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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (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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HK1044769B (zh) * 1999-06-21 2005-02-25 贝林格尔英格海姆法玛两合公司 雙環雜環化合物，含有該化合物的藥物組合物，該化合物的用途及其製備方法
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
DK1660090T3 (da) * 2003-08-14 2012-12-17 Array Biopharma Inc Quinazolin-analoger som receptor-tyrosinkinase-inhibitorer
DE10349113A1 (de) * 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
KR20080095915A (ko) * 2004-05-06 2008-10-29 워너-램버트 캄파니 엘엘씨 4-페닐아미노-퀴나졸린-6-일-아미드
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
JP5688877B2 (ja) 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 癌疾患の治療用キナゾリン誘導体
ATE446294T1 (de) 2005-11-15 2009-11-15 Array Biopharma Inc N4-phenyl-chinazolin-4-aminderivate und verwandte verbindungen als inhibitoren der erbb-typ-i- rezeptortyrosinkinase zur behandlung hyperproliferativer krankheiten
AU2007299080B2 (en) * 2006-09-18 2013-04-18 Boehringer Ingelheim International Gmbh Method for treating cancer harboring EGFR mutations
WO2009035718A1 (en) * 2007-09-10 2009-03-19 Curis, Inc. Tartrate salts or complexes of quinazoline based egfr inhibitors containing a zinc binding moiety
WO2009094216A1 (en) * 2008-01-22 2009-07-30 Concert Pharmaceuticals Inc. Derivatives of gefitinib
WO2009094210A1 (en) * 2008-01-22 2009-07-30 Concert Pharmaceuticals Inc. Vandetanib derivatives
JP2012501654A (ja) * 2008-09-05 2012-01-26 アビラ セラピューティクス， インコーポレイテッド 不可逆的インヒビターの設計のためのアルゴリズム
PT2451445T (pt) 2009-07-06 2019-07-10 Boehringer Ingelheim Int Processo para secagem de bibw2992, dos seus sais e de formulações farmacêuticas sólidas compreendendo este ingrediente ativo
US9556426B2 (en) 2009-09-16 2017-01-31 Celgene Avilomics Research, Inc. Protein kinase conjugates and inhibitors
JP2013516422A (ja) 2009-12-30 2013-05-13 アビラ セラピューティクス， インコーポレイテッド タンパク質のリガンド−指向性共有的修飾
CN102382106A (zh) 2010-08-30 2012-03-21 黄振华 苯胺取代的喹唑啉衍生物
JP6437820B2 (ja) * 2011-07-27 2018-12-12 シャンハイ ファーマシューティカルズ ホールディング カンパニー，リミティド キナゾリン誘導体、その製造方法、中間体、組成物及びその適用
CN103874696B (zh) 2011-10-12 2015-06-03 苏州韬略生物科技有限公司 作为激酶抑制剂的喹唑啉衍生物及其使用方法
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
WO2014187319A1 (en) 2013-05-21 2014-11-27 Jiangsu Medolution Ltd Substituted pyrazolopyrimidines as kinases inhibitors
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
EP3517529B1 (en) 2016-09-23 2022-03-23 Shanghai Pharmaceuticals Holding Co., Ltd. Salt of quinazoline derivative, preparation method therefor and application thereof
BR112020018094A2 (pt) 2018-03-08 2020-12-22 Incyte Corporation Compostos de aminopirazina diol como inibidores de pi3k-¿
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
JP2022502495A (ja) 2018-09-25 2022-01-11 ブラック ダイアモンド セラピューティクス，インコーポレイティド チロシンキナーゼ阻害剤としてのキナゾリン誘導体、組成物、それらの作製方法、およびそれらの使用
BR112021016960A2 (pt) * 2019-03-07 2021-11-23 BioNTech SE Processo para a preparação de uma imidazoquinolina substituída
AU2020328598A1 (en) 2019-08-15 2022-03-03 Black Diamond Therapeutics, Inc. Alkynyl quinazoline compounds
WO2022225238A1 (ko) * 2021-04-22 2022-10-27 보로노이 주식회사 헤테로아릴 유도체 화합물 및 이의 용도
WO2023044364A1 (en) 2021-09-15 2023-03-23 Enko Chem, Inc. Protoporphyrinogen oxidase inhibitors

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EA001595B1 (ru) * 1996-04-12 2001-06-25 Варнер-Ламберт Компани Необратимые ингибиторы тирозинкиназ
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
NL1029762C2 (nl) 2006-03-06
US20040158065A1 (en) 2004-08-12
CA2514933A1 (en) 2004-08-19
NL1029762A1 (nl) 2005-10-13
NL1025414C2 (nl) 2005-11-01
WO2004069791A2 (en) 2004-08-19
KR20050095916A (ko) 2005-10-04
NL1029763C2 (nl) 2006-03-06
CN1745073A (zh) 2006-03-08
RU2005122322A (ru) 2006-03-10
WO2004069791A3 (en) 2004-12-16
AR043027A1 (es) 2005-07-13
PL378576A1 (pl) 2006-05-02
MXPA05007831A (es) 2005-10-18
NL1025414A1 (nl) 2004-08-06
PA8595201A1 (es) 2004-09-16
NL1029763A1 (nl) 2005-10-13
EP1618095A2 (en) 2006-01-25
AU2004209452A1 (en) 2004-08-19
PE20040945A1 (es) 2004-12-14
UY28177A1 (es) 2004-09-30
JP2006517959A (ja) 2006-08-03
TW200420544A (en) 2004-10-16

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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.