BRPI0606905A2 - derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica contendo-os - Google Patents

derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica contendo-os

Info

Publication number
BRPI0606905A2
BRPI0606905A2 BRPI0606905-3A BRPI0606905A BRPI0606905A2 BR PI0606905 A2 BRPI0606905 A2 BR PI0606905A2 BR PI0606905 A BRPI0606905 A BR PI0606905A BR PI0606905 A2 BRPI0606905 A2 BR PI0606905A2
Authority
BR
Brazil
Prior art keywords
optionally substituted
hydrogen atom
substituted alkyl
tyrosine kinase
pharmaceutical composition
Prior art date
Application number
BRPI0606905-3A
Other languages
English (en)
Inventor
Masaharu Kume
Kenji Matsuo
Naoki Omori
Masami Takayama
Aiko Omori
Takeshi Endo
Original Assignee
Shionogi & 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 Shionogi & Co filed Critical Shionogi & Co
Publication of BRPI0606905A2 publication Critical patent/BRPI0606905A2/pt
Publication of BRPI0606905B1 publication Critical patent/BRPI0606905B1/pt

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D407/00Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

DERIVADOS DE QUINAZOLINA TENDO ATIVIDADE INIBITóRIA DE TIROSINA CINASE E COMPOSIçãO FARMACêUTICA CONTENDO-OS. A presente invenção refere-se a um composto que inibe tanto a tirosina cinase do receptor EGF quanto a tirosina cinase HER2. Composto representado pela fórmula geral (I): em que R^ x^ é um grupo representado pela fórmula: em que R^ 1^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; Z é -O-, -N(R^ 10^)-, etc.; R^ 10^ é um átomo de hidrogênio, alquila, etc.; R^ 2^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; R^ 18^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; R^ 19^ é alquila opcionalmente substituida, etc.; W^ 1^ e um grupo contendo nitrogênio não aromático opcionaímente substituído; R^ 17^ é um átomo de hidrogênio, alquila opcionalmente substituida, etc.; R^ 3^ e R^ 4^ são independentemente um átomo de hidrogênio, alquila opcionalmente substituida, etc.; X é -O-, -S-, ou -N(R^ 12^)-, etc.; R^ 2^ é um átomo de hidrogênio, alquila, etc.; e A é fenila opcionalmente tendo um substituinte, etc., seu saí farmaceuticamente aceitável, ou um solvato do mesmo.
BRPI0606905-3A 2005-02-23 2006-02-22 Derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica que os compreende BRPI0606905B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
JP2005-047383 2005-02-23
JP2005047383 2005-02-23
JP2005-156828 2005-05-30
JP2005156828 2005-05-30
PCT/JP2006/303125 WO2006090717A1 (ja) 2005-02-23 2006-02-22 チロシンキナーゼ阻害作用を有するキナゾリン誘導体

Publications (2)

Publication Number Publication Date
BRPI0606905A2 true BRPI0606905A2 (pt) 2009-07-28
BRPI0606905B1 BRPI0606905B1 (pt) 2021-06-01

Family

ID=36927355

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0606905-3A BRPI0606905B1 (pt) 2005-02-23 2006-02-22 Derivados de quinazolina tendo atividade inibitória de tirosina cinase e composição farmacêutica que os compreende

Country Status (16)

