Sankyo Company, Limited

Fujio Saito

Sadao Ishihara

Hiroyuki Koike

Shigeki Miyake

Hiroshi Mizuno

Takao Yoshioka

Akira Yoshida

Mitsuru Kataoka

Hiroshi Kogen

Ichiro Hayakawa

Teiichiro Koga

Eiichi Kitazawa

Koza Oda

Yasuo Ohhata

Norio Fukuda

Ryosuke Yorikane

Takeshi Oshima

Yasuhiro Morisawa

Takashi Kasai

Mitsuo Sugiyama

Hitoshi Nagahori

Yasuo Simoji

An optically active thiazolidinone derivative having the general formula: ##STR1## wherein: R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a phenyl group, a substituted phenyl group (said substituent represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen), a phenyl-C.sub.1 -C.sub.2 alkyl group or a substituted phenyl-C.sub.3 -C.sub.2 alkyl group (the substituent of said phenyl represents C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy or halogen); R.sup.2 represents a C.sub.1 -C.sub.6 alkyl group; and n represents 1 or 2!. Effect The optically active thiazolidinone derivative of the present invention has excellent anti-angina pectoris action and is useful as a preventive agent or a therapeutic agent for angina pectoris.

Optically active thiazolidinone derivative

A thiazolidinone compound represented by general formula (I) or a pharmacoligically acceptable salt thereof, ##STR1## wherein W represents sulfur or oxygen and X represents --N(R.sup.1)--, or alternatively X represents sulfur or oxygen and W represents --N(R.sup.1)--, and R.sup.1 represents hydrogen, alkyl or substituted alkyl; R.sup.2 and R.sup.3 are the same or different from each other, and each represents hydrogen, alkyl, substituted alkyl, aryl, or 5- or 6-membered heteroaryl; R.sup.4 represents hydrogen, alkyl or substituted C.sub.1 -C.sub.4 alkyl; R.sup.5 represents substituted cycloalkyl which may contain nitrogen, provided the substituents include --B--ONO.sub.2 (wherein B represents a single bond or alkylene) as the indispensable member and alkyl groups as optional members; and A represents a single bond or alkylene, has an excellent anti-anginal effect and thus is useful as an angina pectoris remedy or preventive.

Thiazolidinone compounds and composition for angina pectoris comprising

An amino acid compound of the formula: R.sup.1 NH--CH(R.sup.2)--COHN--A--ONO.sub.2, wherein R.sup.1 represents a hydrogen atom, a C.sub.1 -C.sub.7 alkanoyl group, a C.sub.1 -C.sub.6 alkoxycarbonyl group, a C.sub.6 -C.sub.10 arylcarbonyl group, a C.sub.7 -C.sub.13 aralkylcarbonyl group, a C.sub.7 -C.sub.13 aralkyloxycarbonyl group or a 5- or 6-membered aromatic heterocyclic carbonyl group; R.sup.2 represents a substituted C.sub.1 -C.sub.6 alkyl group; and A represents a C.sub.2 -C.sub.5 alkylene group; and pharmacologically acceptable salts thereof. The amino acid compound has an excellent vasodilator action for collateral vessels and is useful for treating angina pectoris.

Amino acid derivatives

Compounds of formula (I) are provided: ##STR1## wherein: R.sup.1 represents an alkyl group; or a group of formula (II), (III), (IV) or (V): ##STR2## and wherein the groups R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are hydrogen or various organic groups; and pharmaceutically acceptable salts thereof; as well as methods for the preparation of such compounds and their use in the treatment and prophylaxis of hypercholesteremia and arteriosclerosis.

Amide and urea derivatives having anti-hypercholesteremic activity,

Nitroxyalkylamide derivatives

Substituted aromatic amides and ureas derivatives having

Compounds of formula (I): ##STR1## wherein W represents an oxygen atom and X represents a group of formula --N(R.sup.1)--; R.sup.1 is hydrogen, alkyl or aralkyl; R.sub.2 and R.sup.3 are each hydrogen, alkyl, aralkyl, aryl or aromatic heterocyclic; R.sup.4 is hydrogen, alkyl or aralkyl; and A is alkylene which is optionally substituted by carboxy; and pharmaceutically acceptable salts and esters thereof, have a valuable vasodilatory activity.

Oxazolidinone compounds and method of using the same as a vasodilator

Compounds of formula (I): ##STR1## wherein W represents a sulfur atom and X represents a group of formula --N(R.sup.1)--, or W represents a group of formula --N(R.sup.1)-- and X represents a sulfur atom; R.sup.1 is hydrogen, alkyl or aralkyl; R.sup.2 and R.sup.3 are each hydrogen, alkyl, aralkyl, aryl or aromatic heterocyclic; R.sup.4 is hydrogen, alkyl or aralkyl; and A is alkylene which is optionally substituted by carboxy; and pharmaceutically acceptable salts and esters thereof, have a valuable vasodilatory activity.

Thiazolidone compounds and method of using the same as a vasodilator

Compounds of formula (I): ##STR1## (in which: R.sup.1 is hydrogen or alkl; R.sup.2 is a variety of groups or atoms; R.sup.3 is optionally substituted hydroxy or --(NH).sub.n --NR.sup.5 R.sup.6, wherein R.sup.5 and R.sup.6 are a variety of groups or atoms, preferably alkyl substituted by heterocyclic, and n is 0 or 1; Q is oxygen or sulfur; and A is a C.sub.1 -C.sub.6 alkylene group) have valuable cardiotionic activity and may be used for the treatment of cardiac disorders. They may be prepared from corresponding compounds containing a benzene ring with a group --QH at the 1-position and a group --CO--CHR.sup.1 --NH--COOR.sup.7 at the 4-position by ring closure and introduction of the group of formula --A--CO--R.sup.3 in any order.

1,2,4-triazinone derivatives, their preparation and use

Growing community of inventors

Tokyo, Japan

Fujio Saito