AR081267A1 - Procedimiento de obtencion de la forma cristalina a del febuxostat - Google Patents
Procedimiento de obtencion de la forma cristalina a del febuxostatInfo
- Publication number
- AR081267A1 AR081267A1 ARP110101868A ARP110101868A AR081267A1 AR 081267 A1 AR081267 A1 AR 081267A1 AR P110101868 A ARP110101868 A AR P110101868A AR P110101868 A ARP110101868 A AR P110101868A AR 081267 A1 AR081267 A1 AR 081267A1
- Authority
- AR
- Argentina
- Prior art keywords
- febuxostat
- solvent
- obtaining
- acetate
- temperature
- Prior art date
Links
- BQSJTQLCZDPROO-UHFFFAOYSA-N febuxostat Chemical compound C1=C(C#N)C(OCC(C)C)=CC=C1C1=NC(C)=C(C(O)=O)S1 BQSJTQLCZDPROO-UHFFFAOYSA-N 0.000 title abstract 5
- 229960005101 febuxostat Drugs 0.000 title abstract 5
- 238000000034 method Methods 0.000 title abstract 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 abstract 9
- 239000002904 solvent Substances 0.000 abstract 5
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 abstract 3
- WBJINCZRORDGAQ-UHFFFAOYSA-N formic acid ethyl ester Natural products CCOC=O WBJINCZRORDGAQ-UHFFFAOYSA-N 0.000 abstract 3
- 238000009835 boiling Methods 0.000 abstract 2
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 abstract 2
- 229940011051 isopropyl acetate Drugs 0.000 abstract 2
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 abstract 2
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000001816 cooling Methods 0.000 abstract 1
- 239000013078 crystal Substances 0.000 abstract 1
- 238000002425 crystallisation Methods 0.000 abstract 1
- 230000008025 crystallization Effects 0.000 abstract 1
- 238000004090 dissolution Methods 0.000 abstract 1
- 238000001035 drying Methods 0.000 abstract 1
- 238000001914 filtration Methods 0.000 abstract 1
- 238000002955 isolation Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 238000003756 stirring Methods 0.000 abstract 1
- 239000000725 suspension Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
- C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
- C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Thiazole And Isothizaole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Steroid Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Procedimiento de obtención de la forma cristalina A del Febuxostat por cristalización en un disolvente elegido entre acetato de etilo, acetato de isopropilo o formiato de etilo. Reivindicación 1: Procedimiento de obtención de la forma cristalina A del Febuxostat, caracterizado porque comprende las siguientes etapas: a) Disolución del Febuxostat en un disolvente elegido del grupo consistente en acetato de etilo, acetato de isopropilo y formiato de etilo en una proporción de 5 a 60 ml de disolvente por gramo de soluto, a una temperatura comprendida entre 50°C y la temperatura de ebullición de la disolución; b) Formación de cristales manteniendo la disolución resultante de la etapa a) a una temperatura comprendida entre 45°C y la temperatura de ebullición de la mezcla durante un período comprendido entre 1 y 24 horas, cuando el disolvente es acetato de etilo o acetato de isopropilo; y c) Aislamiento de la forma cristalina A del Febuxostat por enfriamiento a temperatura ambiente de: c.1.) la suspensión resultante de la etapa b), manteniéndose así durante un período comprendido entre 3 y 15 horas; o c.2.) la disolución resultante de la etapa a), sin pasar por la etapa b), manteniéndose en agitación durante un período comprendido entre 3 y 24 horas, cuando el disolvente es formiato de etilo; seguido de filtración y secado.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| ES201031061 | 2010-07-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR081267A1 true AR081267A1 (es) | 2012-07-18 |
Family
ID=44533538
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110101868A AR081267A1 (es) | 2010-07-13 | 2011-05-31 | Procedimiento de obtencion de la forma cristalina a del febuxostat |
| ARP110102208A AR081659A1 (es) | 2010-07-13 | 2011-06-24 | Procedimiento de obtencion de la forma cristalina ii del febuxostat |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP110102208A AR081659A1 (es) | 2010-07-13 | 2011-06-24 | Procedimiento de obtencion de la forma cristalina ii del febuxostat |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20130184466A1 (es) |
| EP (1) | EP2593442A1 (es) |
| JP (1) | JP2013531021A (es) |
| AR (2) | AR081267A1 (es) |
| TW (1) | TW201217346A (es) |
| UY (1) | UY33511A (es) |
| WO (1) | WO2012007487A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2619191A4 (en) | 2010-09-24 | 2014-03-26 | Hetero Research Foundation | NEW POLYMORPHS OF FEBUXOSTAT |
| EP2718272A2 (en) | 2011-06-06 | 2014-04-16 | Hetero Research Foundation | Process for febuxostat |
| CN104114545B (zh) * | 2011-11-15 | 2018-06-01 | 迈兰实验室有限公司 | 用于制备非布索坦多晶型物的方法 |
| EP2692342A1 (en) | 2012-07-30 | 2014-02-05 | Interquim, S.A. | Process for the preparation of pharmaceutical compositions comprising febuxostat in the form of tablets |
| EP3002006A1 (en) | 2014-10-01 | 2016-04-06 | Bluepharma - Industria Farmacêutica, S.A. | Pharmaceutical composition capable for the incorporation Febuxostat in the crystalline modifications F10, II, G and A |
| CN110526879B (zh) * | 2019-08-28 | 2022-06-21 | 迪嘉药业集团有限公司 | 一种小粒度非布司他的结晶制备方法 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69122084T2 (de) * | 1990-11-30 | 1997-04-03 | Teijin Ltd., Osaka | 2-arylthiazolderivat sowie dieses enthaltendes arzneimittel |
| CN101139325B (zh) | 2006-09-07 | 2010-05-12 | 上海医药工业研究院 | 2-(3-氰基-4-异丁氧基苯基)-4-甲基-5-噻唑甲酸晶型及其制备方法 |
| CN100546985C (zh) * | 2007-06-29 | 2009-10-07 | 上海华拓医药科技发展股份有限公司 | 非布他特微晶及其组合物 |
| CN101412700B (zh) | 2007-10-19 | 2011-06-08 | 上海医药工业研究院 | 非布司他的晶型及其制备方法 |
-
2011
- 2011-05-31 AR ARP110101868A patent/AR081267A1/es not_active Application Discontinuation
- 2011-06-24 AR ARP110102208A patent/AR081659A1/es unknown
- 2011-07-11 TW TW100124419A patent/TW201217346A/zh unknown
- 2011-07-13 JP JP2013519084A patent/JP2013531021A/ja not_active Withdrawn
- 2011-07-13 EP EP11736321.8A patent/EP2593442A1/en not_active Withdrawn
- 2011-07-13 US US13/809,839 patent/US20130184466A1/en not_active Abandoned
- 2011-07-13 UY UY0001033511A patent/UY33511A/es unknown
- 2011-07-13 WO PCT/EP2011/061906 patent/WO2012007487A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| TW201217346A (en) | 2012-05-01 |
| WO2012007487A1 (en) | 2012-01-19 |
| US20130184466A1 (en) | 2013-07-18 |
| WO2012007487A9 (en) | 2012-06-21 |
| EP2593442A1 (en) | 2013-05-22 |
| AR081659A1 (es) | 2012-10-10 |
| UY33511A (es) | 2012-01-31 |
| JP2013531021A (ja) | 2013-08-01 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |