ES2639407T3 - Derivados de cianoquinolina - Google Patents
Derivados de cianoquinolina Download PDFInfo
- 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
- Authority
- 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.)
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- WDXARTMCIRVMAE-UHFFFAOYSA-N quinoline-2-carbonitrile Chemical class C1=CC=CC2=NC(C#N)=CC=C21 WDXARTMCIRVMAE-UHFFFAOYSA-N 0.000 title 1
- 125000001769 aryl amino group Chemical group 0.000 abstract 2
- 125000003118 aryl group Chemical group 0.000 abstract 2
- 125000004104 aryloxy group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 abstract 1
- 125000006799 (C2-C6) alkenylamino group Chemical group 0.000 abstract 1
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000004657 aryl sulfonyl amino group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
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
Landscapes
- 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)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
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.
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 (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5730389B2 (ja) * | 2010-06-09 | 2015-06-10 | 天津和美生物技術有限公司 | シアノキノリン誘導体 |
| CN104203242B (zh) * | 2012-04-04 | 2017-03-15 | 杭州德润玉成生物科技有限公司 | 取代的喹啉类作为布鲁顿酪氨酸激酶抑制剂 |
| AU2014361633B2 (en) * | 2013-12-12 | 2017-07-20 | Tianjin Hemay Oncology Pharmaceutical Co., Ltd | Quinazoline derivative |
| 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 |
| CN109879859B (zh) * | 2015-07-06 | 2022-01-25 | 吉利德科学公司 | Cot调节剂及其使用方法 |
| 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 |
| EP4126231A1 (en) | 2020-03-30 | 2023-02-08 | 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 |
| CN115397824B (zh) | 2020-04-02 | 2024-10-22 | 吉利德科学公司 | 用于制备cot抑制剂化合物的方法 |
| EP4410790A4 (en) * | 2021-09-29 | 2025-12-17 | Haihe Biopharma Co Ltd | SOS1 inhibitors with a hexagonal pyridor ring structure |
| WO2024220236A2 (en) * | 2023-04-21 | 2024-10-24 | University Of Georgia Research Foundation, Inc. | Hydroxylamine-based bcr-abl1 inhibitors for treatment of cancer |
| WO2025151487A2 (en) * | 2024-01-08 | 2025-07-17 | Regents Of The University Of Michigan | Small-molecule inhibitors of adar1 |
Family Cites Families (15)
| 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 |
| JP4548642B2 (ja) * | 1998-09-29 | 2010-09-22 | アメリカン・サイアナミド・カンパニー | プロテインチロシンキナーゼインヒビターとしての置換３−シアノキノリン |
| AU3281600A (en) * | 1999-02-27 | 2000-09-21 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 4-amino-quinazoline and quinoline derivatives having an inhibitory effect on signal transsduction mediated by tyrosine kinases |
| 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 |
| JP4326328B2 (ja) * | 2001-07-16 | 2009-09-02 | アストラゼネカ アクチボラグ | キノリン誘導体及びそれらのチロシンキナーゼ阻害薬としての使用 |
| ATE370123T1 (de) * | 2001-11-27 | 2007-09-15 | Wyeth Corp | 3-cyanochinoline als inhibitoren von egf-r- und her2-kinasen |
| 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 |
| US8198301B2 (en) * | 2006-07-05 | 2012-06-12 | Hesheng Zhang | Quinazoline and quinoline derivatives as irreversibe protein tyrosine kinase inhibitors |
| 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 |
| 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 |
| JP5730389B2 (ja) * | 2010-06-09 | 2015-06-10 | 天津和美生物技術有限公司 | シアノキノリン誘導体 |
-
2011
- 2011-06-08 JP JP2013513536A patent/JP5730389B2/ja active Active
- 2011-06-08 KR KR1020127034332A patent/KR101562347B1/ko active Active
- 2011-06-08 WO PCT/CN2011/075464 patent/WO2011153942A1/zh not_active Ceased
- 2011-06-08 EP EP11791932.4A patent/EP2581372B1/en active Active
- 2011-06-08 CA CA2802130A patent/CA2802130C/en active Active
- 2011-06-08 BR BR112012031340-1A patent/BR112012031340B1/pt active IP Right Grant
- 2011-06-08 US US13/702,987 patent/US9187458B2/en active Active
- 2011-06-08 ES ES11791932T patent/ES2639407T3/es active Active
- 2011-06-08 EP EP17167832.9A patent/EP3222620B1/en active Active
- 2011-06-08 CN CN201180028282.0A patent/CN102933578B/zh active Active
- 2011-06-08 AU AU2011264209A patent/AU2011264209B2/en active Active
- 2011-06-08 ES ES17167832T patent/ES2773693T3/es active Active
- 2011-06-08 RU RU2012156251/04A patent/RU2600928C2/ru active
-
2015
- 2015-10-12 US US14/881,085 patent/US9676724B2/en active Active
-
2017
- 2017-04-13 US US15/487,220 patent/US10246443B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| BR112012031340A2 (pt) | 2016-11-01 |
| BR112012031340B1 (pt) | 2021-09-14 |
| AU2011264209B2 (en) | 2014-08-07 |
| RU2600928C2 (ru) | 2016-10-27 |
| EP2581372A4 (en) | 2013-12-04 |
| AU2011264209A1 (en) | 2013-02-14 |
| KR101562347B1 (ko) | 2015-10-22 |
| CN102933578A (zh) | 2013-02-13 |
| KR20130032335A (ko) | 2013-04-01 |
| US20160185728A1 (en) | 2016-06-30 |
| US9187458B2 (en) | 2015-11-17 |
| US20170226093A1 (en) | 2017-08-10 |
| EP2581372B1 (en) | 2017-06-07 |
| EP3222620A1 (en) | 2017-09-27 |
| EP2581372A1 (en) | 2013-04-17 |
| JP5730389B2 (ja) | 2015-06-10 |
| US9676724B2 (en) | 2017-06-13 |
| US10246443B2 (en) | 2019-04-02 |
| JP2013528189A (ja) | 2013-07-08 |
| CN102933578B (zh) | 2016-09-07 |
| WO2011153942A1 (zh) | 2011-12-15 |
| CA2802130C (en) | 2014-09-09 |
| RU2012156251A (ru) | 2014-07-20 |
| CA2802130A1 (en) | 2011-12-15 |
| US20130225579A1 (en) | 2013-08-29 |
| EP3222620B1 (en) | 2019-11-20 |
| ES2773693T3 (es) | 2020-07-14 |
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