发明名称 Method of identifying interleukin 1 beta converting enzyme inhibitors
摘要 A compound of the formula R1-A2-A1-Asp-p-nitroanilideIwherein: 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, phenalkylaminocarbcnyl 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: <IMAGE>
申请公布号 US5622830(A) 申请公布日期 1997.04.22
申请号 US19950470890 申请日期 1995.06.06
申请人 DAUMY, GASTON O.;REITER, LAURENCE A. 发明人 DAUMY, GASTON O.;REITER, LAURENCE A.
分类号 C07K5/083;C07K5/107;(IPC1-7):G01N33/573;C12Q1/37 主分类号 C07K5/083
代理机构 代理人
主权项
地址