Nisshin Flour Milling Co., Ltd.

Toshiji Sugai

Hiroyasu Koyama

Einosuke Sakurai

Yoshikuni Suzuki

Hiroaki Yamada

Hiroaki Satoh

Noriyoshi Sueda

Katsutoshi Miura

Toshihiro Takahashi

Yoshiyuki Tahara

Norio Oshida

Masahiro Tsuji

Masato Horigome

Koichi Itoh

Masao Nagase

Hiroshi Sakai

Shinji Yokoyama

Tamiko Hamada

Tomomi Tonoike

Yoji Mimaki

Yukiko Muraki

Kazumi Nishimura

Makoto Yanai

Yasuhiko Suzuki

Koichi Watanabe

Motoharu Hasegawa

Kumiko Yamamoto

Kiyohiko Matsumoto

Kohji Shirai

Yuuiti Takarada

Isao Takahasi

Mitsuyo Saito

Yositaka Takayama

Tsutomu Komazawa

Pyridinecarboxamide derivatives

The use of isoquinolinone derivatives as an antiarteriosclerosis agent and antihyperlipoproteinemics. The derivatives are of the formula ##STR1## wherein R.sub.1 is hydrogen or a C.sub.1 -C.sub.6 alkyl group and R.sub.2 is a C.sub.1 -C.sub.6 alkyl group or the pharmaceutically acceptable salt thereof.

Method for treating hyperlipemia

Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.3 alkyl or diphenylmethyl; Y is --NH(CH.sub.2).sub.n --R.sub.2 ; R.sub.2 is OH or --ONO.sub.2 ; m is 2 or 3; and n is 9 to 13 or physiologically acceptable acid addition salts thereof. The compounds of formula (I) are of a blood flow-increasing and hypotensive actions and can be used for the therapy or prevention of diseases in the cardiovascular system.

Pyridinecarboxylic acid amide derivatives and pharmaceutical

Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen or C.sub.1 -C.sub.6 alkyl;

Nicotinic acid derivatives and pharmaceutical compositions comprising

Compounds are disclosed of the formula ##STR1## wherein R.sub.1 is hydrogen; C.sub.1 -C.sub.6 alkyl; C.sub.3 -C.sub.6 cycloalkyl or diphenylmethyl;

Compounds are described of formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, an alkoxy group, a dialkylamino group or a halogen atom; n is 1 to 4; R.sup.2 is a hydrogen atom, an alkyl group, an unsubstituted or substituted aminoalkyl group, an acyl group, an unsubstituted or substituted aralkyl group, a carboxyalkyl group, an alkoxycarbonyalkyl group or ##STR2## wherein X is an unsubstituted or substituted-phenyl, -benzyl, -benzoyl or -furoyl group; A is -NR.sup.3 - where R.sup.3 is hydrogen or alkyl, an alkylene or an alkylidene; and B is a heterocyclic group selected from triazolyl, pyridyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzimidazolyl, benzothiazolyl, quinolyl and isoquinolyl, said heterocyclic group being optionally substituted by one or more alkyl, alkoxy, nitro or phenyl group, and the physiologically acceptable acid addition salts thereof. The compound of formula (I) are or cardiotonic activity and thus may be useful for the treatment of circulatory diseases.

Benzimidazole derivatives

Compounds are described of the formula ##STR1## wherein R.sub.1 is a nitro or trifluoromethyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkyl group; R.sub.3 is a pyridyl or pyridyl N-oxide group which may be substituted with halogen, hydroxyl, haloalkyl, C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl and further may be fused with a benzene or naphthalene ring, said ring being optionally substituted with C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halogen or haloalkyl, and a pharmaceutically acceptable acid addition salt thereof. The compounds of the formula (I) are of vasodilating and blood pressure lowering activities and thus may be useful for the treatment of cardiac diseases, cerebrovascular diseases and hypertension.

1,4-Dihydropyridine derivatives and pharmaceutical compositions

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

Toshiji Sugai