HRP20090446T1 - Kombinacijska terapija za liječenje dijabetesa i stanja povezanih s njim, te za liječenje stanja koja se poboljšavaju povećanjem nivoa glp-1 u krvi - Google Patents
Kombinacijska terapija za liječenje dijabetesa i stanja povezanih s njim, te za liječenje stanja koja se poboljšavaju povećanjem nivoa glp-1 u krvi Download PDFInfo
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- HRP20090446T1 HRP20090446T1 HR20090446T HRP20090446T HRP20090446T1 HR P20090446 T1 HRP20090446 T1 HR P20090446T1 HR 20090446 T HR20090446 T HR 20090446T HR P20090446 T HRP20090446 T HR P20090446T HR P20090446 T1 HRP20090446 T1 HR P20090446T1
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- 101100337060 Caenorhabditis elegans glp-1 gene Proteins 0.000 title 1
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Abstract
Pripravak koji sadrži GPR119 agonist i DPP-IV inhibitor, naznačen time, da navedeni DPP-IV inhibitor nije identičan s 1-[2-[(5-cijanopiridin-2-il)amino]etilamino]acetil-2-cijano-(S)-pirolidinom (NVP-DPP728). Patent sadrži još 50 patentnih zahtjeva.
Claims (51)
1. Pripravak koji sadrži GPR119 agonist i DPP-IV inhibitor, naznačen time, da navedeni DPP-IV inhibitor nije identičan s 1-[2-[(5-cijanopiridin-2-il)amino]etilamino]acetil-2-cijano-(S)-pirolidinom (NVP-DPP728).
2. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist je selektivni GPR119 agonist.
3. Pripravak u skladu sa zahtjevom 2, naznačen time, da GPR119 agonist ima barem 100-struku selektivnost prema GPR119 u odnosu na receptor kortikotropin-oslobađajući faktor-1 (CRF-1).
4. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist ima EC50 manji od 10 μM.
5. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist ima EC50 manji od 1 μM.
6. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist ima EC50 manji od 100 nM.
7. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist je mala molekula.
8. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist je oralno aktivan.
9. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist je agonist humanog GPR119.
10. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor ima barem 10-struku selektivnost prema humanom DPP-IV plazme u odnosu na jedan ili više od PPCE, DPP-II, DPP-8 i DPP-9.
11. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor ima barem 100-struku selektivnost prema humanom DPP-IV plazme u odnosu na jedan ili više od PPCE, DPP-II, DPP-8 i DPP-9.
12. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor ima barem 1000-struku selektivnost prema humanom DPP-IV plazme u odnosu na jedan ili više od PPCE, DPP-II, DPP-8 i DPP-9.
13. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor ima IC50 manji od 10 μM.
14. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor ima IC50 manji od 1 μM.
15. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor ima IC50 manji od 100 nM.
16. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor je oralno aktivan.
17. Pripravak u skladu sa zahtjevom 1, naznačen time, da DPP-IV inhibitor je inhibitor humanog DPP-IV.
18. Pripravak u skladu sa zahtjevom 1, naznačen time, da GPR119 agonist je agonist humanog GPR119, te DPP-IV inhibitor je inhibitor humanog DPP-IV.
19. Pripravak u skladu sa zahtjevom 1, naznačen time, da svaki od GPR119 agonista i DPP-IV inhibitora je izabran među spojevima prikazanim u Tabeli B.
20. Pripravak u skladu sa zahtjevom 1, naznačen time, da pripravak je farmaceutski pripravak koji sadrži GPR119 agonist i DPP-IV inhibitor skupa s barem jednom farmaceutski prihvatljivom podlogom.
21. Dozirni oblik pripravka u skladu sa zahtjevom 20, naznačen time, da GPR119 agonist i DPP-IV inhibitor su u količinama dovoljnim da snize nivo glukoze u krvi kod subjekta.
22. Dozirni oblik u skladu sa zahtjevom 21, naznačen time, da količina samog GPR119 agonista i količina samog DPP-IV inhibitora prisutnih u dozirnom obliku su terapeutski neučinkovite u snižavanju nivoa glukoze u krvi kod subjekta.
23. Dozirni oblik u skladu sa zahtjevom 21, naznačen time, da količina GPR119 agonista i količina DPP-IV inhibitora djeluju sinergistički u snižavanju navedenog nivoa glukoze u krvi.
