5480. Licofelone
Nomenclature
CAS number: 156897-06-2
6-(4-Chlorophenyl)-2,3-dihydro-2,2-dimethyl-7-phenyl-1H-pyrrolizine-5-acetic acid; ML-3000. C23H22ClNO2; mol wt 379.88.
C 72.72%, H 5.84%, Cl 9.33%, N 3.69%, O 8.42%.
Description and references
Dual inhibitor of cyclooxygenase and 5-lipoxygenase. Prepn: G. Dannhardt et al., EP 397175; eidem, US 5260451 (1990, 1993 both to Merckle); S. A. Laufer et al., J. Med. Chem. 37, 1894 (1994); J. Cossy, D. Belotti, Tetrahedron 55, 5145 (1999). Mechanism of action: S. Tries et al., Inflammation Res. 51, 135 (2002). Experience in experimental dog osteoarthritis: D. Lajeunesse et al., Ann. Rheum. Dis. 63, 78 (2004). Gastrointestinal safety profile in dogs: M. Moreau et al., J. Vet. Pharmacol. Ther. 28, 81 (2005). Review of clinical development: S. Laufer, Inflammopharmacology 9, 101-112 (2001); J. M. Alvaro-Gracia, Rheumatology 43, Suppl. 1, i21-i25 (2004).
Properties
Slightly yellowish solid, mp 162-163°.Therapeutic Category
Anti-inflammatory.
Therapeutic Category (Veterinary)
Anti-inflammatory.Keywords
Anti-inflammatory (Nonsteroidal)