C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/37 (2006.01) C07C 237/04 (2006.01) C07K 1/00 (2006.01) C07K 5/083 (2006.01) C07K 5/103 (2006.01) C07K 5/107 (2006.01)
Patent
CA 2109646
A compound of the formula R1-A2-A1-Asp-p-nitroanilide I wherein: A1 is a residue of any of the naturally occurring .alpha.-amino acids or a homolog, analog or derivative of a natural .alpha.-amino acid; A2 is a residue of a lipophilic .alpha.-amino acid; R1 is alkylcarbonyl,phenalkylcarbonyl,alkoxycarbonyl,phenalkoxycarbonyl, alkylaminocarbonyl, phenalkylaminocarbonyl or R2-A3 wherein A3 is a residue of a lipophilic .alpha.-amino acid; and R2 is alkylcarbonyl, alkoxycarbonyl or phenylalkoxycarbonyl, and a method of detecting inhibitors of interleukin 1.beta. converting enzyme (ICE) comprising evaluating a test compound's capacity to inhibit the ICE-induced hydrolysis of a compound of the formula I. The greater the ability of a test compound to inhibit such hydrolysis, the greater its expected activity in treating inflammation as well as diseases whose pathogenesis is induced or sustained by interleukin-1.beta.. Also disclosed is the following intermediate, useful for synthesizing the compounds of formula I: (see above formula)
Daumy Gaston O.
Reiter Lawrence A.
Pfizer Inc.
Smart & Biggar
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