PE54697A1 - PHARMACEUTICAL COMPOSITION INCLUDING A COMBINATION OF A SELECTIVE NMDA ANTAGONIST OF THE PREVIOUS BRAIN AND AN AGENT CAPABLE OF INCREASING EXCITING FEEDBACK - Google Patents
PHARMACEUTICAL COMPOSITION INCLUDING A COMBINATION OF A SELECTIVE NMDA ANTAGONIST OF THE PREVIOUS BRAIN AND AN AGENT CAPABLE OF INCREASING EXCITING FEEDBACKInfo
- Publication number
- PE54697A1 PE54697A1 PE1996000370A PE00037096A PE54697A1 PE 54697 A1 PE54697 A1 PE 54697A1 PE 1996000370 A PE1996000370 A PE 1996000370A PE 00037096 A PE00037096 A PE 00037096A PE 54697 A1 PE54697 A1 PE 54697A1
- Authority
- PE
- Peru
- Prior art keywords
- hidroxi
- alkyl
- levodopa
- combination
- pharmaceutical composition
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
Abstract
SE REFIERE A COMBINACIONES SINERGICAS QUE PERMITEN EL USO DEL POTENCIAL TERAPEUTICO GLOBAL DE LA LEVODOPA, EN EL TRATAMIENTO DE LA ENFERMEDAD DE PARKINSON, Y COMPRENDE LAS SIGUIENTES COMBINACIONES (A + B), (A + C) Y (A + B + C), DONDE: A) ES UN ANTAGONISTA SELECTIVO DEL N-METIL-D-ASPARTATO (NMDA), SUBTIPO NR2B, DEL CEREBRO ANTERIOR, DE FORMULA (I); B) ES UN AGENTE CAPAZ DE AUMENTAR LA RETROALIMENTACION EXCITADORA, TAL COMO: LOS AGONISTAS DE LA DOPAMINA, LOS INHIBIDORES DE LA MAO, ENTRE OTROS, PREFERENTEMENTE LEVODOPA; Y C) ES UN AGENTE INHIBIDOR DE LA LEVODOPA DESCARBOXILASA, PREFERENTEMENTE CARBIDOPA. EN EL COMPUESTO DE FORMULA (I): R1, R2, R3 Y R4 SON H, ALQUILO C1-C6, HALO, CF3, OH o OR7; R5 ES CH3 O C2H5, O DE OTRO MODO MIENTRAS QUE R1, R3 Y R4 PERMANECEN IGUALES R2 Y R5 SE TOMAN JUNTOS Y SON -O-CH2-, FORMANDO UN ANILLO CROMAN-4-OL; R6 SON LOS COMPUESTOS (II); R7 ES ALQUILO C1-C3; R8 ES FENILO OPCIONALMENTE SUSTITUIDO CON 1, 2 o 3 SUSTITUYENTES SELECCIONADOS ENTRE ALQUILO C1-C6, HALO o CF3; "X" ES O, S o (CH2)n; n ES 0, 1, 2 o 3. SIENDO ESTOS COMPUESTOS (I) PREFERENTEMENTE : (+)-(1S,2S)-1-(4-HIDROXI-FENIL)-2-(4-HIDROXI-4-FENILPIPERIDINO)-1-PROPANOL; -(1S,2S)-1-(4-HIDROXI-3-METOXIFENIL)-2-(4-HIDROXI-4-FENILPIPERIDINO)-1-PROPANOL; (3R,4S)-3-(4-(4-FLUOROFENIL)-4-HIDROXIPIPERIDIN-1-IL)-CROMAN-4,7-DIOLREFERS TO SYNERGIC COMBINATIONS THAT ALLOW THE USE OF THE GLOBAL THERAPEUTIC POTENTIAL OF LEVODOPA, IN THE TREATMENT OF PARKINSON'S DISEASE, AND INCLUDES THE FOLLOWING COMBINATIONS (A + B), (A + C) AND (A + B + C) , WHERE: A) IT IS A SELECTIVE ANTAGONIST OF N-METHYL-D-ASPARTATE (NMDA), SUBTYPE NR2B, OF THE PREVIOUS BRAIN, OF FORMULA (I); B) IT IS AN AGENT ABLE TO INCREASE THE EXCITING FEEDBACK, SUCH AS: THE DOPAMINE AGONISTS, THE MAO INHIBITORS, AMONG OTHERS, PREFERABLY LEVODOPA; AND C) IT IS AN INHIBITING AGENT FOR LEVODOPA DECARBOXYLASE, PREFERABLY CARBIDOPA. IN THE COMPOUND OF FORMULA (I): R1, R2, R3 AND R4 ARE H, C1-C6-ALKYL, HALO, CF3, OH or OR7; R5 IS CH3 OR C2H5, OR OTHERWISE WHILE R1, R3 AND R4 REMAIN THE SAME R2 AND R5 ARE TAKEN TOGETHER AND ARE -O-CH2-, FORMING A CHROMAN-4-OL RING; R6 ARE THE COMPOUNDS (II); R7 IS C1-C3 ALKYL; R8 IS OPENLY SUBSTITUTED PHENYL WITH 1, 2 or 3 SELECTED SUBSTITUTES BETWEEN C1-C6, HALO or CF3 ALKYL; "X" IS O, S or (CH2) n; n IS 0, 1, 2 or 3. BEING THESE COMPOUNDS (I) PREFERABLY: (+) - (1S, 2S) -1- (4-HIDROXI-FENIL) -2- (4-HIDROXI-4-FENILPIPERIDINO) - 1-PROPANOL; - (1S, 2S) -1- (4-HIDROXI-3-METOXIFENIL) -2- (4-HIDROXI-4-FENILPIPERIDINO) -1-PROPANOL; (3R, 4S) -3- (4- (4-FLUOROPHENYL) -4-HYDROXIPIPERIDIN-1-IL) -CROMAN-4,7-DIOL
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/IB1995/000398 WO1996037226A2 (en) | 1995-05-26 | 1995-05-26 | Combinations for the treatment of parkinsonism containing selective nmda antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE54697A1 true PE54697A1 (en) | 1998-01-06 |
Family
ID=47225806
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE1996000370A PE54697A1 (en) | 1995-05-26 | 1996-05-22 | PHARMACEUTICAL COMPOSITION INCLUDING A COMBINATION OF A SELECTIVE NMDA ANTAGONIST OF THE PREVIOUS BRAIN AND AN AGENT CAPABLE OF INCREASING EXCITING FEEDBACK |
Country Status (4)
| Country | Link |
|---|---|
| KR (1) | KR960040360A (en) |
| AR (1) | AR003951A1 (en) |
| MY (1) | MY118944A (en) |
| PE (1) | PE54697A1 (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1605935A4 (en) * | 2003-03-06 | 2009-05-20 | Celgene Corp | Methods of using and compositions comprising selective cytokine inhibitory drugs for the treatment and management of disorders of the central nervous system |
-
1996
- 1996-05-14 AR ARP960102562A patent/AR003951A1/en unknown
- 1996-05-22 PE PE1996000370A patent/PE54697A1/en not_active Application Discontinuation
- 1996-05-23 MY MYPI96001941A patent/MY118944A/en unknown
- 1996-05-25 KR KR1019960017930A patent/KR960040360A/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| AR003951A1 (en) | 1998-09-30 |
| KR960040360A (en) | 1996-12-17 |
| MY118944A (en) | 2005-02-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |