Nippon Shinyaku Company, Ltd.

Takara Shuzo Co., Inc.

Matsuda, Masahito

Kitano, Masahiko

Kazuno, Kenji

Kise, Masahiro

Shirahase, Ichiro

Tomii, Yoshifumi

Ozaki, Masakuni

Masakuni Ozaki

Masahiro Kise

Kenji Kazuno

Masahiko Kitano

Jun Segawa

Yoshifumi Tomii

Ichiro Shirahase

Hiroshi Enomoto

Shingo Matsumura

Hisao Watanabe

Masahito Matsuda

Shoji Yasufuki

Teruya Nakamura

Akira Obayashi

Iwao Morita

Koji Kitaguchi

Masami Tsuda

Haruo Tanaka

Shingo Matsumura, Deceased

Hiroyuki Kuroda

Shinichi Tada

Toshihiro Okamura

Katsutoshi Kunimoto

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 ##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 ##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

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

Oxygenated sterylglycoside derivatives of the formula (I) wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and each is hydrogen or lower alkanoyl, Y is ##STR1## and R.sub.5 is 4-methylpentyl, 3-ethyl-4-methylpentyl or 3-ethyl-4-methyl-1-pentenyl are useful for their hemostatic and capillary stabilizing effects.

Steroid glycoside compounds and methods of use

Acylated derivatives of 2-[3-(2-chloroethyl)-3-nitrosoureido]-2-deoxy-D-glucopyranose have antitumor activity.

Acyl derivatives of

Growing community of inventors

Joyo, Japan

Masakuni Ozaki