- 4H-3,1-BENZOXAZIN-4-ONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE INHIBITION OF SERINE PROTEASES
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A 4H-3,1-benzoxazin-4-one compound of the formula (I): STR1 wherein R is a hydrogen atom or alkyl radical, A is an amino acid residue or a peptide having 2 to 3 amino acid residues, which amino acid residue may have a side chain thereof protected by a protective radical, X is an alkyl, fluoroalkyl, OR 1 or NHR 1 radical wherein R 1 is an alkyl radical, and Y is a protective radical for an amino radical, and salts thereof, exhibit an excellent inhibitory activity against serine proteases, especially against human leukocyte elastase, and thus are useful as an effective component of a medicine for inhibiting elastase.
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- 4H-3,1-BENZOXAZIN-4-ONES AND RELATED COMPOUNDS AND USE AS ENZYME INHIBITORS
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Novel 2-amino-4H-3,1-benzoxazin-4-ones represented by the formula wherein R 1, R 2, R 3 and X are defined herein are useful as enzyme inhibitors in animals.
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