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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UA71976C2 (en) * 1999-06-21 2005-01-17 Boehringer Ingelheim Pharma Bicyclic heterocycles and a medicament based thereon
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
WO2005016346A1 (en) * 2003-08-14 2005-02-24 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
GEP20084551B (en) * 2004-05-06 2008-11-25 Warner Lambert Co 4-phenylamino-quinazolin-6-yl-amides
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
US8404697B2 (en) 2005-11-11 2013-03-26 Boehringer Ingelheim International Gmbh Quinazoline derivatives for the treatment of cancer diseases
EP1971601B1 (en) 2005-11-15 2009-10-21 Array Biopharma Inc. N4-phenyl-quinazoline-4 -amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases
CA2663599A1 (en) * 2006-09-18 2008-03-27 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
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
US8609673B2 (en) * 2008-01-22 2013-12-17 Concert Pharmaceuticals, Inc. Vandetanib derivatives
CN105574346A (zh) * 2008-09-05 2016-05-11 新基阿维罗米克斯研究公司 多肽偶联物与不可逆抑制剂的设计方法和检测方法
DK2451445T3 (da) 2009-07-06 2019-06-24 Boehringer Ingelheim Int Fremgangsmåde til at tørre bibw2992, dets salte og faste farmaceutiske formuleringer omfattende denne aktive ingrediens
IN2012DN02534A (es) 2009-09-16 2015-08-28 Avila Therapeutics Inc
BR112012015721A2 (pt) 2009-12-30 2017-09-26 Avila Therapeutics Inc modificação covalente de proteínas dirigida por ligante
CN102382106A (zh) * 2010-08-30 2012-03-21 黄振华 苯胺取代的喹唑啉衍生物
WO2013013640A1 (zh) * 2011-07-27 2013-01-31 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
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
US9388170B2 (en) 2012-05-07 2016-07-12 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
CN107868059B (zh) * 2016-09-23 2022-07-19 上海医药集团股份有限公司 一种喹唑啉衍生物的盐、其制备方法及应用
HRP20220331T1 (hr) 2018-03-08 2022-05-13 Incyte Corporation Spojevi aminopirazin diola kao inhibitori pi3k-y
US11046658B2 (en) 2018-07-02 2021-06-29 Incyte Corporation Aminopyrazine derivatives as PI3K-γ inhibitors
MX2021003517A (es) 2018-09-25 2021-08-16 Black Diamond Therapeutics Inc Composiciones de inhibidor de tirosina quinasa, metodos de fabricacion y metodos de uso.
AU2020231822A1 (en) * 2019-03-07 2021-08-26 BioNTech SE Process for the preparation of a substituted imidazoquinoline
CN117693505A (zh) * 2021-04-22 2024-03-12 沃若诺伊公司 杂芳基衍生物化合物及其用途
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
Publication number Priority date Publication date Assignee Title
NZ332119A (en) * 1996-04-12 2001-08-31 Warner Lambert Co Quinazoline compounds which are irreversible inhibitors of tyrosine kinases
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
NL1029763A1 (nl) 2005-10-13
NL1029762A1 (nl) 2005-10-13
NL1029762C2 (nl) 2006-03-06
PA8595201A1 (es) 2004-09-16
AU2004209452A1 (en) 2004-08-19
NL1025414C2 (nl) 2005-11-01
UY28177A1 (es) 2004-09-30
PL378576A1 (pl) 2006-05-02
MXPA05007831A (es) 2005-10-18
CA2514933A1 (en) 2004-08-19
NL1025414A1 (nl) 2004-08-06
US20040158065A1 (en) 2004-08-12
CN1745073A (zh) 2006-03-08
KR20050095916A (ko) 2005-10-04
AR043027A1 (es) 2005-07-13
EP1618095A2 (en) 2006-01-25
WO2004069791A2 (en) 2004-08-19
NL1029763C2 (nl) 2006-03-06
BRPI0407249A (pt) 2006-01-31
WO2004069791A3 (en) 2004-12-16
TW200420544A (en) 2004-10-16
JP2006517959A (ja) 2006-08-03
RU2005122322A (ru) 2006-03-10

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