PE20110100A1 - Procedimiento de preparacion de n-[trans-4-[4-(ciclopropilmetil)-1-piperazinil]ciclohexil]-4-[[(7r)-7-etil-5,6,7,8-tetrahidro-5-metil-8-(1-metiletil)-6-oxo-2-pteridinil]amino]-3-metoxi-benzamida - Google Patents
Procedimiento de preparacion de n-[trans-4-[4-(ciclopropilmetil)-1-piperazinil]ciclohexil]-4-[[(7r)-7-etil-5,6,7,8-tetrahidro-5-metil-8-(1-metiletil)-6-oxo-2-pteridinil]amino]-3-metoxi-benzamidaInfo
- Publication number
- PE20110100A1 PE20110100A1 PE2010000509A PE2010000509A PE20110100A1 PE 20110100 A1 PE20110100 A1 PE 20110100A1 PE 2010000509 A PE2010000509 A PE 2010000509A PE 2010000509 A PE2010000509 A PE 2010000509A PE 20110100 A1 PE20110100 A1 PE 20110100A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- ethyl
- compound
- methylethyl
- pteridinyl
- Prior art date
Links
Classifications
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- 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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D475/00—Heterocyclic compounds containing pteridine ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Engineering & Computer Science (AREA)
- Hospice & Palliative Care (AREA)
- Molecular Biology (AREA)
- Hematology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Hydrogenated Pyridines (AREA)
Abstract
SE REFIERE A UN PROCESO PARA LA FABRICACION DEL COMPUESTO N-TRANS-4-[4-(CICLOPROPILMETIL)-1-PIPERAZINIL]CICLOHEXIL]-4-[[(7R)-7-ETIL-5,6,7,8-TETRAHIDRO-5-METIL-8-(1-METILETIL)-6-OXO-2-PTERIDINIL]AMINO]-3-METOXI-BENZAMIDA QUE COMPRENDE: A) SINTESIS DEL COMPUESTO DE FORMULA (15c). B) SINTESIS DEL COMPUESTO 2-CLORO-7-ETIL-7,8-DIHIDRO-5-METIL-8-(1-METILETIL)-(7R)-6(5H)-PTERIDINONA C) REACCION DE 23g DEL COMPUESTO SINTETIZADO EN A) CON 16,8g DEL COMPUESTO SINTETIZADO EN B) Y 28,3g DE ACIDO para-TOLUENSULFONICO EN 350mL DE SOLVENTE 2-METIL-4-PENTANOL. D) REFLUJO DE 22 HORAS. E) ADICION DE 300mL DE CLORURO METILENO Y 300mL DE AGUA DISMINERALIZADA. F) LAVADO CON AGUAY SECADO SOBRE SULAFTOM SODICO. G) EVAPORIZACION DEL SOLVENTE Y DISOLUCION DEL RESIDUO EN ACETATO DE ETILO. H) LA MEZCLA SE ENFRIO A 20ºC. I) SE FILTRO Y SE LAVO EL PRECIPITADO CON ACETATO DE ETILO. J) SECAR A 60ºC. DICHO PROCESO POSEE UN RENDIMIENTO DE AL MENOS 66% DE UN PRODUCTO CUYO PUNTO DE FUSION ES 182ºC. EL PRODUCTO ES UN INHIBIDOR DE CICLOQUINASAS
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP06101414 | 2006-02-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20110100A1 true PE20110100A1 (es) | 2011-02-18 |
Family
ID=38008126
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2010000509A PE20110100A1 (es) | 2006-02-08 | 2007-02-06 | Procedimiento de preparacion de n-[trans-4-[4-(ciclopropilmetil)-1-piperazinil]ciclohexil]-4-[[(7r)-7-etil-5,6,7,8-tetrahidro-5-metil-8-(1-metiletil)-6-oxo-2-pteridinil]amino]-3-metoxi-benzamida |
| PE2007000127A PE20071248A1 (es) | 2006-02-08 | 2007-02-06 | Sal especifica, forma anhidra y cristalina de un derivado de dihidropteridiona |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2007000127A PE20071248A1 (es) | 2006-02-08 | 2007-02-06 | Sal especifica, forma anhidra y cristalina de un derivado de dihidropteridiona |
Country Status (21)
| Country | Link |
|---|---|
| US (3) | US7439358B2 (es) |
| EP (2) | EP1984367A1 (es) |
