KR20120090025A - 인 함유 퀴나졸린 화합물 및 그것의 사용 방법 - Google Patents

인 함유 퀴나졸린 화합물 및 그것의 사용 방법 Download PDF

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KR20120090025A
KR20120090025A KR1020127002859A KR20127002859A KR20120090025A KR 20120090025 A KR20120090025 A KR 20120090025A KR 1020127002859 A KR1020127002859 A KR 1020127002859A KR 20127002859 A KR20127002859 A KR 20127002859A KR 20120090025 A KR20120090025 A KR 20120090025A
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South Korea
Prior art keywords
methyl
compound
alkyl
cycloalkyl
quinazolin
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KR1020127002859A
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English (en)
Korean (ko)
Inventor
왕 센
아이민 장
준파 판
샤오링 쩡
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뉴젠 세러퓨틱스 인코포레이티드
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Publication of KR20120090025A publication Critical patent/KR20120090025A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6581—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms
    • C07F9/6584—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and nitrogen atoms with or without oxygen or sulfur atoms, as ring hetero atoms having one phosphorus atom as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6568—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms
    • C07F9/65685—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus atoms as the only ring hetero atoms the ring phosphorus atom being part of a phosphine oxide or thioxide
    • 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
    • A61P35/00—Antineoplastic 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
    • C07D239/74—Quinazolines; Hydrogenated quinazolines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, attached to ring carbon atoms of the hetero ring
    • 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
    • C07D405/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
    • C07F9/6509—Six-membered rings
    • C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
    • C07F9/65128—Six-membered rings having the nitrogen atoms in positions 1 and 3 condensed with carbocyclic rings or carbocyclic ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65586—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system at least one of the hetero rings does not contain nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020127002859A 2009-07-02 2010-07-02 인 함유 퀴나졸린 화합물 및 그것의 사용 방법 Withdrawn KR20120090025A (ko)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22255109P 2009-07-02 2009-07-02
US61/222,551 2009-07-02

Publications (1)

Publication Number Publication Date
KR20120090025A true KR20120090025A (ko) 2012-08-16

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KR1020127002859A Withdrawn KR20120090025A (ko) 2009-07-02 2010-07-02 인 함유 퀴나졸린 화합물 및 그것의 사용 방법

Country Status (13)

Country Link
US (1) US8987284B2 (enExample)
EP (1) EP2448409A4 (enExample)
JP (1) JP5721709B2 (enExample)
KR (1) KR20120090025A (enExample)
CN (1) CN102711472B (enExample)
AU (1) AU2010266725A1 (enExample)
BR (1) BRPI1015363A2 (enExample)
CA (1) CA2804190A1 (enExample)
IL (1) IL217222A0 (enExample)
MX (1) MX2012000166A (enExample)
RU (1) RU2012103492A (enExample)
SG (1) SG177451A1 (enExample)
WO (1) WO2011002523A1 (enExample)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BRPI1015363A2 (pt) 2009-07-02 2015-08-25 Newgen Therapeutics Inc Compostos de quinazolina contendo fósforo, uso dos mesmos, composição e kit
US8916574B2 (en) 2009-09-28 2014-12-23 Qilu Pharmaceutical Co., Ltd. 4-(substituted anilino)-quinazoline derivatives useful as tyrosine kinase inhibitors
CA2875025C (en) 2011-05-31 2021-08-03 Newgen Therapeutics, Inc. Tricyclic inhibitors of poly(adp-ribose)polymerase
CN103772411B (zh) * 2013-04-28 2016-08-03 复旦大学 含硫6-呋喃基喹唑啉-4-胺化合物及其制备方法和用途
CN104610364B (zh) * 2015-01-30 2017-03-29 江苏康缘药业股份有限公司 含磷取代的喹唑啉衍生物的新晶型及其制备方法和应用
CN104558042B (zh) * 2015-01-30 2017-03-29 江苏康缘药业股份有限公司 含磷取代的喹唑啉衍生物的新晶型及其制备方法和应用
CN104558043B (zh) * 2015-01-30 2017-01-11 江苏康缘药业股份有限公司 含磷取代的喹唑啉衍生物的新晶型及其制备方法和应用
CN104558041B (zh) * 2015-01-30 2017-01-11 江苏康缘药业股份有限公司 含磷取代的喹唑啉衍生物的新晶型及其制备方法和应用
CN104558040B (zh) * 2015-01-30 2017-04-05 江苏康缘药业股份有限公司 含磷取代的喹唑啉衍生物的晶型及其制备方法和应用
CN105388242A (zh) * 2015-11-11 2016-03-09 江苏康缘药业股份有限公司 二对甲苯磺酸缘生替尼原料药中残留溶剂的检测方法
CN105424831B (zh) * 2015-11-11 2017-11-10 江苏康缘药业股份有限公司 二对甲苯磺酸缘生替尼原料药中有效成分的定量检测方法
CN105606717B (zh) * 2015-11-11 2017-10-24 江苏康缘药业股份有限公司 二对甲苯磺酸缘生替尼原料药中有关物质的检测方法
CN105237573B (zh) * 2015-11-11 2017-10-24 江苏康缘药业股份有限公司 二对甲苯磺酸缘生替尼的制备方法
CN108285421A (zh) * 2018-01-26 2018-07-17 黑龙江鑫创生物科技开发有限公司 一种微通道反应器合成拉帕替尼中间体的方法
CN119390683A (zh) 2019-08-15 2025-02-07 黑钻治疗公司 炔基喹唑啉化合物
CN113995728B (zh) * 2020-07-28 2023-03-14 江苏康缘药业股份有限公司 一种药物组合物及制备方法

