Novel indazolone derivatives useful as 11b-HSD1 inhibitors
Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R7 have the significances given in the description and claims can be used in the form of pharmaceutical compositions.
-
Page/Page column 19-20
(2008/06/13)
1,5-Disubstituted indazol-3-ols with anti-inflammatory activity
A series of new indazol-3-ol derivatives was synthesized. Some of these compounds exhibit interesting anti-inflammatory activities in various models of inflammation. 5-Methoxy-1-[quinoline-2-yl-methoxy)-benzyl]-1H-indazol-3- ol (27) strongly inhibits the oxidation of arachidonic acid to 5-hydroperoxyeicosatetraenoic acid catalyzed by 5-lipoxpgenase (IC50 = 44 nM). 27 also inhibits the contraction of sensitized guinea pig tracheal segments (IC50 = 2.9 μM). In guinea pigs treated with 27 (1 mg/kg i.p.) 2 h before antigen provocation, there was a marked inhibition (47%) of the antigen-induced airway eosinophilia. After topical application of 1 μg/ear 27 inhibits the arachidonic acid induced mouse ear edema (41%).