CA2432428A1 - Quinazoline derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them - Google Patents

Quinazoline derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them Download PDF

Info

Publication number
CA2432428A1
CA2432428A1 CA002432428A CA2432428A CA2432428A1 CA 2432428 A1 CA2432428 A1 CA 2432428A1 CA 002432428 A CA002432428 A CA 002432428A CA 2432428 A CA2432428 A CA 2432428A CA 2432428 A1 CA2432428 A1 CA 2432428A1
Authority
CA
Canada
Prior art keywords
quinazoline derivatives
preparing
compounds
processes
pharmaceutical compositions
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.)
Granted
Application number
CA002432428A
Other languages
French (fr)
Other versions
CA2432428C (en
Inventor
Frank Himmelsbach
Elke Langkopf
Stefan Blech
Birgit Jung
Anke Baum
Flavio Solca
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Boehringer Ingelheim Pharma GmbH and Co KG
Original Assignee
Individual
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=CA2432428(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Individual filed Critical Individual
Publication of CA2432428A1 publication Critical patent/CA2432428A1/en
Application granted granted Critical
Publication of CA2432428C publication Critical patent/CA2432428C/en
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/16Otologicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/04Antineoplastic agents specific for metastasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth 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)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

The present invention relates to quinazoline derivatives of general formula (see formula I) wherein R a, R b and R c are defined as in claim 1, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibitory effect on signal transduction mediated by tyrosine kinases, their use in the treatment of diseases, especially tumoral diseases and diseases of the lungs and airways, and the preparation thereof.
CA002432428A 2000-12-20 2001-12-12 Quinazoline derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them Expired - Lifetime CA2432428C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10063435A DE10063435A1 (en) 2000-12-20 2000-12-20 Chinazoline derivatives, pharmaceuticals containing these compounds, their use and process for their preparation
DE10063435.4 2000-12-20
PCT/EP2001/014569 WO2002050043A1 (en) 2000-12-20 2001-12-12 Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof

Publications (2)

Publication Number Publication Date
CA2432428A1 true CA2432428A1 (en) 2002-06-27
CA2432428C CA2432428C (en) 2009-09-01

Family

ID=7667887

Family Applications (1)

Application Number Title Priority Date Filing Date
CA002432428A Expired - Lifetime CA2432428C (en) 2000-12-20 2001-12-12 Quinazoline derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them

Country Status (40)

Country Link
EP (2) EP1345910B9 (en)
JP (1) JP3827641B2 (en)
KR (1) KR100852102B1 (en)
CN (1) CN1277822C (en)
AR (1) AR040524A1 (en)
AT (1) ATE430136T1 (en)
AU (2) AU1917402A (en)
BE (1) BE2014C009I2 (en)
BG (1) BG66139B1 (en)
BR (1) BRPI0116266B8 (en)
CA (1) CA2432428C (en)
CY (2) CY1109290T1 (en)
CZ (1) CZ302721B6 (en)
DE (2) DE10063435A1 (en)
DK (1) DK1345910T3 (en)
EA (1) EA006317B1 (en)
EE (1) EE05244B1 (en)
ES (1) ES2326617T3 (en)
FR (1) FR14C0009I2 (en)
HK (1) HK1060571A1 (en)
HR (1) HRP20030504B1 (en)
HU (2) HU228874B1 (en)
IL (2) IL156277A0 (en)
LT (1) LTC1345910I2 (en)
LU (1) LU92370I2 (en)
ME (1) ME02777B (en)
MX (1) MXPA03005559A (en)
MY (1) MY136086A (en)
NO (2) NO325672B1 (en)
NZ (1) NZ526918A (en)
PL (1) PL214798B1 (en)
PT (1) PT1345910E (en)
RS (1) RS50860B (en)
SI (1) SI1345910T1 (en)
SK (1) SK287573B6 (en)
TW (1) TWI295992B (en)
UA (1) UA74614C2 (en)
UY (1) UY27078A1 (en)
WO (1) WO2002050043A1 (en)
ZA (1) ZA200304141B (en)

Cited By (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7846936B2 (en) 2003-04-29 2010-12-07 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US7863281B2 (en) 2002-04-19 2011-01-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
US7960546B2 (en) 2006-01-26 2011-06-14 Boehringer Ingelheim International Gmbh Process for preparing aminocrotonylamino-substituted quinazoline derivatives
US8404697B2 (en) 2005-11-11 2013-03-26 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
US9725439B2 (en) 2013-09-28 2017-08-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Quinazoline derivative and preparation method therefor
US11090323B2 (en) 2013-04-05 2021-08-17 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11666590B2 (en) 2013-04-18 2023-06-06 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11708335B2 (en) 2017-12-18 2023-07-25 Sterngreene, Inc. Pyrimidine compounds useful as tyrosine kinase inhibitors
US11813275B2 (en) 2013-04-05 2023-11-14 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11918596B2 (en) 2013-04-05 2024-03-05 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof

