RS52590B2 - Jedinjenja tipa supstituisanog hinoksalina sa premošćenim piperidinom i njihova upotreba - Google Patents

Jedinjenja tipa supstituisanog hinoksalina sa premošćenim piperidinom i njihova upotreba

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Publication number
RS52590B2
RS52590B2 RS20120549A RSP20120549A RS52590B2 RS 52590 B2 RS52590 B2 RS 52590B2 RS 20120549 A RS20120549 A RS 20120549A RS P20120549 A RSP20120549 A RS P20120549A RS 52590 B2 RS52590 B2 RS 52590B2
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Serbia
Prior art keywords
pharmaceutically acceptable
compound according
compound
acceptable derivative
group
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RS20120549A
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English (en)
Inventor
Jiangchao Yao
John W F Whitehead
Naoki Tsuno
Kouki Fuchino
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Purdue Pharma Lp
Shionogi & Co
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41077776&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=RS52590(B2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Purdue Pharma Lp, Shionogi & Co filed Critical Purdue Pharma Lp
Publication of RS52590B publication Critical patent/RS52590B/sr
Publication of RS52590B2 publication Critical patent/RS52590B2/sr

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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/14—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing 9-azabicyclo [3.3.1] nonane ring systems, e.g. granatane, 2-aza-adamantane; Cyclic acetals thereof

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Claims (29)

  1. ili njegov farmaceutski prihvaljiv derivat gde: svaki R2je nezavisno izabran od -halo; a je ceo broj izabran od 0, 1 ili 2; b je ceo broj izabran od 0 ili 1; svaki R5je nezavisno izabran od -H, -OH, -(C1-C3)alkil, -C(halo)3, ili -halo; R1je -(C9-C14)cikloalkil ili -(C9-C14)bicikloalkil, od kojih je svaki supstituisan sa 1, 2 ili 3 nezavisno izabrane R3grupe; svaki R3je nezavisno izabran od -(C1-C4)alkil, -(C2-C6)alkenil, -(C2-C6)aIkinil, ili -(C3-C6)cikloalkil, i gde je farmaceutsko prihvatljiv derivat izabran iz grupe koju čine farmaceutsko prihvatljive soli, solvati, radioaktivno obeleženi, steroizomer, enantiomer, diasteroizomer, racemska smeša i tautomer.
  2. ili njegov farmaceutski prihvatljiv derivat: svaki R2 je nezavisno izabran od -halo; a je ceo broj izabran od 0, 1 ili 2; b je ceo broj izabran od 0 ili 1; svaki R5je nezavisno izabran od -H, -OH, -(C1-C3)alkil, -C(halo)3, ili -halo; R1je -(C9-C14)cikloalkil ili -(C9-C14)bicikloalkil; i svaki halo je nezavisno izabran od -F, -C1, -Br, ili -I, i gde je farmaceutski prihvatljiv derivat izabran iz grupe koju čine farmaceutski prihvatljiva so, solvat, radioaktivno obeleženi, steroizomer, enantiomer, diasteroeizomer, racemska smeša i tautomer, uz uslov da jedinjenje nije
  3. 3. Jedinjenje prema patentnim zahtevima 1 ili 2, gde svaki R5je nezavisno izabran od -H, -(C1-C3)alkil, -C(halo)3, ili -halo.
  4. 4. Jedinjenje prema bilo kom od patentnih zahteva 1 do 3, gde svaki R5je nezavisno izabran od -H, -CH3, -CF3, ili -F, i poželjno svaki R5je -H.
  5. 5. Jedinjenje 1rema bilo kom od patentnih zahteva 1 do 4, gde a je ceo broj izabran od 0 ili 1, i poželjno je 0.
  6. 6. Jedinjenje prema bilo kom od patentnih zahteva 1 do 5, gde je jedinjenje jedinjenje
    ili njegov farmaceutski prihvatljiv derivat, gde je farmaceutski prihvatljiv derivat izabran iz grupe koju čine farmaceutski prihvatljiva so, solvat, radioaktivno obeleženi, steroizomer, 5 enantiomer, diasteroizomer, racemska smeša i tautomer.
  7. 7. Jedinjenje prema bilo kom od patentnih zahteva 1do 6, gde je R2-F.
  8. 8. Jedinjenje prema bilo kom od patentnih zahteva1 do 7, gde je deojedinjenja 3-okso-3,4-dihidrohinoksalin-2-karboksline kiseline u endo- ili egzo- konformaciji u odnosu na most premošćenog piperidina i poželjno je u endo- konformaciji.
  9. 9. Jedinjenje prema bilo kom od patentnih zahteva 1 do 8, gde R1je -(C9-C12)cikoalkil ili -(C9-C12)bicikloalkil, i gde poželjno (i) R1je -(C9-C12)bicikloalkiI, ili (ii) R1je -indanil, -1,2,3,4-tetrahidronaftalenil, 5,6,7,8-tetrahidronaftalenil,-perhidronaftalenil, biciklo[3.3.1]nonil, biciklo[4.2.1]nonil, biciklo[3.3.2]decil, biciklo[4.2.2]decil, biciklo[4.3.1]decil, bicikio[3.3.3]undeci biciklo[4.3.2]undecil, ili biciklo[4.3.3]dodecil, ili (iii) R1je cikloundecil.
  10. 10. Jedinjenje prema bilo kom od patentnih zahteva 1 do 9, gde je R1biciklo[3.3.1]nonil i poželjno R1je 2-biciklo[3.3.l]nonil, ili 3-biciklo[3.3.1]nonil.
  11. 11. Jedinjenje prema bilo kom od patentnih zahteva 1 do 10, gde je R1, u endo- ili egzo- 5 konformaciji u odnosu na most premošćenog piperidina i poželjno je u egzo- konformaciji.
  12. 12. Jedinjenje prema bilo kom od patentnih zahteva 2 do 11, gde je R1:
  13. <13>Jedinjenje prema bilo kom od patentnih zahteva 1 ,3-11, gde u jedinjenju formule (I') postoje 1,2 ili 3 R3grupe i svaka R3grupa je nezavisno izabrana od (i) -(C1-C4)alkil, -(C2-C6)alkenil, i -(C2-C6)alkinil; ili (ii) -(C1-C4)alkil i -(C3-C6)cikloalkil.
  14. 14. Jedinjenje prema bilo kom od patentnih zahteva 1, 3-11 i l i 13, gde u jedinjenju formule (I') svaka R3grupa je metil.
  15. 15. Jedinjenje prema bilo kom od patentnih zahteva 1 ,3-11 i l i 13-14, gde u jedinjenju formule (I') je prisustna jedna R3grupa.
  16. 16. Jedinjenje prema bilo kom od patentnih zahteva 1, 3-11, 13 i l i 15 , gde u jedinjenju formule (I') postoji jedna R3grupa kojaje (i) -(C1C4)alkil, -(C2-C6)alkenil, ili -(C2-C6)aIkiniI; ili ( i i) -(C1-C4)alkil ili -(C3-C6)cikcloalkil.
  17. 17. Jedinjenje prema bilo kom od patentnih zahteva 1, 3-11, 13 i l i 15-16, gde u jednjenju formule (I') postoji jedna R3grupa kojaje (i) -metil, -etil, -n-propil, -izo-propil, -n-butil, -sek-butil, -izo-butil, ili -tere-butik ili (ii) -metil, -etil, -izo-propil, -izo-butil, ilir -terc-butil; oželjno gde je R3etil ili metil.
