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专利名称：Azaazulene derivative, process for preparing
the same, and antiallergic agent andantiinflammatory agent containing the same
发明人：Nagahara, Michiko,Ieda, Chikara
Development Division,Mimura,Mitsuo,Uchida, Katsuhiro,Sato,Soichiro,Okumura, Makoto
申请号：EP123857.8申请日：191223公开号：EP0376223A3公开日：19910612
摘要：An azaazulene derivative having the general formula (I): wherein R is hydrogenatom or isopropyl group; the bond between C at the 2-position and N at the 1-position issingle bond or double bond; when the bondis single bond, R is 5-tetrazolyl group, R istaken together with carbon atom to form carbonyl group at the 2-position, and R ishydrogen atom, an alkyl group having 1 to 18 carbon atoms, a lower alkenyl group, alower alkyl group having oxygen atom or sulfur atom in carbon chain, a lower alkyl grouphaving a halogen atom or cyano group, a lower alkyl group having heteroaromatic ring, adiphenyl lower alkyl group, or a lower alkyl group having hydrocarbon-aromatic ring withthe general formula: in which W is,single bond or carbonyl group, oxygen atom, sulfuratom or -CH = CH-, n is an integer of 1 to 6, and R' , R and R are the same or different andeach 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 is double bond, N at the 1-position has nosubstituent R, R is cyano group, and R is amino group or a salt thereof, azido group, adiphenyl lower alkyl amino group, a substituted phenyl amino group, a substitutedpiperazinyl group, a substituted homopiperazinyl group, an amino acid residue bondedby N terminal group in which C terminal group is carboxyl group or a lower alkyl esterthereof, or a lower alkyl amino group which may have an alkyl amino group that may becyclic one, or a salt thereof, which is useful as an active ingredient of an antiallergic agentand an antiinflammatory agent and has also an inhibitory activity against histaminerelease, 5-lipoxygenase inhibiting activity, relaxing activity of smooth musculus trachealisand inhibitory activity against carrageenin edema, and further, is useful as medicine forprevention and treatment of bronchial asthma, allergic coryza, allergic conjunctivitis,urticaria, atopic dermatitis, other inflammatory diseases or the like.
申请人：Kaken Pharmaceutical Co., Ltd.
地址：No. 28-8, Honkomagome 2-chome Bunkyo-ku Tokyo JP
国籍：JP
代理机构：Türk, Gille, Hrabal, Leifert
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