Pyridazines as interleukin-1.beta. converting enzyme inhibitors

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United States of America Patent

PATENT NO 6121266
SERIAL NO

08444984

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is 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; R.sub.2 is COOR.sub.5, C(.dbd.O)NH(CHR.sub.5).sub.m --COOR.sub.5, NH(CHR.sub.5).sub.m CON(R.sub.5)R.sub.6, C(.dbd.O)N(R.sub.5)R.sub.6 or NH(CHR.sub.5).sub.m OH; R.sub.3 is H or alkyl; R.sub.4 is H, substituted or unsubstituted aryl, heteroaryl or alkyl; R.sub.5 and R.sub.6 are 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-1.beta. protease activity in a mammal utilizing the compounds and compositions.

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Patent Owner(s)

  • VERTEX PHARMACEUTICALS INCORPORATED;AZURE SOLUTIONS LIMITED

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Ator, Mark A Paoli, PA 9 27
Dolle, Roland E King of Prussia, PA 68 771
Hoyer, Denton W Exton, PA 20 126
Rinker, James M Reading, PA 12 193
Ross, Tina Morgan Audubon, PA 32 224
Schmidt, Stanley J Chester Springs, PA 28 471

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