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)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Urology & Nephrology (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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PT1731511E (pt) * 1999-06-21 2015-11-13 Boehringer Ingelheim Pharma Heterociclos bicíclicos, medicamentos contendo estes compostos, a sua utilização e processos para a sua preparação
US7019012B2 (en) * 2000-12-20 2006-03-28 Boehringer Ingelheim International Pharma Gmbh & Co. Kg Quinazoline derivatives and pharmaceutical compositions containing them
CN102432552B (zh) * 2003-08-14 2016-01-20 阿雷生物药品公司 作为受体酪氨酸激酶抑制剂的喹唑啉类似物
US7501427B2 (en) 2003-08-14 2009-03-10 Array Biopharma, Inc. Quinazoline analogs as receptor tyrosine kinase inhibitors
DE10349113A1 (de) * 2003-10-17 2005-05-12 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Aminocrotonylverbindungen
ME01267B (me) * 2004-05-06 2013-06-20 Warner Lambert Co 4-fenilaminokinazolin-6-ilamidi
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
CA2629244C (en) 2005-11-11 2014-08-05 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
ES2364901T3 (es) * 2005-11-15 2011-09-16 Array Biopharma, Inc. Procesos e intermedios para la preparación de derivados de n4-fenil-quinazolin-4-amina.
WO2008034776A1 (en) * 2006-09-18 2008-03-27 Boehringer Ingelheim International Gmbh Method for treating cancer harboring egfr mutations
AU2008299896B2 (en) 2007-09-10 2012-02-02 Curis, Inc. Tartrate salts or complexes of quinazoline based EGFR inhibitors containing a zinc binding moiety
EP2242493B1 (en) * 2008-01-22 2013-06-05 Concert Pharmaceuticals Inc. Derivatives of gefitinib
WO2009094210A1 (en) * 2008-01-22 2009-07-30 Concert Pharmaceuticals Inc. Vandetanib derivatives
WO2010028236A1 (en) * 2008-09-05 2010-03-11 Avila Therapeutics, Inc. Algorithm for designing irreversible inhibitors
ES2731901T3 (es) 2009-07-06 2019-11-19 Boehringer Ingelheim Int Proceso para el secado de BIBW2992, de sus sales y de formulaciones farmacéuticas sólidas que comprenden este ingrediente activo
KR20120093220A (ko) 2009-09-16 2012-08-22 아빌라 테라퓨틱스, 인크. 단백질 키나아제 컨쥬게이트 및 인히비터
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
US9371292B2 (en) 2011-07-27 2016-06-21 Shanghai Pharmaceuticals Holdings Co., Ltd. Quinazoline derivative, preparation method therefor, intermediate, composition and application thereof
WO2013053206A1 (en) 2011-10-12 2013-04-18 Teligene Ltd Quinazoline derivatives as kinases inhibitors and methods of use thereof
CN104350049B (zh) 2012-05-07 2016-07-13 苏州韬略生物科技有限公司 作为激酶抑制剂的取代氨基喹唑啉
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
CN105408334B (zh) 2013-05-21 2017-10-10 江苏迈度药物研发有限公司 作为激酶抑制剂的取代的吡唑并嘧啶类化合物
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
JP7068280B2 (ja) * 2016-09-23 2022-05-16 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 キナゾリン誘導体の塩、その製造方法および使用
HUE057970T2 (hu) 2018-03-08 2022-06-28 Incyte Corp Aminopirazindiol-vegyületek mint PI3K-Y inhibitorok
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
BR112021005513A2 (pt) 2018-09-25 2021-06-22 Black Diamond Therapeutics, Inc. derivados de quinazolina como inibidor de tirosina quinase, composições, métodos de fabricação e uso dos mesmos
CN113518775A (zh) * 2019-03-07 2021-10-19 生物技术公司 用于制备经取代的咪唑并喹啉的方法
EP4328222A1 (en) * 2021-04-22 2024-02-28 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
RO121900B1 (ro) * 1996-04-12 2008-07-30 Warner-Lambert Company Compuşi inhibitori, ireversibili, ai tirozin kinazelor, compoziţie farmaceutică care îi conţine şi utilizarea acestora
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
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
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
PA8595201A1 (es) 2004-09-16
MXPA05007831A (es) 2005-10-18
UY28177A1 (es) 2004-09-30
US20040158065A1 (en) 2004-08-12
KR20050095916A (ko) 2005-10-04
NL1029762A1 (nl) 2005-10-13
AU2004209452A1 (en) 2004-08-19
EP1618095A2 (en) 2006-01-25
CN1745073A (zh) 2006-03-08
CA2514933A1 (en) 2004-08-19
PE20040945A1 (es) 2004-12-14
PL378576A1 (pl) 2006-05-02
NL1029763A1 (nl) 2005-10-13
JP2006517959A (ja) 2006-08-03
AR043027A1 (es) 2005-07-13
WO2004069791A2 (en) 2004-08-19
NL1029763C2 (nl) 2006-03-06
NL1025414C2 (nl) 2005-11-01
NL1029762C2 (nl) 2006-03-06
NL1025414A1 (nl) 2004-08-06
RU2005122322A (ru) 2006-03-10
TW200420544A (en) 2004-10-16
WO2004069791A3 (en) 2004-12-16

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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.