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Bioorganic & Medicinal Chemistry Letters | 1997

Novel low molecular renin inhibitors which show good oral blood pressure lowering effects in marmosets

Yasuki Yamada; Koji Ando; Kazuya Komiyama; Saizo Shibata; Ikuro Nakamura; Yoshiharu Hayashi; Kiyoteru Ikegami; Itsuo Uchida

A series of low molecular renin inhibitors (molecular weight ∗< 600) were prepared and their biological activities were evaluated. The inhibitors containing indole-2-carbonyl moieties at the P3 position and 2-amino-3,5-anti-diol fragment at the P1-P1′ position showed renin inhibitory activities with IC50 of 10−8 M order and good blood pressure lowering effects after oral administration to sodium-depleted marmosets.


Tetrahedron-asymmetry | 1999

Diastereoselective aldol reaction of an α-alkoxycarbonylamino aldehyde with a silyl enol ether

Yasuki Yamada; Eiji Shirakawa; Koji Ando; Saizo Shibata; Itsuo Uchida

Abstract The aldol reaction of optically active α-alkoxycarbonylamino aldehydes with a silyl enol ether in the presence of a Lewis acid afforded γ-amino-β-hydroxyketones diastereoselectively. The effect of the α-amide proton on the diastereoselectivity is discussed.


Journal of Medicinal Chemistry | 2000

4-Aminoquinolines: novel nociceptin antagonists with analgesic activity.

Hisashi Shinkai; Takao Ito; Tetsuya Iida; Yuki Kitao; Hideki Yamada; Itsuo Uchida


Journal of Medicinal Chemistry | 1998

Isoxazolidine-3,5-dione and Noncyclic 1,3-Dicarbonyl Compounds as Hypoglycemic Agents

Hisashi Shinkai; Syoji Onogi; Masahiro Tanaka; Tsutomu Shibata; Megumi Iwao; Korekiyo Wakitani; Itsuo Uchida


Journal of Medicinal Chemistry | 2000

Bis(2-(Acylamino)phenyl) Disulfides, 2-(Acylamino)benzenethiols, and S-(2-(Acylamino)phenyl) Alkanethioates as Novel Inhibitors of Cholesteryl Ester Transfer Protein

Hisashi Shinkai; Kimiya Maeda; Takahiro Yamasaki; Hiroshi Okamoto; Itsuo Uchida


Journal of Medicinal Chemistry | 1996

Synthesis and Selective Coronary Vasodilatory Activity of 3,4-Dihydro-2,2-bis(methoxymethyl)-2H-1-benzopyran-3-ol Derivatives: Novel Potassium Channel Openers

Hidetsura Cho; Susumu Katoh; Shinsuke Sayama; Kengo Murakami; Hiroyuki Nakanishi; Yasuyuki Kajimoto; Hiroshi Ueno; Hisashi Kawasaki; Kazuo Aisaka; Itsuo Uchida


Journal of Medicinal Chemistry | 2004

Synthesis and structure-activity relationships of 5,6,7,8-tetrahydro-4H-thieno[3,2-b]azepine derivatives: novel arginine vasopressin antagonists.

Hidetsura Cho; Kengo Murakami; Hiroyuki Nakanishi; Akitaka Fujisawa; Hirotaka Isoshima; Misako Niwa; Kazuhide Hayakawa; Yasunori Hase; Itsuo Uchida; Hidenori Watanabe; Korekiyo Wakitani; Kazuo Aisaka


Journal of Organic Chemistry | 1998

A Practical Synthesis of Nelfinavir, an HIV-Protease Inhibitor, Using a Novel Chiral C4 Building Block: (5R,6S)-2,2-Dimethyl-5-hydroxy-1,3-dioxepan-6-ylammonium Acetate

Takashi Inaba; Angela G. Birchler; Yasuki Yamada; Shoichi Sagawa; Katsuyuki Yokota; and Koji Ando; Itsuo Uchida


Journal of Medicinal Chemistry | 2005

Synthesis and structure-activity relationships of novel selective factor Xa inhibitors with a tetrahydroisoquinoline ring.

Hiroshi Ueno; Katsuyuki Yokota; Jun-ichi Hoshi; Katsutaka Yasue; Mikio Hayashi; Yasunori Hase; Itsuo Uchida; Kazuo Aisaka; Susumu Katoh; Hidetsura Cho


Archive | 1994

Chroman derivative and pharmaceutical use thereof

Hidetsura Cho; Shinsuke Sayama; Susumu Katoh; Kazuo Aisaka; Itsuo Uchida

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