 3
- YNAVUWVOSKDBBP-UHFFFAOYSA-N C1NCCOC1 Chemical compound C1NCCOC1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 description 1
- UQXVNXCJRRPPEA-UHFFFAOYSA-N CC(C)(C)CN(CC1)CC1(F)F Chemical compound CC(C)(C)CN(CC1)CC1(F)F UQXVNXCJRRPPEA-UHFFFAOYSA-N 0.000 description 1
- WIPDWLMRCJTCKH-UHFFFAOYSA-N CCCCOC(N)N Chemical compound CCCCOC(N)N WIPDWLMRCJTCKH-UHFFFAOYSA-N 0.000 description 1
- MUPQNDRRTPPWCW-UHFFFAOYSA-N FC(OC1CCNCC1)F Chemical compound FC(OC1CCNCC1)F MUPQNDRRTPPWCW-UHFFFAOYSA-N 0.000 description 1
- QUHVRXKSQHIZNV-UHFFFAOYSA-N FC1(CNC1)F Chemical compound FC1(CNC1)F QUHVRXKSQHIZNV-UHFFFAOYSA-N 0.000 description 1
- MPZGTXRHURNLJL-UHFFFAOYSA-N Nc1cc2c(Nc(c(F)c3Cl)ccc3Cl)ncnc2cc1OCCOC(F)F Chemical compound Nc1cc2c(Nc(c(F)c3Cl)ccc3Cl)ncnc2cc1OCCOC(F)F MPZGTXRHURNLJL-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
-
- 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
-
- 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
- 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
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (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)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662275376P | 2016-01-06 | 2016-01-06 | |
| US62/275,376 | 2016-01-06 | ||
| PCT/CA2017/050015 WO2017117680A1 (en) | 2016-01-06 | 2017-01-06 | Novel fluorinated quinazoline derivatives as egfr inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN108779079A true CN108779079A (zh) | 2018-11-09 |
Family
ID=59273095
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780015324.4A Pending CN108779079A (zh) | 2016-01-06 | 2017-01-06 | 作为egfr抑制剂的新的氟化喹唑啉衍生物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20190016689A1 (enExample) |
| EP (1) | EP3400216A4 (enExample) |
| JP (1) | JP2019504830A (enExample) |
| CN (1) | CN108779079A (enExample) |
| AU (1) | AU2017204973A1 (enExample) |
| CA (1) | CA3008312A1 (enExample) |
| WO (1) | WO2017117680A1 (enExample) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111548314A (zh) * | 2020-05-22 | 2020-08-18 | 上海万巷制药有限公司 | 一种n-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺的生产方法 |
| CN114394942A (zh) * | 2021-03-04 | 2022-04-26 | 江苏康可得生物技术股份有限公司 | 酪氨酸激酶抑制剂及其药物应用 |
| CN115151539A (zh) * | 2019-12-04 | 2022-10-04 | 因赛特公司 | Fgfr抑制剂的衍生物 |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3687981A4 (en) * | 2017-09-26 | 2021-03-31 | The Regents of the University of California | COMPOSITIONS AND METHODS OF TREATMENT OF CANCER |
| CN113811528A (zh) | 2019-03-15 | 2021-12-17 | 加利福尼亚大学董事会 | 用于治疗癌症的组合物和方法 |
| KR20210142154A (ko) | 2019-03-21 | 2021-11-24 | 옹쎄오 | 암 치료를 위한 키나제 억제제와 조합된 dbait 분자 |
| US20220229072A1 (en) | 2019-06-04 | 2022-07-21 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of cd9 as a biomarker and as a biotarget in glomerulonephritis or glomerulosclerosis |
| TWI817018B (zh) | 2019-06-28 | 2023-10-01 | 美商艾瑞生藥股份有限公司 | 用於治療ｂｒａｆ相關的疾病和失調症之化合物 |
| 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 |
| CN116096710B (zh) | 2020-06-09 | 2025-07-25 | 阿雷生物药品公司 | 用于治疗braf相关疾病和障碍的4-氧代-3,4-二氢喹唑啉酮化合物 |
| TWI825637B (zh) | 2021-03-31 | 2023-12-11 | 美商輝瑞股份有限公司 | 啶－１，６（２ｈ，７ｈ）－二酮 |