Families Citing this family (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2375259C (en) 1999-06-21 2009-04-28 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
US7019012B2 (en) 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
DE10204462A1 (en) * 2002-02-05 2003-08-07 Boehringer Ingelheim Pharma Use of tyrosine kinase inhibitors for the treatment of inflammatory processes
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
DE10221018A1 (en) 2002-05-11 2003-11-27 Boehringer Ingelheim Pharma Use of inhibitors of EGFR-mediated signal transduction for the treatment of benign prostatic hyperplasia (BPH) / prostatic hypertrophy
PE20040945A1 (en) * 2003-02-05 2004-12-14 Warner Lambert Co PREPARATION OF SUBSTITUTED QUINAZOLINES
DE10307165A1 (en) * 2003-02-20 2004-09-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation
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
DE10334226A1 (en) * 2003-07-28 2005-02-17 Boehringer Ingelheim Pharma Gmbh & Co. Kg Use of tyrosine kinase inhibitors for the treatment of inflammatory processes
GB0317665D0 (en) 2003-07-29 2003-09-03 Astrazeneca Ab Qinazoline derivatives
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 (en) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Process for the preparation of aminocrotonyl compounds
NZ550796A (en) * 2004-05-06 2010-07-30 Warner Lambert Co 4-phenylamino-quinazolin-6-yl-amides
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
PE20060777A1 (en) 2004-12-24 2006-10-06 Boehringer Ingelheim Int INDOLINONE DERIVATIVES FOR THE TREATMENT OR PREVENTION OF FIBROTIC DISEASES
WO2006081741A1 (en) * 2005-02-05 2006-08-10 Piaoyang Sun Quinazoline compounds or their medical salts and preparation and medical usage thereof
KR100832594B1 (en) * 2005-11-08 2008-05-27 한미약품 주식회사 Quinazoline derivatives as an multiplex inhibitor and method for the preparation thereof
US20090306101A1 (en) * 2005-11-11 2009-12-10 Flavio Solca Combination treatment of cancer comprising egfr/her2 inhibitors
RU2492864C2 (en) 2006-09-18 2013-09-20 Бёрингер Ингельхайм Интернациональ Гмбх Method of treating cancer carrying egfr mutations
EP1921070A1 (en) 2006-11-10 2008-05-14 Boehringer Ingelheim Pharma GmbH & Co. KG Bicyclic heterocycles, medicaments comprising them, their use and process for their preparation
EA200901041A1 (en) 2007-02-06 2010-02-26 Бёрингер Ингельхайм Интернациональ Гмбх BICYCLIC HETEROCYCLES CONTAINING THESE COMPOUNDS MEDICINES, THEIR APPLICATION AND METHOD OF OBTAINING THEM
WO2009098061A1 (en) 2008-02-07 2009-08-13 Boehringer Ingelheim International Gmbh Spirocyclic heterocycles, medicaments containing said compounds, use thereof and method for their production
WO2009138781A1 (en) 2008-05-13 2009-11-19 Astrazeneca Ab Fumarate salt of 4- (3-chloro-2-fluoroanilino) -7-methoxy-6- { [1- (n-methylcarbamoylmethyl) piperidin- 4-yl] oxy}quinazoline
PE20100252A1 (en) 2008-06-06 2010-04-12 Boehringer Ingelheim Int NEW SOLID PHARMACEUTICAL FORMULATIONS INCLUDING 4 - [(3-CHLORO-4-FLUOROPHENYL) AMINO DIMALEATE] -6 - {[4- (N, N-DIMETHYLAMINO) -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
CA2733153C (en) 2008-08-08 2016-11-08 Boehringer Ingelheim International Gmbh Cyclohexyloxy substituted heterocycles, pharmaceutical compositions containing these compounds and processes for preparing them
US8507502B2 (en) 2008-11-10 2013-08-13 National Health Research Institutes Fused bicyclic and tricyclic pyrimidine compounds as tyrosine kinase inhibitors
WO2010081817A1 (en) 2009-01-14 2010-07-22 Boehringer Ingelheim International Gmbh Method for treating colorectal cancer
JP2012526766A (en) 2009-05-14 2012-11-01 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 A novel combination therapy in the treatment of neoplastic and fibrotic diseases
