KR100852102B1 - 퀴나졸린 유도체, 이의 제조방법 및 이를 함유하는 약제 - Google Patents

퀴나졸린 유도체, 이의 제조방법 및 이를 함유하는 약제 Download PDF

Info

Publication number
KR100852102B1
KR100852102B1 KR1020037008246A KR20037008246A KR100852102B1 KR 100852102 B1 KR100852102 B1 KR 100852102B1 KR 1020037008246 A KR1020037008246 A KR 1020037008246A KR 20037008246 A KR20037008246 A KR 20037008246A KR 100852102 B1 KR100852102 B1 KR 100852102B1
Authority
KR
South Korea
Prior art keywords
amino
oxo
chloro
fluorophenyl
buten
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.)
Expired - Lifetime
Application number
KR1020037008246A
Other languages
English (en)
Korean (ko)
Other versions
KR20030071787A (ko
Inventor
프랑크 힘멜스바하
엘케 랑코프
슈테판 블레흐
비르기트 융
안케 바움
플라비오 졸차
Original Assignee
베링거 잉겔하임 파르마 게엠베하 운트 코 카게
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7667887&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=KR100852102(B1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by 베링거 잉겔하임 파르마 게엠베하 운트 코 카게 filed Critical 베링거 잉겔하임 파르마 게엠베하 운트 코 카게
Publication of KR20030071787A publication Critical patent/KR20030071787A/ko
Application granted granted Critical
Publication of KR100852102B1 publication Critical patent/KR100852102B1/ko
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)
KR1020037008246A 2000-12-20 2001-12-12 퀴나졸린 유도체, 이의 제조방법 및 이를 함유하는 약제 Expired - Lifetime KR100852102B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10063435.4 2000-12-20
DE10063435A DE10063435A1 (de) 2000-12-20 2000-12-20 Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
PCT/EP2001/014569 WO2002050043A1 (de) 2000-12-20 2001-12-12 Chinazolinderivate, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung

Publications (2)

Publication Number Publication Date
KR20030071787A KR20030071787A (ko) 2003-09-06
KR100852102B1 true KR100852102B1 (ko) 2008-08-13

Family

ID=7667887

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020037008246A Expired - Lifetime KR100852102B1 (ko) 2000-12-20 2001-12-12 퀴나졸린 유도체, 이의 제조방법 및 이를 함유하는 약제

Country Status (39)

Country Link
EP (2) EP2112140A1 (enExample)
JP (1) JP3827641B2 (enExample)
KR (1) KR100852102B1 (enExample)
CN (1) CN1277822C (enExample)
AR (1) AR040524A1 (enExample)
AT (1) ATE430136T1 (enExample)
AU (2) AU1917402A (enExample)
BE (1) BE2014C009I2 (enExample)
BG (1) BG66139B1 (enExample)
BR (1) BRPI0116266B8 (enExample)
CA (1) CA2432428C (enExample)
CY (2) CY1109290T1 (enExample)
CZ (1) CZ302721B6 (enExample)
DE (2) DE10063435A1 (enExample)
DK (1) DK1345910T3 (enExample)
EA (1) EA006317B1 (enExample)
EE (1) EE05244B1 (enExample)
ES (1) ES2326617T3 (enExample)
FR (1) FR14C0009I2 (enExample)
HR (1) HRP20030504B1 (enExample)
HU (2) HU228874B1 (enExample)
IL (2) IL156277A0 (enExample)
LT (1) LTC1345910I2 (enExample)
LU (1) LU92370I2 (enExample)
ME (1) ME02777B (enExample)
MX (1) MXPA03005559A (enExample)
MY (1) MY136086A (enExample)
NO (3) NO325672B1 (enExample)
NZ (1) NZ526918A (enExample)
PL (1) PL214798B1 (enExample)
PT (1) PT1345910E (enExample)
RS (1) RS50860B (enExample)
SI (1) SI1345910T1 (enExample)
SK (1) SK287573B6 (enExample)
TW (1) TWI295992B (enExample)
UA (1) UA74614C2 (enExample)
UY (1) UY27078A1 (enExample)
WO (1) WO2002050043A1 (enExample)
ZA (1) ZA200304141B (enExample)

Families Citing this family (92)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ516633A (en) 1999-06-21 2004-09-24 Boehringer Ingelheim Pharma Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
DE10204462A1 (de) * 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
US6924285B2 (en) 2002-03-30 2005-08-02 Boehringer Ingelheim Pharma Gmbh & Co. Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing 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
DE10221018A1 (de) * 2002-05-11 2003-11-27 Boehringer Ingelheim Pharma Verwendung von Hemmern der EGFR-vermittelten Signaltransduktion zur Behandlung von gutartiger Prostatahyperplasie (BPH)/Prostatahypertrophie
PE20040945A1 (es) * 2003-02-05 2004-12-14 Warner Lambert Co Preparacion de quinazolinas substituidas
DE10307165A1 (de) * 2003-02-20 2004-09-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, ihre Verwendung und Verfahren zu ihrer Herstellung
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
US20050043233A1 (en) 2003-04-29 2005-02-24 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
DE10334226A1 (de) * 2003-07-28 2005-02-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verwendung von Tyrosinkinase-Inhibitoren zur Behandlung inflammatorischer Prozesse
GB0317665D0 (en) 2003-07-29 2003-09-03 Astrazeneca Ab Qinazoline derivatives
WO2005026150A1 (en) 2003-09-16 2005-03-24 Astrazeneca Ab Quinazoline derivatives as tyrosine kinase inhibitors
US7456189B2 (en) 2003-09-30 2008-11-25 Boehringer Ingelheim International Gmbh Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation
DE10349113A1 (de) * 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
HRP20110958T1 (hr) * 2004-05-06 2012-01-31 Warner-Lambert Company Llc 4-fenilaminokinazolin-6-ilamidi
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
WO2006081741A1 (en) * 2005-02-05 2006-08-10 Piaoyang Sun Quinazoline compounds or their medical salts and preparation and medical usage thereof
KR100832593B1 (ko) * 2005-11-08 2008-05-27 한미약품 주식회사 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법
CA2629249C (en) 2005-11-11 2015-05-05 Boehringer Ingelheim International Gmbh Combination treatment of cancer comprising egfr/her2 inhibitors
CA2833706C (en) 2005-11-11 2014-10-21 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
PL1981863T3 (pl) 2006-01-26 2013-03-29 Boehringer Ingelheim Int Sposób wytwarzania pochodnych chinazoliny podstawionych przez ugrupowanie aminokrotonyloaminowe
CA2663599A1 (en) * 2006-09-18 2008-03-27 Boehringer Ingelheim International Gmbh Method for treating cancer harboring egfr mutations
EP1921070A1 (de) 2006-11-10 2008-05-14 Boehringer Ingelheim Pharma GmbH & Co. KG Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstelllung
JP5377332B2 (ja) 2007-02-06 2013-12-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 二環式へテロ環、それらの化合物を含む薬剤、その使用及びその製法
WO2009098061A1 (de) 2008-02-07 2009-08-13 Boehringer Ingelheim International Gmbh Spirocyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
MX2010012442A (es) 2008-05-13 2011-10-11 Astrazeneca Ab Sal de fumarato de 4-(3-cloro-2-fluoroanilino)-7-metoxi-6-{[1-(n-m etilcarbamoilmetil) piperidin-4-il]oxi}quinazolina.