24. Dozirni oblik pripravka u skladu sa zahtjevom 20, naznačen time, da GPR119 agonist i DPP-IV inhibitor su u količinama dovoljnim da povećaju nivo GLP-1 u krvi kod subjekta.
25. Dozirni oblik u skladu sa zahtjevom 24, naznačen time, da količina samog GPR119 agonista i količina samog DPP-IV inhibitora prisutnih u dozirnom obliku su terapeutski neučinkovite u povećanju nivoa GLP-1 u krvi kod subjekta.
26. Dozirni oblik u skladu sa zahtjevom 24, naznačen time, da količina GPR119 agonista i količina DPP-IV inhibitora djeluju sinergistički u povećanju navedenog nivoa GLP-1 u krvi.
27. Dozirni oblik u skladu s bilo kojim zahtjevom 21 do 26, naznačen time, da dozirni oblik je prisutan u spojenom pripravku za istovremenu, odjeljenu ili uzastopnu uporabu.
28. Dozirni oblik u skladu s bilo kojim zahtjevom 21 do 27, naznačen time, da subjekt je čovjek.
29. Postupak priprave farmaceutskog pripravka, naznačen time, da navedeni postupak obuhvaća miješanje GPR119 agonista i DPP-IV inhibitora skupa s barem jednom farmaceutski prihvatljivom podlogom, pri čemu navedeni DPP-IV inhibitor nije identičan s 1-[2-[(5-cijanopiridin-2-il)amino]etilamino]acetil-2-cijano-(S)-pirolidinom (NVP-DPP728).
30. Postupak u skladu sa zahtjevom 29, naznačen time, da navedeni postupak nadalje obuhvaća korak priprave dozirnog oblika farmaceutskog pripravka u skladu sa zahtjevom 25.
31. Postupak u skladu sa zahtjevom 30, naznačen time, da subjekt je čovjek.
32. Pripravak u skladu sa zahtjevom 1, naznačen time, da služi za uporabu u postupku liječenja ljudskog ili životinjskog tijela terapijom.
33. Pripravak u skladu sa zahtjevom 32, naznačen time, da GPR119 agonist i DPP-IV inhibitor su u količinama dovoljnim da snize nivo glukoze u krvi kod subjekta.
34. Pripravak u skladu sa zahtjevom 32, naznačen time, da GPR119 agonist i DPP-IV inhibitor su u količinama dovoljnim da povećaju nivo GLP-1 u krvi kod subjekta.
35. Pripravak u skladu sa zahtjevom 1, naznačen time, da služi za liječenje ili prevenciju dijabetesa ili stanja povezanih s njim, a obuhvaća primjenu subjektu kojemu je to potrebno terapeutski učinkovite količine navedenog pripravka.
36. Pripravak u skladu sa zahtjevom 35, naznačen time, da služi za liječenje ili prevenciju dijabetesa tipa 2.
37. Pripravak u skladu sa zahtjevom 35, naznačen time, da služi za liječenje ili prevenciju stanja povezanih s dijabetesom izabranih iz skupine koju čine hiperglikemija, smanjena tolerancija glukoze, inzulinska rezistencija, insuficijencija beta-stanica pankreasa, insuficijencija enteroendokrinih stanica, glikozurija, matabolička acidoza, katarakte, dijabetička nefropatija, dijabetička neuropatija, dijabetička retinopatija, dijabetičko oboljenje srčanih arterija, dijabetička cerebrovaskularna bolest, dijabetička periferna vaskularna bolest, metabolički sindrom, hiperlipidemija, ateroskleroza, udar, hipertenzija i debljina.
38. Pripravak u skladu s bilo kojim zahtjevom 35 do 37, naznačen time, da pripravak je dozirni oblik pripravka u skladu s bilo kojim zahtjevom 21 do 28.
