HRP20130935T1 - Bicikliäśki derivat aminokiseline - Google Patents

Bicikliäśki derivat aminokiseline Download PDF

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HRP20130935T1
HRP20130935T1 HRP20130935AT HRP20130935T HRP20130935T1 HR P20130935 T1 HRP20130935 T1 HR P20130935T1 HR P20130935A T HRP20130935A T HR P20130935AT HR P20130935 T HRP20130935 T HR P20130935T HR P20130935 T1 HRP20130935 T1 HR P20130935T1
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pain
hept
aminomethyl
acceptable salt
acetic acid
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HRP20130935AT
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Kousei Shimada
Asuka Kawamura
Naohisa Arakawa
Yuki Domon
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Daiichi Sankyo Company, Limited
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/613Unsaturated compounds containing a keto groups being part of a ring polycyclic
    • C07C49/617Unsaturated compounds containing a keto groups being part of a ring polycyclic a keto group being part of a condensed ring system
    • C07C49/623Unsaturated compounds containing a keto groups being part of a ring polycyclic a keto group being part of a condensed ring system having two rings
    • C07C49/627Unsaturated compounds containing a keto groups being part of a ring polycyclic a keto group being part of a condensed ring system having two rings the condensed ring system containing seven carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/02Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/32Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/221Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having an amino group, e.g. acetylcholine, acetylcarnitine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • A61P21/02Muscle relaxants, e.g. for tetanus or cramps
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/57Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C323/58Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
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    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
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    • C07C2602/20All rings being cycloaliphatic the ring system containing seven carbon atoms
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
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    • C07C2603/94Spiro compounds containing "free" spiro atoms

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  • Organic Chemistry (AREA)
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Oncology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Rheumatology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Indole Compounds (AREA)

Claims (16)

