Nippon Shinyaku Company, Ltd.

Matsuda, Masahito

Kitano, Masahiko

Kazuno, Kenji

Kise, Masahiro

Shirahase, Ichiro

Tomii, Yoshifumi

Ozaki, Masakuni

Kimura, Kiyoshi

Morita, Iwao

Masahiro Kise

Masakuni Ozaki

Kenji Kazuno

Masahiko Kitano

Jun Segawa

Yoshifumi Tomii

Ichiro Shirahase

Iwao Morita

Toshio Tomita

Kiyoshi Kimura

Masami Tsuda

Shoji Yasufuki

Masahito Matsuda

Hiroshi Enomoto

Hiromu Murai

Shoichi Chokai

Koji Kitaguchi

Akira Sano

Yoshihiko Yoshimoto

Shoji Yasufuku

Shinichi Tada

Shingo Matsumura, Deceased

Yasuo Sasaki

Tatsuo Suminokura

Hisao Watanabe

Kenichi Nakamura

Koyishi Kimura

Katsutoshi Kunimoto

Hiroshi Fujisawa

Shoicho Chokai

Pyroglutamide derivatives have been found to be useful as nootropic agents for administration to humans and animals.

Pyroglutamide derivatives

Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and R.sup.3 is hydrogen, halo or straight or branch chain lower alkoxy, are useful for treating bacterial infections in humans and animals.

7[4-(5 methyl-2-oxo-1,3-dioxalen-4-yl)methyl

Compounds of the formula (I): ##STR1## exhibit anti-cholingeric and calcium antagonistic action and are used for treating pollakiuria and incontinence in humans and animals.

Butynylamine derivatives and their production

Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or aryl unsubstituted or substituted by one or two halo moieties, R.sup.3 is hydrogen or alkyl, A is N, W is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.

Thiazetidine compounds

Quinolinecarboxylic acid derivatives of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, straight or branch chain lower alkyl or phenyl unsubstituted or substituted by one or more halo moieties; R.sup.2 is hydrogen or straight or branch chain lower alkyl; and ##STR2## is a 5- or 6-membered ring wherein the nitrogen atom is the only heteroatom or where there is a second heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, said 5- or 6-membered ring being unsubstituted or substituted by lower alkyl, amino or mono- or di-lower alkyl amino are useful for treating bacterial infections in humans and animals.

Derivatives of quinolinecarboxylic acid

Compounds of the formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sup.1 is cycloalkyl of 5 to 7 carbon atoms; aryl of 6 to 10 carbon atoms unsubstituted or substituted by straight or branched chain alkyl of 1 to 4 carbon atoms, halo or trifluoromethyl; or ##STR2## wherein A is oxygen, sulfur or NR.sup.5, wherein R.sup.5 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo, and R.sup.6 is hydrogen, straight or branched chain alkyl of 1 to 4 carbon atoms or halo;

Acylphenol derivatives, useful as anti-inflammatory agents and pain

Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof, R.sup.1 is hydrogen, alkyl or phenyl unsubstituted or substituted by one or two halo moieties, R.sup.2 is hydrogen or alkyl, A CX wherein X is halo, B is O or NR.sup.3 wherein R.sup.3 is hydrogen, alkyl, acyl, haloacyl, 2alkoxycarbonyl or (5-methyl-2-oxo-1,3-dioxolen-4-yl) methyl are useful for treating bacterial infections in humans and animals.

Thiazetidine derivatives

A compound of formula (I): ##STR1## wherein R.sup.1 is alkenyl or alkyl or both of the depicted R.sup.1 groups together represent trimethylene and form a six-membered ring together with the depicted oxygen and phosphorus atoms, R.sup.2 is nitro, trifluoromethyl or halogen, R.sup.3 is alkyl, and R.sup.4 is dimethoxymethyl, formyl, hydroxymethyl or nitrile.

Certain antihypertensive 1,4-dihydro-6-methyl-5-phosphonic

Anti-bacterial and anti-fungal compounds of formula I and pharmaceutically acceptable salts thereof: ##STR1## in which R.sup.1 is hydrogen, alkyl or substituted or unsubstituted phenyl; R.sup.2 is hydrogen, alkyl, alkoxy, hydroxy, halgen, nitro or substituted or unsubstituted amino; R.sup.3 is hydrogen or substituted or unsubstituted alkyl; R.sup.4 and R.sup.5 are the same or different and are alkyl or hydroxyalkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are attached form an unsubstituted or substituted heterocyclic ring having the depicted nitrogen atom as the sole heteroatom or which may have nitrogen, oxygen or sulphur atoms as additional heteroatoms; and X is halogen.

Substituted thiazetoquinoline-3-carboxylic acids and pharmaceutically

A compound of the formula ##STR1## R.sub.1 is hydrogen, alkali metal, alkaline earth metal, lower alkyl, pivaloyloxymethyl or phthalidyl; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are hydrogen, halogen, lower alkoxy or ##STR2## wherein R.sub.6 and R.sub.7 are lower alkyl or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are attached form a five- to seven-membered unsubstituted or substituted heterocyclic ring containing said nitrogen atom as the sole hetero atom or containing nitrogen, sulfur or oxygen as additional hetereo atoms; A is a saturated or unsaturated hydrocarbon chain of one to five carbon atoms, unsubstituted or substituted by lower alkyl; lower alkoxy; lower alkylthio; hydroxy; halogen; lower alkyl substituted by halogen, amino, loweralkoxycarbonyl, carboxy, lower-alkoxy, loweralkylthio, loweracyloxy or hydroxy; loweralkylamino; carboxy; nitro; cyano; carbonyl; imino; or by substituted or unsubstituted phenyl, phenylthio, phenylamino or phenoxy; and R.sub.2 and R.sub.3 or R.sub.3 and R.sub.4 or R.sub.4 and R.sub.5 together may be alkylenedioxy of 1 to 5 carbon atoms which form a ring with the carbon atoms to which they are attached; or a pharmaceutically acceptable salt thereof.

Olinecarboxylic acid derivatives

Quinolinecarboxylic acid derivatives, such as compound 7-fluoro-8-(4-methyl-1-piperazinyl)-5-oxo-1,2-dihydro-5H-thiazolo(3,2-a)-q uinoline-4-carboxylic acid, a pharmaceutical composition containing the same and methods of treatment of bacterial and fungal infections using the same.

Carboxylic acid derivatives

Steryl-6-0-palmitoyl-.beta.-D-glucosides are anti-inflammatory agents. The compounds, of which .beta.-sitosteryl-6-0-palmitoyl-.beta.-D-glucoside is a representative embodiment, are prepared through the reaction of a steryl-6-0-sulfonyl-.beta.-D-glucoside with an alkali metal salt of palmitic acid.

Steryl-.beta.-D-glucoside esters and method of preparation

Growing community of inventors

Kyoto, Japan

Masahiro Kise