PE20040945A1 - Preparacion de quinazolinas substituidas - Google Patents

Preparacion de quinazolinas substituidas

Info

Publication number
PE20040945A1
PE20040945A1 PE2004000120A PE2004000120A PE20040945A1 PE 20040945 A1 PE20040945 A1 PE 20040945A1 PE 2004000120 A PE2004000120 A PE 2004000120A PE 2004000120 A PE2004000120 A PE 2004000120A PE 20040945 A1 PE20040945 A1 PE 20040945A1
Authority
PE
Peru
Prior art keywords
fluoro
phenyl
dimetoxy
chloro
benzyl
Prior art date
Application number
PE2004000120A
Other languages
English (en)
Inventor
Simon Schneider
Klaus Irenaus Steiner
Roy Thomas Winters
Thomas Elliott Jacks
Hubert Gangolf Klemens Barth
Ronald Joseph Heemstra
Nicole Marcia Horne
Bridges Alexander James
Dennis Joseph Mcnamara
Robert Craig Hughes
Peter Laurence Toogood
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 PE20040945A1 publication Critical patent/PE20040945A1/es

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

Abstract

SE REFIERE A UN PROCEDIMIENTO DE ELABORACION DE QUINAZOLINAS SUBSTITUIDAS DE FORMULA I, ENTRE OTRAS, INCLUYENDO SU SAL, ESTER, AMIDA DONDE R1, R2 Y R3 SON H, HALOGENO, NO2, CN, CF3, ENTRE OTROS; R4 Y R6 SON H, HIDROXI, HALOGENO, ALQUILO C1-C4, ENTRE OTROS; R5 ES FENILO, PIRIDILO, FURILO, TIAZOLILO, ENTRE OTROS; Z ES H, HALOGENO, C1-C6, CICLOALQUILO C3-C8, ENTRE OTROS, CON LA CONDICION QUE CUANDO Z ES MONOVALENTE, R5 ESTA AUSENTE. ESTE METODO COMPRENDE ELIMINAR EL GRUPO PROTECTOR G DE UN COMPUESTO DE FORMULA 10 PARA DAR UN COMPUESTO DE FORMULA 1. SON COMPUESTOS PREFERIDOS: (3-CLORO-4-FLUORO-FENIL)-(3,4-DIMETOXI-BENCIL)-(7-FLUORO-6-NITROQUINAZOLIN-4-IL)-AMINA; (3-CLORO-4-FLUORO-FENIL)-(3,4-DIMETOXI-BENCIL)-[7-(3-MORFOLIN-4-IL-PROPOXI)-6-NITROQUINAZOLIN-4-IL]-AMINA; N4-(3-CLORO-4-FLUORO-FENIL)-N4-(3,4-DIMETOXI-BENCIL)-7-(3-MORFOLIN-4-IL-PROPOXI)-QUINAZOLIN-4,6-DIAMINA; ENTRE OTROS. ESTOS COMPUESTOS SON INHIBIDORES IRREVERSIBLES DE TIROSINA QUINASA Y SON UTILES PARA TRATAR CANCER, RESTENOSIS, ATEROESCLEROSIS, ENDOMETRIOSIS Y PSORIASIS
PE2004000120A 2003-02-05 2004-02-02 Preparacion de quinazolinas substituidas PE20040945A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US44509503P 2003-02-05 2003-02-05

Publications (1)

Publication Number Publication Date
PE20040945A1 true PE20040945A1 (es) 2004-12-14

Family

ID=32850969

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2004000120A PE20040945A1 (es) 2003-02-05 2004-02-02 Preparacion de quinazolinas substituidas

Country Status (18)

