PE20091445A1 - Derivados de indolinona y procedimiento para su fabricacion - Google Patents
Derivados de indolinona y procedimiento para su fabricacionInfo
- Publication number
- PE20091445A1 PE20091445A1 PE2008002005A PE2008002005A PE20091445A1 PE 20091445 A1 PE20091445 A1 PE 20091445A1 PE 2008002005 A PE2008002005 A PE 2008002005A PE 2008002005 A PE2008002005 A PE 2008002005A PE 20091445 A1 PE20091445 A1 PE 20091445A1
- Authority
- PE
- Peru
- Prior art keywords
- oxoindoline
- procedure
- carboxylate
- manufacture
- chloroacetyl
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical class C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 1- (CHLOROACETYL) -2-OXOINDOLINE-6-CARBOXYLATE Chemical compound 0.000 abstract 2
- QEQIWWJFXFJXED-UHFFFAOYSA-N 3-[methoxy(phenyl)methylidene]-2-oxo-1h-indole-6-carboxylic acid Chemical compound O=C1NC2=CC(C(O)=O)=CC=C2C1=C(OC)C1=CC=CC=C1 QEQIWWJFXFJXED-UHFFFAOYSA-N 0.000 abstract 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 230000000771 oncological effect Effects 0.000 abstract 1
- 230000000144 pharmacologic effect Effects 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 239000000126 substance Substances 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Indole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Epidemiology (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heat Sensitive Colour Forming Recording (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
REFERIDO A UN COMPUESTO DERIVADO DE INDOLINA DE FORMULA (I), DONDE R1 ES H O CI-CH2-CO, R2 Y R3 SON CADA UNO H O JUNTOS REPRESENTAN UN GRUPO DE FORMULA (II) CON LA CONDICION DE QUE R1 SEA H. SON COMPUESTOS PREFERIDOS: (1-(CLOROACETIL)-2-OXOINDOLINO-6-CARBOXILATO DE METILO), (1-(CLOROACETIL)-3-[METOXI(FENIL)METILEN]-2-OXOINDOLINO-6-CARBOXILATO DE METILO), (3-[METOXI(FENIL)METILEN]-2-OXOINDOLINO-6-CARBOXILATO DE METILO). SE REFIERE TAMBIEN A UN PROCEDIMIENTO PARA SU FABRICACION. DICHOS COMPUESTOS SON INTERMEDIOS UTILES PARA LA SINTESIS DE SUSTANCIAS FARMACOLOGICAS, QUE TRATAN ENFERMEDADES ONCOLOGICAS O NO ONCOLOGICAS A TRAVES DE LA INHIBICION DE LA PROLIFERACION DE LAS CELULAS DIANA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07122123 | 2007-12-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20091445A1 true PE20091445A1 (es) | 2009-10-19 |
Family
ID=40718253
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008002005A PE20091445A1 (es) | 2007-12-03 | 2008-12-01 | Derivados de indolinona y procedimiento para su fabricacion |
Country Status (35)
| Country | Link |
|---|---|
| US (1) | US8067617B2 (es) |
| EP (1) | EP2229360B1 (es) |
| JP (2) | JP5933924B2 (es) |
| KR (2) | KR101712810B1 (es) |
| CN (1) | CN101883755B (es) |
| AR (1) | AR069531A1 (es) |
| AU (1) | AU2008333287B2 (es) |
| BR (1) | BRPI0819991B1 (es) |
| CA (1) | CA2705490C (es) |
| CL (1) | CL2008003599A1 (es) |
| CO (1) | CO6210751A2 (es) |
| CY (1) | CY1123333T1 (es) |
| DK (1) | DK2229360T3 (es) |
| EA (1) | EA016196B1 (es) |
| EC (1) | ECSP10010195A (es) |
| ES (1) | ES2818993T3 (es) |
| HR (1) | HRP20201480T1 (es) |
| HU (1) | HUE051550T2 (es) |
| IL (1) | IL205348A (es) |
| LT (1) | LT2229360T (es) |
| MA (1) | MA31989B1 (es) |
| MX (1) | MX2010005557A (es) |
| MY (1) | MY148574A (es) |
| NZ (1) | NZ585798A (es) |
| PE (1) | PE20091445A1 (es) |
| PL (1) | PL2229360T3 (es) |
| PT (1) | PT2229360T (es) |
| RS (1) | RS60818B1 (es) |
| SI (1) | SI2229360T1 (es) |
| TN (1) | TN2010000248A1 (es) |
| TW (1) | TWI432415B (es) |
| UA (1) | UA97872C2 (es) |
| UY (1) | UY31506A1 (es) |
| WO (1) | WO2009071524A2 (es) |
