Synthesis and Angiotensin Converting Enzyme-Inhibitory Activity of 1,5-Benzothiazepine and 1,5-Benzoxazepine Derivatives. III

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概要

• 論文の詳細を見る

• A seires of (R)-3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-5-acetic acids (8) and (S)-3-amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzoxazepine-5-acetic acids (9) having an (S)-1-carboxy-ω-(4-piperidyl)alkyl group on the amino group at the 3-position was prepared as part of a search for long-acting inhibitors of the angiotensin converting enzyme (ACE). The length (n) of the carbon chain in the piperidylalkyl moiety was varied from two six in order to determine the optimal structure. The most prolonged activity in vivo was observed with (R)-3-[(S)-1-carboxy-5-(4-piperidyl)pentyl]amino-4-oxo-2,3,4,5-tetrahydro-1,5-benzothiazepine-5-acetic acid (8c : CV-5975) on i.v. and p.o. administrations.

• 社団法人日本薬学会の論文
• 1986-09-25

著者

• 西川 浩平

  日本製薬株式会社研究本部

• 西川 浩平

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 伊藤 克己

  Pharmaceutical Research Laboratories Iii Pharmaceutical Research Division Takeda Chemical Industries

• 稲田 義行

  武田薬品工業株式会社研究推進部

• 郡 正城

  Pharmaceutical Research Laboratories, Takeda Chemical Industries, Ltd.,

• 伊藤 克己

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 郡 正城

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 稲田 義行

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 西川 浩平

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 川松 豊

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 杉原 弘貞

  Central Research Division, Takeda Chemical Industries, Ltd.,

• 伊藤 克巳

  武田薬品工業

• 伊藤 克已

  Central Research Division Takeda Chemical Industries Ltd.

• 川松 豊

  干寿製薬株式会社経営戦略室

• 郡 正城

  Pharmaceutical Research Laboratories Takeda Chemical Industries Ltd.

• 稲田 義行

  武田薬品工業株式会社 医療開拓研究本部

• 杉原 弘貞

  Pharamaceutical Research Laboratories I Pharmaceutical Research Division Takeda Chemical Industries

• 杉原 弘貞

  Central Research Division Takeda Chemical Industries. Ltd.

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