Benzoxazinone and benzothiazinone derivatives having cardiovascu

Details Benzoxazinone and benzothiazinone derivatives having cardiovascu Benzoxazinone and benzothiazinone derivatives having cardiovascu

1994-11-23

1996-01-02

Datlow, Philip I.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5442305, 544 50, 544 92, A61K 31535, A61K 3154, C07D27908, C07D26522

Patent

active

054808820

ABSTRACT:
Compounds of formula I ##STR1## wherein R represents hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.7 cycloalkyl, methylene-dioxy or phenyl, which may be substituted by one or two groups independently selected from hydroxy, halogen, nitro, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy; R.sub.1 and R.sub.2 independently represent hydrogen, COOR.sub.3, --CONR.sub.4 R.sub.5, ##STR2## --OCONR.sub.4 R.sub.5, --OCOR.sub.3, --NR.sub.4 R.sub.5, --OCOOR.sub.6, --NR.sub.3 COR.sub.7, --NR.sub.CONR.sub.4 R.sub.5, --N.dbd.CH--NR.sub.4 R.sub.5, NO.sub.2, CN, OH, SR.sub.3, wherein R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 and R.sub.5 independently are hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.6 is C.sub.1 -C.sub.6 alkyl, and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.1 -C.sub.6 alkoxy, with the proviso that R.sub.1 and R.sub.2 cannot be hydrogen at the same time; X is oxygen or sulphur; Y represents a C.sub.2 -C.sub.6 alkylene chain or a C.sub.5 -C.sub.7 cycloalkylene group; and their pharmaceutically acceptable salts are provided and their use in pharmaceutical compositions which may be used in the treatment of cardiovascular diseases.

REFERENCES:
patent: 3459748 (1969-08-01), Krapcho
patent: 3539563 (1970-11-01), Garzia
patent: 5071850 (1991-12-01), Rieu
patent: 5189034 (1993-02-01), Alberto et al.
Burger, Medicinal Chemistry, 3rd ed. (1970), Part I pp. 74-75.
Noller, Chemistry of Organic Compounds, 2nd ed (1957) p. 272.

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