Nippon Shinyaku Company, Ltd.

Matsuda, Masahito

Kitano, Masahiko

Kazuno, Kenji

Kise, Masahiro

Shirahase, Ichiro

Tomii, Yoshifumi

Ozaki, Masakuni

Masahiko Kitano

Masahiro Kise

Masakuni Ozaki

Hiromu Murai

Ichiro Shirahase

Koji Kitaguchi

Kenji Kazuno

Hiroshi Enomoto

Yoshiaki Aoyagi

Katsuya Ohata

Fusao Ueda

Jun Segawa

Toshio Tomita

Akira Sano

Yoshifumi Tomii

Shinichi Tada

Tatsuo Suminokura

Masahito Matsuda

Shingo Matsumura

Iwao Morita

Haruo Tanaka

Satoshi Takata

Massahiro Kise

Toshihiro Okamura

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

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

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

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

2,4-Diamino-6-phenyl-s-triazine derivatives which are substituted in the 3-position of the phenyl ring and optionally further substituted in the 6-position demonstrate anti-ulcer and diuretic properties. A representative embodiment is 2,4-diamino-6-(3-trifluoromethylthiophenyl)-s-triazine.

Benzoguanamine 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

Steryl-6-O-palnitoyl and -2,3,4,6-O-tetrapalmitoyl-.beta.-D-glucosides are anti-inflammatory agents. The compounds, of which .beta.-sitosteryl-2,3,4,6-O-tetrapalmitoyl-.beta.-D-glucoside is a representative embodiment, are prepared through the reaction of a steryl-.beta.-D-glucoside with a lower alkyl ester of palmitic acid in the presence of a basic catalyst.

Steryl-.beta.-D-glucoside ester pharmaceutical compositions and method

A series of novel benzoguanamine derivatives possessing a high anti-peptic ulcer activity with low toxicity has been prepared by the reaction of the corresponding dihalogenobenzonitriles with dicyandiamide or by the reaction of the corresponding carboxylic acids or functional derivatives thereof with biguanide.

Growing community of inventors

Kyoto, Japan

Masahiko Kitano