CN113382986A - 酪氨酸激酶抑制剂组合物、其制备方法和使用方法 - Google Patents

酪氨酸激酶抑制剂组合物、其制备方法和使用方法 Download PDF

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CN113382986A
CN113382986A CN201980077292.XA CN201980077292A CN113382986A CN 113382986 A CN113382986 A CN 113382986A CN 201980077292 A CN201980077292 A CN 201980077292A CN 113382986 A CN113382986 A CN 113382986A
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A·弗洛尔
A·梅威格
G·特雷纳
D·M·爱普斯坦
M·奥康纳
E·巴克
L·阿里斯塔
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Black Diamond Treatment Co
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    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
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    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61K31/53751,4-Oxazines, e.g. morpholine
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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CN201980077292.XA 2018-09-25 2019-09-24 酪氨酸激酶抑制剂组合物、其制备方法和使用方法 Pending CN113382986A (zh)

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US201862736293P 2018-09-25 2018-09-25
US62/736293 2018-09-25
US201962903592P 2019-09-20 2019-09-20
US62/903592 2019-09-20
PCT/US2019/052784 WO2020068867A1 (en) 2018-09-25 2019-09-24 Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use

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US (2) US11034672B1 (https=)
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JP (1) JP2022502495A (https=)
KR (1) KR20210137422A (https=)
CN (1) CN113382986A (https=)
AU (1) AU2019346550A1 (https=)
BR (1) BR112021005513A2 (https=)
CA (1) CA3113241A1 (https=)
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* Cited by examiner, † Cited by third party
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CN114787150A (zh) * 2019-08-15 2022-07-22 黑钻治疗公司 炔基喹唑啉化合物
CN116655599A (zh) * 2023-05-17 2023-08-29 江南大学 一类egfr别构抑制剂的合成及其用途
CN118084767A (zh) * 2024-04-02 2024-05-28 康龙化成手性医药技术(宁波)有限公司 一种外型-6-氟甲基-3-氮杂双环[3,1,0]己烷盐酸盐及其衍生物的合成方法
CN118652239A (zh) * 2024-05-29 2024-09-17 江南大学 一类egfr别构抑制剂的合成及其用途

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019346550A1 (en) 2018-09-25 2021-04-22 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
WO2021195206A1 (en) * 2020-03-24 2021-09-30 Black Diamond Therapeutics, Inc. Polymorphic forms and related uses
AR122450A1 (es) * 2020-05-08 2022-09-14 Lilly Co Eli Compuestos de (trifluorometil)pirimidin-2-amina
US20230265098A1 (en) * 2020-07-02 2023-08-24 Enliven Therapeutics, Inc. Alkyne quinazoline derivatives as inhibitors of erbb2
US20230271936A1 (en) * 2020-08-10 2023-08-31 Abbisko Therapeutics Co., Ltd Efgr inhibitor, preparation method therefor and application thereof
WO2022040377A1 (en) 2020-08-20 2022-02-24 Black Diamond Therapeutics, Inc. Methods for preparing quinazoline derivatives
AU2021347232A1 (en) 2020-09-23 2023-04-27 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022076671A1 (en) * 2020-10-08 2022-04-14 Black Diamond Therapeutics, Inc. Method of treating cancers using quinazoline derivatives
CN116710096A (zh) * 2020-11-02 2023-09-05 黑钻治疗公司 用炔取代的喹唑啉衍生物治疗癌症的方法
US20240075042A1 (en) * 2020-11-02 2024-03-07 Black Diamond Therapeutics, Inc. Method of treating cancers with alkyne substituted quinazoline derivatives
WO2022133345A1 (en) 2020-12-18 2022-06-23 Erasca, Inc. Tricyclic pyridones and pyrimidones
EP4323356A1 (en) 2021-04-13 2024-02-21 Nuvalent, Inc. Amino-substituted heterocycles for treating cancers with egfr mutations
EP4724436A1 (en) * 2023-06-12 2026-04-15 Remix Therapeutics Inc. Compounds and methods for modulating splicing
WO2025096300A1 (en) * 2023-10-30 2025-05-08 Eli Lilly And Company Novel methods for the preparation of 3-azabicylco[3.1,0]hexane-6-carboxamide derivatives

Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6127374A (en) * 1997-07-29 2000-10-03 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
WO2012136099A1 (zh) * 2011-04-02 2012-10-11 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
US20130035350A1 (en) * 2009-12-21 2013-02-07 Qiang Zhang Novel Quinazoline Derivatives
CN103965120A (zh) * 2013-01-25 2014-08-06 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
US20150126537A1 (en) * 2012-05-14 2015-05-07 Hangzhouderenyucheng Biotechnology Ltd Bicyclic compounds as kinases inhibitors
US20160039838A1 (en) * 2013-04-28 2016-02-11 Sunshine Lake Pharma Co., Ltd. Aminoquinazoline derivatives and their salts and methods of use thereof
WO2016055982A1 (en) * 2014-10-10 2016-04-14 Acerta Pharma B.V. Quinoline and quinazoline compounds

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS6041077B2 (ja) 1976-09-06 1985-09-13 喜徳 喜谷 1,2‐ジアミノシクロヘキサン異性体のシス白金(2)錯体
US4261989A (en) 1979-02-19 1981-04-14 Kaken Chemical Co. Ltd. Geldanamycin derivatives and antitumor drug
US5266573A (en) 1989-08-07 1993-11-30 Elf Sanofi Trifluoromethylphenyltetrahydropyridines for the treatment and/or prophylaxis of intestinal motility disorders
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
MX9707453A (es) 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
US5763263A (en) 1995-11-27 1998-06-09 Dehlinger; Peter J. Method and apparatus for producing position addressable combinatorial libraries
HU228446B1 (en) 1996-04-12 2013-03-28 Warner Lambert Co Kinazoline derivatives as irreversible inhibitors of protein-kinase, pharmaceutical compositions containing these compounds and use thereof
TW436485B (en) 1997-08-01 2001-05-28 American Cyanamid Co Substituted quinazoline derivatives
JP3270834B2 (ja) 1999-01-27 2002-04-02 ファイザー・プロダクツ・インク 抗がん剤として有用なヘテロ芳香族二環式誘導体
UA71945C2 (en) 1999-01-27 2005-01-17 Pfizer Prod Inc Substituted bicyclic derivatives being used as anticancer agents
SK288365B6 (sk) 1999-02-10 2016-07-01 Astrazeneca Ab Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy
EE04748B1 (et) 1999-06-21 2006-12-15 Boehringer Ingelheim Pharma Kg Bitsüklilised heterotsüklilised ühendid, neid ühendeid sisaldavad ravimid, nende kasutamine ja meetodid nende valmistamiseks
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB0018891D0 (en) 2000-08-01 2000-09-20 Novartis Ag Organic compounds
ATE350378T1 (de) 2000-04-08 2007-01-15 Boehringer Ingelheim Pharma Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
DE10042061A1 (de) 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE60137273D1 (de) 2000-10-20 2009-02-12 Eisai R&D Man Co Ltd Verfahren zur Herstellung von 4-Phenoxy chinolin Derivaten
DE10063435A1 (de) 2000-12-20 2002-07-04 Boehringer Ingelheim Pharma Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US6995162B2 (en) 2001-01-12 2006-02-07 Amgen Inc. Substituted alkylamine derivatives and methods of use
HUP0500117A3 (en) 2001-11-30 2008-03-28 Pfizer Prod Inc Processes for the preparation of substituted quinazoline derivatives for the treatment of abnormal cell growth
JP4547911B2 (ja) 2002-02-01 2010-09-22 アリアド・ファーマシューティカルズ・インコーポレイテッド リン含有化合物およびその用途
US7375134B2 (en) 2002-03-05 2008-05-20 Axys Pharmaceuticals, Inc. Cathepsin cysteine protease inhibitors
DE10217689A1 (de) 2002-04-19 2003-11-13 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
PE20040945A1 (es) 2003-02-05 2004-12-14 Warner Lambert Co Preparacion de quinazolinas substituidas
US7399865B2 (en) 2003-09-15 2008-07-15 Wyeth Protein tyrosine kinase enzyme inhibitors
AU2004272346A1 (en) 2003-09-16 2005-03-24 Astrazeneca Ab Quinazoline derivatives
CN1972688B (zh) 2004-05-06 2012-06-27 沃尼尔·朗伯有限责任公司 4-苯胺基-喹唑啉-6-基-酰胺类化合物
DK1789390T3 (da) 2004-09-02 2012-02-27 Genentech Inc Pyridyl-inhibitorer af hedgehog-signalering
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
PE20070207A1 (es) 2005-07-22 2007-03-09 Genentech Inc Tratamiento combinado de los tumores que expresan el her
WO2007055513A1 (en) 2005-11-08 2007-05-18 Hanmi Pharm. Co., Ltd. Quinazoline derivatives as a signal transduction inhibitor and method for the preparation thereof
CN101535279B (zh) 2006-09-11 2015-05-20 柯瑞斯公司 含锌结合基的喹唑啉基egfr抑制剂
TWI377944B (en) 2007-06-05 2012-12-01 Hanmi Holdings Co Ltd Novel amide derivative for inhibiting the growth of cancer cells
AU2008298948B2 (en) 2007-09-12 2014-09-04 F. Hoffmann-La Roche Ag Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
WO2010036629A2 (en) 2008-09-26 2010-04-01 National Health Research Institutes Fused multicyclic compounds as protein kinase inhibitors
CN102382106A (zh) 2010-08-30 2012-03-21 黄振华 苯胺取代的喹唑啉衍生物
CN102382065B (zh) 2010-08-30 2014-05-28 山东轩竹医药科技有限公司 苯胺取代的喹唑啉衍生物
CN102452989B (zh) 2010-10-19 2014-10-22 山东轩竹医药科技有限公司 苯胺取代的喹唑啉衍生物
BR112013022552B1 (pt) 2011-03-04 2021-11-23 Newgen Therapeutics, Inc Compostos de quinazolina substituídos com alcino, seu uso, composição farmacêutica, e kit
WO2013013640A1 (zh) 2011-07-27 2013-01-31 上海医药集团股份有限公司 喹唑啉衍生物、其制备方法、中间体、组合物及其应用
CN103987700B (zh) 2012-03-09 2016-08-31 江苏豪森药业集团有限公司 4-喹唑啉胺类衍生物及其用途
CN104513229A (zh) 2013-09-28 2015-04-15 正大天晴药业集团股份有限公司 喹唑啉衍生物及其制备方法
AU2014331794C1 (en) 2013-10-10 2019-09-12 Araxes Pharma Llc Inhibitors of KRAS G12C
WO2016023217A1 (zh) 2014-08-15 2016-02-18 安润医药科技(苏州)有限公司 喹唑啉衍生物、其制备方法、药物组合物和应用
AU2019346550A1 (en) 2018-09-25 2021-04-22 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use

Patent Citations (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6127374A (en) * 1997-07-29 2000-10-03 Warner-Lambert Company Irreversible inhibitors of tyrosine kinases
US20130035350A1 (en) * 2009-12-21 2013-02-07 Qiang Zhang Novel Quinazoline Derivatives
WO2012136099A1 (zh) * 2011-04-02 2012-10-11 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
US20150126537A1 (en) * 2012-05-14 2015-05-07 Hangzhouderenyucheng Biotechnology Ltd Bicyclic compounds as kinases inhibitors
CN103965120A (zh) * 2013-01-25 2014-08-06 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
US20160039838A1 (en) * 2013-04-28 2016-02-11 Sunshine Lake Pharma Co., Ltd. Aminoquinazoline derivatives and their salts and methods of use thereof
WO2016055982A1 (en) * 2014-10-10 2016-04-14 Acerta Pharma B.V. Quinoline and quinazoline compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
M. ASADOLLAHI-BABOLI: "In silico evaluation, molecular docking and QSAR analisis of quinazoline-based EGFR-T790M inhibitors", MOL. DIVERS, vol. 20, pages 729 - 739, XP035999887, DOI: 10.1007/s11030-016-9672-0 *

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114787150A (zh) * 2019-08-15 2022-07-22 黑钻治疗公司 炔基喹唑啉化合物
US12435046B2 (en) 2019-08-15 2025-10-07 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
CN116655599A (zh) * 2023-05-17 2023-08-29 江南大学 一类egfr别构抑制剂的合成及其用途
CN116655599B (zh) * 2023-05-17 2025-07-29 江南大学 一类egfr别构抑制剂的合成及其用途
CN118084767A (zh) * 2024-04-02 2024-05-28 康龙化成手性医药技术(宁波)有限公司 一种外型-6-氟甲基-3-氮杂双环[3,1,0]己烷盐酸盐及其衍生物的合成方法
CN118652239A (zh) * 2024-05-29 2024-09-17 江南大学 一类egfr别构抑制剂的合成及其用途

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