CA2557433C - Quinazoline derivatives and therapeutic use thereof - Google Patents

Quinazoline derivatives and therapeutic use thereof Download PDF

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Publication number
CA2557433C
CA2557433C CA2557433A CA2557433A CA2557433C CA 2557433 C CA2557433 C CA 2557433C CA 2557433 A CA2557433 A CA 2557433A CA 2557433 A CA2557433 A CA 2557433A CA 2557433 C CA2557433 C CA 2557433C
Authority
CA
Canada
Prior art keywords
group
compound
fluorophenyl
tumors
phenyl
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 - Fee Related
Application number
CA2557433A
Other languages
English (en)
French (fr)
Other versions
CA2557433A1 (en
Inventor
Young Bok Lee
Chang Ho Ahn
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.)
Rexahn Corp
Original Assignee
Rexahn Corp
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=34886161&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2557433(C) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Rexahn Corp filed Critical Rexahn Corp
Publication of CA2557433A1 publication Critical patent/CA2557433A1/en
Application granted granted Critical
Publication of CA2557433C publication Critical patent/CA2557433C/en
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CA2557433A 2004-02-19 2005-02-17 Quinazoline derivatives and therapeutic use thereof Expired - Fee Related CA2557433C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US54548704P 2004-02-19 2004-02-19
US60/545,487 2004-02-19
PCT/US2005/005151 WO2005080352A2 (en) 2004-02-19 2005-02-17 Quinazoline derivatives and therapeutic use thereof

Publications (2)

Publication Number Publication Date
CA2557433A1 CA2557433A1 (en) 2005-09-01
CA2557433C true CA2557433C (en) 2013-05-14

Family

ID=34886161

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2557433A Expired - Fee Related CA2557433C (en) 2004-02-19 2005-02-17 Quinazoline derivatives and therapeutic use thereof

Country Status (11)

Country Link
US (2) US7388014B2 (https=)
EP (2) EP2650286A1 (https=)
JP (1) JP4934432B2 (https=)
KR (1) KR100942865B1 (https=)
CN (1) CN1956966B (https=)
AU (1) AU2005214373B2 (https=)
BR (1) BRPI0507903A (https=)
CA (1) CA2557433C (https=)
ES (1) ES2554330T3 (https=)
MX (1) MXPA06009475A (https=)
WO (1) WO2005080352A2 (https=)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8039637B2 (en) * 2005-06-23 2011-10-18 Array Biopharma Inc. Process for preparing benzimidazole compounds
AU2007249762A1 (en) * 2006-05-15 2007-11-22 Senex Biotechnology, Inc Identification of CDKI pathway inhibitors
WO2008124823A1 (en) * 2007-04-10 2008-10-16 Myriad Genetics, Inc. Method of treating melanoma
CN101120945B (zh) * 2007-07-30 2010-11-24 浙江大学 8-芳胺基-3H-咪唑[4,5-g]喹唑啉类衍生物的用途
PH12012500097A1 (en) * 2009-07-21 2011-01-27 Shanghai Inst Organic Chem Potent small molecule inhibitors of autophagy, and methods of use thereof
WO2012006960A1 (en) * 2010-07-14 2012-01-19 Zhejiang Beta Pharma Inc. NOVEL FUSED HETEROCYCLIC DERIVATIVES USEFUL AS c-MET TYROSINE KINASE INHIBITORS
US20140309224A1 (en) * 2011-09-13 2014-10-16 Roninson Igor B TREATMENT OF DISEASES OR DISORDERS CAUSED BY INDUCED NFkB TRANSCRIPTIONAL ACTIVITY
CN103086984A (zh) * 2011-11-03 2013-05-08 南京大学 一类4-苯氨基喹唑啉类衍生物及其制备方法与用途
WO2013135671A1 (en) 2012-03-13 2013-09-19 Basf Se Fungicidal pyrimidine compounds
CN102659692B (zh) 2012-05-04 2014-04-09 郑州泰基鸿诺药物科技有限公司 双联厄洛替尼及其制备方法
CN102875570B (zh) * 2012-10-23 2015-11-04 浙江大学 喹唑啉衍生物及其制备方法和用途
JP6464139B2 (ja) 2013-03-14 2019-02-06 コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ ブロモドメイン含有タンパク質の阻害のための方法および組成物
WO2015036058A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
WO2015036059A1 (en) 2013-09-16 2015-03-19 Basf Se Fungicidal pyrimidine compounds
RU2016112013A (ru) * 2013-09-19 2017-10-24 Пьер Фабр Медикамент Производные хиназолина и их применение в качестве ингибиторов днк-метилтрансферазы
CN104926798B (zh) * 2014-03-21 2019-06-18 江苏豪森药业集团有限公司 阿法替尼中间体的高纯度制备方法
CA3006300C (en) 2015-11-25 2024-02-27 Convergene Llc Bicyclic bet bromodomain inhibitors and uses thereof
JP7191446B2 (ja) * 2017-01-30 2022-12-19 塩野義製薬株式会社 キナゾリン誘導体を含有する固形製剤
EP3897651A4 (en) * 2018-12-21 2022-09-21 University of Notre Dame du Lac DISCOVERY OF BD-OXIDASE INHIBITORS FOR THE TREATMENT OF MYCOBACTERIAL DISEASES
EP4424379A3 (en) 2019-04-24 2024-10-30 Convergene Llc Small molecule bromodomain inhibitors and uses thereof
KR102397359B1 (ko) * 2019-09-30 2022-05-11 한국화학연구원 4-아미노-퀴나졸린 유도체 및 이를 포함하는 항바이러스용 조성물
KR20220132543A (ko) * 2019-12-27 2022-09-30 루핀 리미티드 치환된 삼환 화합물
TWI807787B (zh) * 2021-04-19 2023-07-01 大陸商昆藥集團股份有限公司 苯並嘧啶三環衍生物及製備方法和應用
CN116444443B (zh) * 2023-03-15 2025-09-05 广东省中医院（广州中医药大学第二附属医院、广州中医药大学第二临床医学院、广东省中医药科学院） 一种苯甲酰-喹唑啉酮衍生物及其制备方法与应用

