| 摘要 |
PURPOSE: A class of novel pyrazoles is provided together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock. CONSTITUTION: A compound of the formula (I) is provided, wherein R1 is phenyl, isoquinolin-3-yl, pyrazinyl, pyridin-2-yl, pyridin-2-yl substituted at the 4-position with -(C1-C4)alkyl, (C1-C4)alkoxyl,-CN or -(CH2)nCONH2 where n is 0-2; R2 is phenyl; phenyl substituted with 1 to 3 substituents selected from the group consisting of -(C1-C4)alkyl, -CN, halo, -NO2, CO2(C1-C4)alkyl and -CF3; naphthyl; thiophene or thiophene substituted with 1 to 3 halo groups; R3 is hydrogen; phenyl; phenyl(C2-C6)alkenyl; pyridyl; naphthyl; quinolinyl; (C1-C4)alkylthiazolyl; phenyl substituted with 1 to 2 substituents selected from the group consisting of -(C1-C4)alkyl, -CN, -CONH2, -NO2, -CF3, halo, (C1-C4)alkoxy, CO2(C1-C4)alkyl, phenoxy and SR4 where R4 is -(C1-C4)alkyl or halophenyl; phenyl substituted with one substituent selected from the group consisting of -O(CH2)pR5 where p is 1 to 3 and R5 is -CN, -CO2H, -CONH2, or tetrazolyl, phenyl and -OR6 where R6 is cyclopentyl, cyclohexenyl, or phenyl substituted with halo or (C1-C4)alkoxy; or phenyl substituted with two substituents which, when taken together with the phenyl ring to which they are attached form a methylenedioxy ring; and m is 1 to 5.
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