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

C - Chemistry – Metallurgy – 07 – D

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C07D 413/12 (2006.01) A61K 31/415 (2006.01) A61K 31/535 (2006.01)

Patent

CA 2091440

(see formula I) Compounds having alpha adrenergic activity and useful for the treatment of glaucoma, renal and gastrointestinal disorders and vasoconstrictors have formula (1), where R1 is independently H, or lower alkyl of 1 to 6 carbons; R2 is independently H, or lower alkyl of 1 to 6 carbons or the two R2 symbols jointly represent a carbonyl oxygen; R3 is H, lower alkyl of 1 to 6 carbons, O, OH and OR- where R- is lower alkyl of 1 to 6 carbons, or R3 is COH or COR8 where R8 is lower alkyl of 1 to 6 carbons; R4 and R5 independently is H, Br, Cl, or lower alkyl of 1 to 6 carbons, lower alkenyl or lower alkynyl with the proviso that when the R2 groups symbolize a carbonyl oxygen then R4 and R5 both cannot be hydrogen; R6 is hydrogen, Br, Cl, or lower alkyl of 1 to 6 carbons, lower alkenyl or lower alkynyl, and the R5 and the (2-imidazoline-2-yl)amino substituents are connected mutually exclusively to the 6 and 7 positions of the 1,4-benzoxazine nucleus.

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