DK2632451T3 - Anvendelse af malonnitrilamider ved neuropatisk smerte - Google Patents

Anvendelse af malonnitrilamider ved neuropatisk smerte Download PDF

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Publication number
DK2632451T3
DK2632451T3 DK11784418.3T DK11784418T DK2632451T3 DK 2632451 T3 DK2632451 T3 DK 2632451T3 DK 11784418 T DK11784418 T DK 11784418T DK 2632451 T3 DK2632451 T3 DK 2632451T3
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DK
Denmark
Prior art keywords
neuropathic pain
compound
pain
syndrome
lesions
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Application number
DK11784418.3T
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English (en)
Inventor
Birgit Hasse
Guido Koopmans
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Algiax Pharmaceuticals Gmbh
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Publication of DK2632451T3 publication Critical patent/DK2632451T3/da

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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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/164—Amides, e.g. hydroxamic acids of a carboxylic acid with an aminoalcohol, e.g. ceramides
    • 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
    • A61K31/275—Nitriles; Isonitriles
    • 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
    • A61K31/42—Oxazoles
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Claims (11)

1. Forbindelse til anvendelse i behandling af neuropatisk smerte og/eller neuropatisk smertesyndrom, hvor forbindelsen er et malonnitrilamid, og hvor forbindelsen har formlen
eller
eller farmaceutisk acceptable salte, solvater, tautomerer eller stereoisomerer deraf.
2. Forbindelse til anvendelse ifølge krav 1, hvor forbindelsens tautomer er keto- eller enol-formen, navnlig keto-formen 2-cyan-3-oxo-N-[4-(trifluormethyl)phenyl]-6-heptynamid.
3. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 2, hvor forbindelsens stereoisomer er R- eller S-enantiomeren.
4. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 3, hvor forbindelsen anvendes i behandlingen af perifer og/eller overvejende perifer neuropatisk smerte eller central og/eller overvejende central neuropatisk smerte.
5. Forbindelse til anvendelse ifølge krav 4, hvorved den overvejende perifere neuropatiske smerte er af en type, der er udvalgt ffa følgende typer af neuropatisk smerte og/eller har en årsag, der er udvalgt fra gruppen af følgende årsager: - systemiske sygdomme, f.eks. diabetisk neuropati; - lægemiddelinducerede læsioner, f.eks. neuropati på grund af kemoterapi; - traumatisk syndrom og afklemningssyndrom; - læsioner i nerverødder og posteriore ganglier; - neuropatier efter hiv-infektioner; - neuralgi efter herpes-infektioner; - nerverodsavulsioner; - kranielle nervelæsioner; - kranieile neuralgier, f.eks. trigeminusneuralgi; - neuropatisk cancersmerte; - fantomsmerte; - kompression af perifere nerver, neuroplexus og nerverødder; - paraneoplastisk perifer neuropati og ganglionopati; - komplikationer ved cancerterapier, f.eks. kemoterapi, stråling og kirurgiske indgreb; - komplekst regionalt smertesyndrom; - type I-læsioner (tidligere kendt som sympatisk refleksdystrofi) og - type Il-læsioner (der omtrent svarer til kausalgi); eller hvorved den overvejende centrale neuropatiske smerte er af en type, der har en årsag, der er udvalgt fra følgende gruppe af årsager: - cerebrale læsioner, der er overvejende thalamiske; - infarkt, f.eks. thalamusinfarkt eller hjemestammeinfarkt; - cerebrale tumorer eller abscesser, der komprimerer thalamus eller hjernestammen; - multipel sklerose; - hovedsmertesyndrom forårsaget af centrale smertemekanismer som ved migræne eller migrænesmerte. - hjerneoperationer, f.eks. thalamotomi i tilfælde af motoriske forstyrrelser; - rygmarvslæsioner; - rygmarvsskader; - rygmarvsoperationer, f.eks. anterolateral kordotomi; - iskæmiske læsioner; - anterior spinalarteriesyndrom; - Wallenbergs syndrom og - syringomyeli.
6. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 3, hvor det neuropatiske smertesyndrom er postherpetisk neuralgi (forårsaget af herpes zoster), rodavulsioner, smertefuld traumatisk mononeuropati, smertefuld polyneuropati (navnlig på grund af diabetes), centrale smertesyndromer (eventuelt forårsaget af praktisk talt en hvilken som helst læsion på et hvilket som helst niveau af nervesystemet), postkirurgiske smertesyndromer (f.eks. postmastektomisyndrom, posttorakotomisyndrom, fantomsmerte), komplekst regionalt smertesyndrom (sympatisk refleksdystrofi og kausalgi) og/eller migræne eller migrænesmerte.
7. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 3, hvor den neuropatiske smerte er et centralt smertesyndrom forårsaget af rygmarvsskade og/eller rygmarvskontusion.
8. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 7, hvor den neuropatiske smerte er en kronisk neuropatisk smerte.
9. Forbindelse til anvendelse ifølge et hvilket som helst af kravene 1 til 8, hvor forbindelsen indgives i daglige doser mellem 1 mg-10 g/krop, fortrinsvis 5 mg-5 g/krop og mere fortrinsvis 10 mg-2 g/krop med start efter en skade på nervesystemet.
10. Farmaceutisk sammensætning til anvendelse i behandlingen af neuropatisk smerte og/eller neuropatiske smertesyndromer, der omfatter en forbindelse som defineret i et hvilket som helst af kravene 1 til 3 i fri form eller i form af et farmaceutisk acceptabelt salt, sammen med farmaceutisk acceptable fortyndere eller bærere, og hvor den neuropatiske smerte er en neuropatisk smerte og/eller et neuropatisk smertesyndrom som defineret i et hvilket som helst af kravene 4 til 8.
11. Farmaceutisk sammensætning til anvendelse ifølge krav 10, hvor forbindelsen har formlen
eller farmaceutisk acceptable salte, solvater, tautomerer, stereoisomerer deraf.
DK11784418.3T 2010-10-29 2011-10-28 Anvendelse af malonnitrilamider ved neuropatisk smerte DK2632451T3 (da)