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

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EP1731511B1 (de) 1999-06-21 2015-08-12 Boehringer Ingelheim Pharma GmbH & Co. KG Bicyclische Heterocyclen, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
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
CA2535614C (en) * 2003-08-14 2009-12-22 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
EA011237B1 (ru) 2004-05-06 2009-02-27 УОРНЕР-ЛАМБЕРТ КОМПАНИ Эл-Эл-Си 4-фениламинохиназолин-6-ил-амиды
KR100735639B1 (ko) * 2004-12-29 2007-07-04 한미약품 주식회사 암세포 성장 억제 효과를 갖는 퀴나졸린 유도체 및 이의제조방법
KR100832593B1 (ko) * 2005-11-08 2008-05-27 한미약품 주식회사 신호전달 저해제로서의 퀴나졸린 유도체 및 이의 제조방법
EP3173084B1 (en) 2005-11-11 2019-10-23 Boehringer Ingelheim International GmbH Quinazoline derivatives for the treatment of cancer diseases
CN102887891B (zh) 2005-11-15 2016-03-09 阿雷生物药品公司 N4-苯基-喹唑啉-4-胺衍生物和相关化合物
RU2492864C2 (ru) * 2006-09-18 2013-09-20 Бёрингер Ингельхайм Интернациональ Гмбх Способ лечения рака, несущего мутации egfr
AU2008299896B2 (en) * 2007-09-10 2012-02-02 Curis, Inc. Tartrate salts or complexes of quinazoline based EGFR inhibitors containing a zinc binding moiety
US8609673B2 (en) * 2008-01-22 2013-12-17 Concert Pharmaceuticals, Inc. Vandetanib derivatives
EP2242493B1 (en) * 2008-01-22 2013-06-05 Concert Pharmaceuticals Inc. Derivatives of gefitinib
KR101341876B1 (ko) * 2008-09-05 2013-12-20 셀진 아빌로믹스 리서치, 인코포레이티드 비가역 인히비터 디자인을 위한 알고리즘
US9545381B2 (en) 2009-07-06 2017-01-17 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
RU2012132473A (ru) 2009-12-30 2014-02-10 Селджин Авиломикс,Инк Лиганд-направленная ковалентная модификация белка
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
EP2847186B1 (en) 2012-05-07 2017-08-09 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
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
KR102355955B1 (ko) * 2016-09-23 2022-01-25 상하이 파마슈티컬스 홀딩 컴퍼니 리미티드 퀴나졸린 유도체의 염, 이의 제조 방법 및 응용
TWI827583B (zh) 2018-03-08 2024-01-01 美商英塞特公司 作為ＰＩ３Ｋ-γ抑制劑之胺基吡嗪二醇化合物
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
WO2020068867A1 (en) 2018-09-25 2020-04-02 Black Diamond Therapeutics, Inc. Quinazoline derivatives as tyrosine kinase inhibitor, compositions, methods of making them and their use
AU2020231822A1 (en) * 2019-03-07 2021-08-26 BioNTech SE Process for the preparation of a substituted imidazoquinoline
JP2024515204A (ja) * 2021-04-22 2024-04-05 ボロノイ インコーポレイテッド ヘテロアリール誘導体化合物およびその用途
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
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PT892789E (pt) * 1996-04-12 2002-07-31 Warner Lambert Co Inibidores irreversiveis de quinases de tirosina
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
MXPA05007831A (es) 2005-10-18
PL378576A1 (pl) 2006-05-02
WO2004069791A3 (en) 2004-12-16
JP2006517959A (ja) 2006-08-03
AU2004209452A1 (en) 2004-08-19
CN1745073A (zh) 2006-03-08
TW200420544A (en) 2004-10-16
US20040158065A1 (en) 2004-08-12
WO2004069791A2 (en) 2004-08-19
UY28177A1 (es) 2004-09-30
NL1029763A1 (nl) 2005-10-13
NL1025414A1 (nl) 2004-08-06
CA2514933A1 (en) 2004-08-19
NL1029762A1 (nl) 2005-10-13
NL1025414C2 (nl) 2005-11-01
KR20050095916A (ko) 2005-10-04
RU2005122322A (ru) 2006-03-10
BRPI0407249A (pt) 2006-01-31
EP1618095A2 (en) 2006-01-25
PA8595201A1 (es) 2004-09-16
NL1029762C2 (nl) 2006-03-06
AR043027A1 (es) 2005-07-13
NL1029763C2 (nl) 2006-03-06

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