US20120136004A1 (en) * 2009-05-14 2012-05-31 Boehringer Ingelheim International Gmbh New combination therapy in treatment of cancer and fibrotic diseases
US9545381B2 (en) 2009-07-06 2017-01-17 Boehringer Ingelheim International Gmbh Process for drying of BIBW2992, of its salts and of solid pharmaceutical formulations comprising this active ingredient
EP2509592A1 (en) 2009-12-07 2012-10-17 Boehringer Ingelheim International GmbH Bibw 2992 for use in the treatment of triple negative breast cancer
CN102686581B (en) * 2009-12-21 2015-08-26 张强 Quinazoline derivant
US20120107304A1 (en) 2010-04-27 2012-05-03 Boehringer Ingelheim International Gmbh Combination therapy in treatment of oncological and fibrotic diseases
WO2012027445A1 (en) 2010-08-26 2012-03-01 Boehringer Ingelheim International Gmbh Methods of administering an egfr inhibitor
JP5808818B2 (en) * 2010-11-25 2015-11-10 ラツィオファーム・ゲーエムベーハー Novel salt and polymorphic forms of afatinib
BR112013022552B1 (en) 2011-03-04 2021-11-23 Newgen Therapeutics, Inc QUINAZOLINE COMPOUNDS REPLACED WITH ALCINE, THEIR USE, PHARMACEUTICAL COMPOSITION, AND KIT
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 (en) * 2011-05-17 2015-06-17 江苏康缘药业股份有限公司 4-phenylamino-6-butenamide-7-alkyloxy quinazoline derivatives, preparative method and use thereof
CN102838590B (en) * 2011-06-21 2014-07-09 苏州迈泰生物技术有限公司 Amino quinazoline derivative and application thereof in preparation of antineoplastic drugs
WO2013052157A1 (en) 2011-10-06 2013-04-11 Ratiopharm Gmbh Crystalline forms of afatinib di-maleate
CN103073539B (en) * 2011-10-26 2016-05-11 齐鲁制药有限公司 4-(substituted benzene amino) quinazoline derivant and preparation method thereof, pharmaceutical composition and purposes
WO2013108754A1 (en) 2012-01-17 2013-07-25 アステラス製薬株式会社 Pyrazine carboxamide compound
CN103772380A (en) * 2012-10-23 2014-05-07 杨子娇 Type of compounds for treating narrow chamber angle and use of compounds
US20150368230A1 (en) 2013-02-01 2015-12-24 Boehringer Ingelheim International Gmbh Radiolabeled quinazoline derivatives
WO2014180271A1 (en) * 2013-05-10 2014-11-13 苏州明锐医药科技有限公司 Method for preparing afatinib and intermediate thereof
CN103254182A (en) * 2013-05-10 2013-08-21 苏州明锐医药科技有限公司 Method for preparing Afatinib
CN103254183B (en) * 2013-05-10 2015-11-11 苏州明锐医药科技有限公司 Ah method is for the preparation method of Buddhist nun
CN103242303B (en) * 2013-05-16 2015-03-25 苏州明锐医药科技有限公司 Afatinib preparation method
WO2014183560A1 (en) * 2013-05-16 2014-11-20 苏州明锐医药科技有限公司 Afatinib and preparation method of intermediate thereof
CN103755688B (en) * 2013-12-24 2015-11-18 江苏奥赛康药业股份有限公司 A kind of Ah method is for the preparation method of Buddhist nun's compound
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 (en) 2014-01-02 2018-11-30 Тева Фармасьютикалз Интернэшнл Гмбх Crystalline form alpha of afatinib di-maleate
CN105315263B (en) * 2014-07-30 2018-11-27 正大天晴药业集团股份有限公司 The synthetic method of afatinib intermediate
EP3023421A1 (en) 2014-11-21 2016-05-25 Sandoz Ag Crystalline forms of afatinib dimaleate
CN105801568B (en) 2015-01-15 2019-07-30 杭州普晒医药科技有限公司 One maleate crystal form of Afatinib and preparation method thereof and pharmaceutical composition
JP6704422B2 (en) * 2015-03-20 2020-06-03 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co.,Ltd. Quinazoline derivative salt and method for producing the same
CN105175400B (en) * 2015-09-29 2018-04-10 河北神威药业有限公司 A kind of preparation method of afatinib intermediate
WO2017141271A1 (en) * 2016-02-17 2017-08-24 Sun Pharmaceutical Industries Ltd. Stable pharmaceutical composition of afatinib
CN106442793B (en) * 2016-10-21 2019-05-24 河北神威药业有限公司 A kind of detection method of the intermediate for preparing Afatinib and its enantiomter
TWI808958B (en) 2017-01-25 2023-07-21 美商特普醫葯公司 Combination therapy involving diaryl macrocyclic compounds
CN110437163A (en) * 2018-05-03 2019-11-12 斯特恩格林公司 Pyrimidines as tyrosine kinase inhibitor
