Isoquinoline derivatives and salts thereof

Details Isoquinoline derivatives and salts thereof Isoquinoline derivatives and salts thereof

1990-12-19

1992-05-26

Ivy, C. Warren

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

546145, 546146, 546147, C07D21702, C07D21716, C07D21724, C07D21726

Patent

active

051169851

ABSTRACT:
The invention provides novel compounds and salts thereof, have the structure ##STR1## wherein R.sub.1 is a guianidinobenzoyloxy group and R.sub.2 is a hydrogen atom, a hydroxy, cyano, --COR.sub.3 (wherein R.sub.3 is an amino or lower alkyl group) or --COOR.sub.4 group [wherein R.sub.4 is a hydrogen atom, lower alkyl, phenyl, benzyl or --CH.sub.2 CONR.sub.5 R.sub.6 group (wherein R.sub.5 and R.sub.6 are the same or different and selected from a hydrogen atom and lower alkyl groups)], and wherein R.sub.1 is a hydroxy group and wherein R.sub.2 is a --COR.sub.3 (wherein R.sub.3 is an amino or lower alkyl group) or --COOR.sub.4 group [wherein R.sub.4 is a (C.sub.1, C.sub.3 or C.sub.4) alkyl, phenyl, benzyl or --CH.sub.2 CONR.sub.5 R.sub.6 group (wherein R.sub.5 and R.sub.6 are the same or different and selected from a hydrogen atom and lower alkyl groups)]. The compounds, wherein R.sub.1 is a guanidinobenzoyloxy group, are useful protease inhibitors as anti-trypsin agents.

REFERENCES:
patent: 2538341 (1951-01-01), Ullyot
patent: 4021478 (1977-05-01), White
patent: 4241209 (1980-12-01), Sommer et al.
patent: 4520025 (1985-05-01), Campbell et al.
patent: 4673745 (1987-06-01), Sommer et al.
Georgian et al., "Chemical Abstracts", vol. 58, 1963, col. 4515e.
Journal of Organic Chemistry vol. 27 No. 12 pp. 4571-1479 Dec. 12, 1962 Chemical Abstracts vol. 97 No. 1 p. 569 5th Jul. 1982.

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