UY25177A1 - 5- (2-ETIL-2-H-TETRAZOLE-5-IL) -1-METHYL-1,2,3,6-TETRAHYDROPYRIDINE - Google Patents
5- (2-ETIL-2-H-TETRAZOLE-5-IL) -1-METHYL-1,2,3,6-TETRAHYDROPYRIDINEInfo
- Publication number
- UY25177A1 UY25177A1 UY25177A UY25177A UY25177A1 UY 25177 A1 UY25177 A1 UY 25177A1 UY 25177 A UY25177 A UY 25177A UY 25177 A UY25177 A UY 25177A UY 25177 A1 UY25177 A1 UY 25177A1
- Authority
- UY
- Uruguay
- Prior art keywords
- maleic acid
- acid addition
- addition salt
- tetrahydropyridine
- methyl
- Prior art date
Links
Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención tiene por objetivo proporcionar una forma sólida farmacéuticamente aceptable del compuesto 5-(2-etil-2-H-tetrazol-5-il)-1-metil-1,2,3,6-tetrahidropiridina adecuado para la producción a gran escala de entidades farmacéuticas sólidas, por ejemplo tabletas o cápsulas. De acuerdo a la presente invención, se han suministrado sal de adición de ácido maleico de 5-(2-etil-2-H-tetrazol-5-il)-1-metil-1,2,3,6-tetrahidropiridina y las composiciones farmacéuticas que contienen la sal de adición ácida y el uso de las mismas para el tratamiento de trastornos causados por un mal funcionamiento de la acetilcolina(AcCh) o del sistema muscarínico. Por lo tanto se utiliza, por ejemplo, para tratar el mal de Alzheimer, lesiones traumáticas de cerebro o trastornos psicóticos. La sal de adición de ácido maleico, de acuerdo con la invención, puede obtenerese mediante tratamiento de 5-(2-etil-2-H-tetrazol-5-il)-1-metil-1,2,3,6-tetrahidropiridina o un derivado de sal de la misma con ácido maleico en un solvente inerte, seguido de precipitación, separación y opcionalmente recristalización mediante métodos conocidos y si se desea seguido de micronización del producto cristalino mediante molido húmedo, en seco o mediante cualquier otro proceso conveniente o mediante preparación de partículas de un proceso de emulsificación-disolvente. La precipitación de sal de maleato se realiza en un disolvente aprótico inerte, preferentemente tetrahidrofurano (THF). La sal de adición de ácido maleico es la sal de adición de ácido mono-maleico.The present invention has for its object to provide a pharmaceutically acceptable solid form of the compound 5- (2-ethyl-2-H-tetrazol-5-yl) -1-methyl-1,2,3,6-tetrahydropyridine suitable for the production to Large scale of solid pharmaceutical entities, for example tablets or capsules. In accordance with the present invention, 5- (2-ethyl-2-H-tetrazol-5-yl) -1-methyl-1,2,3,6-tetrahydropyridine maleic acid addition salt has been supplied and the pharmaceutical compositions containing the acid addition salt and the use thereof for the treatment of disorders caused by a malfunction of acetylcholine (AcCh) or the muscarinic system. Therefore it is used, for example, to treat Alzheimer's disease, traumatic brain injury or psychotic disorders. The maleic acid addition salt according to the invention can be obtained by treatment of 5- (2-ethyl-2-H-tetrazol-5-yl) -1-methyl-1,2,3,6-tetrahydropyridine or a salt derivative thereof with maleic acid in an inert solvent, followed by precipitation, separation and optionally recrystallization by known methods and if desired followed by micronization of the crystalline product by wet, dry grinding or by any other convenient process or by preparing particles from an emulsification-solvent process. The maleate salt precipitation is carried out in an inert aprotic solvent, preferably tetrahydrofuran (THF). The maleic acid addition salt is the mono-maleic acid addition salt.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DK78197 | 1997-07-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UY25177A1 true UY25177A1 (en) | 2000-12-29 |
Family
ID=8097489
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY25069A UY25069A1 (en) | 1997-07-01 | 1998-06-29 | PROCEDURE FOR PREPARING 5- (ETHYL-2-H-TETRAZOLE-5-IL) -1-METHYL-1,2,3,6-TETRAHYDROPYRIDINE |
