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Discovery of novel aminobenzisoxazole derivatives as orally available factor IXa inhibitors.
Sakurada, Isao; Endo, Toshiya; Hikita, Katsuyoshi; Hirabayashi, Tomokazu; Hosaka, Yoshitaka; Kato, Yutaka; Maeda, Yoshitaka; Matsumoto, Shigeki; Mizuno, Takashi; Nagasue, Hiroshi; Nishimura, Teruyuki; Shimada, Shunsuke; Shinozaki, Mikihiko; Taguchi, Keiko; Takeuchi, Katsutoshi; Yokoyama, Tooru; Hruza, Alan; Reichert, Paul; Zhang, Ting; Wood, Harold B; Nakao, Kazunari; Furusako, Shoji.
Afiliación
  • Sakurada I; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan. Electronic address: isao.sakurada@mochida.co.jp.
  • Endo T; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Hikita K; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Hirabayashi T; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Hosaka Y; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Kato Y; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Maeda Y; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Matsumoto S; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Mizuno T; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Nagasue H; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Nishimura T; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Shimada S; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Shinozaki M; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Taguchi K; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Takeuchi K; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Yokoyama T; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Hruza A; Department of Structural Chemistry, Merck Research Laboratories, Merck and Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Reichert P; Department of Structural Chemistry, Merck Research Laboratories, Merck and Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Zhang T; Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Wood HB; Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co., Inc., 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA.
  • Nakao K; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
  • Furusako S; Discovery Research, Mochida Pharmaceutical Co. Ltd., 722 Uenohara, Jimba, Gotemba, Shizuoka 412-8524, Japan.
Bioorg Med Chem Lett ; 27(11): 2622-2628, 2017 06 01.
Article en En | MEDLINE | ID: mdl-28408226
Using structure based drug design, novel aminobenzisoxazoles as coagulation factor IXa inhibitors were designed and synthesized. Highly selective inhibition of FIXa over FXa was demonstrated. Anticoagulation profile of selected compounds was evaluated by aPTT and PT tests. In vitro ADMET and pharmacokinetic (PK) profiles were also evaluated.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Factor IXa / Isoxazoles Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Factor IXa / Isoxazoles Tipo de estudio: Prognostic_studies Límite: Animals / Humans Idioma: En Revista: Bioorg Med Chem Lett Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido