Kowa Company Limited

Hiroshi Ishihama

Yasumi Uchida

Setsuro Fujii

Masami Shiratsuchi

Mitsuteru Hirata

Koichiro Watanabe

Eizou Hattori

Kiyoshi Kawamura

Hisashi Kunieda

Toshihiro Akashi

Hamao Umezawa

Yoshinori Kyotani

Hiroyuki Ishiwata

Yoshio Takahashi

Tomio Ohta

Noboru Shimizu

Masaji Oono

Anti-arteriosclerotic pyridyl or imidazolyl derivatives of

A novel racemate K-351A composed of an optical isomer (2'S),(3S)K-351 [3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2H-1-benzop yran] and (2'R),(3R)K-351, a novel racemate K-351B composed of an optical isomer (2'R),(3S)K-351 and (2'S),(3R)K351 and an acid addition salt of these two novel racemates; a process for converting the two racemates to each other; and also to a pharmaceutical composition comprising each of the two racemates useful for the treatment of cardiovascular diseases.

Racemates of

An optical isomer selected from the group consisting of (2'R),(3R)-3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2 H-1-benzopyran, (2'S),(3R)-3,4-dihydro-8-(2'-hydroxy-3'-isopropylamino)propoxy-3-nitroxy-2 H-1-benzopyran and acid addition salts of these isomers, process for producing these isomers and a pharmaceutical composition thereof useful for the treatment of cardiovascular diseases.

Optical isomers, processes for production thereof and pharmaceutical

Phenyl tetrahydronaphthylcarboxylate of the formula: ##STR1## wherein A is a direct bond, or a lower alkylene, vinylene or imino group; B is a direct bond, a lower alkylene or --NH-lower alkylene group, or an --OCH.sub.2 CO-- residual group; and R is a lower alkyl group, with the proviso that A and B are not direct bonds simultaneously, and A, B and R are not a lower alkylene group, a direct bond and a methyl group, respectively, at the same time, are effectively useful as chymotrypsin inhibitors.

1-isopropyl-4[(4-tetrahydro-1-naphthoyloxy

Benzoyl indolecarboxylates of the formula: ##STR1## where R.sup.1 is hydrogen, halogen, lower alkyl or lower alkoxy; R.sup.2 is hydrogen, lower alkyl, acetyl or benzoyl; R.sup.3 is hydrogen or lower alkyl; and A is a direct bond, or lower alkylene or vinylene substituted at the 2-, 3- or 5-position of the indole nucleus, are effective agents as chymotrypsin inhibitors.

Benzoyl indolecarboxylates

An azetidine derivative of the formula, ##STR1## wherein R is a hydrogen atom or a hydroxyl group, and R.sub.a, R.sub.b, R.sub.c, R.sub.a ', R.sub.b ' and R.sub.c ' are identical or different and each are a lower alkyl group.

3-Alkylidine azetidine compound and their production

A compound represented by the following formula ##STR1## wherein R represents a lower alkyl group having 2 to 6 carbon atoms, and n is an integer of from 1 to 5.

N-Nitroxyalkylene benzamide derivatives

A piperazine derivartive represented by the following formula: ##STR1## wherein R.sub.1 : an indolyl group which may optionally be substituted by one or more lower alkyl and/or lower alkoxy groups, naphthyl group which may optionally be saturated partially with 2 or 4 hydrogen atoms, or phenyl or cyclohexyl group which may optionally be substituted by one or more lower alkyl groups;

Growing community of inventors

Higashimurayama, Japan

Hiroshi Ishihama