LV12209B - Ar fenilgrupu aizvietoti heterocikli kā ciklooksigenāzes-2 inhibitori - Google Patents

Ar fenilgrupu aizvietoti heterocikli kā ciklooksigenāzes-2 inhibitori Download PDF

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LV12209B
LV12209B LVP-98-238A LV980238A LV12209B LV 12209 B LV12209 B LV 12209B LV 980238 A LV980238 A LV 980238A LV 12209 B LV12209 B LV 12209B
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furanone
phenyl
methylsulfonyl
pharmaceutical composition
fluorophenyl
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LVP-98-238A
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LV12209A (lv
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Yves Ducharme
Jacques Yves Gauthier
Petpiboon Prasit
Yves Leblanc
Zhaoyin Wang
Serge Leger
Michel Therien
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Merck Frosst Canada & Co/Merck Frosst Canada & Cie
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Application filed by Merck Frosst Canada & Co/Merck Frosst Canada & Cie filed Critical Merck Frosst Canada & Co/Merck Frosst Canada & Cie
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Claims (29)

  1. LV 12209 Izgudrojuma formula 1. 3-(4-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons.
  2. 2. 5,5-dimetil-3-(3-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons.
  3. 3. 5,5-dimetil-3-(4-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons.
  4. 4. 3-(3,4-difluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons.
  5. 5. 3-fenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons.
  6. 6. Savienojums, kas ņemts no rindas: 3-(2,6-difiuorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2,5-difluorfenil)-4-[4-(metiisulfonil)fenil]-2-(5H)-furanons, 3-(3,5-difluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-bromfenil)-4-[4-(metiIsulfonil)fenil]-2-(5H)-furanons, 3-(4-hlorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-metoksifenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2,4-difiuorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2-hlorfenil)-4-[4-(metilsuifonii)fenil]-2-(5H)-furanons, 3-(2-brom-4-fiuorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2-brom-4-hlorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-hlor-2-fluorfenil)-4-[4-(metilsulfonil)fenii]-2-(5H)-furanons, 3-(3-brom-4-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(3-hlorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2-hlor-4-fluorfenil)-4-[4-(metilsulfonii)fenil]-2-(5H)-furanons, 3-(2,4-dihlorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons1 3-(3,4-dih[orfenil)-4-[4-(metilsuifonil)fenii]-2-(5H)-furanons, 3-(4-fiuorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(3-hlor-4-fluorfenil)-4-[4-(metilsulfonii)fenil]-2-(5H)-furanons, 3-(4-trifluormetilfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(3-fIuor-4-metoksifenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(3-hlor-4-metoksifenil)-4-[4-(metilsulfonil)fenii]-2-(5H)-furanons, 3-(3-brom-4-metoksifenil)-4-[4-(metilsulfonil)feniI]-2-(5H)-furanons, 2 3-(2-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-metiltiofenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(3-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2-hlor-6-fiuorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(3-brom-4-metiIfenil)-4-[4-{metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-brom-2-fluorfenil)-4-[4-(metilsulfonil)fenii]-2-(5H)-furanons, a^S^-dibromfenilH-^metilsulfoniOfenilj^SHj-furanons, 3-(4-hlor-3-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-brom-3-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(4-brom-2-fluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(2-naftil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 3-(7-hinolinil)-4-[4-(metilsulfonil)fenii]-2-(5H)-furanons, 3-(3,4-dihlorfenil)-4-[4-(aminosulfonil)fenil3-2-(5H)-furanons, 3-(3-hlor-4-metoksifenil)-4-[4-(aminosulfonil)fenil]-2-(5H)-furanons, 3-(3-brom-4-metoksifenii)-4-[4-(aminosulfonil)fenil]-2-(5H)-furanons,
  7. 7. Savienojums, kas ņemts no rindas: 5.5- dimetil-3-(3-hlorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 5,5<iimetil-3-(3,4<iifluorfenil)-4-[4-(metilsulfonil)fenil]-2-(5H)-furanons, 5.5- dimetii-3-(3,4-dihlorfenil)-4-[4-(metilsuIfonil)fenil]-2-(5H)-furanons, 5.5- dimetil-3-(4-hlorfenil)-4-[4-(metiisulfonii)fenil]-2-(5H)-furanons, 5.5- dimetil-3-(2-naftil)-4-[4-(metiIsulfonil)fenil]-2-(5H)-furanons.
  8. 8. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 1. punkta un farmaceitiski pieņemamu nesēju.
  9. 9. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 2. punkta un farmaceitiski pieņemamu nesēju.
  10. 10. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 3. punkta un farmaceitiski pieņemamu nesēju.
  11. 11. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 4. punkta un farmaceitiski pieņemamu nesēju.
  12. 12. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 5. punkta un farmaceitiski pieņemamu nesēju.
  13. 13. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 6. punkta un farmaceitiski pieņemamu nesēju.
  14. 14. Farmaceitiskā kompozīcija, kas ietver savienojumu pēc 7. punkta un farmaceitiski pieņemamu nesēju.
  15. 15. Farmaceitiskā kompozīcija pēc jebkura no 8. līdz 14. punktam orālai lietošanai piemērotā formā. 3 LV 12209
  16. 16. Farmaceitiskā kompozīcija pēc 15. punkta tabletes veidā.
  17. 17. Farmaceitiskā kompozīcija pēc 15. punkta cietas vai mīkstas želatīna kapsulas veidā.
  18. 18. Savienojuma pēc 1. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 8. punkta ražošanai.
  19. 19. Savienojuma pēc 2. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 9. punkta ražošanai.
  20. 20. Savienojuma pēc 3. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 10. punkta ražošanai.
  21. 21. Savienojuma pēc 4. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 11. punkta ražošanai.
  22. 22. Savienojuma pēc 5. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 12. punkta ražošanai.
  23. 23. Savienojuma pēc 6. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 13. punkta ražošanai.
  24. 24. Savienojuma pēc 7. punkta pielietojums iekaisuma slimību ārstēšanai paredzētas farmaceitiskās kompozīcijas pēc 14. punkta ražošanai.
  25. 25. Pielietojums pēc jebkura no 18. līdz 24. punktam sāpju, drudža vai iekaisuma ārstēšanai paredzētas farmaceitiskās kompozīcijas ražošanai.
  26. 26. Pielietojums pēc jebkura no 18. līdz 24. punktam dismenorejas, galvassāpju, zobu sāpju, izmežģījumu, sastiepumu, miozīta, neiralģijas, sinovīta, reimatoīdā artrīta, osteoartrīta, podagras, deformējošās spondilozes un locītavu somiņu iekaisuma ārstēšanai paredzētas farmaceitiskās kompozīcijas ražošanai.
  27. 27. Pielietojums pēc jebkura no 18. līdz 24. punktam ļaundabīgu audzēju vai audzēja metastāžu ārstēšanai paredzētas farmaceitiskās kompozīcijas ražošanai.
  28. 28. Pielietojums pēc jebkura no 18. līdz 24. punktam demencijas ārstēšanai paredzētas farmaceitiskās kompozīcijas ražošanai.
  29. 29. Pielietojums pēc 28. punkta, kur demencija ir saistīta ar Alcheimera slimību.
LVP-98-238A 1993-06-24 1998-10-26 Ar fenilgrupu aizvietoti heterocikli kā ciklooksigenāzes-2 inhibitori LV12209B (lv)

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