WO2011154586A3 - Procedimientos mejorados para la preparación de derivados de quinoxalina - Google Patents
Procedimientos mejorados para la preparación de derivados de quinoxalina Download PDFInfo
- Publication number
- WO2011154586A3 WO2011154586A3 PCT/ES2011/070424 ES2011070424W WO2011154586A3 WO 2011154586 A3 WO2011154586 A3 WO 2011154586A3 ES 2011070424 W ES2011070424 W ES 2011070424W WO 2011154586 A3 WO2011154586 A3 WO 2011154586A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- varenicline
- present
- solvate
- salt
- provides
- Prior art date
Links
Classifications
-
- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/504—Pyridazines; Hydrogenated pyridazines forming part of bridged 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/34—Tobacco-abuse
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/08—Bridged systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Addiction (AREA)
- Psychiatry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención proporciona un procedimiento mejorado para preparar compuesto de fórmula (IIIA), un intermedio de la síntesis de vareniclina. También, la presente invención proporciona un procedimiento mejorado para preparar vareniclina, o una sal o un solvato de la misma. Además, la presente invención provee un proceso para decolorar vareniclina, o una sal o un solvato de la misma. Además, la presente invención provee un proceso para preparar L- tartrato de vareniclina con rendimiento mejorado. Además la presente invención se refiere al uso de un compuesto de fórmula (V), o una sal o un solvato del mismo, como marcador de referencia y estándar de referencia para evaluar la pureza de vareniclina, o una sal o un solvato de la misma.
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP11791980.3A EP2581375A4 (en) | 2010-06-11 | 2011-06-13 | IMPROVED METHODS FOR THE PREPARATION OF QUINOXALINE DERIVATIVES |
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
ES201030911 | 2010-06-11 | ||
ESP201030911 | 2010-06-11 | ||
US35444210P | 2010-06-14 | 2010-06-14 | |
US61/354,442 | 2010-06-14 | ||
US13/156,739 | 2011-06-09 | ||
US13/156,739 US20120004239A1 (en) | 2010-06-11 | 2011-06-09 | Process for Preparing Quinoxaline Derivatives |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2011154586A2 WO2011154586A2 (es) | 2011-12-15 |
WO2011154586A3 true WO2011154586A3 (es) | 2012-03-22 |
Family
ID=45098460
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/ES2011/070424 WO2011154586A2 (es) | 2010-06-11 | 2011-06-13 | Procedimientos mejorados para la preparación de derivados de quinoxalina |
Country Status (3)
Country | Link |
---|---|
US (1) | US20120004239A1 (es) |
EP (1) | EP2581375A4 (es) |
WO (1) | WO2011154586A2 (es) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP4241775A1 (en) * | 2022-03-11 | 2023-09-13 | Par Pharmaceutical, Inc. | Tablet comprising varenicline and process of preparation thereof |
US11602537B2 (en) | 2022-03-11 | 2023-03-14 | Par Pharmaceutical, Inc. | Varenicline compound and process of manufacture thereof |
Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004108725A1 (en) * | 2003-06-04 | 2004-12-16 | Pfizer Products Inc. | Preparation of substituted quinoxalines from the dianline with 2,3-dihydroxy-1,4-dioxane |
WO2006090236A1 (en) * | 2005-02-24 | 2006-08-31 | Pfizer Products Inc. | Preparation of high purity substituted quinoxaline |
WO2009065872A2 (en) * | 2007-11-20 | 2009-05-28 | Medichem, S.A. | Improved processes for the synthesis of varenicline l-tartrate |
WO2009155403A2 (en) * | 2008-06-19 | 2009-12-23 | Teva Pharmaceutical Industries Ltd. | Processes for the preparation of varenicline and intermediates thereof |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ME00459B (me) | 1997-12-31 | 2011-10-10 | Pfizer Prod Inc | Aril fuzirana azapoliciklična jedinjenja |
AU2002234836B2 (en) | 2001-04-20 | 2007-08-23 | Pfizer Products Inc. | Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic compounds |
WO2009111623A2 (en) | 2008-03-06 | 2009-09-11 | Dr. Reddy's Laboratories Ltd. | Amorphous varenicline tartrate |
US20100010221A1 (en) | 2008-07-10 | 2010-01-14 | Revital Lifshitz-Liron | Processes for purifying varenicline l-tartrate salt and preparing crystalline forms of varenicline l-tartrate salt |
-
2011
- 2011-06-09 US US13/156,739 patent/US20120004239A1/en not_active Abandoned
- 2011-06-13 WO PCT/ES2011/070424 patent/WO2011154586A2/es active Application Filing
- 2011-06-13 EP EP11791980.3A patent/EP2581375A4/en not_active Withdrawn
Patent Citations (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2004108725A1 (en) * | 2003-06-04 | 2004-12-16 | Pfizer Products Inc. | Preparation of substituted quinoxalines from the dianline with 2,3-dihydroxy-1,4-dioxane |
WO2006090236A1 (en) * | 2005-02-24 | 2006-08-31 | Pfizer Products Inc. | Preparation of high purity substituted quinoxaline |
WO2009065872A2 (en) * | 2007-11-20 | 2009-05-28 | Medichem, S.A. | Improved processes for the synthesis of varenicline l-tartrate |
WO2009155403A2 (en) * | 2008-06-19 | 2009-12-23 | Teva Pharmaceutical Industries Ltd. | Processes for the preparation of varenicline and intermediates thereof |
Non-Patent Citations (2)
Title |
---|
J. W. COE ET AL.: "Varenicline: An alpha4beta2 nicotin receptor partial agonist for smoking cessation", J. MED. CHEM., vol. 48, no. 10, 2005, pages 3474 - 3477, XP002474642 * |
See also references of EP2581375A4 * |
Also Published As
Publication number | Publication date |
---|---|
EP2581375A4 (en) | 2014-02-19 |
US20120004239A1 (en) | 2012-01-05 |
EP2581375A2 (en) | 2013-04-17 |
WO2011154586A2 (es) | 2011-12-15 |
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