AZAAZULENE DERIVATIVE, PROCESS FOR PREPARING THE SAME, AND ANTIALLERGIC AGENT AND ANTIINFLAMMATORY AGENT CONTAINING THE SAME

摘要

An azaazulene derivative having the general formula (I): (I) wherein R1 is hydrogen atom or isopropyl group; the bond C----N between C at the 2-position and N at the l-position is single bond or double bond; when the bond C---N is single bond, R2 is 5-tetrazolyl group, R3 is taken together with carbon atom to form carbonyl group at the 2-position, and R4 is hydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, a lower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl group having a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, a diphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring with the general formula: in which W is single bond or carbonyl group, oxygen atom, sulfur atom or -CH=CH-, n is an integer of 1 to 6, and R1 , R2 and R3 are the same or different and each is hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxyl group, trifluoromethyl group, hydroxyl group, a lower alkoxycarbonyl group, carboxyl group, acetyl group or cyano group, when the bond C----N is double bond, N at the l-position has no substituent R4, R2 is cyano group, and R3 is amino group or a salt thereof, azido group, a diphenyl lower alkyl amino group, a substituted phenyl amino group, a substituted piperazinyl group, a substituted homopiperazinyl group, an amino acid residue bonded by N terminal group in which C terminal group is carboxyl group or a lower alkyl ester thereof, or a lower alkyl amino group which may have an alkyl amino group that may be cyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agent and an antiinflammatory agent and has also an inhibitory activity against histamine release, 5lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealis and inhibitory activity against carrageenin edema, and further, is useful as medicine for prevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis, urticaria, atopic dermatitis, other inflammatory diseases or the like.