Substituted heterocyclic compound

Abstract

PURPOSE: To obtain a new substd. heterocyclic compd. which is an inhibitor of human leukocyte elastase(HLE) and is useful as a research tool for pharmacological, diagnostic and related studies and for treatment of diseases in mammals in which HLE is implicated. CONSTITUTION: This is a compd. of the formula [wherein R 0 is a 1-5C alkyl; R is H, AXCO (in which AX is H, CF 3 , 2,2,2-trifluoroethoxy, NH 2 , etc.), AXCJ (in which J is O or S; X is a direct bond, O, S or NH 2 ; A is tetrahydropyran-4- yl, 1-methylpiperid-4-yl, etc.), DWSO 2 (in which DW is OH, NH 2 , CF 3 , etc.), or the like; R 6 is a 1-5C alkyl, a 3-7C cycloalkyl, an aryl or a heteroaryl having no tertiary carbon] or its pharmaceutically acceptable salt in the case that the compd. is an acid or a base, such as 2-[5-amino-6-oxo-2-(2-thienyl)-1,6- dihydro-1-pyrimidinyl]-N-(3,3,3-trifluoro-1-isopropyl-2-oxopropyl)acetamide. COPYRIGHT: (C)1993,JPO