Nisshin Flour Milling Co., Ltd.

Hiroyasu Koyama

Yoshiyuki Tahara

Toshihiro Takahashi

Reiko Kubota

Yasuhiro Komatsu

Yoshikuni Suzuki

Teruhito Yamaguchi

Toshiji Sugai

Hiroaki Yamada

Masahiro Tsuji

Einosuke Sakurai

Katsutoshi Miura

Noriyoshi Sueda

Masato Horigome

Masao Nagase

Hiroaki Satoh

Koichiro Hagihara

Katsura Kogure

Hitoshi Inoue

Kunio Nakagawa

Koichi Watanabe

Hirohiko Komatsu

Masatoshi Yasuda

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;

Disclosed are a compound of the formula ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl or a group --(CH.sub.2).sub.n COOR.sup.3 in which n is an integer of 1 to 4 and R.sup.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, and R.sup.2 is a group --CH.dbd.CH--R.sup.4 or --CH.sub.2 --CH.sub.2 --R.sup.4 in which R.sup.4 is substituted or unsubstituted phenyl or a substituted or unsubstituted 5-membered heterocyclic group, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient. The compounds have an excellent chemical mediator inhibitory activity.

Rhodanine derivatives and pharmaceutical compositions

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

New antiviral nonaprenylamine derivatives represented by the following formula ##STR1## wherein R is 4 or 5 atoms selected from the group consisting of C and N so as to complete, with the non-R nitrogen, a 5- or 6-membered heterocyclic ring, and X is selected from the group consisting of H and hydroxy-lower alkyl and non-toxic, pharmaceutically acceptable acid addition salts thereof and a pharmaceutically acceptable carrier.

Interferon inducing, anti-vaccinia, and/or anti-influenza compositions

2,6-Dimethyl-4-(2- or 3-substituted phenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid diesters, having vasodilating and blood pressure lowering effects, in the ester moiety at the 3-position of which a heterocyclic group is linked to an alkylene group through an ester bond (carbonyloxy group). The diesters are used for treatment of cardiac diseases, cerebrovascular diseases and hypertension.

1,4-dihydropyridine derivatives, and pharmaceutical compositions

Nonyl prenyl-N heterocyclic compounds are prepared, useful as antivirals.

Nonyl prenyl-N heterocyclics

A compound of the formula ##STR1## wherein R.sub.1 is a phenethyl group, R.sub.2 and R.sub.3, taken together with the nitrogen atom to which they are bonded, form an N' hydroxylalkyl substituted piperazine, and (aklylene) is a lower alkylene chain substituted with a hydroxyl group; or an acid addition salt thereof is described.

Isoprenylamine derivatives

This invention relates to isoprenylamine derivatives and acid addition salts thereof, which compounds are useful for controlling virus infection of vertebrate animals.

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

A compound of the formula ##STR1## wherein R.sub.1 is a phenethyl group, R.sub.2 is a hydrogen atom, R.sub.3 is a lower alkyl group, and (alkylene) is a lower alkylene chain substituted with a hydroxyl group; or an acid addition salt thereof is described.

Compounds of the formula ##STR1## wherein R.sub.1 and R.sub.3 each is benzyl or substituted with up to 3 methoxy groups, R.sub.2 is a hydrogen atom and (alkylene) is lower alkyl and the compounds are useful for controlling viral infections.

This invention relates to new isoprenylamine derivatives and acid addition salts thereof, which are useful as medicines for controlling virus infection of vertebrate animals, or the intermediates therefor.

Compounds of the formula R.sub.1 --CO--NH.sub.2 wherein R.sub.1 is ##STR1## are described. The compounds are useful in the treatment of hypertension and hyperlipidemia.

Growing community of inventors

Ageo, Japan

Hiroyasu Koyama