ES2639407T3 - Derivados de cianoquinolina - Google Patents

Derivados de cianoquinolina Download PDF

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Publication number
ES2639407T3
ES2639407T3 ES11791932T ES11791932T ES2639407T3 ES 2639407 T3 ES2639407 T3 ES 2639407T3 ES 11791932 T ES11791932 T ES 11791932T ES 11791932 T ES11791932 T ES 11791932T ES 2639407 T3 ES2639407 T3 ES 2639407T3
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ES
Spain
Prior art keywords
substituted
unsubstituted
group
heteroaryl
heteroaralkyloxy
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES11791932T
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English (en)
Inventor
Hesheng Zhang
Yingwei Chen
Qingchao He
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Tianjin Hemay Oncology Pharmaceutical Co Ltd
Original Assignee
Tianjin Hemay Oncology Pharmaceutical Co Ltd
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Publication date
Application filed by Tianjin Hemay Oncology Pharmaceutical Co Ltd filed Critical Tianjin Hemay Oncology Pharmaceutical Co Ltd
Application granted granted Critical
Publication of ES2639407T3 publication Critical patent/ES2639407T3/es
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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/02—Heterocyclic 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
    • C07D405/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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 three or more hetero rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/12—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

Un compuesto de fórmula I, un estereoisómero del mismo, un isómero cis-trans del mismo, un tautómero del mismo, o una mezcla de los mismos, o una sal farmacéuticamente aceptable del mismo, o un solvato del mismo,**Fórmula** en la que: R1 se selecciona del grupo que consiste en alquilacilamino C1-C6, alquenilacilamino C2-C6, alquinilacilamino C2-C6, arilacilamino C6-C18 y amino sustituido con alquilo C1-C6; R2 y R3 se seleccionan cada uno independientemente del grupo que consiste en hidrógeno, aralquilo C7-C24, arilo C6-C18 sustituido o sin sustituir, heteroarilo C5-C18 sustituido o sin sustituir, en el que un sustituyente en el arilo se selecciona del grupo que consiste en alquinilo C2-C6, halógeno, aralquiloxi C7-C24, heteroaralquiloxi C6-C24, ariloxi C6-C18 y heteroariloxi C5-C18, y un sustituyente en el heteroarilo se selecciona del grupo que consiste en aralquilo C7- C24, arilacilamino C6-C18, arilsulfonilamino C6-C18, heteroarilacilamino C5-C18, cicloalquilacilamino C3-C10, arilaminoacilo C6-C18, aralquiloxi C7-C24, heteroaralquiloxi C6-C24 y ariloxi C6-C18; o R2 y R3 junto con el átomo de nitrógeno al que están unidos forman un heterociclilo C3-C18 sustituido o sin sustituir; y R4 es heterociclilo C3-C18 sustituido o sin sustituir o heteroarilo C5-C18 sustituido o sin sustituir.
ES11791932T 2010-06-09 2011-06-08 Derivados de cianoquinolina Active ES2639407T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201010199467 2010-06-09
PCT/CN2011/075464 WO2011153942A1 (zh) 2010-06-09 2011-06-08 氰基喹啉衍生物

Publications (1)

Publication Number Publication Date
ES2639407T3 true ES2639407T3 (es) 2017-10-26

Family

ID=45097544

Family Applications (2)

Application Number Title Priority Date Filing Date
ES11791932T Active ES2639407T3 (es) 2010-06-09 2011-06-08 Derivados de cianoquinolina
ES17167832T Active ES2773693T3 (es) 2010-06-09 2011-06-08 Derivados de cianoquinolina

Family Applications After (1)

Application Number Title Priority Date Filing Date
ES17167832T Active ES2773693T3 (es) 2010-06-09 2011-06-08 Derivados de cianoquinolina

Country Status (11)