PE20100252A1 (es) 2008-06-06 2010-04-12 Boehringer Ingelheim Int Nuevas formulaciones farmaceuticas solidas que comprenden dimaleato de 4-[(3-cloro-4-fluorofenil) amino]-6-{[4-(n,n-dimetilamino)-1-oxo-2-buten-1-il] amino}-7-((s)-tetrahidrofuran-3-iloxi)-quinazolina
US8426430B2 (en) 2008-06-30 2013-04-23 Hutchison Medipharma Enterprises Limited Quinazoline derivatives
EP2313397B1 (de) 2008-08-08 2016-04-20 Boehringer Ingelheim International GmbH Cyclohexyloxy-substituierte heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung
WO2010054285A2 (en) 2008-11-10 2010-05-14 National Health Research Institutes Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors
JP2012515184A (ja) 2009-01-14 2012-07-05 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 大腸がんの治療方法
KR20110118668A (ko) 2009-02-13 2011-10-31 베링거 인겔하임 인터내셔날 게엠베하 1형 당뇨병, 2형 당뇨병, 내당능 장애 또는 고혈당증을 치료하기 위한 sglt­2 억제제
EP2429520A1 (en) 2009-05-14 2012-03-21 Boehringer Ingelheim International GmbH New combination therapy in treatment of oncological and fibrotic diseases
WO2010130758A1 (en) * 2009-05-14 2010-11-18 Boehringer Ingelheim International Gmbh New combination therapy in treatment of cancer and fibrotic diseases
SI2451445T1 (sl) 2009-07-06 2019-07-31 Boehringer Ingelheim International Gmbh Postopek za sušenje BIBW2992, njegovih soli in trdnih farmacevtskih formulacij, ki obsegajo to aktivno sestavino
WO2011069962A1 (en) 2009-12-07 2011-06-16 Boehringer Ingelheim International Gmbh Bibw 2992 for use in the treatment of triple negative breast cancer
US8735409B2 (en) * 2009-12-21 2014-05-27 Qiang Zhang Quinazoline derivatives
US20120107304A1 (en) 2010-04-27 2012-05-03 Boehringer Ingelheim International Gmbh Combination therapy in treatment of oncological and fibrotic diseases
US20130289056A1 (en) 2010-08-26 2013-10-31 Boehringer Ingelheim International Gmbh Methods of administering an egfr inhibitor
JP5808818B2 (ja) * 2010-11-25 2015-11-10 ラツィオファーム・ゲーエムベーハー アファチニブの新規塩及び多形形態
EP2680850B1 (en) 2011-03-04 2018-05-23 Newgen Therapeutics, Inc. Alkyne substituted quinazoline compound and methods of use
US8828391B2 (en) 2011-05-17 2014-09-09 Boehringer Ingelheim International Gmbh Method for EGFR directed combination treatment of non-small cell lung cancer
CN102918029B (zh) * 2011-05-17 2015-06-17 江苏康缘药业股份有限公司 4-苯胺-6-丁烯酰胺-7-烷醚喹唑啉衍生物及其制备方法和用途
CN102838590B (zh) * 2011-06-21 2014-07-09 苏州迈泰生物技术有限公司 氨基喹唑啉衍生物及其在制备抗恶性肿瘤药物中的用途
US20150232457A1 (en) 2011-10-06 2015-08-20 Ratiopharm Gmbh Crystalline forms of afatinib di-maleate
CN103073539B (zh) * 2011-10-26 2016-05-11 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
HUE033177T2 (en) 2012-01-17 2017-11-28 Astellas Pharma Inc Pyrazine carboxamide compound
CN103772380A (zh) * 2012-10-23 2014-05-07 杨子娇 一类治疗房角狭窄的化合物及其用途
EP2951171A1 (en) 2013-02-01 2015-12-09 Boehringer Ingelheim International GmbH Radiolabeled quinazoline derivatives
US11813275B2 (en) 2013-04-05 2023-11-14 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
HRP20190101T1 (hr) 2013-04-05 2019-03-08 Boehringer Ingelheim International Gmbh Terapeutske uporabe empagliflozina
CA2812519A1 (en) 2013-04-05 2014-10-05 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US20140303097A1 (en) 2013-04-05 2014-10-09 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
