NO323696B1 - Anvendelse av sentrale cannabinoid-reseptor-antagonister for regulering av appetitt - Google Patents
Anvendelse av sentrale cannabinoid-reseptor-antagonister for regulering av appetitt Download PDFInfo
- Publication number
- NO323696B1 NO323696B1 NO19993634A NO993634A NO323696B1 NO 323696 B1 NO323696 B1 NO 323696B1 NO 19993634 A NO19993634 A NO 19993634A NO 993634 A NO993634 A NO 993634A NO 323696 B1 NO323696 B1 NO 323696B1
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- Norway
- Prior art keywords
- receptor antagonists
- alcohol
- administration
- cannabinoid receptor
- receptor antagonist
- Prior art date
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- 239000003536 cannabinoid receptor antagonist Substances 0.000 title description 4
- 235000021407 appetite control Nutrition 0.000 title 1
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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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P25/00—Drugs for disorders of the nervous system
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P3/04—Anorexiants; Antiobesity agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
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- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Addiction (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Child & Adolescent Psychology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Steroid Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Description
Sammendrag
Oppfinnelsen angår anvendelse av en sentral cannabinoid-reseptorantagonist, alene eller sammen med en forbindelse
for regulering av metaboliske forstyrrelser, spesielt en
p3-adrenergisk reseptor-agonist, for fremstilling av
medikamenter som er nyttige ved behandling av
appetittforstyrrelser.
Foreliggende oppfinnelse angår anvendelse av sentrale cannabinoid-reseptor-antagonister for fremstilling av medikament nyttig ved behandling av spiseforstyrrelser.
Mer spesielt angår oppfinnelsen anvendelse av CBi-reseptor-antagonister for fremstilling av medikamenter som er nyttige ved behandling av spiseforstyrrelser. Formålet med medikamenter er å regulere matlysten, spesielt lysten til å nyte sukker, karbohydrater eller alkohol.
I foreliggende beskrivelse og i kravene er spiseforstyrrelser ment å skulle bety spiseforstyrrelser som kan henføres til appetittvekkende substanser så som sukkere, karbohydrater og alkohol.
Delta-9-tetrahydrocannabinol eller A<9->THC, er den hovedsakelige aktive bestanddel ekstrahert fra Cannabis sativa (Tuner, 1985; i Marijuana, 84, Ed. Harvey, DY, IRL Press, Oxford).
Virkningene av cannabinoider er på grunn av en vekselvirkning med spesifikke høyaffrnitetsreseptorer koblet til G-proteiner. To typer av reseptorer er for tiden beskrevet: CBi-reseptorene, som foreligger overveiende i sentralnerve-systemet (Devan et al., Molekular Pharmacology, 1988, 34.605 - 613), og CEfe-reseptorene, som foreligger i det immune system (Nye et al., The Journal of Pharmacology and Experimental Terapeutics, 1985,234,784 - 791; Kaminski et al., 1992, Molecular Pharmacology, 42, 736 - 742; Munro et al., Nature, 1993, 365.
61 - 65). Karakterisering av disse reseptorer er blitt gjort mulig ved utviklingen av syntetiske ligander så som CP 55,940 (J. Pharmacol. Exp. Ther., 1988,247,1046 -1051) og WIN 55212-2 (J. Pharmacol. Exp. Ther., 1993,264,1352 -1363) og, mer nylig, på grunn av oppdagelsen av den selektive CBi-reseptor-antagonist SR 141716 A (M. Rinaldi-Carmona et al., FEBS Lett., 1994, 350,240-244).
Grupper av forbindelser som har affinitet til cannabinoid-reseptorene, er beskrevet i flere patenter eller patentsøknader, spesielt europeisk patentsøknad EP-576 357, som beskriver pyrazolderivater, og patentsøknad WO 96/02248, som beskriver spesielt benzofuranderivater.
