Shin-etsu Chemical Co., Ltd.

Ajinomoto Co., Ltd.

Sanwa Kagaku Kenkyusho Co., Ltd.

Other

Mitsui Co., Ltd.

Tobishi Pharmaceutical Co., Ltd.

Mitsubishi Burlington Co., Ltd.

Maruzen Pharmaceutical Co., Ltd.

Ajinomoto Company Incoporated

Shigeshi Toyoshima

Ryuichi Sato

Toshio Shinohara

Yasushi Yamamoto

Yoshiko Seto

Izumi Kumashiro

Koichi Ito

Shoji Ichinohe

Masayasu Kurono

Ryoichi Unno

Koji Fukushima

Masatoshi Arai

Hajime Fujimura

Akira Ishikawa

Hiromoto Kimura

Yoshiteru Hirose

Shiro Ikegami

Yukihito Ishida

Koji Toi

Setsuo Tomisawa

Hiroshi Sato

Minoru Sato

Hisashi Shinkai

Haruhisa Fujita

Mariko Fukuma

Munemoto Itoh

Mikiro Fujiwara

Syosuke Yamamura

Mie Itoh

Shunsuke Ito

Yasuji Kondo

A compound of D-phenylalanine derivative for hypoglycemic use, represented by the general formula ##STR1## R.sup.1 is selected from hydrogen, alkyl of 1 to 5 carbon atoms, aryl of 6 to 12 carbon atoms, aralkyl of 6 to 12 carbon atoms, ##STR2## --CH.sub.2 CO.sub.2 R.sup.3, --CH(CH.sub.3)--OCO--R.sup.3, and --CH.sub.2 --OCO--C(CH.sub.3).sub.3 ; R.sup.2 is selected from groups comprising aryl of 6 to 12 carbon atoms, a hetero six-membered ring, a hetero five-membered ring, cycloalkyl, or cycloalkenyl, any of which groups may have one or more substituents; and R.sup.3 is selected from hydrogen and alkyl of 1 to 5 carbon atoms; the salts thereof, and precursors which can be converted thereto in the human or animal body. Some of the compounds are novel per se.

Hypoglycemic agent

Novel organo-silicone compounds represented by the formula, ##STR1## wherein R is hydrogen, halogen or alkyl group, R.sup.1, R.sup.2 and R.sup.3 are alkyl group, alkoxy group, phenyl radical, substituted phenyl radical, alkylcarbonyloxy group, or trialkylsilyloxy group, respectively, R.sup.4 is hydrogen, alkyl or alkenyl grup, and m and n are an integer, respectively but those do not represent same integer of 2, when all of R.sup.1, R.sup.2 and R.sup.3 represents methyl radical, a process for the manufacture of the compounds, and an anti-tumor agent which comprises as an effective component, at least one of the compounds.

Organo-silicon compounds, process for the manufacture of same, and

An absorption promoter is disclosed which interacts with hydrophobic amino acid residues of polypeptide derivative medications and substantially increases the absorption of that medication administered orally or rectally. The promoter and medication can be compounded into unit dosages in capsule, tablet, or suppository form, or combined into elixir solutions, suspensions, etc. The absorption promoters are phenylalanine derivatives which may be prepared through conventional N-acylation techniques.

Pharmaceutical composition having an excellent absorption property

A compound represented by the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, a fluorine atom, a nitro group, a hydroxyl group or a hydroxyl group protected by an esterifying group; X is CO or SO.sub.2 ; --Y-- is a straight bond, a lower alkylene group, a substituted or unsubstituted vinylene group, or group having the formula --CH.sub.2 --O-- or --O--CH.sub.2 --; R.sup.2 is a substituted or unsubstituted phenyl or naphthyl group, or R.sup.2 --Y--CO is N-benzyloxycarbonylphenylalanyl, N-benzyloxycarbonyl-4-fluorophenylalanyl or N-(m-methoxycinnamoyl)-phenylalanyl group; or a non-toxic salt thereof is disclosed along with pharmaceutical compositions containing these compounds and methods of using these compositions to increase the rate of absorption of medicines.

A novel organosilicon compound represented by a formula ##STR1## wherein A is methylene, carbonyl or sulfonyl group; R, R.sub.1 and R.sub.2 are alkyl group, respectively; R.sub.3 is alkyl, substituted alkyl, alkenyl, phenyl, substituted phenyl, naphthyl, substituted naphthyl, pyridyl, substituted pyridyl, furyl, substituted furyl, thienyl, substituted thienyl group or cycloalkyl group together with the substituent A; R.sub.4 is hydrogen, alkyl or alkenyl group; and R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11 and R.sub.12 are hydrogen, alkyl or substituted alkyl, respectively, a non-toxic salt thereof, a process for the preparation of said compound or salt, as well as an antitumor agent comprising as an effective agent at least one of said compound and salt.

Organosilicon compounds and antitumor agents containing the compound as

11-Deoxoglycyrrhetinic acid hydrogen maleate of the following formula ##STR1## and its salts, and this compound is prepared by reacting 11-deoxoglycyrrhetinic acid with maleic anhydride, and if desired, converting the resulting 11-deoxoglycyrrhetinic acid hydrogen maleate to its salt. The compound is useful as medicament for treating an ulcer or inflammation in man or another animal or activating the cellular immunity of man or the animal.

11-Deoxoglycyrrhetinic acid hydrogen maleate, process for its

An antimicrobial carpet having bacteriostatic and sterilizing effect against molds, bacteria and viruses is prepared by incorporating into fibrous materials prior to or after fabrication into a carpet an amino acid type surfactant represented by the formula: ##STR1## wherein RCO is a C.sub.8 -C.sub.16 fatty acid residue.

Antimicrobial carpet containing amino acid type surfactant

The invention provides a novel compound 2-(3-trimethylsilylpropyl)benzothiazole having remarkable anti-tumor effects or, in particular, inhibiting growth of melanoma cells in test animals. The compound is synthesized by the ring-closing intramolecular dehydration condensation of 2-mercapto-(.gamma.-trimethylsilyl)butyroanilide which in turn is obtained by the dehydrochlorination condensation of 2-aminothiophenol and .gamma.-trimethylsilylbutyryl chloride in a polar solvent in the presence of an acid acceptor.

2-(3-Trimethylsilylpropyl)benzothiazole

A novel medicament which is effective as an antihypertensive agent is proposed which contains, as its effective ingredient, an organosilicon compound represented by the general formula

Medicaments containing an organosilicon compound

The invention provides a novel anti-tumor agent highly effective for inhibiting growth of several tumor or cancer cells with low toxicity. The active ingredient contained in the anti-tumor agent is an .omega.-triorganosilyl-substituted linear alkanoic acid anilide which is a hitherto unknown novel compound prepared by the reaction of corresponding acid chloride and aniline.

Novel organosilicon compounds and anti-tumor agents containing the same

The invention provides a novel class of organosilicon compounds and a method for the preparation thereof as well as an anti-tumor agent containing the compound having very remarkable anti-tumor activity but with very low toxicity. The inventive compound is a (trihydrocarbylsilylmethyloxyimino)alkane, which is a silicon-containing oxime compound hitherto not described in any prior art literatures, represented by the general formula R.sup.1.sub.3 Si--CH.sub.2 --O--N.dbd.Y, R.sup.1 is a substituted or unsubstituted monovalent hydrocarbon group having from 1 to 10 carbon atoms and Y is a divalent hydrocarbon group denoted by .dbd.CR.sup.2 R.sup.3 or .dbd.CR.sup.4, R.sup.2 and R.sup.3, which may be identical or different, having the same meaning as R.sup.1 defined above and R.sup.4 being an alkylene group to form a ring structure jointly with the carbon atom directly bonded to the nitrogen atom. Typical examples of the compounds are: 2-(trimethylsilylmethyloxyimino) butane, 2-(trimethylsilylmethyloxyimino)propane, 2-(dimethylphenylsilylmethyloxyimino) butane and trimethylsilylmethyloxyiminocyclohexane.

Novel organosilicon compounds and anti-transplanted tumor agents

The present invention presents a novel class of compounds bis(triorganosilylalkyl) phosphites, e.g. bis(trimethylsilylmethyl) phosphite. The compound is readily prepared by the reaction of a corresponding triorganosilyl alkanol with phosphorus trichloride or by the partial hydrolysis of a corresponding tris(triorganosilylalkyl) phosphite with an equimolar amount of water followed by distillation of the reaction mixture. The compound has a remarkable anti-transplanted tumor effectiveness as established by the test with mice as the test animals for preventing the growth of Ehrlich's cancer cells and Sarcoma 180 cells. The compound has very low toxicity when orally administrated.

Bis(triorganosilylalkyl) phosphites

A process for preparing an antimalignant agent which comprises cultivating Staphylococcus epidermidis STF (Bikoken(or Microbic Industry Technological Institute)Deposit No. 3706; ATCC 31310) in a liquid culture medium, removing solid matter from the culture solution, concentrating the remaining solution, washing the precipitate thus formed with water, re-dissolving the precipitate, fractionating the solution into a number of fractions by an adsorptive filtration gel or the molecular sieve method, taking a fraction exhibiting antimalignant activity, concentrating the fraction, further purifying the fraction by ion-exchange chromatography and separating the active ingredient; and the antimalignant agent thus obtained.

Agent for inhibiting tumor induced by leukemia virus

Novel pharmacologically important organic germanium compounds (3-hydroxygermyl propionic acid salts) represented by the formula ##STR1## WHEREIN Met is a monovalent cation selected from the group consisting of Na, K, NH.sub.4, and NH.sub.2 (CH.sub.3).sub.2, or divalent cation selected from the group consisting of Ca and Mg, and wherein x is 1 when Met is a monovalent cation and x is 2 when Met is a divalent cation. These compounds possess valuable therapeutic properties for treating such physiological abnormalities as psychiatric and neurological disorders, metabolic disorder, cardivascular disorder, disorder of digestive organs, skin disease, allergic disease, Kidney dysfunction, hepatic dysfunction, obstetric and pediatric diseases, etc., and the process for preparing thereof.

Growing community of inventors

Funabashi, Japan

Shigeshi Toyoshima