| ZA (1) | ZA201002723B (es) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY31506A1 (es) * | 2007-12-03 | 2009-08-03 | Derivados de indolinona y procedimiento para su preparacion | |
| US20170065529A1 (en) | 2015-09-09 | 2017-03-09 | Boehringer Ingelheim International Gmbh | Pharmaceutical dosage form for immediate release of an indolinone derivative |
| WO2012068441A2 (en) | 2010-11-19 | 2012-05-24 | Ratiopharm Gmbh | Intedanib salts and solid state forms thereof |
| CN103787949A (zh) * | 2012-10-31 | 2014-05-14 | 韩冰 | 一类保护移植器官的化合物及其用途 |
| US20140350022A1 (en) | 2013-05-10 | 2014-11-27 | Boehringer Ingelheim International Gmbh | Efficacious treatment of NSCLC and predictive clinical marker of the responsiveness of a tumour to a treatment |
| EP3027026B1 (en) | 2013-07-31 | 2024-11-13 | Avalyn Pharma Inc. | Aerosol tyrosine kinase inhibitor compounds and uses thereof |
| US20140342772A1 (en) * | 2013-09-12 | 2014-11-20 | Bandwidth.Com, Inc. | Predictive Caching of IP Data |
| CN104262232B (zh) * | 2014-09-09 | 2016-05-04 | 苏州明锐医药科技有限公司 | 尼泰达尼的制备方法 |
| CN105712923A (zh) * | 2014-12-03 | 2016-06-29 | 江苏先声药业有限公司 | 一种尼达尼布杂质及其制备方法与应用 |
| WO2016178064A1 (en) | 2015-05-06 | 2016-11-10 | Suven Life Sciences Limited | Polymorph of nintedanib ethanesulphonate, processes and intermediates thereof |
| CN105001143A (zh) * | 2015-07-24 | 2015-10-28 | 南京正大天晴制药有限公司 | 一种制备高纯度乙磺酸尼达尼布的方法 |
| WO2017077551A2 (en) | 2015-11-03 | 2017-05-11 | Mylan Laboratories Limited | An amorphous nintedanib esylate and solid dispersion thereof |
| CN109415314A (zh) * | 2016-05-19 | 2019-03-01 | 上海诚妙医药科技有限公司 | 尼达尼布的新晶型及其制备方法及其用途 |
| CN106543069A (zh) * | 2016-09-20 | 2017-03-29 | 北京万全德众医药生物技术有限公司 | 6‑甲氧基羰基‑2‑氧代二氢吲哚的制备 |
| CN108610308A (zh) * | 2016-12-09 | 2018-10-02 | 上海奥博生物医药技术有限公司 | 一锅法制备尼达尼布中间体的方法 |
| CN106841495B (zh) * | 2017-04-21 | 2018-05-11 | 常州佳德医药科技有限公司 | 乙磺酸尼达尼布中基因毒性杂质的高灵敏度分析方法 |
| WO2019048974A1 (en) * | 2017-09-06 | 2019-03-14 | Glenmark Pharmaceuticals Limited | Process for the preparation of nintedanib |
| EP3710427B1 (en) | 2017-11-17 | 2023-03-08 | Fermion Oy | Synthesis of a 2-indolinone derivative known as intermediate for preparing nintedanib |
| CN110746378B (zh) * | 2018-12-03 | 2021-11-05 | 江苏豪森药业集团有限公司 | 一种胺基中间体的制备方法 |
| CN111377845A (zh) * | 2018-12-27 | 2020-07-07 | 江苏先声药业有限公司 | 3-(二甲氨基(苯基)亚甲基)-2-氧化吲哚-6-羧酸甲酯及其制备方法与应用 |
| CN111662223B (zh) * | 2019-03-08 | 2023-07-14 | 四川科伦药物研究院有限公司 | 二氢吲哚酮衍生物及其中间体的制备方法 |
| CA3191013A1 (en) * | 2020-08-07 | 2022-02-10 | Bdr Lifesciences Private Limited | An improved highly efficient process for the prepration of nintedanib and pharmaceutically acceptable salt thereof |
| CN116947732A (zh) * | 2023-07-28 | 2023-10-27 | 江苏阿尔法药业股份有限公司 | 一种尼达尼布中间体的合成方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS4876863A (es) * | 1972-01-22 | 1973-10-16 | ||
| US6469181B1 (en) * | 1995-01-30 | 2002-10-22 | Catalytica, Inc. | Process for preparing 2-oxindoles and N-hydroxy-2-oxindoles |
| GB9516943D0 (en) * | 1995-08-18 | 1995-10-18 | Cancer Soc Auckland Div Nz Inc | Novel cyclopropylindoles and their secoprecursors,and their use as prodrugs |
| EP1115704B1 (de) | 1998-09-25 | 2003-06-18 | Boehringer Ingelheim Pharma GmbH & Co.KG | Neue substituierte indolinone mit einer inhibierenden wirkung auf verschiedene kinasen und cyclin/cdk-komplexe |
| US7291641B2 (en) * | 1999-10-11 | 2007-11-06 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Derivatives of heterocycles with 5 members, their preparation and their use as medicaments |
