PURPOSE: To provide a new compound which acts as an inhibiting factor against protease for serine-protein and is useful for curing degenerative diseases such as emphysema, chronic rheumatic arthritis, pancreatitis, bronchitis and inflammatory enteritis.
CONSTITUTION: The compound of formula I, e.g. 4,6-dimethoxy-2- saccharinylmethyl 2,6-dichlorobenzoate, is obtained by allowing a 4-R4-R5-2- halomethylsccharin of formula II (X is a halogen) and an arylcarboxylic acid of the formula; ArCOOH to react with each other in the presence of an acid acceptor (e.g. triethylamine) and in a solvent such as toluene. This compound inhibits a leuco-elastase and chymotrypsinoid enzymes. In the formula I, Ar is phenyl, naphthyl, anthryl, etc.; R4 is H, a halogen, lower alkyl, lower alkenyl, lower alkoxy, etc.; R5 is H, a halogen, cyano, nitro, etc.
NEIRU UOOREN BOOTSU
ARUBAATO JIYOZEFU MURA
BIRENDORA KUMAA
CHIYAKURAPANI SUBURAMANYAMU
RAJITSUTO CHIMANRARU DESAI
DENISU JIYON FURASUTA
MANOHAA TATSUKURAMU SEINDAN
MARUKORUMU RAISU BERU
JIYON JIYOZEFU KOOTO
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