US 4,789,675 AGranted

1,4-benzoxazine derivatives and pharmaceutical use

AssigneeTakeda Chemical Industries, Ltd.

InventorsKanji Meguro, Kohei Nishikawa

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Abstract

1,4-Benzoxazine derivatives representable by the general formula; ##STR1## wherein R.sup.1 and R.sup.2 independently stand for hydrogen, halogen atom, nitro group, an optionally substituted lower alkyl group, an optionally substituted amino group, an optionally substituted hydroxyl group, a lower alkoxycarbonyl group, or when R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 combinedly stand for a ring representable by --CH.sub.2).sub.m (wherein m denotes an integer of 3 to 5) or --O--CH.sub.2).sub.n O-- (wherein n denotes an integer of 1 to 3), R.sup.3 stands for hydrogen or a lower alkyl group, R.sup.4 and R.sup.5 independently stand for hydrogen, halogen atom, an optionally substituted lower alkyl group or an optionally substituted hydroxyl group, and A stands for an alkylene group or acid addition salts thereof, are useful as prophylactic or therapeutic drugs for, among others, hypertension or ischemic dieases.

Claims19

Dependent claims

A compound of the formula:

##STR19## wherein R.sup.1 and R.sup.2 independently represent (1) hydrogen, (2) halogen, (3) nitro, (4) lower alkyl which is unsubstituted or is substituted by 1 to 3 substituents selected from halogen, hydroxyl and lower alkoxy, (5) amino which is unsubstituted or is substituted by (a) 1 or 2 .beta.-hydroxyethyl groups, (b) 1 or 2 lower alkyl groups, (c) alkanoyl of 2 to 4 carbon atoms or (d) sulfonyl, (6) hydroxyl which is unsubstituted or is substituted by alkyl of 1 to 6 carbon atoms, phenyl-C.sub.1-4 alkyl, or alkanoyl of 2 to 4 carbon atoms or (7) lower alkoxycarbonyl, or
when R.sup.1 and R.sup.2 are adjacent to each other,
R.sup.1 and R.sup.2 together may represent a ring represented by --CH.sub.2).sub.m wherein m denotes an integer of 3 to 5 or --O--CH.sub.2).sub.n O-- wherein n denotes an integer of 1 to 3,
R.sup.3 represents hydrogen or lower alkyl,
R.sup.4 and R.sup.5 independently represent (1) hydrogen, (2) halogen, (3) lower alkyl which is unsubstituted or is substituted by 1 to 3 substituents selected from halogen, hydroxyl and lower alkoxy, or (4) hydroxyl which is unsubstituted or is substituted by alkyl of 1 to 6 carbon atoms, phenyl-C.sub.1-4 alkyl, alkanoyl of 2 to 4 carbon atoms, or R.sup.4 and R.sup.5 combine to form methylenedioxy, and
A represents an alkylene group
or an acid addition salt thereof.

4 more elements

Dependencies are inferred from the claim text.