PL2986304T3 (pl) 2013-04-18 2022-05-02 Boehringer Ingelheim International Gmbh Kompozycja farmaceutyczna, sposoby leczenia i jej zastosowania
WO2014180271A1 (zh) * 2013-05-10 2014-11-13 苏州明锐医药科技有限公司 阿法替尼及其中间体的制备方法
CN103254182A (zh) * 2013-05-10 2013-08-21 苏州明锐医药科技有限公司 一种阿法替尼的制备方法
CN103254183B (zh) * 2013-05-10 2015-11-11 苏州明锐医药科技有限公司 阿法替尼的制备方法
CN103242303B (zh) * 2013-05-16 2015-03-25 苏州明锐医药科技有限公司 阿法替尼的制备方法
WO2014183560A1 (zh) * 2013-05-16 2014-11-20 苏州明锐医药科技有限公司 阿法替尼及其中间体的制备方法
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
CN103755688B (zh) * 2013-12-24 2015-11-18 江苏奥赛康药业股份有限公司 一种阿法替尼化合物的制备方法
US9242965B2 (en) 2013-12-31 2016-01-26 Boehringer Ingelheim International Gmbh Process for the manufacture of (E)-4-N,N-dialkylamino crotonic acid in HX salt form and use thereof for synthesis of EGFR tyrosine kinase inhibitors
EA031059B1 (ru) 2014-01-02 2018-11-30 Тева Фармасьютикалз Интернэшнл Гмбх Кристаллическая форма альфа дималеата афатиниба
CN105315263B (zh) * 2014-07-30 2018-11-27 正大天晴药业集团股份有限公司 阿法替尼中间体的合成方法
EP3023421A1 (en) 2014-11-21 2016-05-25 Sandoz Ag Crystalline forms of afatinib dimaleate
CN105801568B (zh) 2015-01-15 2019-07-30 杭州普晒医药科技有限公司 阿法替尼一马来酸盐晶型及其制备方法和药物组合物
HK1244278B (zh) 2015-03-20 2020-04-17 正大天晴药业集团股份有限公司 喹唑啉衍生物的盐及其制备方法
CN105175400B (zh) * 2015-09-29 2018-04-10 河北神威药业有限公司 一种阿法替尼中间体的制备方法
WO2017141271A1 (en) * 2016-02-17 2017-08-24 Sun Pharmaceutical Industries Ltd. Stable pharmaceutical composition of afatinib
CN106442793B (zh) * 2016-10-21 2019-05-24 河北神威药业有限公司 一种制备阿法替尼的中间体及其对映异构体的检测方法
WO2018087132A1 (en) 2016-11-10 2018-05-17 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
JP2021506974A (ja) * 2017-12-18 2021-02-22 スターングリーン、インク. チロシンキナーゼ阻害剤として有用なピリミジン化合物
CN110437163A (zh) * 2018-05-03 2019-11-12 斯特恩格林公司 作为酪氨酸激酶抑制剂的嘧啶类化合物
WO2020068867A1 (en) 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
CN109265449B (zh) * 2018-11-07 2021-11-23 沈阳工业大学 Egfr和her2双靶点酪氨酸激酶抑制剂及制备方法和用途
BR112021011894A2 (pt) 2018-12-21 2021-09-08 Daiichi Sankyo Company, Limited Composição farmacêutica
CN109824657A (zh) * 2019-03-26 2019-05-31 石药集团中奇制药技术(石家庄)有限公司 一种二马来酸阿法替尼新晶型及其制备方法和应用
AU2020328598B2 (en) 2019-08-15 2026-07-02 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
CN110590682A (zh) * 2019-10-14 2019-12-20 重庆医科大学 一种制备阿法替尼杂质的方法以及制备的杂质
US20210161897A1 (en) 2019-11-12 2021-06-03 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
US20230056604A1 (en) 2020-01-20 2023-02-23 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
US20210369709A1 (en) 2020-05-27 2021-12-02 Astrazeneca Ab EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER
CN115894383B (zh) * 2021-09-30 2025-12-19 北京赛特明强医药科技有限公司 一种喹唑啉类化合物、组合物及其应用
CN119278041A (zh) 2022-03-31 2025-01-07 阿斯利康(瑞典)有限公司 用于治疗癌症的与akt抑制剂组合的表皮生长因子受体(egfr)酪氨酸激酶抑制剂
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application in the treatment of cancer
AU2023262556A1 (en) 2022-04-28 2024-12-05 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2023209088A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their use in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
JP2025525410A (ja) 2022-06-27 2025-08-05 アストラゼネカ・アクチエボラーグ 癌を治療するための上皮成長因子受容体チロシンキナーゼ阻害剤を伴う組み合わせ

