Nippon Shinyaku Company, Ltd.

Other

Mitsubishi Chemical Industries Limited

Takara Shuzo Co., Inc.

Hiroshi Enomoto

Yoshiaki Aoyagi

Yoshiaki Yoshikuni

Shingo Matsumura

Hiromu Murai

Masahiro Yagi

Katsuya Ohata

Shoichi Chokai

Katsuhide Saito

Kohei Kura

Yoji Ezure

Ichiro Shirahase

Yukio Fujita

Tatsuhiko Kono

Takayuki Ozaki

Koji Kitaguchi

Haruo Tanaka

Akira Nomura

Tamiki Mori

Fusao Ueda

Kenji Sempuku

Yoshihisa Shibata

Masao Murase

Kichiro Inoue

Tadatoshi Nomura

Yasuo Yasutomi

Masahiko Kitano

Masanobu Kawamata

Masakuni Ozaki

Makio Kobayashi

Iwao Morita

Nobutoshi Ojima

Kazuo Wagatsuma

Shingo Matsumura, Deceased

Hiroaki Munakata

Mitsuhiro Machara

Mitsuhiro Maehara

Makoto Tsurufuji

Shigeru Sato

Masahiro Adachi

Hiroshi Nishida

Katsushige Ikai

Teruya Nakamura

Masahiro Kise

Makoto Sugiyama

Shigeaki Maruo

Toshio Tomita

Hiroyuki Kuroda

Kiyotaka Konno

Masato Matsuda

Yoshitsugu Nomiyama

Toshihiro Okamura

Katsahide Saito

Susumu Sano

Takashi Okubo

Phenylacetic acid derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen or ##STR2## wherein R.sup.5 is an alkyl group of 1-6 carbon atoms or an aryl group; R.sup.2 and R.sup.3 are independently hydrogen or an alkyl group of 1-4 carbon atoms; R.sup.4 is hydrogen or an alkyl group of 1-4 carbon atoms, have been found to possess immunomodulating activity.

Immunomodulating agent

4-Quinolone derivatives of the present invention are useful for their anti-inflammatory, anti-allergenic, antitussive, expectorant and antithrombotic activity. Pharmaceutical compositions containing said compounds and pharmaceutically acceptable salts thereof and methods of treating humans and animals are described herein.

4-quinolone derivatives having anti-inflammatory, anti-allergic,

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

2,4-diamino-6-(2,5-dichlorophenyl)-1,3,5-triazine and pharmaceutically acceptable acid addition salts thereof in finely pulverized form so that the average particle diameter is 20 microns or less have been found to be particularly useful for the treatment of peptic ulcers. When administered to humans in need thereof, 1 to 4 mg per day has been found effective.

Low dosage compositions of finely pulverized

1-phenoxy-3-(4-phenylpiperazino)-2-propanol derivatives of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, halo or lower alkyl; R.sup.2 is pyrrolidino, piperidino, morpholino or perhydroazepino unsubstituted or substituted by carbonyl at the alpha-position; R.sup.3 is hydrogen, lower alkyl or lower alkoxycarbonyl; and R.sup.4 is hydrogen, lower alkyl unsubstituted or alpha-substituted by lower alkoxy, lower alkoxy, halo or lower alkanoyl are useful for their alpha and beta-adrenergic blocking action and their hypotensive activity in humans and animals.

1-phenoxy-3-(4-phenylpiperidino)-2-propand having both alpha- and

3-methylflavone derivatives which are useful in the treatment of allergies, asthma and inflammation.

Methylflavone-8-carboxylates

Compounds of the formula (I): ##STR1## and pharmaceutically acceptable salts thereof wherein R.sup.1 is hydrogen, alkyl of 1 to 10 carbon atoms or acyl of 1 to 6 carbon atoms; R.sup.2 is hydrogen or halo; R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms or acyl of 1 to 6 carbon atoms; R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms; R.sup.5 is hydrogen or acyl of 1 to 6 carbon atoms; X is CONH.sub.2, hydroxyalkyl of 1 to 4 carbon atoms or COOR.sup.6 wherein R.sup.6 is hydrogen or alkyl of 1 to 4 carbon atoms; and Y is CONH.sub.2, hydroxyalkyl of 1 to 4 carbon atoms or COOR.sup.7 wherein R.sup.7 is hydrogen, alkyl of 1 to 10 carbon atoms or benzyl are useful for inhibiting the activity of amino-peptidase B, exhibit immunomodulating action against living organisms and exhibit anti-inflammatory activity.

OF4949

N-aralkylmoranoline and N-aralkenylmoranoline, and their pharmaceutical acceptable non-toxic acid addition salts thereof, pharmaceutical compositions containing the same and methods of inhibiting the increase in blood sugar level by administration of the same.

Antihyperglycemic moranoline derivatives

2,4-Diamino-6-(2,5-dichlorophenyl)-1,3,5-triazine and pharmaceutically acceptable acid addition salts thereof in finely pulverized form so that the average particle diameter is 20 microns or less have been found to be particularly useful for the treatment of peptic ulcers.

Finely pulverized 2,4-diamino-6-(2,5-dichloro-phenyl)-1,3,5-triazine and

4-Hydroxy-2-quinolone derivatives are useful for their anti-inflammatory, anti-allergenic, antitussive and expectorant activity. Pharmaceutical compositions containing said compounds and pharmaceutically acceptable salts thereof and methods of treating humans and animals are described herein.

Pharmaceutically active 4-hydroxy-3-benzoyl-2-quinolone derivatives

A method of prevention and/or treatment of disorders of the liver, kidney, colon or rectum in mammals including humans which comprises administering to the patient a therapeutically effective amount of 2,4-diamino-6-(2',5-dichlorophenyl)-s-triazine maleate sufficient to prevent and/or overcome said disorders, and pharmaceutical compositions therefor.

Treatment of diseases of the liver, kidney, colon and rectum

Glutamine derivatives and non-toxic salts thereof have been found to have immunomodulating activities.

Glutamine derivatives

4-(3-Aryloxy-2-hydroxypropyl)piperazines bearing a carbamyl group in the 1-position are .beta.-adrenergic blockers. A typical example is 1-carbamyl-4-{3-[2-allyl-3-(2-carbethoxyaminoethyl)phenoxy]-2-hydroxypropy l}piperazine.

Carbamylpiperazine compounds

Compounds useful in the treatment of rheumatism or allergic nephritis which have the formula ##STR1## wherein X is halogen, hydroxy, lower alkyl, lower alkenyl, lower alkoxy, nitro or amino;

Nicotinic 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

Growing community of inventors

Nagaokakyo, Japan

Hiroshi Enomoto