Country Link
US (3) US9187458B2 (es)
EP (2) EP2581372B1 (es)
JP (1) JP5730389B2 (es)
KR (1) KR101562347B1 (es)
CN (1) CN102933578B (es)
AU (1) AU2011264209B2 (es)
BR (1) BR112012031340B1 (es)
CA (1) CA2802130C (es)
ES (2) ES2639407T3 (es)
RU (1) RU2600928C2 (es)
WO (1) WO2011153942A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2600928C2 (ru) * 2010-06-09 2016-10-27 Тяньцзинь Химэй Байо-Тек Ко., Лтд Цианохинолиновые производные
WO2013152135A1 (en) * 2012-04-04 2013-10-10 Dawei Zhang Substituted quinolines as bruton's tyrosine kinases inhibitors
CN109265441A (zh) * 2013-12-12 2019-01-25 天津和美奥康医药科技有限公司 喹唑啉衍生物
CN105461689B (zh) * 2015-05-19 2018-12-04 上海麦步医药科技有限公司 一种表皮生长因子受体(egfr)抑制剂来那替尼的新型制备方法
EP3896064A1 (en) 2015-07-06 2021-10-20 Gilead Sciences, Inc. 4,6-diamino-quinoline-3-carbonitrile derivatives as cancer osaka thyroid (cot) modulators for treating crohn's disease and ulcerative colitis
CN105175331B (zh) * 2015-08-14 2019-04-26 江苏苏中药业集团股份有限公司 一种egfr类分子靶向抗肿瘤药物的制备方法
CN105085485B (zh) * 2015-08-21 2017-08-29 哈尔滨珍宝制药有限公司 一种来那替尼的制备方法
TWI770527B (zh) 2019-06-14 2022-07-11 美商基利科學股份有限公司 Cot 調節劑及其使用方法
CA3175541A1 (en) 2020-03-30 2021-10-07 Gilead Sciences, Inc. Solid forms of (s)-6-(((1-(bicyclo[1.1.1]pentan-1-yl)-1h-1,2,3-triazol-4-yl)2-methyl-1-oxo-1,2- dihydroisoquinolin-5-yl)methyl)))amino)8-chloro-(neopentylamino)quinoline-3-carb onitrile a cot inhibitor compound
AU2021245924B2 (en) 2020-04-02 2024-02-29 Gilead Sciences, Inc. Process for preparing a Cot inhibitor compound

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA73073C2 (uk) * 1997-04-03 2005-06-15 Уайт Холдінгз Корпорейшн Заміщені 3-ціанохіноліни, спосіб їх одержання та фармацевтична композиція
ZA986729B (en) * 1997-07-29 1999-02-02 Warner Lambert Co Irreversible inhibitors of tyrosine kinases
BR9914167B1 (pt) * 1998-09-29 2011-03-09 compostos e composições farmacêuticas compreendendo 3-ciano quinolinas substituìdas.
ID29800A (id) * 1999-02-27 2001-10-11 Boehringer Ingelheim Pharma Turunan-turunan 4-amino-kinazolin dan kinolin yang mempunyai efek inhibitor pada transduksi signal yang dimediasi oleh tirosin kinase
GB9910577D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
DE10042061A1 (de) * 2000-08-26 2002-03-07 Boehringer Ingelheim Pharma Bicyclische Heterocyclen,diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung
US7501516B2 (en) * 2001-07-16 2009-03-10 Astrazeneca Ab Quinoline derivatives and their use as tyrosine kinase inhibitors
PL370137A1 (en) * 2001-11-27 2005-05-16 Wyeth Holdings Corporation 3-cyanoquinolines as inhibitors of egf-r and her2 kinases
TWI275390B (en) 2002-04-30 2007-03-11 Wyeth Corp Process for the preparation of 7-substituted-3- quinolinecarbonitriles
GB0215823D0 (en) * 2002-07-09 2002-08-14 Astrazeneca Ab Quinazoline derivatives
RU2317290C2 (ru) * 2003-07-31 2008-02-20 Санофи-Авентис Производные аминохинолина и их применение в качестве лигандов аденозина а3
CN101100466B (zh) * 2006-07-05 2013-12-25 天津和美生物技术有限公司 不可逆蛋白质酪氨酸磷酰化酶抑制剂及其制备和应用
US8198301B2 (en) * 2006-07-05 2012-06-12 Hesheng Zhang Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors
CN101824029A (zh) * 2009-03-05 2010-09-08 厦门艾德生物医药科技有限公司 酪氨酸激酶不可逆抑制剂、其药物组合物及其用途
RU2600928C2 (ru) * 2010-06-09 2016-10-27 Тяньцзинь Химэй Байо-Тек Ко., Лтд Цианохинолиновые производные

Also Published As

Publication number Publication date
RU2012156251A (ru) 2014-07-20
EP3222620A1 (en) 2017-09-27
BR112012031340B1 (pt) 2021-09-14
US20160185728A1 (en) 2016-06-30
EP3222620B1 (en) 2019-11-20
BR112012031340A2 (pt) 2016-11-01
EP2581372B1 (en) 2017-06-07
US20130225579A1 (en) 2013-08-29
CN102933578A (zh) 2013-02-13
AU2011264209A1 (en) 2013-02-14
US10246443B2 (en) 2019-04-02
EP2581372A1 (en) 2013-04-17
JP2013528189A (ja) 2013-07-08
US20170226093A1 (en) 2017-08-10
WO2011153942A1 (zh) 2011-12-15
KR20130032335A (ko) 2013-04-01
CA2802130C (en) 2014-09-09
US9187458B2 (en) 2015-11-17
ES2773693T3 (es) 2020-07-14
JP5730389B2 (ja) 2015-06-10
EP2581372A4 (en) 2013-12-04
RU2600928C2 (ru) 2016-10-27
KR101562347B1 (ko) 2015-10-22
US9676724B2 (en) 2017-06-13
CA2802130A1 (en) 2011-12-15
AU2011264209B2 (en) 2014-08-07
CN102933578B (zh) 2016-09-07

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