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BRPI0407249A - Preparação de quinazolinas substituìdas - Google Patents

Preparação de quinazolinas substituìdas

Info

Publication number
BRPI0407249A
BRPI0407249A BR0407249-9A BRPI0407249A BRPI0407249A BR PI0407249 A BRPI0407249 A BR PI0407249A BR PI0407249 A BRPI0407249 A BR PI0407249A BR PI0407249 A BRPI0407249 A BR PI0407249A
Authority
BR
Brazil
Prior art keywords
preparation
inhibitors
substituted quinazolines
diacryloylamino
quinazolins
Prior art date
Application number
BR0407249-9A
Other languages
English (en)
Inventor
Hubert Gangolf Klemens Barth
Alexander James Bridges
Ronald Joseph Heemstra
Nicole Marcia Horne
Robert Craig Hughes
Thomas Elliott Jacks
Dennis Joseph Mcnamara
Simon Schneider
Klaus Irenous Steiner
Peter Laurence Toogood
Roy Thomas Winters
Original Assignee
Warner Lambert Co
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
Application filed by Warner Lambert Co filed Critical Warner Lambert Co
Publication of BRPI0407249A publication Critical patent/BRPI0407249A/pt

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
    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dermatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

"PREPARAçãO DE QUINAZOLINAS SUBSTITUìDAS". A presente invenção refere-se a métodos e materiais para preparar inibidores irreversíveis de tirosina-cinases de Fórmula geral (1). Estes inibidores, os quais incluem N-¢4-(3-cloro-4-flúor-fenilamino)-7-(3-morfolin-4-il-propóxi)-quinazolin- 6-il!-acrilamida, são úteis para tratar o câncer, restenose, aterosclerose, endometriose e psoríase. Os métodos descritos utilizam esquemas de proteção para minimizar produtos secundários indesejáveis de diacriloilamino-quinazolina.
BR0407249-9A 2003-02-05 2004-02-03 Preparação de quinazolinas substituìdas BRPI0407249A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US44509503P 2003-02-05 2003-02-05
PCT/IB2004/000321 WO2004069791A2 (en) 2003-02-05 2004-02-03 Preparation of substituted quinazolines

Publications (1)

Publication Number Publication Date
BRPI0407249A true BRPI0407249A (pt) 2006-01-31

Family

ID=32850969

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0407249-9A BRPI0407249A (pt) 2003-02-05 2004-02-03 Preparação de quinazolinas substituìdas

Country Status (18)

Country Link
US (1) US20040158065A1 (pt)
EP (1) EP1618095A2 (pt)
JP (1) JP2006517959A (pt)
KR (1) KR20050095916A (pt)
CN (1) CN1745073A (pt)
AR (1) AR043027A1 (pt)
AU (1) AU2004209452A1 (pt)
BR (1) BRPI0407249A (pt)
CA (1) CA2514933A1 (pt)
MX (1) MXPA05007831A (pt)
NL (3) NL1025414C2 (pt)
PA (1) PA8595201A1 (pt)
PE (1) PE20040945A1 (pt)
PL (1) PL378576A1 (pt)
RU (1) RU2005122322A (pt)
TW (1) TW200420544A (pt)
UY (1) UY28177A1 (pt)
WO (1) WO2004069791A2 (pt)

