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IL156277A - Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof - Google Patents

Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof

Info

Publication number
IL156277A
IL156277A IL156277A IL15627703A IL156277A IL 156277 A IL156277 A IL 156277A IL 156277 A IL156277 A IL 156277A IL 15627703 A IL15627703 A IL 15627703A IL 156277 A IL156277 A IL 156277A
Authority
IL
Israel
Prior art keywords
amino
chloro
fluorophenyl
tetrahydrofuran
quinazoline
Prior art date
Application number
IL156277A
Other languages
Hebrew (he)
Original Assignee
Boehringer Ingelheim Pharma
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=IL156277(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Pharma filed Critical Boehringer Ingelheim Pharma
Publication of IL156277A publication Critical patent/IL156277A/en

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)
  • 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)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (7)

- 32 - 156277/3 CLAIMS:
1. A compound of formula I wherein Ra is a benzyl, 1-phenylethyl, or 3-chloro-4-fluorophenyl group; Rb is a dimethylamino group; and Rc is a tetrahydrofuran-3-yloxy, tetrahydrofuran-2-ylmethoxy, tetrahydrofuran-3-ylmethoxy, tetrahydropyran-4-yloxy, or tetrahydropyran-4-ylmethoxy group, or a stereoisomer or physiologically acceptable salt thereof.
2. The compound of formula I according to claim 1, wherein : Ra is a 1-phenylethyl or 3-chloro-4-fluorophenyl group; or a stereoisomer or physiologically acceptable salt thereof.
3. The compounds of claim 1, wherein Ra is a 3-chloro-4-fluorophenyl group, or a stereoisomer or physiologically acceptable salt thereof.
4. The following compounds of general formula I according to claim 1 : (a) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)- l-oxo-2-buten-l-yl]amino}-7-((fl)-tetrahydrofuran-3-yloxy)- quinazoline, (b) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)- l-oxo-2-buten-l-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)- quinazoline, - 33 - 156277/3 (c) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)- l-oxo-2-buten-l-yl]amino}-7-(tetrahydropyran-4-yloxy)- quinazoline, (d) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dirnethylamino)- l-oxo-2-buten-l-yl]amino}-7-[(tetrahydrofuran-2-yl)methoxy]- quinazoline, (e) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)- l-oxo-2-buten-l-yl]amino}-7-[(tetrahydrofuran-3-yl)methoxy]- quinazoline, (f) 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)- -l-oxo-2-buten-l-yl]amino}-7-[(S)-(tetrahydrofuran-2- yl)methoxy]-quinazoline, the tautomers, the stereoisomers and the salts thereof.
5. The following compound of general formula I according to claim 1 : 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-l- oxo-2-buten-l-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline, the tautomers, the stereoisomers and the salts thereof.
6. Pharmaceutical compositions containing a compound according to at least one of claims 1 to 5 optionally together with one or more inert carriers and/or diluents.
7. Use of a compound according to at least one of claims 1 to 5 for preparing a pharmaceutical composition which is suitable for treating benign or malignant tumours, for preventing and treating diseases of the airways and lungs and for treating diseases of the gastrointestinal tract and the bile duct and gall bladder. For the Applicants, REINHOLD COHN AND PARTNERS
IL156277A 2000-12-20 2003-06-03 Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof IL156277A (en)

Applications Claiming Priority (2)

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
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 (1)

Publication Number Publication Date
IL156277A true IL156277A (en) 2009-12-24

Family

ID=7667887

Family Applications (2)

Application Number Title Priority Date Filing Date
IL15627701A IL156277A0 (en) 2000-12-20 2001-12-12 Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof
IL156277A IL156277A (en) 2000-12-20 2003-06-03 Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof

Family Applications Before (1)

Application Number Title Priority Date Filing Date
IL15627701A IL156277A0 (en) 2000-12-20 2001-12-12 Quinazoline derivatives, medicaments containing said compounds, their utilization and method for the production thereof

Country Status (40)

Country Link
EP (2) EP2112140A1 (en)
JP (1) JP3827641B2 (en)
KR (1) KR100852102B1 (en)
CN (1) CN1277822C (en)
AR (1) AR040524A1 (en)
AT (1) ATE430136T1 (en)
AU (2) AU2002219174B2 (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 (3) 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)