| UA75054C2 (uk) * | 1999-10-13 | 2006-03-15 | Бьорінгер Інгельхайм Фарма Гмбх & Ко. Кг | Заміщені в положенні 6 індолінони, їх одержання та їх застосування як лікарського засобу |
| DE10117204A1 (de) * | 2001-04-06 | 2002-10-10 | Boehringer Ingelheim Pharma | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| DE10233500A1 (de) * | 2002-07-24 | 2004-02-19 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | 3-Z-[1-(4-(N-((4-Methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylen]-6-methoxycarbonyl-2-indolinon-Monoethansulfonat und dessen Verwendung als Arzneimittel |
| US7148249B2 (en) | 2002-09-12 | 2006-12-12 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinones substituted by heterocycles, the preparation thereof and their use as medicaments |
| WO2008056634A1 (fr) * | 2006-11-06 | 2008-05-15 | Theravalues Corporation | Nouveau dérivé d'hydroxyindole |
| RU2525114C2 (ru) * | 2007-12-03 | 2014-08-10 | Бёрингер Ингельхайм Интернациональ Гмбх | Способ получения производного индолинона |
| UY31506A1 (es) * | 2007-12-03 | 2009-08-03 | Derivados de indolinona y procedimiento para su preparacion |
-
2008
- 2008-12-01 UY UY31506A patent/UY31506A1/es not_active Application Discontinuation
- 2008-12-01 PE PE2008002005A patent/PE20091445A1/es not_active Application Discontinuation
- 2008-12-02 LT LTEP08857503.0T patent/LT2229360T/lt unknown
- 2008-12-02 JP JP2010535407A patent/JP5933924B2/ja active Active
- 2008-12-02 NZ NZ585798A patent/NZ585798A/en unknown
- 2008-12-02 KR KR1020157026969A patent/KR101712810B1/ko active Active
- 2008-12-02 MX MX2010005557A patent/MX2010005557A/es active IP Right Grant
- 2008-12-02 PL PL08857503T patent/PL2229360T3/pl unknown
- 2008-12-02 EA EA201000883A patent/EA016196B1/ru not_active IP Right Cessation
- 2008-12-02 RS RS20201116A patent/RS60818B1/sr unknown
- 2008-12-02 EP EP08857503.0A patent/EP2229360B1/en active Active
- 2008-12-02 TW TW097146808A patent/TWI432415B/zh not_active IP Right Cessation
- 2008-12-02 CA CA2705490A patent/CA2705490C/en active Active
- 2008-12-02 AR ARP080105254A patent/AR069531A1/es unknown
- 2008-12-02 MY MYPI2010002337A patent/MY148574A/en unknown
- 2008-12-02 KR KR1020107012251A patent/KR101676261B1/ko active Active
- 2008-12-02 PT PT88575030T patent/PT2229360T/pt unknown
- 2008-12-02 CN CN2008801190684A patent/CN101883755B/zh active Active
- 2008-12-02 UA UAA201007864A patent/UA97872C2/ru unknown
- 2008-12-02 AU AU2008333287A patent/AU2008333287B2/en active Active
- 2008-12-02 DK DK08857503.0T patent/DK2229360T3/da active
- 2008-12-02 BR BRPI0819991-4A patent/BRPI0819991B1/pt active IP Right Grant
- 2008-12-02 WO PCT/EP2008/066581 patent/WO2009071524A2/en not_active Ceased
- 2008-12-02 HU HUE08857503A patent/HUE051550T2/hu unknown
- 2008-12-02 HR HRP20201480TT patent/HRP20201480T1/hr unknown
- 2008-12-02 SI SI200832138T patent/SI2229360T1/sl unknown
- 2008-12-02 US US12/745,788 patent/US8067617B2/en active Active
- 2008-12-02 ES ES08857503T patent/ES2818993T3/es active Active
- 2008-12-02 CL CL2008003599A patent/CL2008003599A1/es unknown
-
2010
- 2010-04-19 ZA ZA2010/02723A patent/ZA201002723B/en unknown
- 2010-04-26 IL IL205348A patent/IL205348A/en active IP Right Grant
- 2010-05-21 EC EC2010010195A patent/ECSP10010195A/es unknown
- 2010-06-01 TN TN2010000248A patent/TN2010000248A1/fr unknown
- 2010-06-03 CO CO10067260A patent/CO6210751A2/es active IP Right Grant
- 2010-07-01 MA MA32974A patent/MA31989B1/fr unknown
-
2014
- 2014-10-27 JP JP2014218112A patent/JP6044025B2/ja active Active
-
2020
- 2020-09-08 CY CY20201100845T patent/CY1123333T1/el unknown
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FC | Refusal |