CN103874696B - 作为激酶抑制剂的喹唑啉衍生物及其使用方法 - Google Patents
作为激酶抑制剂的喹唑啉衍生物及其使用方法 Download PDFInfo
- Publication number
- CN103874696B CN103874696B CN201280049954.0A CN201280049954A CN103874696B CN 103874696 B CN103874696 B CN 103874696B CN 201280049954 A CN201280049954 A CN 201280049954A CN 103874696 B CN103874696 B CN 103874696B
- Authority
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- China
- Prior art keywords
- compound
- base
- amino
- piperidin
- acid amides
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- 0 *c(ccc(Nc1c(cc(c(O*)c2)NC(C=CCN3CCCCC3)=O)c2ncn1)c1)c1C#C Chemical compound *c(ccc(Nc1c(cc(c(O*)c2)NC(C=CCN3CCCCC3)=O)c2ncn1)c1)c1C#C 0.000 description 2
- NAVGIMRWOWYNEP-DHZHZOJOSA-N COc1cc2ncnc(Nc3cc(C#C)ccc3)c2cc1NC(/C=C/CN1CCCCC1)=O Chemical compound COc1cc2ncnc(Nc3cc(C#C)ccc3)c2cc1NC(/C=C/CN1CCCCC1)=O NAVGIMRWOWYNEP-DHZHZOJOSA-N 0.000 description 2
- NNKQLUVBPJEUOR-UHFFFAOYSA-N C#Cc1cc(N)ccc1 Chemical compound C#Cc1cc(N)ccc1 NNKQLUVBPJEUOR-UHFFFAOYSA-N 0.000 description 1
- DSXOBDJKBFVEOH-JXMROGBWSA-N C#Cc1cccc(Nc2c(cc(c(OC3COCC3)c3)NC(/C=C/CN4CCCCC4)=O)c3ncn2)c1 Chemical compound C#Cc1cccc(Nc2c(cc(c(OC3COCC3)c3)NC(/C=C/CN4CCCCC4)=O)c3ncn2)c1 DSXOBDJKBFVEOH-JXMROGBWSA-N 0.000 description 1
- FIRLRXLVZWBQGD-JXMROGBWSA-N C#Cc1cccc(Nc2c(cc(c(OCCF)c3)NC(/C=C/CN4CCCCC4)=O)c3ncn2)c1 Chemical compound C#Cc1cccc(Nc2c(cc(c(OCCF)c3)NC(/C=C/CN4CCCCC4)=O)c3ncn2)c1 FIRLRXLVZWBQGD-JXMROGBWSA-N 0.000 description 1
- GLXNDRSJAWNESC-XFUPSFMQSA-N CCO/C(/C=C(\C(C)(C)CNc1cc(C#C)ccc1)/N=C\N)=C\[NH2+2] Chemical compound CCO/C(/C=C(\C(C)(C)CNc1cc(C#C)ccc1)/N=C\N)=C\[NH2+2] GLXNDRSJAWNESC-XFUPSFMQSA-N 0.000 description 1
- QGNJYSSGXZKMQS-FPLPWBNLSA-N CCOC(C(C)C=C1C(NC/C=C\C=C)=N)C=C1N=C Chemical compound CCOC(C(C)C=C1C(NC/C=C\C=C)=N)C=C1N=C QGNJYSSGXZKMQS-FPLPWBNLSA-N 0.000 description 1
- SMXJAXRPRKVDDR-BQYQJAHWSA-N COc1cc2ncnc(Nc(cc3)cc(C#C)c3F)c2cc1NC(/C=C/CN1CCCCC1)=O Chemical compound COc1cc2ncnc(Nc(cc3)cc(C#C)c3F)c2cc1NC(/C=C/CN1CCCCC1)=O SMXJAXRPRKVDDR-BQYQJAHWSA-N 0.000 description 1
- DPMPFAYUUAKQEM-UHFFFAOYSA-N O=NC1C=C(C(NC=N2)Cl)C2=CC1F Chemical compound O=NC1C=C(C(NC=N2)Cl)C2=CC1F DPMPFAYUUAKQEM-UHFFFAOYSA-N 0.000 description 1
- NFZOHOJPYXFOQW-SNAWJCMRSA-N OC(/C=C/CN1CCCCC1)=O Chemical compound OC(/C=C/CN1CCCCC1)=O NFZOHOJPYXFOQW-SNAWJCMRSA-N 0.000 description 1
Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161627359P | 2011-10-12 | 2011-10-12 | |
| US61/627,359 | 2011-10-12 | ||
| PCT/CN2012/001371 WO2013053206A1 (en) | 2011-10-12 | 2012-10-12 | Quinazoline derivatives as kinases inhibitors and methods of use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN103874696A CN103874696A (zh) | 2014-06-18 |
| CN103874696B true CN103874696B (zh) | 2015-06-03 |
Family
ID=48081378
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201280049954.0A Active CN103874696B (zh) | 2011-10-12 | 2012-10-12 | 作为激酶抑制剂的喹唑啉衍生物及其使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US9388160B2 (enExample) |
| EP (1) | EP2766356B1 (enExample) |
| JP (1) | JP2014532063A (enExample) |
| KR (1) | KR20140093223A (enExample) |
| CN (1) | CN103874696B (enExample) |
| WO (1) | WO2013053206A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013173254A1 (en) * | 2012-05-14 | 2013-11-21 | Dawei Zhang | Bicyclic compounds as kinases inhibitors |
| WO2014177038A1 (en) | 2013-04-28 | 2014-11-06 | Sunshine Lake Pharma Co., Ltd. | Aminoquinazoline derivatives and their salts and methods of use thereof |
| US10196365B2 (en) | 2014-08-15 | 2019-02-05 | Arromax Pharmatech Co., Ltd. | Quinazoline derivative, preparation method therefor, and pharmaceutical composition and application thereof |
| AU2017204973A1 (en) * | 2016-01-06 | 2018-07-12 | Trillium Therapeutics Inc. | Novel fluorinated quinazoline derivatives as EGFR inhibitors |