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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
US7501427B2 (en) 2003-08-14 2009-03-10 Array Biopharma, Inc. Quinazoline analogs as receptor tyrosine kinase inhibitors
JP4828421B2 (ja) * 2003-08-14 2011-11-30 アレイ バイオファーマ、インコーポレイテッド 受容体チロシンキナーゼ阻害剤としてのキナゾリン誘導体
DE10349113A1 (de) * 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
SI1746999T1 (sl) * 2004-05-06 2012-01-31 Warner Lambert Co 4-fenilamino-kinazolin-6-il-amidi
KR100735639B1 (ko) * 2004-12-29 2007-07-04 한미약품 주식회사 암세포 성장 억제 효과를 갖는 퀴나졸린 유도체 및 이의제조방법
KR100832594B1 (ko) * 2005-11-08 2008-05-27 한미약품 주식회사 다중저해제로서의 퀴나졸린 유도체 및 이의 제조방법
CA2833852C (en) 2005-11-11 2014-10-21 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
DK1971601T3 (da) 2005-11-15 2010-02-08 Array Biopharma Inc N4-phenyl-quinazolin-4-aminderivater og beslægtede forbindelser som ERBB Type 1-receptortyrosinkinase-inhibitorer til behandling af hyperproliferative sygdomme
US8877764B2 (en) * 2006-09-18 2014-11-04 Boehringer Ingelheim International Gmbh Method for treating cancer harboring EGFR mutations
EP2190287B1 (en) 2007-09-10 2014-10-29 Curis, Inc. Tartrate salts or complexes of quinazoline based egfr inhibitors containing a zinc binding moiety
WO2009094210A1 (en) * 2008-01-22 2009-07-30 Concert Pharmaceuticals Inc. Vandetanib derivatives
JP2011510079A (ja) * 2008-01-22 2011-03-31 コンサート ファーマシューティカルズ インコーポレイテッド ゲフィチニブ誘導体
CN102405284B (zh) * 2008-09-05 2016-01-20 新基阿维罗米克斯研究公司 设计不可逆抑制剂的算法
EP2451445B1 (en) 2009-07-06 2019-04-03 Boehringer Ingelheim International GmbH Process for drying of bibw2992, of its salts and of solid pharmaceutical formulations comprising this active ingredient
EP2478361A4 (en) 2009-09-16 2014-05-21 Celgene Avilomics Res Inc CONJUGATES AND INHIBITORS OF PROTEIN KINASE
CN102812167A (zh) 2009-12-30 2012-12-05 阿维拉制药公司 蛋白的配体-介导的共价修饰
CN102382106A (zh) 2010-08-30 2012-03-21 黄振华 苯胺取代的喹唑啉衍生物
CN102898386B (zh) * 2011-07-27 2015-07-29 上海医药集团股份有限公司 喹唑啉衍生物、其制备方法、中间体、组合物及其应用
JP2014532063A (ja) * 2011-10-12 2014-12-04 テリジェン リミテッドＴｅｌｉｇｅｎｅ Ｌｔｄ キナーゼ阻害剤としてのキナゾリン誘導体およびその使用方法
WO2013166952A1 (en) 2012-05-07 2013-11-14 Teligene Ltd Substituted aminoquinazolines useful as kinases inhibitors
CN103965120B (zh) * 2013-01-25 2016-08-17 上海医药集团股份有限公司 喹啉及喹唑啉衍生物、制备方法、中间体、组合物及应用
CN103242244B (zh) * 2013-05-16 2015-03-25 苏州明锐医药科技有限公司 一种卡奈替尼的制备方法
JP6139782B2 (ja) 2013-05-21 2017-05-31 チャンスー メドリューション リミテッド 置換ピラゾロピリミジン化合物、及びその薬学的に許容される塩、並びにこれらの溶媒和物、立体異性体、及び互変異性体、並びにこれらを含む医薬組成物
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
US10870627B2 (en) 2016-09-23 2020-12-22 Shanghai Pharmaceuticals Holding Co., Ltd. Salt of quinazoline derivative, preparation method therefor and application thereof
CN112074505B (zh) 2018-03-08 2024-04-05 因赛特公司 作为PI3K-γ抑制剂的氨基吡嗪二醇化合物
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
KR20210137422A (ko) 2018-09-25 2021-11-17 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 티로신 키나아제 억제제로서의 퀴나졸린 유도체, 조성물, 이들의 제조 방법 및 이들의 용도
JP7576038B2 (ja) * 2019-03-07 2024-10-30 バイオエヌテック エスエー 置換イミダゾキノリンの調製方法
CN119390683A (zh) 2019-08-15 2025-02-07 黑钻治疗公司 炔基喹唑啉化合物
US20240246940A1 (en) * 2021-04-22 2024-07-25 Voronoi Inc. Heteroaryl derivative compound and use thereof
WO2023044364A1 (en) 2021-09-15 2023-03-23 Enko Chem, Inc. Protoporphyrinogen oxidase inhibitors

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2174250T5 (es) * 1996-04-12 2010-04-21 Warner-Lambert Company Llc Inhibidores irreversibles de tirosina quinasas.
US6664390B2 (en) * 2000-02-02 2003-12-16 Warner-Lambert Company Llc Method for the simplified production of (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazoline-4-yl]-amine or (3-chloro-4-fluorophenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazoline-4-yl]-amine
DE10009267A1 (de) * 2000-02-26 2001-08-30 Goedecke Ag Verfahren zur einfachen Herstellung von (3-Chlor-4-fluor-phenyl)-[7-(3-morpholin-4-yl-propoxy)-6-nitro-quinazolin-4-yl]-amin bzw. (3-Chlor-4-fluor-phenyl)-[7-(3-morpholin-4-yl-propoxy)-6-amino-quinazolin-4-yl]-amin
US6627634B2 (en) * 2000-04-08 2003-09-30 Boehringer Ingelheim Pharma Kg Bicyclic heterocycles, pharmaceutical compositions containing them, their use, and processes for preparing them
DE10063435A1 (de) * 2000-12-20 2002-07-04 Boehringer Ingelheim Pharma Chinazolinderviate,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung

Also Published As

Publication number Publication date
CN1745073A (zh) 2006-03-08
KR20050095916A (ko) 2005-10-04
US20040158065A1 (en) 2004-08-12
PE20040945A1 (es) 2004-12-14
NL1025414C2 (nl) 2005-11-01
TW200420544A (en) 2004-10-16
WO2004069791A2 (en) 2004-08-19
NL1029763A1 (nl) 2005-10-13
NL1029762A1 (nl) 2005-10-13
JP2006517959A (ja) 2006-08-03
EP1618095A2 (en) 2006-01-25
NL1029763C2 (nl) 2006-03-06
MXPA05007831A (es) 2005-10-18
PA8595201A1 (es) 2004-09-16
CA2514933A1 (en) 2004-08-19
AU2004209452A1 (en) 2004-08-19
UY28177A1 (es) 2004-09-30
PL378576A1 (pl) 2006-05-02
AR043027A1 (es) 2005-07-13
WO2004069791A3 (en) 2004-12-16
RU2005122322A (ru) 2006-03-10
NL1025414A1 (nl) 2004-08-06
NL1029762C2 (nl) 2006-03-06

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Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 6A, 7A E 8A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2159 DE 22/05/2012.