4-pyridazinecarboxamides and esters as interleukin-1β...

Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system

Reexamination Certificate

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C544S114000, C544S224000, C544S232000, C544S239000, C544S241000, C514S085000, C514S236500, C514S247000, C514S252010, C514S252030, C514S252040, C514S252050

Reexamination Certificate

active

06995261

ABSTRACT:
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof:whereinR1is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate;R2is COOR5, C(═O)NH(CHR5)m—COOR5, NH(CHR5)mCON(R5)R6, C(═O)N(R5)R6or NH(CHR5)mOH;R3is H or alkyl;R4is H, substituted or unsubstituted aryl, heteroaryl or alkyl;R5and R6are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0–6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1β protease activity in a mammal utilizing the compounds and compositions.

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