Benzoxazine derivatives and their application in therapy

Details Benzoxazine derivatives and their application in therapy Benzoxazine derivatives and their application in therapy

1994-02-24

1995-09-05

Datlow, Philip I.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

5142305, 544105, 540594, A61K 31535, C07D26536, C07D41306

Patent

active

054479282

ABSTRACT:
Compounds of the formula ##STR1## in which Y represents hydrogen, fluorine, chlorine, methyl or methoxy, R.sub.1 represents phenyl substituted by fluorine, methyl, methoxy, trifluoromethyl or phenyl, or R.sub.1 represents 2-thienyl, R.sub.2 represents methyl, and R.sub.3 represents (C.sub.1 -C.sub.4)-alkyl, or phenyl-(C.sub.1 -C.sub.2)-alkyl optionally substituted on the ring by 2 to 3 methoxy groups, or 2-(2-pyridyl)ethyl, or R.sub.2 and R.sub.3 form, with the adjacent nitrogen, 4-phenyl(1-piperidyl), 4-phenylmethyl(1-piperidyl), 1,2,3,4-tetrahydro-2-isoquinolyl, 6-methoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 5,8-dimethoxy-1,2,3,4-tetrahydro-2-isoquinolyl, 6,7-dimethoxy 1,2,3,4-tetrahydro-2-isoquinolyl, 2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, or 7,8-dimethoxy-2,3,4,5-tetrahydro-1H-3-benzazepin-3-yl, and X represents carbonyl or sulphonyl, and their salts are useful as neuroprotective and antiiischaemic agents.

REFERENCES:
Cecil Textbook of Medicine, 19th edition (1992) Wyngaarden, M.D. editor, pp. 2075-2078.
Techer, H., "Tetrahydro-1,2,3,3a 4H-pyrrolo-(2.1-c) benzoxazine-1,4 et Derivatives", Comptes Rendus des Seances de L'Academie des Sciences, Serie C., vol. 274, No. 11, 1972, pp. 1081-1083.

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