| WO2023128350A1 (ko) * | 2021-12-30 | 2023-07-06 | 주식회사 비투에스바이오 | 헤테로아릴 유도체 및 이를 유효성분으로 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| WO2024218632A1 (en) | 2023-04-17 | 2024-10-24 | Array Biopharma Inc. | Erk protein kinase inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102838550A (zh) * | 2011-06-21 | 2012-12-26 | 苏州迈泰生物技术有限公司 | 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 |
| CN103874696A (zh) * | 2011-10-12 | 2014-06-18 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的喹唑啉衍生物及其使用方法 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1746999B1 (en) * | 2004-05-06 | 2011-11-16 | Warner-Lambert Company LLC | 4-phenylamino-quinazolin-6-yl-amides |
| CN102731485B (zh) * | 2011-04-02 | 2016-06-15 | 齐鲁制药有限公司 | 4-(取代苯氨基)喹唑啉衍生物及其制备方法、药物组合物和用途 |
| CN104350049B (zh) * | 2012-05-07 | 2016-07-13 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的取代氨基喹唑啉 |
| CN104910140A (zh) * | 2014-03-14 | 2015-09-16 | 齐鲁制药有限公司 | 喹唑啉类化合物、其制备方法及应用 |
| US10196365B2 (en) * | 2014-08-15 | 2019-02-05 | Arromax Pharmatech Co., Ltd. | Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof |
-
2017
- 2017-01-06 AU AU2017204973A patent/AU2017204973A1/en not_active Abandoned
- 2017-01-06 CN CN201780015324.4A patent/CN108779079A/zh active Pending
- 2017-01-06 EP EP17735790.2A patent/EP3400216A4/en not_active Withdrawn
- 2017-01-06 WO PCT/CA2017/050015 patent/WO2017117680A1/en not_active Ceased
- 2017-01-06 JP JP2018535293A patent/JP2019504830A/ja not_active Withdrawn
- 2017-01-06 US US16/066,574 patent/US20190016689A1/en not_active Abandoned
- 2017-01-06 CA CA3008312A patent/CA3008312A1/en not_active Abandoned
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102838550A (zh) * | 2011-06-21 | 2012-12-26 | 苏州迈泰生物技术有限公司 | 喹唑啉巴豆基化合物及其在制备抗恶性肿瘤药物中的用途 |
| CN103874696A (zh) * | 2011-10-12 | 2014-06-18 | 苏州韬略生物科技有限公司 | 作为激酶抑制剂的喹唑啉衍生物及其使用方法 |
Non-Patent Citations (2)
| Title |
|---|
| LI XING ET AL.: "Fluorine in Drug Design: A Case Study with Fluoroanisoles", 《CHEMMEDCHEM》 * |
| LONG ZHANG ET AL.: "Structure-activity study of quinazoline derivatives leading to the discovery of potent EGFR-T790M inhibitors", 《EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY》 * |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115151539A (zh) * | 2019-12-04 | 2022-10-04 | 因赛特公司 | Fgfr抑制剂的衍生物 |
| CN111548314A (zh) * | 2020-05-22 | 2020-08-18 | 上海万巷制药有限公司 | 一种n-(3-氯-4-氟苯基)-7-氟-6-硝基-4-喹唑啉胺的生产方法 |
| CN114394942A (zh) * | 2021-03-04 | 2022-04-26 | 江苏康可得生物技术股份有限公司 | 酪氨酸激酶抑制剂及其药物应用 |
| WO2022184119A1 (zh) * | 2021-03-04 | 2022-09-09 | 江苏康可得生物技术股份有限公司 | 酪氨酸激酶抑制剂及其药物应用 |
| CN114394942B (zh) * | 2021-03-04 | 2024-12-10 | 江苏康可得生物技术股份有限公司 | 酪氨酸激酶抑制剂及其药物应用 |
| US12435045B2 (en) | 2021-03-04 | 2025-10-07 | Jiangsu Concord Biotechnology Co., Ltd | Tyrosine kinase inhibitors and pharmaceutical application thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| US20190016689A1 (en) | 2019-01-17 |
| EP3400216A1 (en) | 2018-11-14 |
| WO2017117680A1 (en) | 2017-07-13 |
| EP3400216A4 (en) | 2019-08-14 |
| AU2017204973A1 (en) | 2018-07-12 |
| CA3008312A1 (en) | 2017-07-13 |
| JP2019504830A (ja) | 2019-02-21 |
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| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| WD01 | Invention patent application deemed withdrawn after publication | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20181109 |