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Negi Shigeto, Miyazawa Mamoru: (Ja) 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物およびその製造方法, (En) Composition containing chloromethyl phosphate derivative with improved stability and process for producing the same. Eisai R & D Management, Negi Shigeto, Miyazawa Mamoru, INABA Yoshiyuki, March 22, 2007: WO/2007/032263 (23 worldwide citation)

(EN) A process for producing a chloromethyl phosphate derivative useful for producing a water-soluble prodrug. It is excellent in working, operation, and energy saving. The process, which is for producing a composition comprising a compound represented by the following formula (I) and a tertiary ami ...


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Yoshizawa Kazuhiro, Nakamura Taiju, Negi Shigeto: (Ja) イソインドール誘導体の製造方法, (En) Process for the production of isoindole derivatives. Eisai R & D Management, Yoshizawa Kazuhiro, Nakamura Taiju, Negi Shigeto, SHIMIZU Hatsushi, February 23, 2006: WO/2006/018955 (4 worldwide citation)

(EN) A process for the production of isoindole derivatives (compounds (II)) represented by the general formula (II) or salts thereof: (II) [wherein R1 and R2 are each independently C1-6 alkyl], which comprises the step (1) of cyclizing a compound (I) represented by the general formula (I) or a salt ...


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Sato Keizo, Abe Shinya, Yoshizawa Kazuhiro, Wakasugi Kazunori, Negi Shigeto, Miyazawa Mamoru: (Ja) 安定性が改善されたクロロメチルフォスフェイト誘導体を含む組成物及びその製造方法, (En) Composition containing chloromethyl phosphate derivative with improved stability and method for producing the same. Eisai R & D Management, Sato Keizo, Abe Shinya, Yoshizawa Kazuhiro, Wakasugi Kazunori, Negi Shigeto, Miyazawa Mamoru, INABA Yoshiyuki, September 12, 2008: WO/2008/108384 (2 worldwide citation)

(EN) Disclosed is a method for producing a chloromethyl phosphate derivative which is useful for producing a water-soluble prodrug. This method is excellent from the viewpoints of workability, operability and energy saving. Specifically disclosed is a method for producing a composition containing a ...


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Machida Yoshimasa, Ikuta Hironori, Negi Shigeto, Nomoto Seiichiro, Saito Isao, Kitoh Kyosuke: Procede dobtention de derives de la 7.alpha.- methoxycephalosporine et remedes a proprietes antibacteriennes, 7.alpha.-methoxycephalosporin derivatives, process for the preparation thereof and antibacterial drugs containing the same. Negi Shigeto, Kitoh Kyosuke, Ikuta Hironori, Saito Isao, Nomoto Seiichiro, Eisai, MARKS & CLERK, April 17, 1984: CA1165759

Abstract of the disclosure: Novel 7.alpha.-methoxycephalosporin derivatives, theirpharmaceutically acceptable salts, process for thepreparation thereof, and antibacterial drugs involvingthe derivative or salt. The derivatives or salts areeffective against the Gram-positive bacteria and the Gram-nega ...


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Kai Yasunobu, Komatu Yuuki, Machida Yoshimasa, Nakamura Takaharu, Sugiyama Isao, Nomoto Seiichiro, Kamiya Takashi, Negi Shigeto, Naito Toshihiko, Yamauchi Hiroshi, Katsu Kanemasa, Kitoh Kyosuke: Derive de 2-propenylcephem, 3-propenylcephem derivative. Kai Yasunobu, Komatu Yuuki, Machida Yoshimasa, Nakamura Takaharu, Sugiyama Isao, Nomoto Seiichiro, Kamiya Takashi, Negi Shigeto, Naito Toshihiko, Yamauchi Hiroshi, Katsu Kanemasa, Kitoh Kyosuke, Eisai, MARKS & CLERK, October 15, 1991: CA1290748

ABSTRACT A 3-propenylcephem derivative of the followingformula: Imagewherein R1 represents a fluoro-substituted lower alkylgroup or a cyano-substituted lower alkyl group, and Arepresents a cyclic or an acylic ammonio group, or apharmaceutically acceptable salt thereof, exhibitingexcellent anti-bacte ...