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EP0912559B1 (en) 1996-07-13 2002-11-06 Glaxo Group Limited Fused heterocyclic compounds as protein tyrosine kinase inhibitors
TR200102505T2 (tr) 1999-02-27 2003-01-21 Boehringer Ingelheim Pharma Kg 4-amino-kinazolin ve kinolin türevleri.
DE19911509A1 (de) 1999-03-15 2000-09-21 Boehringer Ingelheim Pharma Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
JP2003504363A (ja) 1999-07-09 2003-02-04 グラクソ グループ リミテッド プロテインチロシンキナーゼ阻害剤としてのアニリノキナゾリン類
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EA008775B1 (ru) * 2002-04-26 2007-08-31 Джилид Сайэнс, Инк. Ингибиторы протеазы вич для лечения инфекции вич и фармацевтическая композиция
WO2004046101A2 (en) 2002-11-20 2004-06-03 Array Biopharma, Inc. Cyanoguanidines and cyanoamidines as erbb2 and egfr inhibitors
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 (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
DE10349113A1 (de) 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
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WO2005105094A2 (en) 2004-04-16 2005-11-10 Smithkline Beecham Corporation Cancer treatment method
CN101421269A (zh) 2006-01-13 2009-04-29 环状药物公司 酪氨酸激酶抑制剂及其用途
JP5241513B2 (ja) 2006-01-26 2013-07-17 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 アミノクロトニルアミノ置換キナゾリン誘導体の合成方法
US20080234267A1 (en) * 2007-03-20 2008-09-25 Karen Elizabeth Lackey Compounds and Methods of Treatment
BRPI1015363A2 (pt) 2009-07-02 2015-08-25 Newgen Therapeutics Inc Compostos de quinazolina contendo fósforo, uso dos mesmos, composição e kit

Also Published As

Publication number Publication date
US8987284B2 (en) 2015-03-24
RU2012103492A (ru) 2013-08-10
CA2804190A1 (en) 2011-01-06
HK1176519A1 (zh) 2013-08-02
CN102711472A (zh) 2012-10-03
US20120196833A1 (en) 2012-08-02
WO2011002523A1 (en) 2011-01-06
EP2448409A4 (en) 2013-04-10
CN102711472B (zh) 2015-12-02
MX2012000166A (es) 2012-04-02
BRPI1015363A2 (pt) 2015-08-25
JP2012532100A (ja) 2012-12-13
JP5721709B2 (ja) 2015-05-20
IL217222A0 (en) 2012-02-29
AU2010266725A1 (en) 2012-02-23
SG177451A1 (en) 2012-02-28
EP2448409A1 (en) 2012-05-09

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