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RS52590B2 - Jedinjenja tipa supstituisanog hinoksalina sa premošćenim piperidinom i njihova upotreba - Google Patents
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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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RS
Serbia
Prior art keywords
pharmaceutically acceptable
compound according
compound
acceptable derivative
group
Prior art date
Application number
RS20120549A
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English (en)
Inventor
Jiangchao Yao
John W F Whitehead
Naoki Tsuno
Kouki Fuchino
Original Assignee
Purdue Pharma Lp
Shionogi & Co
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Family has litigation
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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    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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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    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P25/00—Drugs for disorders of the nervous system
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/22—Anxiolytics
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    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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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  • Hydrogenated Pyridines (AREA)

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

Publications (2)

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

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US (6) US8476271B2 (sr)
EP (2) EP2324013B3 (sr)
JP (1) JP5416210B2 (sr)
KR (1) KR101333660B1 (sr)
CN (1) CN102105465B (sr)
AR (1) AR072578A1 (sr)
AU (1) AU2009275218C1 (sr)
BR (1) BRPI0911031B8 (sr)
CA (1) CA2730288C (sr)
CL (1) CL2011000148A1 (sr)
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DK (1) DK2324013T6 (sr)
ES (1) ES2393849T7 (sr)
HR (1) HRP20120841T4 (sr)
IL (2) IL210549A (sr)
MX (1) MX2011000872A (sr)
MY (1) MY153948A (sr)
NZ (1) NZ590416A (sr)
PE (2) PE20140102A1 (sr)
PL (1) PL2324013T6 (sr)
PT (1) PT2324013E (sr)
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