Country Link
US (2) US8202879B2 (pt)
EP (1) EP1854789B1 (pt)
JP (1) JP4137174B2 (pt)
KR (1) KR100910333B1 (pt)
CN (1) CN101163684B (pt)
AU (1) AU2006216266C1 (pt)
BR (1) BRPI0606905B1 (pt)
CA (1) CA2599328C (pt)
DK (1) DK1854789T3 (pt)
ES (1) ES2431843T3 (pt)
NO (1) NO343403B1 (pt)
PL (1) PL1854789T3 (pt)
PT (1) PT1854789E (pt)
RU (1) RU2414457C2 (pt)
TW (1) TWI372147B (pt)
WO (1) WO2006090717A1 (pt)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1854789T3 (da) * 2005-02-23 2013-10-21 Shionogi & Co Quinazolinderivat med tyrosin-kinase inhibitorisk aktivitet
CN101003514A (zh) * 2006-01-20 2007-07-25 上海艾力斯医药科技有限公司 喹唑啉衍生物、其制备方法及用途
US7547781B2 (en) * 2006-09-11 2009-06-16 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
AU2007296746B2 (en) * 2006-09-11 2012-07-05 Curis, Inc. Quinazoline based EGFR inhibitors containing a zinc binding moiety
EP3269395A1 (en) 2008-11-07 2018-01-17 Massachusetts Institute Of Technology Aminoalcohol lipidoids and uses thereof
TWI466872B (zh) * 2008-12-25 2015-01-01 Shionogi & Co 喹唑啉衍生物之製造方法
EP2691443B1 (en) 2011-03-28 2021-02-17 Massachusetts Institute of Technology Conjugated lipomers and uses thereof
PE20181541A1 (es) * 2011-10-27 2018-09-26 Massachusetts Inst Technology Derivados de aminoacidos funcionalizados en la terminal n capaces de formar microesferas encapsuladoras de farmaco
CN103288756B (zh) * 2012-02-29 2016-04-20 江苏先声药物研究有限公司 一种喹唑啉中间体的甲醇溶剂合物及其制备方法
EA201591746A1 (ru) 2013-03-14 2016-08-31 КОНВЕРДЖЕН ЭлЭлСи Способы и композиции для ингибирования бромодомен-содержащих белков
WO2015182682A1 (ja) * 2014-05-29 2015-12-03 塩野義製薬株式会社 アルキニルケトン誘導体の製造方法
ES2908349T3 (es) * 2015-07-29 2022-04-28 Shionogi & Co Sal de derivado de quinazolina o cristal de la misma, y método para producir sal de derivado de quinazolina o cristal de la misma
JP6740354B2 (ja) 2015-10-05 2020-08-12 ザ トラスティーズ オブ コロンビア ユニバーシティー イン ザ シティー オブ ニューヨーク オートファジーの流れ及びホスホリパーゼd及びタウを含むタンパク質凝集体のクリアランスの活性化剤ならびにタンパク質症の治療方法
JP6882289B2 (ja) 2015-11-25 2021-06-02 コンバージーン・リミテッド・ライアビリティ・カンパニーConvergene Llc 二環式betブロモドメイン阻害剤及びその使用
US20180030403A1 (en) 2016-07-28 2018-02-01 Bobban Subhadra Devices, systems and methods for the production of humanized gut commensal microbiota
WO2018139626A1 (ja) 2017-01-30 2018-08-02 塩野義製薬株式会社 キナゾリン誘導体を含有する固形製剤
WO2020219168A1 (en) 2019-04-24 2020-10-29 Convergene, Llc Small molecule bromodomain inhibitors and uses thereof

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SG64322A1 (en) 1991-05-10 1999-04-27 Rhone Poulenc Rorer Int Bis mono and bicyclic aryl and heteroaryl compounds which inhibit egf and/or pdgf receptor tyrosine kinase
NZ243082A (en) 1991-06-28 1995-02-24 Ici Plc 4-anilino-quinazoline derivatives; pharmaceutical compositions, preparatory processes, and use thereof
GB9300059D0 (en) 1992-01-20 1993-03-03 Zeneca Ltd Quinazoline derivatives
GB9323290D0 (en) 1992-12-10 1994-01-05 Zeneca Ltd Quinazoline derivatives
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GB9603095D0 (en) * 1996-02-14 1996-04-10 Zeneca Ltd Quinazoline derivatives
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Also Published As

Publication number Publication date
US8202879B2 (en) 2012-06-19
US8349857B2 (en) 2013-01-08
AU2006216266B2 (en) 2010-02-18
CA2599328C (en) 2012-04-17
US20090143414A1 (en) 2009-06-04
KR100910333B1 (ko) 2009-07-31
EP1854789A1 (en) 2007-11-14
PT1854789E (pt) 2013-10-23
TW200640880A (en) 2006-12-01
AU2006216266C1 (en) 2010-08-26
AU2006216266A2 (en) 2006-08-31
CA2599328A1 (en) 2006-08-31
WO2006090717A1 (ja) 2006-08-31
NO20074311L (no) 2007-11-23
CN101163684B (zh) 2012-08-29
RU2007135023A (ru) 2009-03-27
EP1854789A4 (en) 2009-06-17
JP4137174B2 (ja) 2008-08-20
KR20070098941A (ko) 2007-10-05
RU2414457C2 (ru) 2011-03-20
AU2006216266A8 (en) 2009-04-02
AU2006216266A1 (en) 2006-08-31
CN101163684A (zh) 2008-04-16
NO343403B1 (no) 2019-02-25
US20120123114A1 (en) 2012-05-17
JPWO2006090717A1 (ja) 2008-07-24
BRPI0606905B1 (pt) 2021-06-01
TWI372147B (en) 2012-09-11
ES2431843T3 (es) 2013-11-28
EP1854789B1 (en) 2013-10-09
PL1854789T3 (pl) 2014-03-31
DK1854789T3 (da) 2013-10-21

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B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B06T Formal requirements before examination [chapter 6.20 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 22/02/2006, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF