Toray Industries, Inc.

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Takara Shuzo Co., Inc.

Kanegafuchi Chemical Industry Co., Ltd.

Masaji Ohno

Mutsuo Kataoka

Hamao Umezawa

Norio Kawabe

Masato Mutoh

Hiroyuki Odawara

Keiichi Matsunaga

Kiyoshi Watanabe

Junzo Hasegawa

Akira Obayashi

Shigeki Hamaguchi

Hajime Kawaharada

Masahiro Ogura

Hirokazu Kotani

Osamu Tanabe

Yoshio Noguchi

Go Hata

Hisao Kondo

Kazuo Hosoi

Masazumi Kanaoka

Toru Yamazaki

Toshinori Miyabe

Satoshi Hanada

A platinum complex represented by the formula: ##STR1## where X is ##STR2## wherein R.sup.1 is a (C1-18) alkyl group, a (C1-18)alkenyl group or a group --Z--R.sup.4 in which Z is --CH.dbd.CH-- or a (C1-5)alkylene group, and R.sup.4 is a phenyl group, a hydroxyphenyl group, a (C7-12)alkoxyphenyl group, a halogenophenyl group, a nitrophenyl group, or (C8-13)alkoxycarbonylphenyl group, a cyclohexyl group having a (C1-5)alkyl substituent, ##STR3## R.sup.2 is hydrogen or a (C1-18)alkyl group, R.sup.3 is hydrogen or a (C1-3) alkyl group, R.sup.2 and R.sup.3 are linked together to form a (C2-7)alkylene group; the dotted line indicates that the bond may be either a single bond or a double bond; the chain line indicates a conjugated system; the 1,2-diaminocyclohexane moiety has a cis-, trans-l- or trans-d-configuration; and Y is an anion. This platinum complex is useful in the treatment of tumors.

Platinum complex, process for preparing same and antitumor agent

A platinum complex represented by the formula: ##STR1## wherein R.sup.1 is a (Cl-18) alkyl group, a (Cl-18)-alkenyl group or a group ----X--R.sup.5 in which X is --CH.dbd.CH-- or a (Cl-5)alkylene group, and R.sup.5 is a phenyl group, a hydroxyphenyl group, a (C7-12) alkoxyphenyl group, a halogenophenyl group, a nitrophenyl group, or (C8-13)alkoxycarbonylphenyl group, a cyclohexyl group having a (Cl--5)alkyl substituent, ##STR2## R.sup.2 is a (Cl-18 alkyl group, R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 are linked together to form a (C2-7)alkylene group, R.sup.4 is OH or NO.sub.3 ; the dotted line indicates that the bond may be either a single bond or a double bond; the chain line indicates a conjugated system; n is a number of from 1 to 2, and the 1,2-diaminocyclohexane moiety has a cis-, trans-l- or trans-d-configuration. This platinum complex is useful in the treatment of tumors.

The present invention provides a process for preparing a optically active .beta.-(S)-aminoglutaric acid monoalkyl ester of the formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 carbon atoms, which comprises subjecting a .beta.-N-protected aminoglutaric acid dialkyl ester of the formula: ##STR2## wherein each R is as defined above and A is an easily removable protecting group, to an action of an enzyme produced by a microorganism belonging to the genera Flavobacterium, Achromobacter, Xanthomonas, Alcaligenes, Serratia, Gluconobacter, Chromobacterium and Acetobacter, to selectively hydrolyze only one of the two ester groups, and then removing the protecting group.

Method of preparing optically active .beta.-(S)-aminoglutaric acid

A process is disclosed in which an optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid is prepared by subjecting a dialkyl ester of .beta.-protected aminoglutaric acid to the action of a culture broth, cells, or treated cells of a microorganism capable of stereoselectively hydrolyzing only one of the ester groups in the above-mentioned dialkyl ester to produce an optically active monoalkyl ester of .beta.-protected (S)-aminoglutaric acid, and then removing the amino-protecting group from the product. An optically active monoalkyl ester of .beta.-(S)-aminoglutaric acid is useful as a starting material for synthesizing .beta.-lactam antibiotics of carbapenem type such as thienamycin.