Mer spesielt er N-piperidino-5-(4-klorfenyl)-1-(2,4-diklofrenyl)-4-metyl-pyrazol-3-karboksamtd, også kalt SR 141716, med formelen dets farmasøytisk godtagbare salter og deres solvater beskrevet i europeisk patentsøknad EP-656 354 som sentraleCBi-reseptor-antagonister.
SR 141716 A er hydrokloridet av SR 141716.
Det er kjent at delta-9-tetrahydrocannabinol, hvis internasjonale trivialnavn er Dronabinol, blir anvendt ved behandling av anorexia, spesielt i pasienter som lider av AIDS (J. Pain Symptom Manage., 1995,10 (2), 89 - 97) eller kreft (J. Palliat. Care, 1994,10 (1), 14 -18).
Det er videre beskrevet at SR 141716 og dets salter, som er sentrale cannabinoid-reseptor-antagonister, kan anvendes ved behandling av appetittforstyrrelser, spesielt som anorexigene midler og ved behandling av forstyrrelser forbundet med anvendelse av psykotrope substanser.
Konvensjonelle anorexigene midler forårsaker appetittreduksjon som er generelt uavhengig av maten som skal fortæres.
Overraskende er det nå funnet at CBi-reseptor-antagonistene har den spesifikk egenskap at de innvirker valgfritt på spiseforstyrrelser som henfører seg til appetittvekkende substanser.
Således gjør administreringen av en CBrreseptor-antagonist det mulig å regulere ønsket om å nyte ikke-essensielle næringstoffer så som et overskudd av sukker, et overskudd av karbohydrater, alkohol eller medikamenter.
Det er faktisk blitt iakttatt en ny adferd hos dyr etter at det er blitt utført tester på dem: Dyrefestene har avslørt en ny adferd: Dyret viser ikke lenger
spontan appetitt for bestanddelen, for eksempel sukker eller alkohol, som vanligvis fremkaller lyst på å fortære den. Denne mangel på appetitt manifesterer seg også selv når dyret er blitt forhåndsbehandlet med et neuropeptid som er kjent for å øke appetitten, for eksempel neuropeptid Y (NPY).
I henhold til ett aspekt angår foreliggende oppfinnelse anvendelse av en CBrreseptor-antagonist for fremstilling av medikamenter som er nyttige ved behandling av spiseforstyrrelser.
CBi-reseptor-antagonistene som er egnet for formålene ifølge foreliggende oppfinnelse er N-piperidino-5-(4-klorfenyl)-1 -(2,4-diklorfenyl)-4-metylpyrazol-3-karboksamid, dets farmasøytisk godtagbare salter og deres solvater for fremstilling av medikamenter som er nyttige ved behandling av spiseforstyrrelser.
Medikamentet beskrevet over er egnet for oral, sublingual, subkutan, intramuskulær, intravenøs, transdermal, lokal eller rektal administrering. Medikamentet kan administreres til dyr og mennesker i enhetsformer for administrering blandet med konvensjonelle farmasøytiske bærere. En passende enhetsform for administrering omfatter orale former så som tabletter, gelatinkapsler, pulvere, granuler og løsninger eller suspensjoner som skal tas oralt eller sublingvalt, og bukkale former for administrering, aerosol-preparater, implantater, subkutane, intramuskulære, intravenøse, intranasale eller intraokulære former for administrering og rektale former for administrering.
I medikamentet som beskrevet over er det aktive prinsipp normalt formulert i doseenheter. Doseenheten inneholder fra 0,5 til 1000 mg, med fordel fra 1 til 500 mg og fortrinnsvis fra 2 til 200 mg CBrreseptor-antagonist pr. doseenhet for daglig administrering.
Når et fast preparat er fremstilt fra medikamentet i form av tabletter, kan et fuktemiddel så som natriumlaurylsulfat tilsettes til det/de mikroniserte eller ikke-mikrontserte aktive prinsipp(er), og det hele blir blandet med en farmasøytisk konstituent så som silika, stivelse, laktose, magnesiumstearat, talkum eller lignende. Tabletten kan belegges med sukrose, en rekke polymerer eller andre passende substanser, eller ellers kan de behandles slik at de har en vedvarende eller forsinket aktivitet og slik at de frigjør en forutbestemt mengde av det aktive prinsipp kontinuerlig.
Et preparat i form av gelatinkapsler blir oppnådd ved blanding av det aktive prinsipp eller aktive prinsipper med et fortynningsmiddel, så som en glykol eller en glycerolester og innlemme den resulterende blanding i bløte eller harde gelatinkapsler.
Et preparat i form av en sirup eller eliksir kan inneholde det aktive prinsipp eller aktive prinsipper sammen med et søtningsstoff, som er fortrinnsvis kalorifritt, metylparaben og propylparaben som antiseptikum, et aromastoff og et passende farvestoff.
Vann-dispergerbare pulvere eller granuler kan inneholde det aktive prinsipp blandet med dispergeringsmidler eller fuktemidler eller med suspendeirngsmidler så som polyvinylpyrrolidon eller polyvidon, så vel som med søtningsstoffer eller smaksforbed rende midler.
Rektal administrering utføres ved anvendelse av suppositorier, som blir fremstilt med bindemidler som smelter ved den rektale temperatur, for eksempel kakaosmør eller polyetylenglykoler.
Parenteral administrering utføres ved anvendelse av vandige suspensjoner, isotoniske saltvannsoppløsninger eller injiserbare sterile løsninger inneholdende farmakologisk kompatible dispergeringsmidler og/eller solubiliseringsmidler, for eksempel propylenglykol eller butylenglykol.
For således å fremstille en vandig løsning for intravenøs injeksjon er det mulig å anvende et ko-oppløsningsmiddel, for eksempel alkohol så som etanol eller en glykol så som polyetylenglykol eller propylenglykol og en hydrofil surfaktant så som Tween<®> 80. For å fremstille en oljeaktig løsning for intramuskulær injeksjon kan det aktive prinsipp være solubilisert med et triglycerid eller en glycerolester.
Transdermal administrering kan utføres ved anvendelse av plastere i multilaminar form eller med et reservoar hvor det aktive prinsipp er i alkoholisk løsning.
Oet aktive prinsipp kan også formuleres som mikrokapsler eller mikrosfærer, eventuelt med én eller flere bærere eller additiver.
Det aktive prinsipp kan også presenteres i form av komplekser med et cyklodekstrin, for eksempel a-, (5- eller y-Cyklod ekst rin, 2-hydroksypropyl-p-Cyklodekstrin eller metyl-p-Cyklodekstrin.
Blant de forsinkede frigjøringsformer som er nyttige ved kroniske behandlinger, er det mulig å anvende implantater. Disse kan fremstilles i form av en oljeaktig suspensjon eller i form av en suspensjon av mikrosfærer i et isotonisk medium.
TEST nr. 1: Virkningen av SR 141716 A på inntaket av en sukroseløsnina i rotter
Forsøket utfører i henhold til W.C. Lynch et al., Physiol. Behav., 1993, 54, 877 - 880.
Sprague-Dawley-hannrotter som veier 190 til 210 g, er under en normal lyssyklus (fra klokken.07-17) og får vann og mat ad libitum. 16 dager, mellom kl. 11 og kl. 15 inndras maten og vannflaskene, og rottene fåren 5% sukroseløsning å drikke.Rotter som drikker mindre enn 3 g sukroseløsning elimineres.På den syvende dag utføres testen i henhold til følgende fremgangsmåte:
Klokken 09: inndragelse av maten,
Klokken 10: oral administrering av SR 141716 A,
Klokken 11= TO: innføring av flasker inneholdende en avveiet sukroseløsning, TO + 1 time, TO + 2 timer, TO + 3 timer, TO + 4 timer: måling av sukroseforbruket ved å veie flaskene.
Det kan ses av resultatene angitt i TABELL 1 at administreringen av
SR 141716 A reduserer betydelig konsumpsjonen av vandig sukkerløsning ved eller over en dose på 0,3 mg/kg.
