- Emedastine hydrochloride intermediate compound and preparation method thereof
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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
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- Substituted 4-(1H-benzimidazol-2-yl)[1,4]diazepanes useful for the treatment of allergic disease
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The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. 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.
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- Synthesis of benzimidazole derivatives as antiallergic agents with 5- lipoxygenase inhibiting action
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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.
- Nakano, Hiroyuki,Inoue, Tsutomu,Kawasaki, Nobuhide,Miyataka, Hideki,Matsumoto, Hitoshi,Taguchi, Takeo,Inagaki, Naoki,Nagai, Hiroichi,Satoh, Toshio
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p. 1573 - 1578
(2007/10/03)
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- 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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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.
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- Synthesis and antihistaminic H1 activity of 1,2,5(6)-trisubstituted benzimidazoles
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A number of benzimidazoles, having several substituents on the azole and benzene nuclei and C-2 (methylamino, ethylenediamine, morpholine, piperazine and piperidine) were prepared. Regioselective synthesis was designed for the N1-alkyl substituted benzimidazoles (14-15). X-Ray structure analysis of (14) was also revealed. Compounds were evaluated for their in vitro H1- antihistaminic activity in the isolated guinea-pig ileum method. The compound (11) exhibits best activity.
- Goeker, Hakan,Ayhan-Kilcigil, Guelguen,Tuncbilek, Meral,Kus, Canan,Ertan, Rahmiye,Kendi, Engin,Oezbey, Sueheyla,Fort, Merce,Garcia, Celia,Farre, Antonio J.
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p. 2561 - 2573
(2007/10/03)
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