HRP20170955T1 - Derivati kinolin-8-sulfonamida s antikancerogenim djelovanjem - Google Patents

Derivati kinolin-8-sulfonamida s antikancerogenim djelovanjem Download PDF

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HRP20170955T1
HRP20170955T1 HRP20170955TT HRP20170955T HRP20170955T1 HR P20170955 T1 HRP20170955 T1 HR P20170955T1 HR P20170955T T HRP20170955T T HR P20170955TT HR P20170955 T HRP20170955 T HR P20170955T HR P20170955 T1 HRP20170955 T1 HR P20170955T1
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pharmaceutically acceptable
acceptable salt
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structural formula
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HRP20170955TT
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Jeffrey O. Saunders
Francesco G. Salituro
Shunqi Yan
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Agios Pharmaceuticals, Inc.
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Claims (40)

1. Tvar formule (II) ili njena farmaceutski prihvatljiva sol, pri čemu: [image] W, X, Y i Z su svaki nezavisno odabrani između CH ili N; D i D1 su nezavisno odabrani između veze ili NRb; L je veza, -C(O)-, -(CRcRc)m-, -OC(O)-, -(CRcRc)m-OC(O)-, -(CRcRc)m-C(O)-, -NRbC(S)-, ili -NRbC(O)-; R1 je odabran između alkila, cikloalkila, arila, heteroarila i heterociklila; od kojih je svaki supstituiran s 0-5 pojavljivanja Rd; svaki R3 je nezavisno odabran između halo, haloalkila, alikila, hidroksila i –ORa; svaki Ra je nezavisno odabran između alikila, acila, hidroksialkila i haloalkila; svaki Rb je nezavisno odabran između vodika i alikila; svaki Rc je nezavisno odabran između vodika, halo, alkila, alkoksi i halo alkoksi ili dva Rc uzeta zajedno s atomima ugljika za koje su pričvršćeni tvore opcionalno supstituirani cikloalkil; svaki Rd je nezavisno odabran između halo, haloalkila, haloalkoksi, alkila, alkinila, nitro, cijano, hidroksila, -C(O)Ra, -OC(O)Ra, -C(O)ORa, -SRa, -NRaRb i -ORa, ili dva Rd uzeta zajedno s atomima ugljika za koje su pričvršćeni tvore opcionalno supstituirani heterociklil; n je 0, 1 ili 2; m je 1, 2 ili 3; h je 1; i g je 1.
2. Tvar iz patentnog zahtjeva 1, pri čemu su W, X, Y i Z jednaki CH.
3. Tvar iz patentnog zahtjeva 2, pri čemu je D NRb i D1 je veza.
4. Tvar iz patentnog zahtjeva 3, pri čemu je Rb H, metil ili etil.
5. Tvar iz bilo kojeg od patentnih zahtjeva 1-4, pri čemu je L veza, -(CRcRc)m-,-NRbC(O)-, -(CRcRc)m-C(O)-, -C(O)-, -(CRcRc)m-OC(O)-, ili -O(CO)-,
6. Tvar iz patentnog zahtjeva 5, pri čemu je L -(CRcRc)m-.
7. Tvar iz patentnog zahtjeva 6, pri čemu je R1 cikloalkil, aril, heteroaril i heterociklil s 0-5 pojavljivanja Rd.
8. Tvar iz patentnog zahtjeva 6, pri čemu je Rb vodik.
9. Tvar iz bilo kojeg od patentnih zahtjeva 6-8, pri čemu je n 0.
10. Tvar iz bilo kojeg od patentnih zahtjeva 6-8, pri čemu je n 1 i R3 je CH3, CH2CH3, OCH3, OCH2CH3, OH, F, Cl ili CF3.
11. Tvar iz patentnog zahtjeva 1 ili njena farmaceutski prihvatljiva sol, pri čemu je tvar tvar formule: [image]
12. Tvar iz patentnog zahtjeva 1, pri čemu je tvar odabrana iz grupe koja se sastoji od: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili njena farmaceutski prihvatljiva sol.
13. Tvar iz patentnog zahtjeva 1, pri čemu je tvar odabrana iz grupe koja se sastoji od: [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] [image] ili njena farmaceutski prihvatljiva sol.
14. Tvar iz patentnog zahtjeva 1 ili njena farmaceutski prihvatljiva sol, odabrana iz grupe koja se sastoji od: [image] [image] [image] i
15. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
16. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
17. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
18. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
19. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
20. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
21. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
22. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
23. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
24. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
25. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
26. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
27. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
28. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
29. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
30. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
31. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
32. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
33. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
34. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
35. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
36. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
37. Tvar u skladu s patentnim zahtjevom 1 ili njena farmaceutski prihvatljiva sol koja ima sljedeću strukturnu formulu: [image]
38. Farmaceutski sastav sadrži tvar iz bilo kojeg od patentnih zahtjeva 1 do 37, ili njenu farmaceutski prihvatljivu sol.
39. Tvar ili farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 38 za uporabu kao lijek.
40. Tvar ili farmaceutski sastav iz bilo kojeg od patentnih zahtjeva 1 do 38 za uporabu u liječenju raka povezanog s PKM2 aktivnosti u potrebitog subjekta.
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