Benzoylpiperazine esters and a process for their production

Details Benzoylpiperazine esters and a process for their production Benzoylpiperazine esters and a process for their production

1985-11-12

1990-02-06

Daus, Donald G.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544235, 544237, 544283, 544353, 544363, 544365, 544373, 544375, 544377, 544380, 544387, C07D24104

Patent

active

048988766

ABSTRACT:
A benzopylpiperazine ester of the following formula: ##STR1## wherein A represents a single bond or an alkylene group, vinylene group, --O--alkylene group or methine group, R.sub.1 represents a bicyclic carbon ring residue which may be substituted with a lower alkyl group, lower alkoxy group, oxo group or nitro group or a halogen atom, or may be partially saturated; a fluorene residue which may contain an oxo group; a fluorenylidene group; an anthracene residue; a phenanthrene residue which may be substituted with a lower alkyl group, or may be partially saturated; a benzofuran residue or thianaphthene residue which may be substituted with a lower alkyl group or lower alkoxy group; a benzopyran residue or benzoazine residue which may be substituted with an oxo group or phenyl group and partially saturated; a phthalimide residue; a benzodiazine residue; an isozazole residue which may be substituted with a lower alkyl group or phenyl group; or an alkylene dioxybenzene residue or xanthene residue; and R.sub.2 represents an alkyl group, cycloalkyl group, cycloalkylalkyl group or aralkyl group, excepting the case where A is a single bond, R.sub.1 is ##STR2## and R.sub.2 is a methyl group, exhibits excellent chymotrypsin inhibitive activity.

REFERENCES:
patent: T620005 (1986-10-01), Fujii et al.
patent: 4443603 (1984-04-01), Fujii et al.
Mach, Advanced Organic Chemistry, 2nd ed., McGraw-Hill N.Y. (1977) pp. 364-365.
Journal of Biochemistry, vol. 62, No. 4, 1967, pp. 408-418.
English Abstract of Japanese 158737.
Kohjin Co. Ltd., Chem. Abstracts 99:38809 (1983).
Kowa Co. Ltd., Chem. Abstracts 96:180955 (1982).

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