39. Pripravak u skladu sa zahtjevom 1, naznačen time, da služi za liječenje ili prevenciju stanja koja se poboljšavaju povećanjem nivoa GLP-1 u krvi, a obuhvaća primjenu subjektu kojemu je to potrebno terapeutski učinkovite količine navedenog pripravka, pri čemu je stanje koje se može poboljšati povećanjem nivoa GLP-1 u krvi izabrano iz skupine koju čine dijabetes, stanje povezano s dijabetesom, srčani infarkt, smanjeno pamćenje, smanjeno učenje i neurodegenerativni poremećaj; ili
pri čemu je stanje koje se može poboljšati povećanjem nivoa GLP-1 u krvi je neurodegenerativni poremećaj izabran iz skupine koju čine ekscitoksično oštećenje mozga uzrokovano jakim epileptičkim događajima, Alzheimer-ova bolest, Parkinson-ova bolest, Huntington-ova bolest, bolest povezana s prionom, udar, motoričko-neuronska bolest, smanjeno učenje ili pamćenje, traumatsko oštećenje mozga, oštećenje leđne moždine i periferna neuropatija.
40. Pripravak u skladu sa zahtjevom 39, naznačen time, da pripravak je dozirni oblik pripravka u skladu s bilo kojim zahtjevom 24 do 28.
41. Pripravak u skladu sa zahtjevom 1, naznačen time, da služi za povećanje nivoa GLP-1 u krvi, a obuhvaća primjenu subjektu koji je deficitaran u GLP-1 terapeutski učinkovite količine navedenog pripravka.
42. Pripravak u skladu sa zahtjevom 41, naznačen time, da pripravak je dozirni oblik pripravka u skladu s bilo kojim zahtjevom 24 do 28.
43. Pripravak u skladu s bilo kojim zahtjevom 33 do 42, naznačen time, da subjekt je čovjek.
44. Uporaba pripravka u skladu sa zahtjevom 1, naznačena time, da se koristi za izradu lijeka za liječenje ili prevenciju dijabetesa ili stanja povezanih s njim.
45. Uporaba u skladu sa zahtjevom 44, naznačena time, da se navedeni lijek koristi za liječenje ili prevenciju dijabetesa tipa 2.
46. Uporaba u skladu sa zahtjevom 44, naznačena time, da se navedeni lijek koristi za stanja povezana s dijabetesom izabrana iz skupine koju čine hiperglikemija, smanjena tolerancija glukoze, inzulinska rezistencija, insuficijencija beta-stanica pankreasa, insuficijencija enteroendokrinih stanica, glikozurija, matabolička acidoza, katarakte, dijabetička nefropatija, dijabetička neuropatija, dijabetička retinopatija, dijabetičko oboljenje srčanih arterija, dijabetička cerebrovaskularna bolest, dijabetička periferna vaskularna bolest, metabolički sindrom, hiperlipidemija, ateroskleroza, udar, hipertenzija i debljina.
47. Uporaba u skladu s bilo kojim zahtjevom 44 do 46, naznačena time, da se koristi pripravak koji je dozirni oblik pripravka u skladu s bilo kojim zahtjevom 21 do 28.
48. Uporaba pripravka u skladu sa zahtjevom 1, naznačena time, da se koristi za izradu lijeka za liječenje ili prevenciju stanja koja se poboljšavaju povećanjem nivoa GLP-1 u krvi, pri čemu je stanje koje se može poboljšati povećanjem nivoa GLP-1 u krvi izabrano iz skupine koju čine dijabetes, stanje povezano s dijabetesom, srčani infarkt, smanjeno pamćenje, smanjeno učenje i neurodegenerativni poremećaj; ili
pri čemu je stanje koje se može poboljšati povećanjem nivoa GLP-1 u krvi je neurodegenerativni poremećaj izabran iz skupine koju čine ekscitoksično oštećenje mozga uzrokovano jakim epileptičkim događajima, Alzheimer-ova bolest, Parkinson-ova bolest, Huntington-ova bolest, bolest povezana s prionom, udar, motoričko-neuronska bolest, smanjeno učenje ili pamćenje, traumatsko oštećenje mozga, oštećenje leđne moždine i periferna neuropatija.
49. Uporaba u skladu sa zahtjevom 48, naznačena time, da se koristi pripravak koji je dozirni oblik pripravka u skladu s bilo kojim zahtjevom 24 do 28.
50. Uporaba pripravka u skladu sa zahtjevom 1, naznačena time, da se koristi za izradu lijeka za liječenje ili prevenciju nedostatka GLP-1.
51. Uporaba u skladu sa zahtjevom 50, naznačena time, da se koristi pripravak koji je dozirni oblik pripravka u skladu s bilo kojim zahtjevom 24 do 28.
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