SI1919465T1 - Gsk-3 inhibitorji - Google Patents

Gsk-3 inhibitorji Download PDF

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SI1919465T1
SI1919465T1 SI200632241T SI200632241T SI1919465T1 SI 1919465 T1 SI1919465 T1 SI 1919465T1 SI 200632241 T SI200632241 T SI 200632241T SI 200632241 T SI200632241 T SI 200632241T SI 1919465 T1 SI1919465 T1 SI 1919465T1
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disease
substituted
unsubstituted
compound
dementia
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Gil Ana Martinez
Padilla Miguel Medina
Cascon Mercedes Alonso
Huerta Ana Fuertes
Rico Maria Luisa Navarro
Puerto Maria Jose Perez
Morera Ana Castro
Aparicio Ester Martin
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Asd Therapeutics Partners Llc
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    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
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    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated

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Claims (15)

  1. GSK-3 INHIBITORJI Patentni zahtevki
    1. Uporaba spojine s formulo (I)
    ali farmacevtsko sprejemljive soli ali topljenca le-tega, pri čemer: Rb skupina je izbrana med
    R3, R,, R’2, R*3, R’4, R’5 in R’6 so neodvisno izbrani med vodikom, substituiranim ali nesubstituiranim alkilom, substimiranim ali nesubstituiranim cikloalkilom, substituiranim ali nesubstituiranim alkenilom, substituiranim ali nesubstituiranim arilom, substituiranim ali nesubstituiranim heterociklom, -C(=0)R7, -C(=0)0Re, -C(=0)NR9Rio, -C=NRn, -CN, -OR12, -0C(=0)Ri3, -S(0),-Ri4, -NR15R16, -NRi7C(=0)Ri8, -NO2, -N=CRi9R20 ali halogenom, pri čemer lahko R3 in R4 skupaj tvorita =0 skupino, in pri čemer lahko kateri koli par iz R3R’2, RsR^, I^R^, R4R’6, R^R^, R^R^, R’4R’s, R’sR’6, RisRi6> R17R18 ali R19R20 skupaj tvori ciklični substituent; t je 0,1, 2, 3 R.7, Re, R9, RlOi Ril, R13, Rl4, R15, R16, R17, Ris» R19 in R20 so neodvisno izbrani med vodikom, substituiranim ali nesubstituiranim alkilom, substituiranim ali nesubstituiranim cikloalkilom, substituiranim ali nesubstituiranim alkenilom, substituiranim ali nesubstituiranim arilom, substituiranim ali nesubstituiranim heterociklom, substituiranim ali nesubstituiranim alkoksijem, substituiranim ali nesubstituiranim ariloksijem, halogenom, R12 je izbran med vodikom, nesubstituiranim alkilom, substituiranim ali nesubstituiranim cikloalkilom, substituiranim ali nesubstituiranim alkenilom, substituiranim ali nesubstituiranim arilom, substituiranim ali nesubstituiranim heterociklom, halogenom, pri izdelavi zdravila za zdravljenje in/ali preprečevanje GSK-3 posredovane bolezni ali stanja, pri čemer je bolezen ali stanje izbrano iz skupine z diabetesom, stanji, povezanimi z diabetesom, kroničnimi nevrodegenerativnimi stanji, ki vključujejo demence, kot so alzheimerjeva bolezen, parkinsonova bolezen, progresivna supranukleama paraliza, subakutni sklerozirajoči pancefalitni parkinsonizem, postencefalitični parkinsonizem, pugilistični encefalitis, kompleks Guam parkinsonizma - demence, pickova bolezen, kortikobazalna degeneracija, frontotemporalna demenca, huntingtonova bolezen, z aidsem povezana demenca, amiotrofična laterlana skleroza, multipla skleroza in nevrotravmatične bolezni, kot so akutna možganska kap, epilepsija, motnje razpoloženja, kot so depresija, shizofrenija in bipolarne motnje, spodbujanje funkcionalnega obnavljanja po kapi, cerebralna krvavitev zaradi samotne cerebralne amiloidne angiopatije, izpadanje las, debelost, hipertenzija, sindrom policističnih jajčnikov, sindrom X, ishemija, možganska poškodba, travmatična možganska poškodba, rak, levkopenija, downov sindrom, bolezen z Lewyjevimi telesci, vnetje, kronične vneme bolezni, rak in hiperproliferativne bolezni, kot je hiperplazija, in imunska pomanjkljivost.
