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Dive into the research topics where Yuichiro Kai is active.

Publication


Featured researches published by Yuichiro Kai.


Bioorganic & Medicinal Chemistry Letters | 2008

Orally active factor Xa inhibitors: investigation of a novel series of 3-amidinophenylsulfonamide derivatives using an amidoxime prodrug strategy.

Masahiko Uchida; Kosuke Okazaki; Harunobu Mukaiyama; Hidetoshi Isawa; Hiroaki Kobayashi; Hiroaki Shiohara; Hideyuki Muranaka; Yuichiro Kai; Norihiko Kikuchi; Hideki Takeuchi; Kenji Yokoyama; Eiichi Tsuji; Tomonaga Ozawa; Yuji Hoyano; Takashi Koizumi; Keiko Misawa; Kiyoto Hara; Shigeru Nakano; Yasuoki Murakami; Hiroaki Okuno

A series of novel and potent 3-amidinophenylsulfonamide derivatives of factor Xa inhibitors were designed and synthesized using an amidoxime prodrug strategy. We focused on systemic clearance of parent compounds in rats, and performed in vivo pharmacokinetic screening. Incorporation of a carboxymethoxy group markedly improved systemic clearance (compound 43), and the related amidoxime 44 showed sufficient prodrug conversion. Compound 45, the double prodrug of 43, exhibited practicable bioavailability after oral administration in rats. Among the various compounds under investigation, KFA-1982 was selected for clinical development.


Archive | 1998

3-amidinoaniline derivatives, activated blood coagulation factor x inhibitors, and intermediates for producing both

Satoshi Akahane; Masahiko Uchida; Hideotoshi Isawa; Norihiko Kikuchi; Tomonaga Ozawa; Hiroaki Kobayashi; Yuichiro Kai; Kenji Akahane


Archive | 2004

Amino alcohol derivatives, pharmaceutical compositions containing the same, and use thereof

Junichi Kobayashi; Tetsuya Nakamura; Ritsu Suzuki; Hideyuki Kissei Pharmaceutical Co. Ltd. Muranaka; Tomonaga Ozawa; Yuichiro Kai; Takehiro Ishikawa; Tatsuhiro Kondo; Tetsuro Kissei Pharmaceutical Co. Ltd. Tamai; Satoshi Akahane


Archive | 2001

5-amidino-2-hydroxybenzenesulfonamide derivatives, pharmaceutical compositions containing the same and intermediates for their preparation

Kosuke Okazaki; Masahiko Uchida; Harunobu Mukaiyama; Hiroaki Kobayashi; Yuichiro Kai; Hideki Takeuchi; Kenji Yokoyama; Yoshihiro Terao; Yuji Hoyano; Hiroaki Shiohara; Norihiko Kikuchi


Archive | 2002

5-amidino-2-hydroxybenzenesulfonamide derivatives, medicinal compositions containing the same, medicinal use thereof and intermediates in the production thereof

Masahiko Uchida; Hiroaki Kobayashi; Yuichiro Kai; Kenji Yokoyama; Yoshihiro Terao; Hideyuki Muranaka


Archive | 2000

3-amidinobenzenesulfonamide derivatives, medicinal compositions containing the same and intermediates in the production thereof

Satoshi Akahane; Masahiko Uchida; Hidetoshi Isawa; Norihiko Kikuchi; Yuichiro Kai; Kiyoto Hara; Toshiki Honma


Archive | 2002

5-amidino-n-(2-aminophenethyl)-n-hydroxy-benzenesulffonamide derivative, medical composition containing the same, pharmaceutical use thereof and intermediate therefor

Kosuke Okazaki; Masahiko Uchida; Hiroaki Kobayashi; Yuichiro Kai; Hideki Takeuchi; Kenji Yokoyama; Yoshihiro Terao; Ritsu Suzuki


Organic Process Research & Development | 2012

Crystallization Control and Physicochemical Properties of Polymorphic Forms of the Factor Xa Inhibitor KFA-1982

Hideki Takeuchi; Koji Kamata; Eiichi Tsuji; Harunobu Mukaiyama; Yuichiro Kai; Kenji Yokoyama; Kazumichi Jo; Katsuhide Terada


Archive | 2003

Novel crystals of 5-hydroxycarbamimidoyl-2-hydroxybenzenesulfonamide derivative

Harunobu Mukaiyama; Yuichiro Kai; Hideki Takeuchi; Kenji Yokoyama; Yoshihiro Terao; Satoshi Akahane


Archive | 2002

5-amidino-n-(2-aminophenethyl)-hydroxybenzenesulfonamide derivative, medicinal composition containing the same, and intermediate therefor

Kosuke Okazaki; Masahiko Uchida; Hiroaki Kobayashi; Yuichiro Kai; Hideki Takeuchi; Kenji Yokoyama; Yoshihiro Terao; Ritsu Suzuki

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Yasuoki Murakami

Chiba Institute of Science

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