152537-56-9Relevant articles and documents
Synthetic studies on condensed-azole derivatives. V. Synthesis and anti- asthmatic activities of ω-sulfamoylalkyloxy[1,2,4]triazolo[1,s-b]pyridazines
Kuwahara, Masaaki,Kawano, Yasuhiko,Kajino, Masahiro,Ashida, Yasuko,Miyake, Akio
, p. 1447 - 1457 (2007/10/03)
A series of novel ([1,2,4]triazolo[1,5-b]pyridazin-6- yl)oxyalkylsulfonamides was synthesized and evaluated for the ability to inhibit platelet activating factor (PAF)-induced bronchoconstriction in guinea pigs. The compounds bearing a gem-dialkyl or a cycloalkylidene group at the 2 position of the sulfamoylpropyloxy group in the side chain and a methyl group at the 7 position were found to have potent activity. Among them, 2,2-diethyl-3-(7-methyl[l,2,4]-triazolo[1,5-b]pyridazin-6- yl)oxypropanesulfonamide (13) showed excellent anti-asthmatic activity. Compouds 13 may be of significant value in the treatment of asthma and other respiratory diseases. The structure-activity relationships in this series of compounds are discussed.
Triazolopyridazine compounds, their production and use
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, (2008/06/13)
Novel compound represented by the formula: STR1 wherein R1 stands for H, an optionally substituted lower alkyl group or a halogen; R2 and R3 respectively stands for a hydrogen or an optionally substituted lower alkyl group, or R2 and R3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for O, SO or SO2 ; Y stands for a group of the formula: STR2 (R4 and R5 respectively stand for H or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R6 and R7 each stands for H, an optionally substituted lower alkyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R6 and R7 may, taken together with the adjacent N, form an optionally substituted N-containing heterocyclic group; m stands for 0 to 4; n stands for 0 to 4, or a salt thereof, which has excellent anti-PAF activities anti-LTC4 activities and anti-ET-1 activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmasceutical compositions.