  18. 18. Jedinjenje prema bilo kom od patentnih zahteva 1 do 17, gde u jedinjenju formule (I') ugljenikov atom R1grupe koji je vezan za atom azota premošćenog piperidina je nesupstituisan sa R3grupom.
  19. 19. Jedinjenje prema bilo kom od patentnih zahteva 1, 3-11, 13-16, 17 opcija (i) i ( i i ) kao i R3koji je metil, ili 18, gde u jedinjenju formule (I') R1i R3zajedno su:
  20. ili njegov farmaceutski prihvatljiv derivat, gde farmaceutski prihvatljiv derivat je izabran iz grupe koju čine farmaceutski prihvatljiva so, solvat, radioaktivno obeleženi steroizomer, enantiomer, diasteroizomer, racemska smeša i tautomer.
  21. 21. Jedinjenje prema patentnom zahtevu 2 koje ima formulu:
    ili njegova farmaceutski prihvatljiv derivat, gde je farmaceutski prihvatljiv derivat izabran iz grupe koju sadrže farmaceutski prihvatljiva so, solvat, radioaktivno obeleženi, steroizomer, enantiomer, diasteroizomer, racemska smeša i tautomer. 5
  22. 22. Jedinjenje prema bilo kom od patentnih zahteva 1 do 21, gde farmaceutski prihvatljiv derivat je farmaceutski prihvatljiva so, i poželjno je so p- toluensulfonske kiseline, sulfatna so ili so fosforne kiseline, a poželjno je so p - toluensulfonske kiseline. 10
  23. 23. Kompozicija koja sadrži efikasnu količinu jedinjenja ili njegovog farmaceutski prihvatljivog derivata prema bilo kom od patentnih zahteva 1 do 22 i farmaceutki prihvatljiv nosač ili ekscipijent.
  24. 24. In vitro postupak moduliranja funkcije ORL-1 receptora u ćeliji, koji obuhvata 15 dovođenje u kontakt ćelije koja je u stanju da eksprimuje ORL-1 receptor sa efikasnom količinom jedinjenja ili njegovog farmaceutski prihvatljivog derivata jedinjenja prema bi lo kom od patentnih zahteva 1 do 22, gde farmaceutski prihvatljiv derivat je izabran iz grupe koju čine farmaceutski prihvatljiva so, solvat radioaktivno obleženi, steroizomer, enantiomer, diasteroizomer, racemska smeša i tutomer. 20
  25. 25. In vitro postupak prema patentnom zahtevu 24, gde jedinjenje ili njegov farmaceutski prihvatljiv derivat ili deluje kao agonist ORL-1 receptora, kao parcijalni agonist ORL-1 receptora, ili kao antagonist ORL-1receptora, gde farmaceutski prihvatljiv derivat je izabran iz grupe koju čine farmaceutki prihvatljiva so, solvat radioaktivno obleženi, steroizomer. 25 enantiomer, diasteroizomer, racemska smeša i tutomer.
  26. 26. Komplet koji sadrži sud koji sadrži efikasnu količinu jedinjenja ili farmaceutski prihvatljiv derivat jedinjenja prema bi lo kom od patentnih zahteva 1 do 22.
  27. 27. Postupak za dobijanje kompozicije, koja sadrži stupanj mešanja jedinjenja ili farmaceutski prihvatljivog derivata jedinjenja prema bilo kom od patentnih zahteva 1 do 22 i farmaceutski prihvatljiv nosač ili ekscipijent.
  28. 28. Upotreba jedinjenja prema bilo kom od patentnih zahteva 1 do 22 u proizvodnji leka korisnog u lečenju bola, poremećaja pamćenja, gojaznosti, konstipacije, depresije, demencije, parkinsonizma, uznemirenosti, kašlja, diareje, visokog krvnog pritiska, epilepsije,anoreksije/kaheksije, urinarne inkotinencije ili zlopuotrebe droga.
  29. 29. Jedinjenje prema bilo kom od patentnih zahteva 1 do 22 za upotrebu u lečenju bola, poremećaja pamćenja, gojaznosti, konstipacije, depresije, demencije, parkinsonizma, uznemirenosti, kašlja, visokog krvnog pritiska, epilepsije, anoreksije/kaheksije, urinarne inkotinencije ili zloupotrebe droga.
RS20120549A 2008-07-21 2009-07-20 Jedinjenja tipa supstituisanog hinoksalina sa premošćenim piperidinom i njihova upotreba RS52590B2 (sr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US8248208P 2008-07-21 2008-07-21
EP20090786064 EP2324013B3 (en) 2008-07-21 2009-07-20 Substituted-quinoxaline-type bridged-piperidine compounds and the uses thereof
PCT/IB2009/006356 WO2010010458A1 (en) 2008-07-21 2009-07-20 Substituted-quinoxaline-type bridged-piperidine compounds and the uses thereof

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RS52590B RS52590B (sr) 2013-04-30
RS52590B2 true RS52590B2 (sr) 2018-05-31

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