TEST nr. 2: Virkningen av SR 141716 A på konsumpsjonen av en alkoholløsnino i mus
C 57 BL 6-hannmus (Iffa-Credo) blir isolert på ankomstdagen i et dyreavlukke under en reverssyklus (fra kl. 22-10) med 2 flasker fylt med vann. Etter 1 uke erstattes én av vannflaskene med en flaske fylt med en 10% alkoholløsning i 6 timer av testen. Hver dag, 30 minutter før flasken med alkohol innføres, behandles musen subkutant med SR 141716 A. Mengdene av alkohol og vann som fortæres, måles etter 6 timer. Testen gjentas i 4 dager.
Resultatene viser at alkoholkonsumpsjonen reduseres meget vesentlig for de behandlede dyr: fra 1,9 ± 0,1 g for et ubehandlet dyr til 1,0 ± 0,2 g for et dyr som fikk 3 mg/kg av SR 141716 A; vannkonsumpsjonen økte parallelt: fra 1,1 ± 0,1 til 1,6 ±0,3 g.
EKSEMPEL 1: Gelatinkapsel inneholdende en 1 mg dose av CBrreseptor-antagonist EKSEMPEL 2: Gelatin kapsel inneholdende en 10 mg dose av CBi-reseptor-antagonist
For en nr. 3 opak hvit gelatinkapsel fylt opp til 170 mg
EKSEMPEL 3: Gelatinkapsel inneholdende en 30 mg dose av CBrreseptor-antagonist
For en nr. 3 opak hvit gelatinkapsel fylt opp til 170 mg
EKSEMPEL 4: Tablett inneholdende en 30 mg dose av en CBrreseptor-antagonist EKSEMPEL 5: Tablett inneholdende 30 mg CB1-reseptor-antagonist og 200 mg p3-agonist
EKSEMPEL 6: Tablett inneholdende 10 mg CBrreseptor-antagonist og 100 mg pVagonist
Claims (4)
1. Anvendelse av CBi-reseptor-antagonisten N-piperidino-5-(4-klorfenyl)-1 - (2,4-diklorfenyl)-4-metylpyrazol-3-karboksamid, et av dets farmasøytisk godtagbare salter eller et av dens solvater for fremstilling av et medikament som er nyttig ved behandling av spiseforstyrrelser som kan henføres til appetittvekkende substanser så som sukkere, karbohydrater og alkohol.
2. Anvendelse ifølge krav 1, hvor de appetittvekkende substanser er sukkere og karbohydrater.
3. Anvendelse ifølge krav 2, hvor de appetittvekkende substanser er sukkere.
4. Anvendelse ifølge krav 1, hvor den appetittvekkende substanser er alkohol.
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| PCT/FR1998/000154 WO1998032441A1 (fr) | 1997-01-28 | 1998-01-28 | Utilisation des antagonistes des recepteurs aux cannabinoides centraux pour reguler l'appetance |
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| IL79323A (en) | 1985-07-10 | 1990-03-19 | Sanofi Sa | Phenylethanolaminotetralines,their preparation and pharmaceutical compositions containing them |
| IE65511B1 (en) * | 1989-12-29 | 1995-11-01 | Sanofi Sa | New phenylethanolaminomethyltetralins |
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| FR2692575B1 (fr) * | 1992-06-23 | 1995-06-30 | Sanofi Elf | Nouveaux derives du pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant. |
| EP0627407A1 (fr) * | 1993-05-28 | 1994-12-07 | MIDY S.p.A. | Acide (7S)-7-[(2R)-2(3-chlorophényl)-2-hydroxyéthylamino]-5,6,7,8-tétrahydronaphtalèn-2-yloxy acétique, ses sels pharmaceutiquement acceptables, à action agoniste bêta-3 adrénergique et compositions pharmaceutiques le contenant |
| US5578638A (en) * | 1993-11-05 | 1996-11-26 | American Cyanamid Company | Treatment of glaucoma and ocular hypertension with β3 -adrenergic agonists |
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