SI2632451T1 - Uporaba malononitrilamidov pri nevropatski bolečini - Google Patents

Uporaba malononitrilamidov pri nevropatski bolečini Download PDF

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Publication number
SI2632451T1
SI2632451T1 SI201131372T SI201131372T SI2632451T1 SI 2632451 T1 SI2632451 T1 SI 2632451T1 SI 201131372 T SI201131372 T SI 201131372T SI 201131372 T SI201131372 T SI 201131372T SI 2632451 T1 SI2632451 T1 SI 2632451T1
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Slovenia
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compound
neuropathic pain
syndrome
pain
use according
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SI201131372T
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English (en)
Inventor
Birgit Hasse
Guido Koopmans
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Algiax Pharmaceuticals Gmbh
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Publication of SI2632451T1 publication Critical patent/SI2632451T1/sl

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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]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (11)

  1. EP 2632451 BI Uporaba malononitrilamidov pri nevropatski bolečini Patentni zahtevki
    1. Spojina za uporabo pri zdravljenju nevropatske bolečine in/ali nevropatskega bolečinskega sindroma, kjer je spojina malononitrilamid in kjer ima spojina formulo: ali
    ali farmacevtsko sprejemljive soli, solvati, tavtomeri ali stereoizomeri le-te.
  2. 2. Spojina za uporabo po zahtevku 1, kjer je tavtomer spojine keto ali enolna oblika, zlasti keto oblika 2-ciano-3-okso-N-[4-(trifluorometil) fenil]-6-heptinamid.
  3. 3. Spojina za uporabo po katerem koli od zahtevkov 1-2, kjer je stereoizomer spojine R- ali S-enantiomer.
  4. 4. Spojina za uporabo po katerem koli od zahtevkov 1-3, kjer se spojina uporabi pri zdravljenju periferne in/ali pretežno periferne nevropatske bolečine ali centralne in/ali pretežno centralne nevropatske bolečine.
  5. 5. Spojina za uporabo po zahtevku 4, pri čemer je pretežno periferna nevropatska bolečina tipa, ki je izbran izmed naslednjih tipov nevropatske bolečine in/ali ima vzrok, kije izbran iz skupine naslednjih vzrokov: - sistemske bolezni, npr. diabetična nevropatija; - lezije, inducirane z zdravili, npr. nevropatija zaradi kemoterapije; - travmatski sindrom in utesnitveni sindrom; - lezije v živčnih koreninah in posteriomih ganglijih; - nevropatije po infekcijah s HIV; - nevralgija po herpesnih infekcijah; - avulzije živčnih korenin; - lezije kranialnih živcev; - kranialne nevralgije, npr. trigeminalna nevralgija; - nevropatska bolečina zaradi raka; - fantomska bolečina; - kompresija perifernih živcev, nevropleksusa in živčnih korenin; - paraneoplastična periferna nevropatija in ganglionopatija; - komplikacije pri terapijah raka, npr. kemoterapiji, obsevanju in kirurških intervencijah; - kompleksni regionalni bolečinski sindrom; - lezije tipa I (prej znane kot refleksna simpatična distrofija); in - lezije tipa II (približno odgovarjajoče kavzalgiji); ali pri čemer je pretežno centralna nevropatska bolečina tipa, ki ima vzrok, kije izbran iz naslednje skupine vzrokov: - cerebralne lezije, ki so pretežno talamične; - infarkt, npr. talamični infarkt ali infarkt možganskega debla; - cerebralni tumorji ali abscesi, ki komprimirajo talamus ali možgansko deblo; - multipla skleroza; - glavobolni sindrom, povzročen z mehanizmi centralne bolečine, kot pri migreni ali migrenski bolečini; - možganske operacije, npr. talamotomija v primerih motoričnih motenj; - lezije hrbtenjače; - poškodbe hrbtenjače; - operacije hrbtenjače, npr. anterolateralna kordotomija; - ishemične lezije; - sindrom sprednje spinalne arterije; - Wallenbergov sindrom; in - siringomielija.
  6. 6. Spojina za uporabo po katerem koli od zahtevkov 1-3, kjer je nevropatski bolečinski sindrom postherpetična nevralgija (povzročena s herpesom zostrom), avulzije korenin, boleča travmatska mononevropatija, boleča polinevropatija (zlasti zaradi diabetesa), centralni bolečinski sindromi (potencialno povzročeni z dejansko katero koli ležijo na katerem koli nivoju živčnega sistema), pokirurški bolečinski sindromi (npr. sindrom postmastektomije, sindrom posttorakotomije, fantomska bolečina), kompleksni regionalni bolečinski sindrom (refleksna simpatična distrofija in kavzalgija) in/ali migrena ali migrenska bolečina.
  7. 7. Spojina za uporabo po katerem koli od zahtevkov 1-3, kjer je nevropatska bolečina centralni bolečinski sindrom, povzročen s poškodbo hrbtenjače in/ali kontuzijo hrbtenjače.
  8. 8. Spojina za uporabo po katerem koli od zahtevkov 1-7, kjer je nevropatska bolečina
  9. 9. Spojina za uporabo po katerem koli od zahtevkov 1-8, kjer se da spojino v dnevnih odmerkih med 1 mg in 10 g na telo, prednostno med 5 mg in 5 g na telo in bolj prednostno med 10 mg in 2 g na telo, začenjajoč po poškodbi živčnega sistema.
  10. 10. Farmacevtski sestavek za uporabo pri zdravljenju nevropatske bolečine in/ali nevropatskih bolečinskih sindromov, obsegajoč spojino, kot je definirana v katerem koli od zahtevkov 1-3, v prosti obliki ali v obliki farmacevtsko sprejemljive soli skupaj s farmacevtsko sprejemljivimi razredčili ali nosilci, in pri čemer je nevropatska bolečina nevropatska bolečina in/ali nevropatski bolečinski sindrom, kot je definirano v katerem koli od zahtevkov 4-8.
  11. 11. Farmacevtski sestavek za uporabo po zahtevku 10, kjer ima spojina formulo:
    ali farmacevtsko sprejemljive soli, solvati, tavtomeri, stereoizomeri le-te.
SI201131372T 2010-10-29 2011-10-28 Uporaba malononitrilamidov pri nevropatski bolečini SI2632451T1 (sl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US40819510P 2010-10-29 2010-10-29
EP10014122 2010-10-29
EP11784418.3A EP2632451B1 (en) 2010-10-29 2011-10-28 Use of malononitrilamides in neuropathic pain
PCT/EP2011/005452 WO2012055567A2 (en) 2010-10-29 2011-10-28 Use of malononitrilamides in neuropathic pain

