4-Benzyl-1-(2H)-phthalazineone derivatives having an amino acid

Details 4-Benzyl-1-(2H)-phthalazineone derivatives having an amino acid 4-Benzyl-1-(2H)-phthalazineone derivatives having an amino acid

1988-05-09

1989-09-19

Lee, Mary C.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

540599, C07D40304, C07D40314, A61K 3155, A61K 3150

Patent

active

048681750

ABSTRACT:
Anti-asthmatically acting compounds of formula ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, fluorine, chlorine, bromine, trifluoromethyl, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy and the radical A is the group ##STR2## wherein R.sub.3 is hydrogen, a phenyl radical, an indolyl-(3)-methyl radical, imidazolyl-(4)-methyl radical, a C.sub.1 -C.sub.10 -alkyl group or wherein R.sub.3 represents a C.sub.1 -C.sub.10 -alkyl group which is substituted by a carboxy group, a C.sub.1 -C.sub.6 -alkoxycarbonyl group, an aminocarbonyl group, a hydroxy group, a C.sub.1 -C.sub.6 -alkoxy group, a C.sub.2 -C.sub.6 -alkanoyl-oxy group, a mercapto group, a C.sub.1 -C.sub.6 -alkylthio group, a C.sub.2 -C.sub.6 -alkanoylmercapto group, a phenyl group, a hydroxyphenyl group, a dihydroxyphenyl group, an amino-C.sub.1 -C.sub.6 -alkylthio group, an amino-C.sub.1 -C.sub.6 -alkyloxy group, an amino group, a ureido group (H.sub.2 NCONH--) or a guanidino group or wherein R.sub.3 together with the structural moiety >CH(NHR.sub.4) represents the pyrrolidine-2-yl-radical (proline radical) or the 4-hydroxypyrrolidine-2-yl radical, R.sub.4 is hydrogen, benzyl or a C.sub.1 -C.sub.6 -alkyl radical, R.sub.5 is hydrogen, benzyl, a C.sub.1 -C.sub.6 -alkyl radical, a C.sub.2 -C.sub.6 -alkanoyl radical or the group. ##STR3## where R.sub.3 and R.sub.4 have the meanings given above and R.sub.6 is hydrogen, benzyl or C.sub.2 -C.sub.6 -alkanoyl, and physiologically acceptable salts therof, and processes for their preparation.

REFERENCES:
patent: 3813384 (1974-05-01), Vogelsang et al.
patent: 3894015 (1975-07-01), Stachel, deceased et al.
patent: 4746656 (1988-05-01), Atwal
CA: 63654; Basically Substituted Benzylpthalazone Derivatives, Vogelsang et al., 5/28/74.
CA: 126670b, Histamindytic Basically Substituted Benzylpthalazone Derivatives, Vogelsang, 7/27/72.

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