Synthesis and Evaluation of 1-Arylsulfony1-3-piperazinone Derivatives as Factor Xa Inhibitors^<1-3)> IV. A Series of New Derivatives Containing a Spiro [5H-oxazolo [3, 2-a] pyrazine-2 (3H), 4'-piperidin] -5-one Skeleton
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概要
- 論文の詳細を見る
In the course of development of factor Xa (FXa) inhibitor in an investigation involving the synthesis of 1-arylsulfony1-3-piperazinone derivatives, we found new compounds containing a unique spiro skeleton. Among such compounds, (-) -7- [(6-chloro-2-naphthalenyl) sulfonyl] tetrahydro-8a- (methoxymethyl) -1'- (4-pyridinyl) -spiro [5H-oxazolo [3, 2-a] pyrazine-2 (3H), 4'-piperidin] -5-one (28, M55529) had activity more favorable than those of previously reported compounds. The inhibitory activity of M55529 for FXa is IC_<50>=2 nM, with high selectivity for FXa over thrombin and trypsin.
- 公益社団法人日本薬学会の論文
- 2004-04-01
著者
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Mizuno Masashi
Division Of Science Of Biological Resources The Graduate School Of Science And Technology
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Mizuno Masashi
Division Of Life Science Graduate School Of Science And Technology Kobe University
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Mizuno Masashi
Graduate School Of Science And Technology Kobe University
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Mizuno Masashi
Nagano Japan Radio Co. Ltd. Currently With Kyushu Institute Of Technology
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Okamoto A
Discovery Research Center Mochida Pharmaceutical Co. Ltd.
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Mizuno M
Kobe Univ. Kobe Jpn
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NISHIDA Hidemitsu
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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MUKAIHIRA Takafumi
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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SAITOH Fumihiko
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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MATSUSUE Tomokazu
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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OKAMOTO Atsushi
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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HOSAKA Yoshitaka
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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MATSUMOTO Miwa
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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OHNISHI Shuhei
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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MOCHIZUKI Hidenori
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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HARADA Kousuke
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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FUKUI Miyuki
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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SHIROMIZU Ikuya
Discovery Research Center, Mochida Pharmaceutical Co., Ltd.
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Okamoto Atsushi
Discovery Research Center Mochida Pharmaceutical Co. Ltd.
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Fukui M
Discovery Research Center Mochida Pharmaceutical Co. Ltd.
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Harada K
Roman Industries Co. Ltd.
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SAITOH Fumihiko
Pharmaceutical Research Center, Mochida Pharmaceutical Co., Ltd.
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NISHIDA Hidemitsu
Pharmaceutical Research Center, Mochida Pharmaceutical Co., Ltd.
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MUKAIHIRA Takafumi
Pharmaceutical Research Center, Mochida Pharmaceutical Co., Ltd.
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MATSUSUE Tomokazu
Pharmaceutical Research Center, Mochida Pharmaceutical Co., Ltd.
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SHIROMIZU Ikuya
Pharmaceutical Research Center, Mochida Pharmaceutical Co., Ltd.
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HOSAKA Yoshitaka
Pharmaceutical Research Center, Mochida Pharmaceutical Co., Ltd.
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Mizuno M
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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Morimoto M
Graduate School Of Science And Technology Kobe University
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Saitoh F
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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Shiromizu Ikuya
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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Hosaka Y
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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Matsusue Tomokazu
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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Nishida H
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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Mochizuki Hidenori
Discovery Research Center Mochida Pharmaceutical Co. Ltd.
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Mukaihira Takafumi
Pharmaceutical Research Center Mochida Pharmaceutical Co. Ltd.
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