Piperidine Carboxylic Acid Derivatives of 10H-Pyrazino[2,3-b][1,4] benzothiazine as Orally-Active Adhesion Molecule Inhibitors
スポンサーリンク
概要
- 論文の詳細を見る
Novel piperidine carboxylic acid derivatives of 10H-pyrazino[2, 3-b][1, 4]benzothiazine were prepared and evaluated for their inhibitory activity on the upregulation of adhesion molecules such as intercellular adhesion molecule-1 (ICAM-1). Replacement of the methanesulfonyl group on the piperidine ring of previously prepared derivatives with a carboxylic acid-containing moiety resulted in a number of potent adhesion molecule inhibitors. Of these, (anti) [3-(10H-pyrazino[2, 3-b][1, 4]benzothiazin-8-yl)methyl-3-azabicyclo[3.3.1]non-9-yl]acetic acid 2q (ER-49890), showed the most potent oral inhibitory activities against neutrophil migration in an interleukin-1 (IL-1) induced paw inflammation model using mice, and leukocyte accumulation in a carrageenan pleurisy model in the rat, and therapeutic effect on collagen-induced arthritis in rats.
- 社団法人日本薬学会の論文
- 2004-06-01
著者
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竹中 修
京都大学霊長類研究所
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KOBAYASHI Seiichi
Eisai Research Institute, Eisai Co., Ltd
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竹中 修
京大・霊長類研
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CLARK Richard
Tsukuba Research Laboratories, Eisai Co., Ltd.,
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Clark R
Eisai Co. Ltd. Ibaraki Jpn
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Kaneko Tetsuo
Department Of Pharmaceutical Science Hiroshima International University
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Kobayashi S
Eisai Research Institute Of Boston Inc.
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Kobayashi Seiichi
Eisai Research Institute Eisai Co. Ltd
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KANEKO Toshihiko
Tsukuba Research Laboratories, Eisai Co. Ltd.
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OHI Norihito
Tsukuba Research Laboratories, Eisai Co. Ltd.
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OZAKI Fumihiro
Tsukuba Research Laboratories, Eisai Co. Ltd.
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KAWAHARA Tetsuya
Tsukuba Research Laboratories, Eisai Co. Ltd.
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KAMADA Atsushi
Tsukuba Research Laboratories, Eisai Co. Ltd.
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OKANO Kazuo
Tsukuba Research Laboratories, Eisai Co. Ltd.
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YOKOHAMA Hiromitsu
Tsukuba Research Laboratories, Eisai Co. Ltd.
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OHKURO Masayoshi
Tsukuba Research Laboratories, Eisai Co. Ltd.
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MURAMOTO Kenzo
Tsukuba Research Laboratories, Eisai Co. Ltd.
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TAKENAKA Osamu
Tsukuba Research Laboratories, Eisai Co. Ltd.
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Okano K
Eisai Co. Ltd. Ibaraki Jpn
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Okano Kazuo
Department Of Electrical System Engineering Polytechnic University
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Muramoto Kenzo
Tsukuba Research Laboratories Eisai Co. Ltd.
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Takenaka O
Kyoto University
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Takenaka O
Tsukuba Research Laboratories Eisai Co. Ltd.
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Takenaka Osamu
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kamada Atsushi
Department Of Agricultural Chemistry The University Of Tokyo
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Ohi Norihito
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kobayashi Shoichi
Laboratory Of Food And Health Science Department Of Agro-bioscience Faculty Of Agriculture Iwate Uni
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Kamada Atsushi
Tsukuba Research Laboratories Eisai Co. Ltd.
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Ohkuro Masayoshi
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kawahara Tetsuya
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kaneko Toshihiko
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kobayashi Shigeki
Department Of Analytical Chemistry Of Medicines Showa Phamaceutical University
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Yokohama Hiromitsu
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kobayashi Shigeki
Department Of Analytical Chemistry Of Medicines Showa Pharmaceutical University
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Kaneko T
Department Of Pharmaceutical Science Hiroshima International University
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Clark Richard
Tsukuba Research Laboratories Eisai Co. Ltd.
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Kobayashi Shigeki
Div. Of Analytical Chemistry Of Medicines Showa Pharmaceutical Univ.
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Kawahara T
Department Of Nutrition School Of Medicine University Of Tokushima
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Kawahara T
Hiroshima Univ. Higashi‐hiroshima Jpn
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