| JP2021527088A (ja) * | 2018-06-14 | 2021-10-11 | 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 | Ｈｅｒ２阻害剤としてのシアノキノリンアミド化合物及び使用方法 |
| KR102260995B1 (ko) * | 2018-11-28 | 2021-06-04 | 국립암센터 | Plk1의 활성 억제제를 유효성분으로 포함하는 암 예방 또는 치료용 약학적 조성물 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003089439A1 (de) * | 2002-04-19 | 2003-10-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, ihre verwendung und verfahren zu ihrer herstellung |
| CN1751033A (zh) * | 2003-02-20 | 2006-03-22 | 贝林格尔·英格海姆国际有限公司 | 双环杂环类,含所述化合物的药物制剂，其用途及制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA02009855A (es) | 2000-04-08 | 2003-03-27 | Boehringer Ingelheim Pharma | Heterociclos biciclicos, medicamentos que contienen estos compuestos, su empleo y procedimientos para su preparacion. |
| US7019012B2 (en) | 2000-12-20 | 2006-03-28 | Boehringer Ingelheim International Pharma Gmbh & Co. Kg | Quinazoline derivatives and pharmaceutical compositions containing them |
| US20040044014A1 (en) | 2002-04-19 | 2004-03-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof |
| PE20040945A1 (es) | 2003-02-05 | 2004-12-14 | Warner Lambert Co | Preparacion de quinazolinas substituidas |
| US7223749B2 (en) | 2003-02-20 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them |
| EP1746999B1 (en) | 2004-05-06 | 2011-11-16 | Warner-Lambert Company LLC | 4-phenylamino-quinazolin-6-yl-amides |
| US7905352B2 (en) * | 2004-12-06 | 2011-03-15 | Washington Biotech Corporation | Kits containing medicine injection devices and containers |
| DE102005030733A1 (de) * | 2005-07-01 | 2007-01-04 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Neue Arzneimittelkombinationen zur Behandlung von Atemwegserkrankungen enthaltend langwirksame Beta-2-Agonisten und wenigstens einen weiteren Wirkstoff |
| US8198301B2 (en) | 2006-07-05 | 2012-06-12 | Hesheng Zhang | Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors |
| CN101100466B (zh) * | 2006-07-05 | 2013-12-25 | 天津和美生物技术有限公司 | 不可逆蛋白质酪氨酸磷酰化酶抑制剂及其制备和应用 |
| DK3012251T3 (en) * | 2008-01-18 | 2017-10-09 | Natco Pharma Ltd | PROCEDURE FOR PREPARATION 6,7-DIALCOXY-QUINAZOLINE DERIVATIVES |
| 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 |
-
2012
- 2012-10-12 JP JP2014534918A patent/JP2014532063A/ja active Pending
- 2012-10-12 WO PCT/CN2012/001371 patent/WO2013053206A1/en not_active Ceased
- 2012-10-12 CN CN201280049954.0A patent/CN103874696B/zh active Active
- 2012-10-12 US US14/351,557 patent/US9388160B2/en active Active
- 2012-10-12 KR KR1020147011460A patent/KR20140093223A/ko not_active Withdrawn
- 2012-10-12 EP EP12839322.0A patent/EP2766356B1/en not_active Not-in-force
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003089439A1 (de) * | 2002-04-19 | 2003-10-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, ihre verwendung und verfahren zu ihrer herstellung |
| CN1751033A (zh) * | 2003-02-20 | 2006-03-22 | 贝林格尔·英格海姆国际有限公司 | 双环杂环类,含所述化合物的药物制剂，其用途及制备方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| KR20140093223A (ko) | 2014-07-25 |
| JP2014532063A (ja) | 2014-12-04 |
| EP2766356B1 (en) | 2018-08-01 |
| US20140235658A1 (en) | 2014-08-21 |
| US9388160B2 (en) | 2016-07-12 |
| EP2766356A1 (en) | 2014-08-20 |
| EP2766356A4 (en) | 2015-03-25 |
| CN103874696A (zh) | 2014-06-18 |
| WO2013053206A1 (en) | 2013-04-18 |
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Date of cancellation: 20190816 Granted publication date: 20150603 |
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Address after: 215123 unit 416, building A4, bio nano Park, 218 Xinghu street, industrial park, Suzhou, Jiangsu Patentee after: Suzhou Taolue Biotechnology Co., Ltd Address before: 215123 d33, floor 2, North Block A1, 218 Xinghu street, industrial park, Suzhou, Jiangsu Patentee before: Suzhou Taolue Biotechnology Co., Ltd |