| UY25177A UY25177A1 (en) | 1997-07-01 | 1998-09-10 | 5- (2-ETIL-2-H-TETRAZOLE-5-IL) -1-METHYL-1,2,3,6-TETRAHYDROPYRIDINE |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY25069A UY25069A1 (en) | 1997-07-01 | 1998-06-29 | PROCEDURE FOR PREPARING 5- (ETHYL-2-H-TETRAZOLE-5-IL) -1-METHYL-1,2,3,6-TETRAHYDROPYRIDINE |
Country Status (25)
| Country | Link |
|---|---|
| EP (1) | EP0994869A1 (en) |
| JP (1) | JP2002507215A (en) |
| KR (1) | KR20010014297A (en) |
| CN (1) | CN1261361A (en) |
| AR (1) | AR013096A1 (en) |
| AU (1) | AU735751B2 (en) |
| BG (1) | BG103933A (en) |
| BR (1) | BR9810331A (en) |
| CA (1) | CA2293324A1 (en) |
| CO (1) | CO4940483A1 (en) |
| EA (1) | EA200000081A1 (en) |
| HU (1) | HUP0002876A2 (en) |
| IL (1) | IL133093A0 (en) |
| IS (1) | IS5278A (en) |
| JO (1) | JO2031B1 (en) |
| MA (1) | MA25138A1 (en) |
| NO (1) | NO996580D0 (en) |
| PE (1) | PE116099A1 (en) |
| PL (1) | PL337184A1 (en) |
| SK (1) | SK187399A3 (en) |
| TN (1) | TNSN98120A1 (en) |
| TR (1) | TR199903283T2 (en) |
| UY (2) | UY25069A1 (en) |
| WO (1) | WO1999001448A1 (en) |
| ZA (1) | ZA985498B (en) |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8714789D0 (en) * | 1987-06-24 | 1987-07-29 | Lundbeck & Co As H | Heterocyclic compounds |
| SK58198A3 (en) * | 1995-11-06 | 1998-10-07 | Lundbeck & Co As H | Treatment of traumatic brain injury |
-
1998
- 1998-06-18 AR ARP980102925A patent/AR013096A1/en not_active Application Discontinuation
- 1998-06-24 ZA ZA985498A patent/ZA985498B/en unknown
- 1998-06-25 PE PE1998000563A patent/PE116099A1/en not_active Application Discontinuation
- 1998-06-25 JO JO19982031A patent/JO2031B1/en active
- 1998-06-26 CO CO98036576A patent/CO4940483A1/en unknown
- 1998-06-29 UY UY25069A patent/UY25069A1/en not_active Application Discontinuation
- 1998-06-30 TN TNTNSN98120A patent/TNSN98120A1/en unknown
- 1998-07-01 AU AU81020/98A patent/AU735751B2/en not_active Ceased
- 1998-07-01 EP EP98930655A patent/EP0994869A1/en not_active Withdrawn
- 1998-07-01 IL IL13309398A patent/IL133093A0/en unknown
- 1998-07-01 PL PL98337184A patent/PL337184A1/en unknown
- 1998-07-01 HU HU0002876A patent/HUP0002876A2/en unknown
- 1998-07-01 EA EA200000081A patent/EA200000081A1/en unknown
- 1998-07-01 MA MA25155A patent/MA25138A1/en unknown
- 1998-07-01 TR TR1999/03283T patent/TR199903283T2/en unknown
- 1998-07-01 SK SK1873-99A patent/SK187399A3/en unknown
- 1998-07-01 KR KR1019997012429A patent/KR20010014297A/en not_active Application Discontinuation
- 1998-07-01 JP JP50616699A patent/JP2002507215A/en active Pending
- 1998-07-01 WO PCT/DK1998/000294 patent/WO1999001448A1/en not_active Application Discontinuation
- 1998-07-01 CN CN98806497A patent/CN1261361A/en active Pending
- 1998-07-01 BR BR9810331-8A patent/BR9810331A/en not_active Application Discontinuation
- 1998-07-01 CA CA002293324A patent/CA2293324A1/en not_active Abandoned
- 1998-09-10 UY UY25177A patent/UY25177A1/en not_active Application Discontinuation
-
1999
- 1999-11-30 IS IS5278A patent/IS5278A/en unknown
- 1999-11-30 BG BG103933A patent/BG103933A/en unknown
- 1999-12-30 NO NO996580A patent/NO996580D0/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| TNSN98120A1 (en) | 2005-03-15 |
| TR199903283T2 (en) | 2000-06-21 |
| IL133093A0 (en) | 2001-03-19 |
| CN1261361A (en) | 2000-07-26 |
| CA2293324A1 (en) | 1999-01-14 |
| KR20010014297A (en) | 2001-02-26 |
| AU735751B2 (en) | 2001-07-12 |
| EP0994869A1 (en) | 2000-04-26 |
| WO1999001448A1 (en) | 1999-01-14 |
| UY25069A1 (en) | 1998-12-21 |
| SK187399A3 (en) | 2000-06-12 |
| BR9810331A (en) | 2000-09-05 |
| NO996580L (en) | 1999-12-30 |
| AR013096A1 (en) | 2000-12-13 |
| AU8102098A (en) | 1999-01-25 |
| EA200000081A1 (en) | 2000-08-28 |
| BG103933A (en) | 2000-07-31 |
| PL337184A1 (en) | 2000-08-14 |
| JO2031B1 (en) | 1999-05-15 |
| PE116099A1 (en) | 1999-11-23 |
| HUP0002876A2 (en) | 2001-06-28 |
| NO996580D0 (en) | 1999-12-30 |
| MA25138A1 (en) | 2001-04-02 |
| ZA985498B (en) | 1999-01-20 |
| CO4940483A1 (en) | 2000-07-24 |
| JP2002507215A (en) | 2002-03-05 |
| IS5278A (en) | 1999-11-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| 109 | Application deemed to be withdrawn |
Effective date: 20101008 |