Troglitazone compounds for treating climacteric

Details Troglitazone compounds for treating climacteric Troglitazone compounds for treating climacteric

A - Human Necessities

61

K

A61K 31/495 (2006.01) A61K 31/41 (2006.01) A61K 31/42 (2006.01) A61K 31/425 (2006.01) A61K 31/426 (2006.01) A61K 31/427 (2006.01) A61K 31/44 (2006.01) A61K 31/4439 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01)

Patent

CA 2283791

The present invention is directed toward the use of the drug Troglitazone and related thiazolidinedione compounds in the treatment of the climacteric and cancer. This use is based on the novel discovery that Troglitazone inhibits steroidogenesis in granulosa cell cultures. This activity is believed to result from the ability of thiazolidinedione derivatives to act as a ligand for the orphan steroid receptor peroxisome proliferator-activated receptor gamma (PPAR.gamma.). Troglitazone and related compounds can therefore be used to prevent excessive uterine bleeding during. Further, enhanced translocation of this orphan nuclear receptor into the nucleus of cells will block transcription in rapidly proliferating cancer cells that express PPAR.gamma., resulting in loss of cell viability.

L'invention porte sur l'utilisation de la troglitazone et des composés de thiazolidinedione associés pour traiter l'âge critique et le cancer. Cette utilisation se base sur la récente découverte de l'inhibition par la troglitazone de la stéroïdogénèse dans des cultures de cellules de la granulosa. On pense que cette activité résulte de la capacité des dérivés de la thiazolidinedione à agir comme ligand d'un récepteur stéroïdien orphelin, le récepteur activé par les proliférateurs des péroxysomes de type .gamma. (PPAR.gamma.). La troglitazone et ses composés associés peuvent ainsi servir à prévenir les saignements excessifs de l'utérus. La translocation améliorée de ce récepteur nucléaire orphelin dans le noyau cellulaire bloque par ailleurs la transcription dans les cellules cancéreuses à prolifération rapide exprimant le PPAR.gamma., d'où résulte la perte de la viabilité cellulaire.

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