  2. 2. Uporaba po zahtevku 1, pri čemer sta R3 in R4 H.
  3. 3. Uporaba po zahtevku 1, pri čemer so R’2, R’3, RJ4, R’s in R*6 neodvisno izbrani med vodikom, substituiranim ali nesubstituiranim alkilom, -C(=0)R7, -C(=0)0R8, -OR12, -NR15R16 ali halogenom, pri čemer so R?, Re, R12, Ris in Rie, kot so definirani v zahtevku 1.
  4. 4. Uporaba po zahtevku 1, pri čemer so R’2, R’3, R’4, R’s in R’e H.
  5. 5. Uporaba po zahtevku 1, pri čemer je spojina s formulo (I) izbrana med:
  6. 6. Uporaba po zahtevku 1, pri čemer je bolezen alzheimerjeva bolezen.
  7. 7. Uporaba po zahtevku 1, pri čemer je bolezen diabetes tipa II.
  8. 8. Uporaba po zahtevku 1, pri čemer je bolezen depresija.
  9. 9. Uporaba po zahtevku 1, pri čemer je bolezen možganska poškodba.
  10. 10. Spojina s formulo
  11. 11. Spojina s formulo za uporabo kot zdravilo.
  12. 12. Farmacevtska sestava, ki obsega spojino, kot je definirana po katerem koli od zahtevkov 10 ali 11, in farmacevtsko sprejemljiv nosilec, adjuvant ali pripomoček.
  13. 13. Farmacevtska sestava po zahtevku 12 za oralno dajanje.
  14. 14. Uporaba spojine s formulo (I), kot je definirana po katerem koli od zahtevkov 1 do 5, kot reaktivne snovi za zaviranje GSK-3 pri bioloških preiskavah.
  15. 15. Spojina s formulo (I), kot je definirana v zahtevkih 1 do 5, ali farmacevtska sestava le-te za uporabo pri zdravljenju ali preprečevanju GSK-3 posredovane bolezni ali stanja, pri čemer je bolezen ali stanje izbrano iz skupine z diabetesom, stanji, povezanimi z diabetesom, kroničnimi nevrodegenerativnimi stanji, ki vključujejo demence, kot so alzheimerjeva bolezen, parkinsonova bolezen, progresivna supranukleama paraliza, subakutni sklerozirajoči pancefalitni parkinsonizem, postencefalitični parkinsonizem, pugilistični encefalitis, kompleks Guam parkinsonizma - demence, pickova bolezen, kortikobazalna degeneracija, frontotemporalna demenca, huntingtonova bolezen, z aidsem povezana demenca, amiotrofična laterlana skleroza, multipla skleroza in nevrotravmatične bolezni, kot so akutna možganska kap, epilepsija, motnje razpoloženja, kot so depresija, shizofrenija in bipolarne motnje, spodbujanje funkcionalnega obnavljanja po kapi, cerebralna krvavitev zaradi samotne cerebralne amiloidne angiopatije, izpadanje las, debelost, hipertenzija, sindrom policističnih jajčnikov, sindrom X, ishemija, možganska poškodba, travmatična možganska poškodba, rak, levkopenija, downov sindrom, bolezen z Lewyjevimi telesci, vnetje, kronične vneme bolezni, rak in hiperproliferativne bolezni, kot je hiperplazija, in imunska pomanjkljivost.
SI200632241T 2005-07-29 2006-07-28 Gsk-3 inhibitorji SI1919465T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP05380176A EP1749523A1 (en) 2005-07-29 2005-07-29 GSK-3 inhibitors
EP06776492.8A EP1919465B1 (en) 2005-07-29 2006-07-28 Gsk-3 inhibitors
PCT/EP2006/007520 WO2007017145A2 (en) 2005-07-29 2006-07-28 Gsk-3 inhibitors

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JP (1) JP5484726B2 (sl)
KR (1) KR101471999B1 (sl)
CN (1) CN101257900B (sl)
AU (1) AU2006278829B2 (sl)
BR (1) BRPI0615968B1 (sl)
CA (1) CA2616451C (sl)
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HR (1) HRP20180109T1 (sl)
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LT (1) LT1919465T (sl)
NO (1) NO341454B1 (sl)
NZ (1) NZ566380A (sl)
PL (1) PL1919465T3 (sl)
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RU2010136954A (ru) * 2008-02-06 2012-03-20 Носсира С.А. (Es) Фенилпрениловые производные морского и синтетического происхождения для лечения нарушения познавательной способности, нейродегенеративных или нервных заболеваний или нарушений
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