Nisshin Flour Milling Co., Ltd.

Masao Nagase

Toshihiro Takahashi

Hitoshi Inoue

Koichi Nakamaru

Masanori Sugita

Masato Horigome

Kenichi Momose

Chikako Suzuki

Shinji Nagai

Kouichi Katsuyama

Yoshiyuki Tahara

Hiroyasu Koyama

Yoshikuni Suzuki

Noriyoshi Sueda

Masahiro Tsuji

Toshiji Sugai

Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R; R represents pyridyl or substituted amino of NR.sub.1 R.sub.2 ;

Indole derivatives

Disclosed are indole derivatives of formula (I) ##STR1## wherein X and Y each independently represent H or --CH.sub.2 CH.sub.2 R;

Disclosed are indole derivatives of formula (I) ##STR1## wherein Y represents H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or halogen;

Indole derivatives and anti-ulcer compositions thereof

Four different optical isomers of a new compound, 1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4'-isocarbostyriloxy)-2-p ropanol are now provided as new substances. These four optical isomers are now named as (2R, 1'S)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4'-isocarbostyriloxy )-2-propanol, (2S, 1'S)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4'-isocarbostyriloxy )-2-propanol, (2S, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4'-isocarbostyriloxy )-2-propanol, and (2R, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4'-isocarbostyriloxy )-2-propanol, respectively. These four optical isomers have different activities for their .beta.-adrenergic-blocking effect and .alpha.-adrenergic-blocking effect and are useful as valuable agents for therapeutic treatment of various cardiovascular diseases, as compared to an optically inactive racemic mixture of said isomer compounds. These four optical isomers may be produced and isolated from each other by chromatographing (1'S)- or (1'R)-N-[2'-(o-methoxyphenoxy)-1'-methylethyl]-5-(4'-isocarbostyriloxymeth yl)-2-oxazolidones to isolate either its (5R, 1'S)-isomer and its (5S, 1'S)-isomer, or its (5S, 1'R)-isomer and its (5R, 1'R)-isomer therefrom separately and then hydrolyzing each of these isolated isomers under alkaline conditions to obtain separately (2R, 1'S)-, (2S, 1'S)-, (2S, 1'R)- and (2R, 1'R)-1-[2'-(o-methoxyphenoxy)-1'-methylethylamino]-3-(4'-isocarbostyriloxy )-2-propanols.

Optically active isocarbostyril derivatives and a method of preparing

Compounds of the structure ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as herein defined, effective as .beta.-blockers and hypotensive agents, are described.

Isocarbostyril derivatives

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Saitama, Japan

Masao Nagase