Process for preparation of an optically active monoalkyl ester of

A process for continuously separating, in liquid phase, fructose from a liquid feed mixture of sugars containing essentially fructose and glucose by contact with a solid sorbent of zeolite. The process utilizes a simulated countercurrent flow system wherein a liquid stream flows through serially and circularly interconnected desorption, rectification and sorption zones each zone being divided into a plurality of sections. In the zones water as desorbent is introduced into the desorption zone, the liquid feed mixture of sugars is introduced into the sorption zone, a desorption effluent is withdrawn from the desorption zone and a raffinate effluent is withdrawn from the sorption zone, and all of the points of introduction and withdrawal of the liquids are simultaneously shifted, one section at a time at predetermined intervals of time, in a downstream direction.

Continuous separation of fructose from a mixture of sugars

High purity cis-epoxysuccinic acid and salts thereof are economically and systematically prepared by contacting an aqueous solution, obtained by reacting a maleic acid salt and hydrogen peroxide in the presence of a tungstate or molybdate catalyst under a specified condition, with a strongly basic Type II anion exchange resin.

Process for preparing CIS-epoxysuccinic acid salts of high purity

New compounds of the formula ##STR1## WHEREIN Ar is selected from the group consisting of phenylethyl, furyl, methylfuryl, thienyl, pyrrolyl, naphthyl, hydroxynaphthyl, and phenyl substituted by at least one member selected from the group consisting of halogen, hydroxyl, cyano, trifluoromethyl, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, carbamoyl, amino of the formula --NR'R', alkoxycarbonyl of the formula --CO--OR' wherein R' and R' are each alkyl of 1-4 carbon atoms, and alkylenedioxy of the formula --O--R''--O-- wherein R'' is alkylene of 1-4 carbon atoms, provided that said substituted phenyl is not 3,4-di-methoxyphenyl, and the addition salts thereof with the cation of an organic or inorganic base inhibit the enzyme activities of tyrosine hydroxylase and dopamine .beta.-hydroxylase and are useful chemotherapeutic agents in the treatment of essential hypertension.

Method and composition for treating hypertension

Fructose is effectively separated from a mixture of sugars by contacting an aqueous solution of a mixture of sugars with crystalline alumino-silicate.

Separation of fructose from a mixture of sugars

As new compound, a series of 2-hydrocinnamoyl-1,3-cyclopentanedione derivative of the general formula: ##STR1## WHEREIN Ar stands for a mono-valent aromatic radical, for example, phenyl and 3,4-methylenedioxy-phenyl, substituted or unsubstituted, have been found to have an activity to inhibit the action of tyrosine hydroxylase and to be useful as hypotensive agent. These new compounds may be produced by condensing 2-acetyl-1,3-cyclopentanedione with an aromatic aldehyde of the formula Ar-CHO wherein Ar is as defined, according to Claisen-Schmidt condensation, followed by the hydrogenation of the condensation product obtained, or the new compounds may also be produced by reacting 2-acetyl-1,3-cyclopentanedione with an aromatic halide of the formula Ar-CH.sub.2 X wherein Ar is as defined and X is a halogen, for example, in liquid ammonia and in the presence of an alkali metal amide.

2-Hydrocinnampyl-1,3-cyclopentanediones

New compounds of the formula ##SPC1## Wherein Ar is selected from the group consisting of phenylethyl, furyl, methylfuryl, thienyl, pyrrolyl, naphthyl, hydroxynaphthyl, and phenyl substituted by at least one member selected from the group consisting of halogen, hydroxyl, cyano, trifluoromethyl, akyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, carbamoyl, amino of the formula --NR'R', alkoxycarbonyl of the formula --CO--OR' wherein R'and R'are each alkyl of 1-4 carbon atoms, and alkylenedioxy of the formula --O--R ''--O-- wherein R'' is alkylene of 1-4 carbon atoms, provided that said substituted phenyl is not 3,4-di-methoxyphenyl, and the addition salts thereof with the cation of an organic or inorganic base inhibit the enzyme activities of tyrosine hydroxylase and dopamine .beta.-hydroxylase and are useful chemotherapeutic agents in the treatment of essential hypertension.

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Kamakura, Japan

Masaji Ohno