Development of mPGES-1 inhibitors for treatment of inflammatory pain

Our laboratory has been involved in a long-term collaboration project with Swedish company BIOLIPOX aimed at the development of a medication for treatment of inflammatory pain, such as from rheumatoid arthritis.

The goal of the project was design of selective inhibitor of membrane-bound prostaglandin (PG) E synthase (mPGES-1), an enzyme necessary for the production of Prostaglandin E2 (PGE2).

In 2010, a candidate drug for further clinical development has been selected (OREXO press-release).

Patents:

  1. Olofsson, K.; Suna E.; Pelcman, B.; Ozola, V.; Katkevics, M.; Kalvins, I. Indoles useful in the treatment of inflammation. WO 2005/005415 A1, 20 Jan 2005
  2. Olofsson, K.; Suna E.; Pelcman, B.; Ozola, V.; Katkevics, M.; Kalvins, I. Indoles useful in the treatment of inflammation. WO 2005/123673 A1, 29 Dec 2005
  3. Olofsson, K.; Suna E.; Pelcman, B.; Ozola, V.; Katkevics, M.; Kalvins, I.; Schaal, W. Indoles useful in the treatment of inflammation. WO 2005/123674 A1, 29 Dec 2005
  4. Olofsson, K.; Suna E.; Pelcman, B.; Ozola, V.; Katkevics, M.; Kalvins, I.; Schaal, W. Indoles useful in the treatment of inflammation. WO 2005/123675 A1, 29 Dec 2005
  5. Pelcman, B; Olofsson, K.; Katkevics, M.; Ozola, V.; Suna E.;. Kalvins, I.; Trapencieris, P. Indoles useful in the treatment of inflammation. WO 2006/077364 A1, 27 July 2006
  6. Pelcman, B; Olofsson, K.; Katkevics, M.; Ozola, V.; Suna E.;. Kalvins, I.; Schaal, W. Indoles useful in the treatment of inflammation. WO 2006/077365 A1, 27 July 2006
  7. Pelcman, B; Olofsson, K.; Katkevics, M.; Ozola, V.; Suna E.;. Kalvins, I.; Trapencieris, P.; Katkevica, D.; Schaal, W. Indoles useful in the treatment of inflammation. WO 2006/077366 A1, 27 July 2006
  8. Pelcman, B; Olofsson, K.; Katkevics, M.; Ozola, V.; Suna E.;. Kalvins, I.; Trapencieris, P.; Katkevica, D.; Schaal, W. Indoles useful in the treatment of inflammation. WO 2006/077367 A1, 27 July 2006
  9. Pelcman, B; Olofsson, K.; Arsenjans, P.; Kalvins, I.; Suna E.;. Katkevics, M.; Madre, M.; Ozola, V. Pyrrolopyridines useful in the treatment of inflammation. WO 2006/077401 A1, 27 July 2006
  10. Pelcman, B; Olofsson, K.; Arsenjans, P.; Ozola, V.; Suna E.; Kalvins, I. Thienopyrroles useful in the treatment of inflammation. WO 2006/077412 A1, 27 July 2006
  11. Pelcman, B; Olofsson, K.; Schaal, W.; Kalvins, I.; Katkevics, M.; Ozola, V.; Suna E. Benzoxazoles useful in the treatment of inflammation. WO 2007/042816 A1, 19 April 2007
  12. Pelcman, B; Olofsson, K.; Habarova, O.; Kalvins, I.; Suna E.; Trapencieris, P.; Andrianov, V. Naphthalene-disulfonamides useful for the treatment of inflammation. WO 2007/042817 A1, 19 April 2007
  13. Pelcman B.; Olofsson K.; Katkevics M.; Ozola V.; Suna E.; Kalvins I.; Arsenjans P. Indoles useful in the treatment of inflammation. WO 2008/009924 A2, 24 January, 2008
  14. Pelcman, B.; Olofsson, K.; Kalvins, I.; Suna E.; Ozola, V.; Schaal, W. Benzoxazoles useful in the treatment of inflammation. WO 2008/071944, 19 June, 2008
  15. Pelcman, B.; Olofsson, K.; Suna E.; Kalvins, I.; Ozola, V.; Krasikovs, A. Disulfonamides useful in the treatment of inflammation. WO 2008/129288 A2, 30 October, 2008
  16. Pelcman, B.; Olofsson, K.; Suna E.; Kalvins, I.; Ozola, V.; Andrianov, V. Disulfonamides useful in the treatment of inflammation. WO 2008/129276 A1, 30 October, 2008
  17. Pfau, R.; Arndt, K.; Doods, H.; Klinder, K.; Kuelzer, R.; Lubriks, D.; Mack, J.; Pelcman, B.; Priepke, H.; Rönn, R.; Stenkamp, D.; Suna E. 3H-Imidazo-[4,5-c]-pyridine-6-carboxamides as anti-inflammatory agents. WO2010/100249 A1, 10 September, 2010
  18. Priepke, H.; Doods, H.; Kuelzer, R.; Pfau, R.; Stenkamp, D.; Pelcman, B.; Rönn, R.; Lubriks, D.; Suna E. 2-(Arylamino)-3H-imidazo-[4,5-b]-pyridine-6-carboxamide derivatives and their use as MPGES-1 inhibitors. WO2012/022792 A1, 23 February, 2012
  19. Priepke, H.; Kuelzer, R.; Mack, J.; Pfau, R.; Stenkamp, D.; Pelcman, B.; Rönn, R.; Lubriks, D.; Suna E. 2-Aminobenz imidazole derivatives useful in the treatment of inflammation WO2012/076672 A1, 14 June, 2012
  20. Priepke, H.; Doods, H.; Kuelzer, R.; Pfau, R.; Stenkamp, D.; Pelcman, B.; Rönn, R.; Lubriks, D.; Suna E. Imidazo(4,5-b)pyridine-6-carboxamides as anti-inflammatory agents. WO2012/076674 A1, 14 June, 2012