Citations (1)

* 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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100503580C (zh) * 1996-04-12 2009-06-24 沃尼尔·朗伯公司 酪氨酸激酶的不可逆抑制剂
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
TR200102505T2 (tr) * 1999-02-27 2003-01-21 Boehringer Ingelheim Pharma Kg 4-amino-kinazolin ve kinolin türevleri.
DE19911366A1 (de) * 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19908567A1 (de) * 1999-02-27 2000-08-31 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
DE19911509A1 (de) * 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
NZ516633A (en) * 1999-06-21 2004-09-24 Boehringer Ingelheim Pharma Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
DE50111799D1 (de) * 2000-04-08 2007-02-15 Boehringer Ingelheim Pharma Bicyclische heterocyclen, diese verbindungen enthaltende arzneimittel, deren verwendung und verfahren zu ihrer herstellung

Patent Citations (1)

* 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

Also Published As

Publication number Publication date
RS50860B (sr) 2010-08-31
PL214798B1 (pl) 2013-09-30
MY136086A (en) 2008-08-29
ZA200304141B (en) 2004-04-15
EP1345910B1 (de) 2009-04-29
ATE430136T1 (de) 2009-05-15
BR0116266A (pt) 2004-02-17
NO2014003I2 (no) 2015-10-19
HK1060571A1 (en) 2004-08-13
DK1345910T3 (da) 2009-07-20
NZ526918A (en) 2006-11-30
CY1109290T1 (el) 2014-07-02
CZ302721B6 (cs) 2011-09-21
FR14C0009I1 (fr) 2014-03-07
SK287573B6 (sk) 2011-03-04
EE200300300A (et) 2003-10-15
KR20030071787A (ko) 2003-09-06
ES2326617T3 (es) 2009-10-16
CY2014008I1 (el) 2014-07-02
HRP20030504B1 (en) 2011-09-30
BG66139B1 (bg) 2011-07-29
EP1345910A1 (de) 2003-09-24
JP2004516283A (ja) 2004-06-03
IL156277A (en) 2009-12-24
HUS1400005I1 (hu) 2017-08-28
EE05244B1 (et) 2009-12-15
BE2014C009I2 (enExample) 2021-02-04
DE10063435A1 (de) 2002-07-04
BG107929A (bg) 2005-01-31
PL361798A1 (en) 2004-10-04
SK7712003A3 (en) 2003-10-07
EA006317B1 (ru) 2005-10-27
ES2326617T9 (es) 2014-09-10
TWI295992B (en) 2008-04-21
HUP0301852A2 (hu) 2003-09-29
JP3827641B2 (ja) 2006-09-27
LTC1345910I2 (lt) 2022-06-10
AU2002219174B2 (en) 2007-09-06
CY2014008I2 (el) 2015-12-09
NO20032726L (no) 2003-06-16
YU49603A (sh) 2006-05-25
LU92370I2 (fr) 2014-03-31
EP2112140A1 (de) 2009-10-28
AU1917402A (en) 2002-07-01
LU92370I9 (enExample) 2019-01-17
MEP59508A (en) 2011-05-10
NO20032726D0 (no) 2003-06-16
SI1345910T1 (sl) 2009-08-31
IL156277A0 (en) 2004-01-04
NO325672B1 (no) 2008-07-07
BRPI0116266B8 (pt) 2021-07-27
HUP0301852A3 (en) 2008-03-28
EP1345910B9 (de) 2014-06-04
PT1345910E (pt) 2009-07-14
EA200300671A1 (ru) 2004-06-24
CN1481370A (zh) 2004-03-10
NO2022028I1 (no) 2022-07-01
LTPA2014005I1 (lt) 2022-05-25
ME02777B (me) 2011-10-10
HU228874B1 (en) 2013-06-28
CA2432428C (en) 2009-09-01
FR14C0009I2 (fr) 2014-11-14
UA74614C2 (en) 2006-01-16
HRP20030504A2 (en) 2005-06-30
BRPI0116266B1 (pt) 2017-10-31
DE50114874D1 (de) 2009-06-10
AR040524A1 (es) 2005-04-13
CN1277822C (zh) 2006-10-04
UY27078A1 (es) 2002-07-31
WO2002050043A1 (de) 2002-06-27
CZ20031930A3 (cs) 2003-10-15
MXPA03005559A (es) 2004-10-14
NO2014003I1 (no) 2014-06-02
CA2432428A1 (en) 2002-06-27

