6- or 7- (2-imino-2-imidazolidine)-1,4-benzoxazines as .alpha. a

Details 6- or 7- (2-imino-2-imidazolidine)-1,4-benzoxazines as .alpha. a 6- or 7- (2-imino-2-imidazolidine)-1,4-benzoxazines as .alpha. a

1990-09-12

1992-02-25

Lee, Mary C.

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

Organic compounds

Chalcogen in the nitrogen containing substituent

C07D26534

Patent

active

050915282

ABSTRACT:
Compounds having .alpha. adrenergic activity and useful for the treatment of glaucoma, renal and gastrointestinal disorders and vasoconstictors have the formula ##STR1## where R.sub.1 is independently H, or lower alkyl or 1 to 6 carbons; R.sub.2 is independently H, or lower alkyl of 1 to 6 carbons or the two R.sub.2 symbols jointly represent a carbonyl oxygen; R.sub.3 is H, lower alkyl of one to 6 carbons, O, OH and OR.sub.7 where R.sub.7 is lower alkyl of 1 to 6 carbons, or R.sub.3 is COH or COR.sub.8 where R.sub.8 is lower alkyl of 1 to 6 carbons; R.sub.4 and R.sub.5 independently is H, Br, Cl, or lower alkyl of 1 to 6 carbons, lower alkenyl or lower alkynyl with the proviso that when the R.sub.2 groups symbolize a carbonyl oxygen then R.sub.4 and R.sub.5 both cannot be hydrogen; R.sub.6 is hydrogen, Br, Cl, or lower alkyl of 1 to 6 carbons, lower alkenyl or lower alkynyl, and the R.sub.5 and the (2-imidazoline-2-yl)amino substituents are connected mutually exclusively to the 6 and 7 positions of the 1,4-benzoxazine nucleus.

REFERENCES:
patent: 3636219 (1972-01-01), Culik et al.
patent: 3890319 (1975-06-01), Danielewicz et al.
patent: 4515800 (1985-05-01), Cavero et al.
patent: 4587257 (1986-05-01), DeSantis et al.
"Heteroaromatic Analogues of the .alpha..sub.2 -Adrenoreceptor Partial Agonist Clonidine", J. Med. Chem., 1989, 32, 1627-1630, Chapelo et al.

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