1. Spoj predstavljen općom formulom (I) ili njegova farmakološki prihvatljiva sol: [image] gdje R1, R2, R2’, R4, R5, R6, R7, R8, i R8’ su svaki nezavisno atom vodika; i R3 je atom vodika, metilna skupina, etilna skupina, propilna skupina, ili butilna skupina.
2. Spoj prema zahtjevu 1 ili njegova farmakološki prihvatljiva sol, gdje R3 je atom vodika ili etilna skupina.
3. Farmakološki prihvatljiva sol spoja prema zahtjevu 1 ili zahtjevu 2, gdje je farmakološki prihvatljiva sol klorovodik, benzensulfonat ili p-toluensulfonat.
4. Spoj prema zahtjevu 1 ili njegova farmakološki prihvatljiva sol, predstavljen općom formulom (Ia) ili njegova farmakološki prihvatljiva sol: [image] gdje R1, R2, R2’, R3, R4, R5, R6, R7, R8, i R8’ su kako je definirano u zahtjevu 1.
5. Spoj prema zahtjevu 1 ili njegova farmakološki prihvatljiva sol, predstavljen općom formulom (Ib) ili njegova farmakološki prihvatljiva sol: [image] gdje R1, R2, R2’, R3, R4, R5, R6, R7, R8, i R8’ su kako je definirano u zahtjevu 1.
6. Spoj prema zahtjevu 1 ili njegova farmakološki prihvatljiva sol, izabrani iz grupe koja obuhvaća sljedeće: (6)-[(1S,5R,6R)-6-(aminometil)biciklo(3.2.0)hept-3-en-6-il]octena kiselina; (6)-[(1S,5R,6R)-6-aminometil-3-metilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina; (6)-[(1S,5R,6R)-6-aminometil-3-etilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina; (6)-[(1S,5R,6R)-6-aminometil-3-propilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina; (6)-[(1S,5R,6R)-6-aminometil-3-butilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina; [(1R,5S,6S)-6-(aminometil)biciklo[3.2.0]hept-3-en-6-il]octena kiselina; [(1S,5R,6R)-6-(aminometil)biciklo[3.2.0]hept-3-en-6-il]octena kiselina; [(1S,5R,6R)-6-(aminometil)biciklo[3.2.0]hept-3-en-6-il]octena kiselina klorovodik; [(1S,5R,6R)-6-(aminometil)biciklo[3.2.0]hept-3-en-6-il]octena kiselina benzensulfonat; [(1R,5S,6S)-6-aminometil-3-etilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina; [(1R,5S,6S)-6-aminometil-3-etilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina p-toluensulfonat; [(1R,5S,6S)-6-(aminometil)-3-etilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina benzensulfonat; i [(1S,5R,6R)-6-aminometil-3-etilbiciklo[3.2.0]hept-3-en-6-il]octena kiselina.
7. Farmaceutski pripravak koji kao djelatnu tvar sadrži spoj ili njegovu farmakološki prihvatljivu sol prema bilo kojem od zahtjeva 1 do 6.
8. Farmaceutski pripravak prema zahtjevu 7, za uporabu u liječenju i/ili prevenciji boli.
9. Farmaceutski pripravak prema zahtjevu 7, za uporabu u liječenju i/ili prevenciji bolesti izabrane iz grupe koja obuhvaća akutnu bol, kroničnu bol, bol uzrokovanu ozljedom mekog tkiva ili perifernom ozljedom, neuralgiju nakon herpesa, okcipitalnu neuralgiju, trigeminalnu neuralgiju, mijelomernu ili interkostanu neuralgiju, centralnu bol, neuropatsku bol, migrenu, bol povezanu s osteoartritisom ili artikularnom reumom, bol povezanu s udarcem, uganućem, ili traumom, spondilalgiju, bol uzrokovanu ozljedom leđne moždine ili moždanog debla, bol u donjem dijelu leđa, išijas, zubobolju, sindrom miofascijalne boli, bol od epiziotomije, bol od gihta, bol uzrokovanu opeklinom, srčanu bol, mišićnu bol, bol u očima, upalnu bol, orofacijalnu bol, abdominalnu bol, bol povezanu s dismenorejom, porođajnu bol, ili endometriozu, bol tijela, bol povezanu s ozljedom živaca ili radijalnom ozljedom, bol povezanu s amputacijom, tic douloureux, neurom, ili angiitis, bol uzrokovanu dijabetičkom neuropatijom (ili dijabetička periferna neuropatska bol), bol uzrokovanu kemoterapijom-induciranom neuropatijom, atipičnu facijalnu neuralgiju, neuropatsku bol u donjem dijelu leđa, neuralgiju povezanu s HIV-om, neuralgiju povezanu s AIDS-om, hiperalgeziju, goruću bol, iznenadnu bol, bol uzrokovanu kemoterapijom, okcipitalnu neuralgiju, psihogenu bol, bol povezanu sa žučnim kamencima, neuropatsku ili ne-neuropatsku bol povezanu s rakom, fantomsku bol udova, funkcionalnu abdominalnu bol, glavobolju, akutnu ili kroničnu tenzijsku glavobolju, sinusnu glavobolju, klaster glavobolju, temporomandibularnu bol zglobova, bol od maksilarnih sinusa, bol uzrokovanu ankilozantnim spondiloartritisom, postoperativnu bol, bol ožiljka, kroničnu ne-neuropatsku bol, fibromijalgiju, amiotropnu lateralnu sklerozu, epilepsiju (parcijalnu epilepsiju, adultni parcijalni napad, i parcijalni napad u bolesnika s epilepsijom), generalizirani anksiozni poremećaj i sindrom nemirnih nogu.
10. Farmaceutski pripravak prema zahtjevu 7, za uporabu u liječenju i/ili prevenciji boli koja je uzrokovana dijabetičkom neuropatijom.
11. Uporaba spoja ili njegove farmakološki prihvatljive soli prema bilo kojem od zahtjeva 1 do 6 za proizvodnju farmaceutskog pripravka za liječenje i/ili prevenciju boli.
12. Uporaba prema zahtjevu 11, gdje farmaceutski pripravak je pripravak za liječenje i/ili prevenciju boli koja je uzrokovana dijabetičkom neuropatijom.
13. Farmaceutski pripravak prema zahtjevu 7, za uporabu u liječenju i/ili prevenciji neuralgije nakon herpesa.
14. Uporaba spoja ili njegove farmakološki prihvatljive soli prema bilo kojem od zahtjeva 1 do 6 za proizvodnju farmaceutskog pripravka za liječenje i/ili prevenciju neuralgije nakon herpesa.
15. Farmaceutski pripravak prema zahtjevu 7, za uporabu u liječenju i/ili prevenciji fibromialgije.
16. Uporaba spoja ili njegove farmakološki prihvatljive soli prema bilo kojem od zahtjeva 1 do 6 za proizvodnju farmaceutskog pripravka za liječenje i/ili prevenciju fibromialgije.
HRP20130935AT 2007-09-28 2013-10-07 Bicikliäśki derivat aminokiseline HRP20130935T1 (hr)

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JP2007255430 2007-09-28
PCT/JP2008/067223 WO2009041453A1 (ja) 2007-09-28 2008-09-25 二環性γ-アミノ酸誘導体

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US (1) US7947738B2 (hr)
EP (2) EP2657219B1 (hr)
JP (1) JP4479974B2 (hr)
KR (2) KR101409079B1 (hr)
CN (2) CN101878193B (hr)
AU (1) AU2008304933B2 (hr)
BR (2) BR122013020635A2 (hr)
CA (1) CA2701110C (hr)
CO (1) CO6270314A2 (hr)
CY (1) CY1114836T1 (hr)
DK (1) DK2192109T3 (hr)
ES (2) ES2433890T3 (hr)
HK (2) HK1139381A1 (hr)
HR (1) HRP20130935T1 (hr)
IL (1) IL204621A (hr)
MX (1) MX2010003394A (hr)
MY (2) MY172034A (hr)
NZ (1) NZ584699A (hr)
PH (1) PH12013501663B1 (hr)
PL (1) PL2192109T3 (hr)
PT (1) PT2192109E (hr)
RU (1) RU2446148C2 (hr)
SI (1) SI2192109T1 (hr)
TW (2) TWI526425B (hr)
WO (1) WO2009041453A1 (hr)
ZA (1) ZA201002013B (hr)

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