Family Cites Families (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH492395A (de) 1966-04-26 1970-06-30 Sandoz Ag Mittel zur Bekämpfung von Pflanzenschädlingen und Verwendung des Mittels
US4559157A (en) 1983-04-21 1985-12-17 Creative Products Resource Associates, Ltd. Cosmetic applicator useful for skin moisturizing
LU84979A1 (fr) 1983-08-30 1985-04-24 Oreal Composition cosmetique ou pharmaceutique sous forme aqueuse ou anhydre dont la phase grasse contient un polyether oligomere et polyethers oligomeres nouveaux
US4820508A (en) 1987-06-23 1989-04-11 Neutrogena Corporation Skin protective composition
GT198900008A (es) * 1988-01-29 1990-07-17 Derivados de quinolina, quinazolina y cinolina.
US4992478A (en) 1988-04-04 1991-02-12 Warner-Lambert Company Antiinflammatory skin moisturizing composition and method of preparing same
US5480883A (en) * 1991-05-10 1996-01-02 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US5710158A (en) * 1991-05-10 1998-01-20 Rhone-Poulenc Rorer Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
US6645969B1 (en) * 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5721237A (en) * 1991-05-10 1998-02-24 Rhone-Poulenc Rorer Pharmaceuticals Inc. Protein tyrosine kinase aryl and heteroaryl quinazoline compounds having selective inhibition of HER-2 autophosphorylation properties
AU661533B2 (en) * 1992-01-20 1995-07-27 Astrazeneca Ab Quinazoline derivatives
GB9314884D0 (en) * 1993-07-19 1993-09-01 Zeneca Ltd Tricyclic derivatives
IL112248A0 (en) * 1994-01-25 1995-03-30 Warner Lambert Co Tricyclic heteroaromatic compounds and pharmaceutical compositions containing them
AU5108196A (en) * 1995-03-20 1996-10-08 Dr. Karl Thomae Gmbh Imidazoquinazolines, drugs containing these compounds, their use and process for their preparation
MX9707453A (es) * 1995-03-30 1997-12-31 Pfizer Derivados de quinazolina.
GB9508565D0 (en) 1995-04-27 1995-06-14 Zeneca Ltd Quiazoline derivative
US6046206A (en) * 1995-06-07 2000-04-04 Cell Pathways, Inc. Method of treating a patient having a precancerous lesions with amide quinazoline derivatives
GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
GB9613021D0 (en) * 1996-06-21 1996-08-28 Pharmacia Spa Bicyclic 4-aralkylaminopyrimidine derivatives as tyrosine kinase inhibitors
EP0907642B1 (en) 1996-06-24 2005-11-02 Pfizer Inc. Phenylamino-substituted tricyclic derivatives for treatment of hyperproliferative diseases
HUP9900790A3 (en) 1996-08-30 2001-11-28 Kyowa Hakko Kogyo Kk Imidazoquinazoline derivatives
US6258820B1 (en) * 1999-03-19 2001-07-10 Parker Hughes Institute Synthesis and anti-tumor activity of 6,7-dialkoxy-4-phenylamino-quinazolines
ES2267748T3 (es) 2000-04-07 2007-03-16 Astrazeneca Ab Compuestos de quinazolina.
US6653305B2 (en) * 2000-08-26 2003-11-25 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
DE10042060A1 (de) * 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung

Also Published As

Publication number Publication date
US8404698B2 (en) 2013-03-26
EP1720841B1 (en) 2015-11-04
BRPI0507903A (pt) 2007-07-10
CN1956966B (zh) 2012-04-18
JP4934432B2 (ja) 2012-05-16
KR20070028340A (ko) 2007-03-12
US20090030021A1 (en) 2009-01-29
EP1720841A2 (en) 2006-11-15
WO2005080352A3 (en) 2006-02-16
JP2007523177A (ja) 2007-08-16
US20050187231A1 (en) 2005-08-25
MXPA06009475A (es) 2007-05-15
EP2650286A1 (en) 2013-10-16
CA2557433A1 (en) 2005-09-01
KR100942865B1 (ko) 2010-02-17
AU2005214373A1 (en) 2005-09-01
US7388014B2 (en) 2008-06-17
WO2005080352A2 (en) 2005-09-01
AU2005214373B2 (en) 2011-07-28
CN1956966A (zh) 2007-05-02
ES2554330T3 (es) 2015-12-18

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Effective date: 20210831

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Effective date: 20200217