HRP20181052T1 - Derivati 1,2,4-oksadiazola kao imunomodulatori - Google Patents

Derivati 1,2,4-oksadiazola kao imunomodulatori Download PDF

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HRP20181052T1
HRP20181052T1 HRP20181052TT HRP20181052T HRP20181052T1 HR P20181052 T1 HRP20181052 T1 HR P20181052T1 HR P20181052T T HRP20181052T T HR P20181052TT HR P20181052 T HRP20181052 T HR P20181052T HR P20181052 T1 HRP20181052 T1 HR P20181052T1
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compound according
pharmaceutically acceptable
acceptable salt
following structure
amino acid
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HRP20181052TT
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Pottayil Govindan Nair Sasikumar
Muralidhara Ramachandra
Seetharamaiah Setty Sudarshan Naremaddepalli
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Aurigene Discovery Technologies Limited
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Claims (48)

1. Spoj formule (I) , naznačen time što: Q je S ili O; R1 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Ser i Thr, koji može biti supstituiran s alkilom ili acilom; R2 je vodik ili -CO-Aaa; Aaa je aminokiselinski ostatak, kojeg se bira između Thr i Ser; gdje je njegov C-kraj slobodni kraj, amidiran ili esterificiran; R3 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Asn, Asp, Gln, te Glu; ----- je izborna veza; R4 i R5 su neovisno vodici ili su odsutni; R6 je vodik, alkil ili acil; ili njegova farmaceutski prihvatljiva sol.
2. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je Q O.
3. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R6 H.
4. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R6 je -C(O)CH3, -C(O)CH2CH3, -C(O)(CH2)2CH3, -C(O)(CH2)3CH3, -C(O)(CH2)4CH3 ili -C(O)(CH2)5CH3.
5. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R2 -CO-Aaa.
6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (I) spoj formule (IA): , ili njegova farmaceutski prihvatljiva sol; gdje: R1 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Ser i Thr, koji može biti supstituiran s alkilom ili acilom; R3 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Asn, Asp, Gln, te Glu; i Aaa je aminokiselinski ostatak, kojeg se bira između Thr i Ser; gdje je C-kraj njegov slobodni kraj, amidiran ili esterificiran.
7. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je Aaa aminokiselinski ostatak, kojeg se bira između Thr i Ser; gdje je C-kraj slobodni kraj.
8. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je spoj formule (I) spoj formule (IB): , ili njegova farmaceutski prihvatljiva sol; gdje: R1 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Ser i Thr, koji može biti supstituiran s alkilom ili acilom; i R3 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Asn, Asp, Gln, te Glu.
9. Spoj u skladu s patentnim zahtjevom 1, naznačen time što: R1 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Ser i Thr.
10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R1 supstituiran s C1-5 alkilom.
11. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R3 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Asn i Glu.
12. Spoj u skladu s patentnim zahtjevom 1, naznačen time što: R1 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Ser i Thr; R2 je -CO-Aaa; Aaa je aminokiselinski ostatak, kojeg se bira između Thr i Ser; gdje je C-kraj slobodni kraj; R3 predstavlja pobočni lanac aminokiselinskog ostatka kojeg se bira između Asn i Glu.
13. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R1 predstavlja pobočni lanac aminokiselinskog ostatka Ser.
14. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R1 predstavlja pobočni lanac aminokiselinskog ostatka Thr.
15. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je Aaa Ser.
16. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je Aaa Thr.
17. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R3 predstavlja pobočni lanac aminokiselinskog ostatka Asn.
18. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R3 predstavlja pobočni lanac aminokiselinskog ostatka Asp.
19. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R3 predstavlja pobočni lanac aminokiselinskog ostatka Gln.
20. Spoj u skladu s patentnim zahtjevom 1, naznačen time što R3 predstavlja pobočni lanac aminokiselinskog ostatka Glu.
21. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je R2 H.
22. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
23. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
24. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
25. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
26. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
27. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
28. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
29. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
30. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
31. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
32. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
33. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
34. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
35. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
36. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
37. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
38. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
39. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
40. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
41. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
42. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
43. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
44. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
45. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
46. Spoj u skladu s patentnim zahtjevom 1, naznačen time što ima sljedeću strukturu: ; ili njegova farmaceutski prihvatljiva sol.
47. Farmaceutski pripravak, naznačen time što sadrži farmaceutski prihvatljivu podlogu ili pomoćnu tvar, kao i najmanje jedan spoj u skladu s bilo kojim od patentnih zahtjeva 1-46, ili njegovu farmaceutski prihvatljivu sol.
48. Farmaceutski pripravak u skladu s patentnim zahtjevom 47, naznačen time što dodatno sadrži najmanje jedno sredstvo, koje se bira između sredstva protiv raka, kemoterapeutskog sredstva, te antiproliferativnog spoja.
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