| JP (1) | JP5134552B2 (es) |
| KR (2) | KR101462879B1 (es) |
| CN (2) | CN102093360B (es) |
| AR (1) | AR059349A1 (es) |
| AU (1) | AU2007213752B2 (es) |
| BR (1) | BRPI0707604A8 (es) |
| CA (1) | CA2635834C (es) |
| EA (2) | EA018663B1 (es) |
| EC (1) | ECSP088589A (es) |
| IL (2) | IL193217A (es) |
| NO (1) | NO20082610L (es) |
| NZ (2) | NZ570987A (es) |
| PE (2) | PE20110100A1 (es) |
| SG (2) | SG10201404755SA (es) |
| TW (1) | TW200738716A (es) |
| UA (2) | UA101060C2 (es) |
| UY (1) | UY30136A1 (es) |
| WO (1) | WO2007090844A1 (es) |
| ZA (1) | ZA200804587B (es) |
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| US20060058311A1 (en) | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| US7728134B2 (en) * | 2004-08-14 | 2010-06-01 | Boehringer Ingelheim International Gmbh | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament |
| US7759485B2 (en) * | 2004-08-14 | 2010-07-20 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dihydropteridinones |
| EP1632493A1 (de) * | 2004-08-25 | 2006-03-08 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| EP1630163A1 (de) * | 2004-08-25 | 2006-03-01 | Boehringer Ingelheim Pharma GmbH & Co.KG | Dihydropteridinonderivative, Verfahren zu deren Herstellung und deren Verwendung als Arzneimittel |
| DE102004058337A1 (de) * | 2004-12-02 | 2006-06-14 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Verfahren zur Herstellung von annelierten Piperazin-2-on Derivaten |
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| US7439358B2 (en) | 2006-02-08 | 2008-10-21 | Boehringer Ingelheim International Gmbh | Specific salt, anhydrous and crystalline form of a dihydropteridione derivative |
| CN101437795A (zh) * | 2006-03-07 | 2009-05-20 | 阿斯利康(瑞典)有限公司 | 哌啶衍生物,制备它们的方法,它们作为治疗剂的用途和含有它们的药物组合物 |
| CA2873524C (en) | 2006-05-04 | 2018-02-20 | Boehringer Ingelheim International Gmbh | A polymeric form of 1-((4-methyl-quinazolin-2-yl)methyl)-3-7-(2-butyn-1-yl)-8-(3-(r)-aminopiperidin-1-yl)xanthine |
| WO2009019205A1 (en) | 2007-08-03 | 2009-02-12 | Boehringer Ingelheim International Gmbh | Crystalline form of a dihydropteridione derivative |
| JP4642085B2 (ja) | 2008-01-17 | 2011-03-02 | 日本下水道事業団 | 予測健全度を利用した施設管理および更新計画システム |
| EP2100894A1 (en) | 2008-03-12 | 2009-09-16 | 4Sc Ag | Pyridopyrimidines used as Plk1 (polo-like kinase) inhibitors |
| EP2509592A1 (en) | 2009-12-07 | 2012-10-17 | Boehringer Ingelheim International GmbH | Bibw 2992 for use in the treatment of triple negative breast cancer |
| WO2011101369A1 (en) | 2010-02-17 | 2011-08-25 | Boehringer Ingelheim International Gmbh | Dihydropteridinones, method for production and use thereof |
| US8546566B2 (en) | 2010-10-12 | 2013-10-01 | Boehringer Ingelheim International Gmbh | Process for manufacturing dihydropteridinones and intermediates thereof |
| US9358233B2 (en) | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| US20130131069A1 (en) | 2011-05-13 | 2013-05-23 | Boehringer Ingelheim International Gmbh | Method for treatment of solid malignancies including advanced or metastatic solid malignancies |
| US9370535B2 (en) | 2011-05-17 | 2016-06-21 | Boehringer Ingelheim International Gmbh | Method for treatment of advanced solid tumors |
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