Families Citing this family (87)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
YU90901A (en) 1999-06-21 2004-07-15 Boehringer Ingelheim Pharma Gmbh. & Co.Kg. 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 (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
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 (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
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
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
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 (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
GEP20084551B (en) * 2004-05-06 2008-11-25 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
JP5688877B2 (en) * 2005-11-11 2015-03-25 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 Quinazoline derivatives for the treatment of cancer diseases
SI1948180T1 (en) * 2005-11-11 2013-06-28 Boehringer Ingelheim International Gmbh Combination treatment of cancer comprising egfr/her2 inhibitors
PT1981863E (en) 2006-01-26 2012-12-07 Boehringer Ingelheim Int Process for preparing aminocrotonylamino-substituted quinazoline derivatives
JP2010503717A (en) 2006-09-18 2010-02-04 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 Methods for treating tumors with 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
US7998949B2 (en) 2007-02-06 2011-08-16 Boehringer Ingelheim International Gmbh Bicyclic heterocycles, drugs containing said compounds, use thereof, and method for production thereof
ME01461B (en) 2008-02-07 2014-04-20 Boehringer Ingelheim Int Spirocyclic heterocycles, medicaments containing said compounds, use thereof and method for their production
BRPI0912170A2 (en) 2008-05-13 2015-10-13 Astrazeneca Ab compound, form, process for preparation thereof, pharmaceutical composition, use of a compound, and method for treating cancer in a warm-blooded animal
UY31867A (en) 2008-06-06 2010-01-29 Boehringer Ingelheim Int NEW SOLID PHARMACEUTICAL FORMULATIONS THAT INCLUDE BIBW 2992
US8426430B2 (en) 2008-06-30 2013-04-23 Hutchison Medipharma Enterprises Limited Quinazoline derivatives
WO2010015522A1 (en) 2008-08-08 2010-02-11 Boehringer Ingelheim International Gmbh Cyclohexyloxy-substituted heterocyclics, medicines containing these compounds and method for the production thereof
KR101703941B1 (en) 2008-11-10 2017-02-07 내셔날 헬스 리서치 인스티튜트 Fused Bicyclic and Tricyclic Pyrimidine Compounds as Tyrosine Kinase Inhibitors
JP2012515184A (en) 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 How to treat colorectal cancer
EP2429527A1 (en) * 2009-05-14 2012-03-21 Boehringer Ingelheim International GmbH New combination therapy in treatment of cancer and fibrotic diseases
EP2429520A1 (en) 2009-05-14 2012-03-21 Boehringer Ingelheim International GmbH New combination therapy in treatment of oncological and fibrotic diseases
HUE044629T2 (en) 2009-07-06 2019-11-28 Boehringer Ingelheim Int Process for drying of bibw2992, of its salts and of solid pharmaceutical formulations comprising this active ingredient
JP2013512882A (en) 2009-12-07 2013-04-18 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 BIBW2992 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
PT2608792T (en) 2010-08-26 2018-01-15 Boehringer Ingelheim Int Methods of administering an egfr inhibitor
EP2643314B1 (en) 2010-11-25 2016-07-13 ratiopharm GmbH Novel salts and polymorphic forms of afatinib
CA2828713C (en) 2011-03-04 2022-08-16 Newgen Therapeutics, Inc. Alkyne substituted quinazoline compounds 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 (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
JP5532366B2 (en) 2012-01-17 2014-06-25 アステラス製薬株式会社 Pyrazinecarboxamide compounds
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
ES2702174T3 (en) 2013-04-05 2019-02-27 Boehringer Ingelheim Int Therapeutic uses of empagliflozin
US11813275B2 (en) 2013-04-05 2023-11-14 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
SI2986304T1 (en) 2013-04-18 2022-04-29 Boehringer Ingelheim International Gmbh Pharmaceutical composition, methods for treating and uses thereof
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
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
CN103242303B (en) * 2013-05-16 2015-03-25 苏州明锐医药科技有限公司 Afatinib preparation method
CN104513229A (en) 2013-09-28 2015-04-15 正大天晴药业集团股份有限公司 Quinazoline derivatives and preparation method 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
EP3089976B1 (en) 2014-01-02 2019-08-14 Teva Pharmaceuticals International GmbH Crystalline forms of afatinib dimaleate
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
ES2775614T3 (en) 2015-03-20 2020-07-27 Chai Tai Tianqing Pharmaceutical Group Co Ltd Quinazoline derivative salts and method of preparation thereof
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
JP2021506974A (en) * 2017-12-18 2021-02-22 スターングリーン、インク． Pyrimidine compounds useful as tyrosine kinase inhibitors
CN110437163A (en) * 2018-05-03 2019-11-12 斯特恩格林公司 Pyrimidines as tyrosine kinase inhibitor
CA3113241A1 (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 (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 A kind of method for preparing Afatinib impurity and prepared impurity
US20210161897A1 (en) 2019-11-12 2021-06-03 Astrazeneca Ab Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer
CA3166980A1 (en) 2020-01-20 2021-07-29 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
WO2023051687A1 (en) * 2021-09-30 2023-04-06 北京赛特明强医药科技有限公司 Quinazoline compound, composition, and application thereof
IL315848A (en) 2022-03-31 2024-11-01 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
KR20250006237A (en) 2022-04-28 2025-01-10 아스트라제네카 아베 Condensed bicyclic heteroaromatic compounds and their use in the treatment of cancer
US20240116926A1 (en) 2022-04-28 2024-04-11 Astrazeneca Ab Heteroaromatic compounds
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
CN119421895A (en) 2022-06-27 2025-02-11 阿斯利康(瑞典)有限公司 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
DE69710712T3 (en) * 1996-04-12 2010-12-23 Warner-Lambert Co. Llc REVERSIBLE INHIBITORS OF TYROSINE KINASEN
ZA986732B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitiors of tyrosine kinases
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
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
AU3281600A (en) * 1999-02-27 2000-09-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transsduction mediated by tyrosine kinases
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
DE19911509A1 (en) * 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclic heterocycles, medicaments containing these compounds, their use and processes for their preparation
YU90901A (en) * 1999-06-21 2004-07-15 Boehringer Ingelheim Pharma Gmbh. & Co.Kg. Bicyclic heterocycles, medicaments containing these compounds, their use and methods for the production thereof
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

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