BR112021005513A2 (en) 2018-09-25 2021-06-22 Black Diamond Therapeutics, Inc. quinazoline derivatives as a tyrosine kinase inhibitor, compositions, manufacturing methods and use thereof
CN109265449B (en) * 2018-11-07 2021-11-23 沈阳工业大学 EGFR and HER2 double-target tyrosine kinase inhibitor and preparation method and application thereof
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
CN109824657A (en) * 2019-03-26 2019-05-31 石药集团中奇制药技术(石家庄)有限公司 Two maleic acid Afatinib novel crystal forms of one kind and its preparation method and application
CN110590682A (en) * 2019-10-14 2019-12-20 重庆医科大学 Method for preparing afatinib impurity and prepared impurity
WO2021094379A1 (en) 2019-11-12 2021-05-20 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
MX2022008874A (en) 2020-01-20 2022-08-11 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
WO2023187037A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
WO2023209090A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds and their application 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
WO2023209084A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
WO2023209086A1 (en) 2022-04-28 2023-11-02 Astrazeneca Ab Bicyclic heteroaromatic compounds for treating cancer
WO2024002938A1 (en) 2022-06-27 2024-01-04 Astrazeneca Ab Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI0892789T2 (en) * 1996-04-12 2010-03-31 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
ZA986732B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
ID29800A (en) * 1999-02-27 2001-10-11 Boehringer Ingelheim Pharma 4-AMINO-KINAZOLIN AND KINOLIN DISTRICTS THAT HAVE INHIBITOR EFFECTS ON SIGNAL TRANSDUKSI MEDIUMED BY THYROSIN KINASE
DE19908567A1 (en) * 1999-02-27 2000-08-31 Boehringer Ingelheim Pharma New 4-amino-quinazoline or quinoline derivatives, are tyrosine kinase-mediated signal transduction inhibitors useful e.g. for treating tumors, polyps or respiratory or gastrointestinal diseases
DE19911366A1 (en) * 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma New 4-amino-quinazoline or quinoline derivatives, are tyrosine kinase-mediated signal transduction inhibitors useful e.g. for treating tumors, polyps or respiratory or gastrointestinal diseases
DE19911509A1 (en) * 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation
CA2375259C (en) * 1999-06-21 2009-04-28 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2403152C (en) * 2000-04-08 2008-10-28 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7863281B2 (en) 2002-04-19 2011-01-04 Boehringer Ingelheim Pharma Gmbh & Co. Kg Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for the preparation thereof
US7846936B2 (en) 2003-04-29 2010-12-07 Boehringer Ingelheim International Gmbh Combinations for the treatment of diseases involving cell proliferation, migration or apoptosis of myeloma cells or angiogenesis
US8404697B2 (en) 2005-11-11 2013-03-26 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
US7960546B2 (en) 2006-01-26 2011-06-14 Boehringer Ingelheim International Gmbh Process for preparing aminocrotonylamino-substituted quinazoline derivatives
US11090323B2 (en) 2013-04-05 2021-08-17 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11813275B2 (en) 2013-04-05 2023-11-14 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11833166B2 (en) 2013-04-05 2023-12-05 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11918596B2 (en) 2013-04-05 2024-03-05 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US11666590B2 (en) 2013-04-18 2023-06-06 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
US9725439B2 (en) 2013-09-28 2017-08-08 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Quinazoline derivative and preparation method therefor
US11708335B2 (en) 2017-12-18 2023-07-25 Sterngreene, Inc. Pyrimidine compounds useful as tyrosine kinase inhibitors

