Taisho Pharmaceutical Co., Ltd.

Jiro Sawada

Kaoru Sota

Takehiro Amano

Toshihisa Ogawa

Yoshiaki Watanabe

Katsuo Hatayama

Toshifumi Asaka

Sadafumi Omura

Kazuya Kameo

Kazunori Hanada

Chihiro Yokoo

Kensei Yoshikawa

Masaharu Tamai

Shoichi Ito

Michitada Sasajima

Yasuhide Tachi

Ichiro Tanaka

Kazuyuki Tomisawa

Shigeo Morimoto

Tohru Tanami

Yoshiaki Kamano

Yutaka Ohuchi

Sadakazu Yokomori

Tatsuhiko Sano

Akira Onodera

Masami Goi

Kiyoshi Oguma

Toru Matsunaga

Jozi Nakagami

Kazuhiko Michishita

Yoshinori Shiobara

Aturo Nakazato

Michinori Shibata

Sadao Machida

Kazuaki Kyogoku

Mitsunori Washitake

The compounds of the formula ##STR1## wherein R is alkyl having 1 to 4 carbon atoms or nitratoalkyl having 2 or 3 carbon atoms, and R' is nitratoalkyl having 2 or 3 carbon atoms, are disclosed. These compounds are useful as therapeutic agents for cardiovascular disorders such as coronary artery disease, cerebral artery disease, hypertension and the like.

1,4-Dihydropyridine derivatives and use as vasodilators

Novel compounds having the general formula ##STR1## wherein X is hydrogen or halogen, Y is hydrogen, halogen, methoxy or alkyl having 1 to 3 carbon atoms, Z is hydrogen, alkylcarbonyl having 2 to 6 carbon atoms or benzoyl, and R is hydrogen, alkali metal or alkyl having 1 to 5 carbon atoms, are disclosed. These compounds exhibit excellent hypolipidemic activity and little or no side effect.

3-Benzoyl-2-mercaptopropionic acid derivatives

A novel carboxylic acid ester having the following general formula ##STR1## wherein R is alkoxyalkyl having 2 to 6 carbon atoms, cycloalkyl having 5 or 6 carbon atoms, tetrahydrofurfuryl, or alkyl having 1 to 6 carbon atoms optionally substituted with 1 or 2 hydroxyl groups, is a useful anti-inflammatory and analgesic agent.

Esters of the carboxylic acid

The epoxysuccinic acid derivatives of this invention are prepared by esterification of an epoxysuccinic acid or a halide thereof, by partial hydrolysis of an epoxysuccinic acid diester, by amidation of an epoxysuccinic acid monoester, or by hydrolysis of an epoxysuccinic acid amide monoester. These epoxysuccinic acid derivatives have excellent thiol protease inhibitory activity and anti-inflammatory activity without the acceleration of vascular permeability.

Epoxysuccinic acid derivatives

The epoxysuccinamic acid compounds of the present invention are prepared by reaction of monoesters of epoxysuccinic acid or monoesters of epoxysuccinic acid chloride with amino compounds. These epoxysuccinamic acid compounds have excellent anti-inflammatory activity, thiol protease inhibitory activity, muscular dystrophy inhibitory activity and anti-hypertensive activity without acceleration of vascular permeability.

Epoxysuccinamic acid compounds

Novel cephalosporin compounds having the general formula ##STR1## wherein X represents hydrogen atom or hydroxy group, and the non-toxic pharmacologically acceptable salts thereof are disclosed. These compounds are useful as antibacterial agents.

Cephalosporin compounds

17.alpha.-butyryloxy-11.beta.-hydroxy-21-propionyloxy-4-pregnen-3,20-dione, i.e., hydrocortisone 17-butyrate 21-propionate of the present invention is prepared by acylating hydrocortisone 17-butyrate with propionic acid anhydride or halide. The compound of the present invention has excellent anti-inflammatory effect, percutaneous absorption and less side effect.

Novel hydrocortisone derivative

2-(p-prenylphenyl)propionic acid and pharmaceutically acceptable salts thereof are disclosed. They exhibit anti-inflammatory and analgesic activity with low gastrointestinal action.

2-(p-Prenylphenyl)propionic acid

Novel penicillin derivatives of the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R is hydrogen or hydroxy, are produced by acylating ampicillin, amoxicillin or a salt thereof with 4-hydroxy-pyrazino[2,3-f]quinoline-3-carboxylic acid or its functional derivative. They have high anti-pseudomonas activity and other antibacterial activity against gram-positive and gram-negative bacteria, and are of extremely low toxicity.

Novel penicillin derivatives

Anilinotropone derivatives represented by the following formula: ##STR1## wherein R is hydrogen or methyl and pharmaceutically acceptable salts thereof are disclosed. They exhibit anti-inflammatory and analgesic activity with low gastrointestinal action.

Anilionotropone derivatives

D-Penicillamine and salts thereof may be prepared by reacting certain aryl amines with 4-thiazolidinecarboxylic acid compounds obtained by splitting the .beta.-lactam ring of penicillin derivatives such as benzylpenicillin or phenoxymethylpenicillin.

Method for preparing d-penicillamine and salts thereof

Novel 2'-(carboxymethoxy)-chalcones of the formula ##STR1## wherein one or two of X.sup.1, X.sup.2 and X.sup.3 are 3-methyl-2-butenyloxy and the other or others are hydrogen, possess excellent antigastric and anti-duodenal ulcer activities, together with a high absorptive ratio in the living body and low acute and chronic toxicity.

2-(Carboxymethoxy)-chalcones

A new polyether group antibiotic, TM-481, having the estimated empirical formula C.sub.42-45 H.sub.71-75 O.sub.14-15 Na and possessing an antibacterial activity against pathogenic microorganisms, particularly Gram-positive bacteria is obtained by culturing a TM-481 producing microorganism of the Streptomyces ribosidificus group in a nutrient medium therefor.

Growing community of inventors

Kodaira, Japan

Jiro Sawada