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E Ohshima T Kumazawa H Takizawa H Harakawa H Sato H Obase Y Oiji A Ishii H Ishii K Ohmori 《Chemical & pharmaceutical bulletin》1991,39(10):2724-2728
A new series of 11-substituted 6,11-dihydrodibenz[b,e]oxepin derivatives was synthesized and evaluated for antiallergic activity. Convenient methods for the preparation of sulfides from alcohols were developed. Structure-activity relationships are described. Compound 7, 11-[2-(dimethylamin)ethyl]thio-6,11-dihydrodibenz[b,e] oxepin-2-carboxylic acid hydrochloride, was the most potent in the rat passive cutaneous anaphylaxis test (ED50 = 0.92 mg/kg p.o.). It had a potent inhibitory effect on anaphylactic bronchoconstriction in guinea pigs (ED50 = 0.029 mg/kg p.o.) and H1 receptor antagonistic effect (Ki = 14 nM) with few central nervous system side effects. Additionally, an antagonistic effect against prostaglandin D2-induced contraction of isolated guinea pig trachea (pA2 = 5.73) was an attractive mechanism of action of the new antiallergic agent. Compound 7 was selected for further evaluation as KW-4994. 相似文献
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Fukuji Higashi Khoji Nakajima Wen Xion Zhang 《Journal of polymer science. Part A, Polymer chemistry》1994,32(4):747-752
It is proposed that depression of the transition temperatures, especially the melting point (Tm), can be achieved by the introduction of a different amide bond structure into the copolyamides of dicarboxylic acids and diamines by copolymerization of aminocarboxylic acids, such as p-aminobenzoic acid. The effect was examined by the amount and distribution of the structure in the copolylamindes. Copolycondensations of PEG3, p-aminobenzoic acid, and diamines with different chain lengths showed that the structural change of the amide bond in the copolymers, especially its distribution, was more important than its total amount in them. Several types of aminocarboxylic acids were briefly examined to study the effect. © 1994 John Wiley & Sons, Inc. 相似文献
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A finite element method for solving shallow water flow problems is presented. The standard Galerkin method is employed for spatial discretization. The numerical integration scheme for the time variation is the explicit two step scheme, which was originated by the authors and their co-workers. However, the original scheme has been improved to remove the erroneous artifical damping effect. Since the improved scheme employs a combination of lumped and unlumped coefficients, the scheme is referred to as a selective lumping scheme. Stability conditions and accuracy are investigated by considering several numerical examples. The method has been applied to the tidal flow in Osaka Bay and Yatsushiro Bay. 相似文献
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Taisei Ueda Satoko Asai Khoji Oiji Shin-Ichi Nagai Akito Nagatsu Jinsaku Sakakibara 《Journal of heterocyclic chemistry》1997,34(3):761-764
Treatment of 5-acylamino-6-hydroxy (or benzoyloxy)methyl-3-phenylpyrimidin-4(3H)-one 5,10 with 5% aqueous sodium hydroxide in ethanol gave 2-alkyl-5-hydroxymethyl-4-phenylcarbamoyl-1H-imidazoles 7,11 . Oxidation of 5-amino-6-benzoyloxymethyl-3-phenylpyrimidin-4(3H)-one 9 in the presence of copper( II ) chloride in alcohol gave 2-alkoxy-5-alkoxymethyl-4-phenylcarbamoyl-1H-imidazoles 12a,b accompanied by 5-amino-6-alkoxymethyl-3-phenylpyrimidin-4(3H)-ones 13a,b. 相似文献
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T Kumazawa E Ohshima H Harakawa H Sato H Obase Y Oiji A Ishii H Ishii K Ohmori 《Chemical & pharmaceutical bulletin》1991,39(10):2729-2733
New methods for the preparation of multi-functionalized-6,11-dihydrodibenz[b,e]oxepins were developed. The structural requirements of KW-4994 (1), a promising orally active antiallergic agent, were defined. A carboxyl group at C-2 was critical for enhanced antiallergic activity of 1. The introduction of bromine atom at C-9 of 1 could elongate the duration of the action of the parent. Antiplatelet activity, a new pharmacological property of this series of compounds, was observed in one of the derivatives of 1. 相似文献
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