Also Published As

Publication number Publication date
EP1345910B9 (en) 2014-06-04
AU2002219174B2 (en) 2007-09-06
TWI295992B (en) 2008-04-21
KR20030071787A (en) 2003-09-06
DK1345910T3 (en) 2009-07-20
NO20032726L (en) 2003-06-16
BR0116266A (en) 2004-02-17
NO2014003I2 (en) 2015-10-19
BG107929A (en) 2005-01-31
WO2002050043A1 (en) 2002-06-27
NO20032726D0 (en) 2003-06-16
BE2014C009I2 (en) 2021-02-04
CY1109290T1 (en) 2014-07-02
ATE430136T1 (en) 2009-05-15
HRP20030504B1 (en) 2011-09-30
ZA200304141B (en) 2004-04-15
BG66139B1 (en) 2011-07-29
EP1345910A1 (en) 2003-09-24
HRP20030504A2 (en) 2005-06-30
LTPA2014005I1 (en) 2022-05-25
FR14C0009I1 (en) 2014-03-07
EE200300300A (en) 2003-10-15
YU49603A (en) 2006-05-25
CZ20031930A3 (en) 2003-10-15
IL156277A0 (en) 2004-01-04
AR040524A1 (en) 2005-04-13
HU228874B1 (en) 2013-06-28
NO2014003I1 (en) 2014-06-02
KR100852102B1 (en) 2008-08-13
EE05244B1 (en) 2009-12-15
EA006317B1 (en) 2005-10-27
LU92370I9 (en) 2019-01-17
DE10063435A1 (en) 2002-07-04
IL156277A (en) 2009-12-24
UA74614C2 (en) 2006-01-16
SK287573B6 (en) 2011-03-04
NZ526918A (en) 2006-11-30
PT1345910E (en) 2009-07-14
ES2326617T3 (en) 2009-10-16
HUP0301852A2 (en) 2003-09-29
ES2326617T9 (en) 2014-09-10
LU92370I2 (en) 2014-03-31
MY136086A (en) 2008-08-29
AU1917402A (en) 2002-07-01
JP3827641B2 (en) 2006-09-27
DE50114874D1 (en) 2009-06-10
MXPA03005559A (en) 2004-10-14
NO325672B1 (en) 2008-07-07
FR14C0009I2 (en) 2014-11-14
UY27078A1 (en) 2002-07-31
CZ302721B6 (en) 2011-09-21
SI1345910T1 (en) 2009-08-31
EP2112140A1 (en) 2009-10-28
LTC1345910I2 (en) 2022-06-10
HK1060571A1 (en) 2004-08-13
HUS1400005I1 (en) 2017-08-28
PL361798A1 (en) 2004-10-04
SK7712003A3 (en) 2003-10-07
CY2014008I2 (en) 2015-12-09
CN1481370A (en) 2004-03-10
ME02777B (en) 2011-10-10
RS50860B (en) 2010-08-31
CY2014008I1 (en) 2014-07-02
MEP59508A (en) 2011-05-10
EA200300671A1 (en) 2004-06-24
CA2432428C (en) 2009-09-01
EP1345910B1 (en) 2009-04-29
CN1277822C (en) 2006-10-04
JP2004516283A (en) 2004-06-03
BRPI0116266B8 (en) 2021-07-27
HUP0301852A3 (en) 2008-03-28
PL214798B1 (en) 2013-09-30
BRPI0116266B1 (en) 2017-10-31

Similar Documents

Publication Publication Date Title
CA2432428A1 (en) Quinazoline derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2417652A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2417897A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2417050A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2375259A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2361174A1 (en) 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases
CA2368059A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
CA2403152A1 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
MY127771A (en) Bicyclic heterocyclic compounds, pharmaceutical compositions containing these compounds, their use and process for preparing them
CA2199401A1 (en) Pyrimido[5,4-d]pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
NO984084L (en) 4-Amino-pyrimidine derivatives, medicaments containing these compounds, their use and method of preparation thereof
AU2001295482A1 (en) Bicyclic heterocycles, medicaments containing these compounds, their use, and methods for the production thereof
TW200730508A (en) Bicyclic heterocycles, drugs containing said compounds, the use thereof and method for preparing same
NO984081L (en) Pyrimido [5,4-d] pyrimidines, medicaments containing these compounds, their use and method of preparation thereof
TW200510341A (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
BRPI0407709A (en) bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for their preparation
CA2387134A1 (en) Cyclopropanes as cgrp antagonists, medicaments containing said compounds and method for the production thereof
WO2000055162A3 (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
EA200901041A1 (en) BICYCLIC HETEROCYCLES CONTAINING THESE COMPOUNDS MEDICINES, THEIR APPLICATION AND METHOD OF OBTAINING THEM
MY140484A (en) Bicyclic heterocycles, pharmaceutical compositions containing these compounds, their use and processes for preparing them
YU60501A (en) 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transduction mediated by tyrosine kinases

Legal Events

Date Code Title Description
EEER Examination request
MKEX Expiry

Effective date: 20211213