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EP (1) EP2632451B1 (sl)
JP (1) JP6257326B2 (sl)
CN (1) CN103179962B (sl)
CA (1) CA2814371C (sl)
DK (1) DK2632451T3 (sl)
ES (1) ES2655084T3 (sl)
HR (1) HRP20171848T1 (sl)
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PT (1) PT2632451T (sl)
RS (1) RS56713B1 (sl)
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WO (1) WO2012055567A2 (sl)

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PL2632451T3 (pl) 2018-04-30
WO2012055567A3 (en) 2012-07-05
RS56713B1 (sr) 2018-03-30
US20130217737A1 (en) 2013-08-22
CA2814371C (en) 2019-03-19
EP2632451A2 (en) 2013-09-04
CN103179962B (zh) 2017-03-22
WO2012055567A2 (en) 2012-05-03
US9468615B2 (en) 2016-10-18
CN103179962A (zh) 2013-06-26
LT2632451T (lt) 2018-02-12
JP2013545730A (ja) 2013-12-26
JP6257326B2 (ja) 2018-01-10
HUE034890T2 (hu) 2018-03-28
HRP20171848T1 (hr) 2018-02-09
PT2632451T (pt) 2017-12-14
ES2655084T3 (es) 2018-02-16
EP2632451B1 (en) 2017-10-18
US20140357722A1 (en) 2014-12-04
CA2814371A1 (en) 2012-05-03
DK2632451T3 (en) 2017-12-18
NO2632451T3 (sl) 2018-03-17

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