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Use of peptide derivatives for the manufacture of endopeptidase inhibiting drugs 24.15 and 24.16.

机译:肽衍生物在生产内肽酶抑制药物24.15和24.16中的用途。

摘要

The invention relates to the use of peptide derivatives for the manufacture of endopeptidase inhibiting drugs 24.15 and 24.16. BR/ These peptide derivatives have the formula: BR/ (CF DRAWING IN BOPI) BR/ BR/ in which R1 is an optionally substituted aryl or aralkyl group, R2 is Pro, Hyp, thiazolidine or dehydroproline, R3 is H or an alkyl radical, R4 is an alkyl group or the side chain of an amino acid, R5 and R6 may be H, NH4 + or metals. By way of example, N- (phenylethylphosphonyl) -Gly-Pro-aminohexanoic acid has an inhibition constant of 0.9nM vis-à-vis the endopeptidase 24.16. / P
机译:本发明涉及肽衍生物在生产内肽酶抑制药物24.15和24.16中的用途。
这些肽衍生物的分子式为:
(CF BOBOING IN BOPI)

其中R1为任选取代的芳基或芳烷基,R2为Pro,Hyp,噻唑烷或脱氢脯氨酸R 3为H或烷基,R 4为烷基或氨基酸的侧链,R 5和R 6可以为H,NH 4 +或金属。举例来说,相对于内肽酶24.16,N-(苯乙基膦酰基)-Gly-Pro-氨基己酸的抑制常数为0.9nM。

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