87233-54-3Relevant articles and documents
Emedastine hydrochloride intermediate compound and preparation method thereof
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, (2017/09/01)
The invention provides an antihistamine medicine emedastine hydrochloride intermediate and a preparation method thereof, and is used for solving the problems of many reaction steps, operation complexity and high production cost in the preparation process
SUBSTITUTED N-METHYL-N-(4-(4-(1H-BENZIMIDAZOL-2-YL) {1,4}DIAZEPAN-1-YL)-2-(ARYL)BUTYL) BENZAMIDES USEFUL FOR THE TREATMENT OF ALLERGIC DISEASES
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, (2008/06/13)
The present invention relates to novel N-methyl-N-(4-(4-(1H-benzimidazol-2-yl)[1,4]diazepan-1-yl)-2-(aryl)butyl)benzamide derivatives of the formula: STR1 stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonists. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.
Synthesis of benzimidazole derivatives as antiallergic agents with 5- lipoxygenase inhibiting action
Nakano, Hiroyuki,Inoue, Tsutomu,Kawasaki, Nobuhide,Miyataka, Hideki,Matsumoto, Hitoshi,Taguchi, Takeo,Inagaki, Naoki,Nagai, Hiroichi,Satoh, Toshio
, p. 1573 - 1578 (2007/10/03)
Syntheses were conducted of novel benzimidazole derivatives that suppress histamine release from mast cells, inhibit 5-lipoxygenase, and possess antioxidative action. Among the compounds synthesized, 1-[2-[2-(4- hydroxy-2,3,5-trimethylphenoxy)ethoxy]ethyl]-2-(4-methyl-1- homopiperazino)benzimidazole (22) potently suppressed histamine release from rat peritoneal mast cells triggered by the antigen-antibody reaction, inhibited 5-lipoxygenase in rat basophilic leukemia-1 (RBL-1) cells, and prevented the NADPH-dependent lipid peroxidation induced by Fe3+-ADP in rat liver microsomes, in addition to an antagonizing the contraction of guinea pig ileum caused by histamine.