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Kamiya Takashi, Machida Yoshimasa, Katsu Kanemasa, Yamauchi Hiroshi, Negi Shigeto, Naito Toshihiko, Kitoh Kyosuke, Nomoto Seiichiro, Sugiyama Isao, Komatu Yuuki, Kai Yasunobu, Nakamura Takaharu: Intermediaires pour la preparation de derives 3-propenylcephem, Intermediates for preparing 3-propenylcephem derivatives. Kamiya Takashi, Machida Yoshimasa, Katsu Kanemasa, Yamauchi Hiroshi, Negi Shigeto, Naito Toshihiko, Kitoh Kyosuke, Nomoto Seiichiro, Sugiyama Isao, Komatu Yuuki, Kai Yasunobu, Nakamura Takaharu, Eisai, MARKS & CLERK, July 21, 1992: CA1305487

ABSTRACT A 3-propenylcephem derivative of the followingformula: Imagewherein R1 represents a fluoro-substituted lower alkylgroup or a cyano-substituted lower alkyl group, and Arepresents a cyclic or an acylic ammonio group, or apharmaceutically acceptable salt thereof, exhibitingexcellent anti-bacte ...


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Kayano Akio, Chiba Hiroyuki, Nakamura Taiju, Sakurai Shin, Ishizuka Hiroyuki, Saito Hiroyuki, Komatsu Yuuki, Sasho Manabu, Sato Nobuaki, Negi Shigeto: Process for the preparation of basic antibiotic-inorganic acid addition salts and intermediate oxalates. Eisai, Kayano Akio, Chiba Hiroyuki, Nakamura Taiju, Sakurai Shin, Ishizuka Hiroyuki, Saito Hiroyuki, Komatsu Yuuki, Sasho Manabu, Sato Nobuaki, Negi Shigeto, FURUYA Kaoru, February 8, 2001: WO/2001/009135

An industrially excellent novel process for the preparation of addition salts of basic antibiotics with inorganic acids (such as hydrochloric acid), by subjecting a basic antibiotic-oxalic acid addition salt (II) to salt-exchange with an inorganic acid salt (III) of an alkaline earth metal, wherein ...


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Negi Shigeto, Shimizu Toshikazu, Kuroda Hiroshi, Shimomura Naoyuki, Sasho Manabu, Hoshino Yorihisa, Kubota Manabu: (Ja) ピラゾール縮合環誘導体の製造方法, (En) Process for production of pyrazole-fused ring derivatives. Eisai R & D Management, Negi Shigeto, Shimizu Toshikazu, Kuroda Hiroshi, Shimomura Naoyuki, Sasho Manabu, Hoshino Yorihisa, Kubota Manabu, INAMI Minoru, October 27, 2005: WO/2005/100354

(EN) The invention aim at finding intermediates useful in the synthesis of pyrazole-fused ring derivatives (such as 7-phenylpyrazolo[1,5-a]pyridine derivatives) and a process for the production thereof. A process for the production of compounds represented by the general formula (II), salts thereof, ...


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Sasyou Manabu, Haga Toyokazu, Kayano Akio, Negi Shigeto, Naka Hiroyuki: Pyrrolidine derivative and process for producing the same. Eisai, Sasyou Manabu, Haga Toyokazu, Kayano Akio, Negi Shigeto, Naka Hiroyuki, INAMI Minoru, October 24, 2002: WO/2002/083636

A pyrrolidine derivative which is an intermediate for a quinuclidine derivative side chain useful as a squalene synthase inhibitor. It is a pyrrolidine derivative (X) represented by the following formula (X) (wherein R?1¿ and R?2¿ each means hydroxy, C¿1-6? alkoxy, etc.; and R?3¿ means hydrogen, ben ...