Similar Documents

Publication Publication Date Title
CA2432428C (en) Quinazoline derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
USRE43431E1 (en) Quinazoline derivatives and pharmaceutical compositions containing them
AU775285B2 (en) Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
KR100862873B1 (ko) 이환식 헤테로사이클, 당해 화합물을 함유하는 약제 및 이의 제조방법
CA2484395C (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
AU2004213129A1 (en) Bicyclic heterocycles, medicaments containing said compounds, use thereof, and method for the production thereof
US20110136806A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, the use thereof and processes for the preparation thereof
DE10326186A1 (de) Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung

Legal Events

Date Code Title Description
PA0105 International application

St.27 status event code: A-0-1-A10-A15-nap-PA0105

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

R15-X000 Change to inventor requested

St.27 status event code: A-3-3-R10-R15-oth-X000

R16-X000 Change to inventor recorded

St.27 status event code: A-3-3-R10-R16-oth-X000

PG1501 Laying open of application

St.27 status event code: A-1-1-Q10-Q12-nap-PG1501

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

R17-X000 Change to representative recorded

St.27 status event code: A-3-3-R10-R17-oth-X000

A201 Request for examination
E13-X000 Pre-grant limitation requested

St.27 status event code: A-2-3-E10-E13-lim-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

PA0201 Request for examination

St.27 status event code: A-1-2-D10-D11-exm-PA0201

E902 Notification of reason for refusal
PE0902 Notice of grounds for rejection

St.27 status event code: A-1-2-D10-D21-exm-PE0902

T11-X000 Administrative time limit extension requested

St.27 status event code: U-3-3-T10-T11-oth-X000

P11-X000 Amendment of application requested

St.27 status event code: A-2-2-P10-P11-nap-X000

P13-X000 Application amended

St.27 status event code: A-2-2-P10-P13-nap-X000

E701 Decision to grant or registration of patent right
PE0701 Decision of registration

St.27 status event code: A-1-2-D10-D22-exm-PE0701

GRNT Written decision to grant
PR0701 Registration of establishment

St.27 status event code: A-2-4-F10-F11-exm-PR0701

PR1002 Payment of registration fee

St.27 status event code: A-2-2-U10-U12-oth-PR1002

Fee payment year number: 1

PG1601 Publication of registration

St.27 status event code: A-4-4-Q10-Q13-nap-PG1601

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 4

R18-X000 Changes to party contact information recorded

St.27 status event code: A-5-5-R10-R18-oth-X000

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 5

FPAY Annual fee payment

Payment date: 20130726

Year of fee payment: 6

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 6

S14-X000 Exclusive voluntary license recorded

St.27 status event code: A-4-4-S10-S14-lic-X000

A101 Application to extend term of patent right by permit
PA0101 Application to register extension of term of patent right by permit, etc.

St.27 status event code: A-4-4-G10-G18-tex-PA0101

Protection beyond ip right term event data comment text: Claim Total Quantity : 8, Claim Number : 1, 2, 3, 4, 5, 6, 9, 10, Period Limitation Text : 1489, Comment Text : 88

FPAY Annual fee payment

Payment date: 20140725

Year of fee payment: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 7

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 8

PE0702 Decision to register extension of term of patent right by permit, etc.

St.27 status event code: A-4-4-G10-G20-tex-PE0702

Protection beyond ip right term event data comment text: Claim Total Quantity : 8, Claim Number : 1, 2, 3, 4, 5, 6, 9, 10, Period Limitation Text : 1489, Comment Text : 88

FPAY Annual fee payment

Payment date: 20160729

Year of fee payment: 9

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 9

FPAY Annual fee payment

Payment date: 20170728

Year of fee payment: 10

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 10

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 11

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 12

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 13

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 14

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 15

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 16

PR1001 Payment of annual fee

St.27 status event code: A-4-4-U10-U11-oth-PR1001

Fee payment year number: 17

PC1801 Expiration of term

St.27 status event code: N-4-6-H10-H14-oth-PC1801

Not in force date: 20260110

Ip right cessation event data comment text: Termination Category : EXPIRATION_OF_DURATION