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US40819510P 2010-10-29 2010-10-29
EP10014122 2010-10-29
PCT/EP2011/005452 WO2012055567A2 (en) 2010-10-29 2011-10-28 Use of malononitrilamides in neuropathic pain

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EP (1) EP2632451B1 (da)
JP (1) JP6257326B2 (da)
CN (1) CN103179962B (da)
CA (1) CA2814371C (da)
DK (1) DK2632451T3 (da)
ES (1) ES2655084T3 (da)
HR (1) HRP20171848T1 (da)
HU (1) HUE034890T2 (da)
LT (1) LT2632451T (da)
NO (1) NO2632451T3 (da)
PL (1) PL2632451T3 (da)
PT (1) PT2632451T (da)
RS (1) RS56713B1 (da)
SI (1) SI2632451T1 (da)
WO (1) WO2012055567A2 (da)

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Publication number Publication date
CA2814371A1 (en) 2012-05-03
NO2632451T3 (da) 2018-03-17
EP2632451A2 (en) 2013-09-04
CN103179962A (zh) 2013-06-26
HUE034890T2 (hu) 2018-03-28
RS56713B1 (sr) 2018-03-30
HRP20171848T1 (hr) 2018-02-09
JP2013545730A (ja) 2013-12-26
US9468615B2 (en) 2016-10-18
JP6257326B2 (ja) 2018-01-10
CA2814371C (en) 2019-03-19
CN103179962B (zh) 2017-03-22
US20140357722A1 (en) 2014-12-04
PT2632451T (pt) 2017-12-14
LT2632451T (lt) 2018-02-12
SI2632451T1 (en) 2018-02-28
WO2012055567A2 (en) 2012-05-03
US20130217737A1 (en) 2013-08-22
ES2655084T3 (es) 2018-02-16
PL2632451T3 (pl) 2018-04-30
EP2632451B1 (en) 2017-10-18
WO2012055567A3 (en) 2012-07-05

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