Asahi Kasei Kogyo Kabushiki Kaisha

Mitsuru Shibukawa

Chisei Shibuya

Akio Mimura

Katsumi Yuasa

Kunihiko Ishii

Joji Nishikido

Torao Ishida

Hiroshi Hayashi

Eiji Kodama

Yasuyuki Takahashi

Akio Hasegawa

Takao Kiyota

Hirataka Itoh

Takashi Shirai

Sadayuki Horiguchi

Yukiji Shimojima

A secalonic acid derivative of the formula (I); ##STR1## wherein R is ##STR2## wherein R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-4 alkyl group; R.sub.3 is a hydrogen atom, a C.sub.1-4 alkyl group, and aryl group, a C.sub.1-5 alkoxy group, a halogen atom, a cyano group, a carboxyl group, a sulfonic acid group, a carboxylic acid amide group or a sulfonic acid amide group; and R.sub.4 is a saturated or unsaturated C.sub.1-22 alkyl group, an aryl group or an aryl alkyl group, and may have a substituent; and the pharmaceutically acceptable salts thereof.

Secalonic acid derivatives as antitumor agents

A cephalosporin compound of the general formula (I): ##STR1## wherein X is a hydrogen atom, a chlorine atom, a methyl group, a methoxy group, an acetoxymethyl group or --CH.sub.2 SHet wherein Het is a 5- or 6-membered heterocyclic ring containing therein 1 to 4 nitrogen, oxygen or sulfur atoms;

Cephalosporin compound

A method for improving the intestinal absorption of a cephalosporin derivative by bonding an oligopeptide having the general formula (I): ##STR1## wherein X is a hydrogen atom, C.sub.1-15 alkyl group, R.sub.3 CO-- group wherein R.sub.3 is a hydrogen atom or straight or branched chain C.sub.1-15 alkyl group or a protective group easily removable by acid hydrolysis, hydrogenolysis or enzyme existing in a living body;

Method for improving intestinal absorption of cephalosporin derivatives

Microorganisms are immobilized by adding microorganism cells to an aqueous solution of a mixture of a polymerizable starch and a polymerizable monomer, and, thereafter, polymerizing the polymerizable starch and polymerizable monomer, to prepare a polymer gel with microorganism cells enclosed therein. The polymerizable starch is prepared by introducing an acrylamidomethyl group into starch. The polymer gel has high mechanical strength and can be used repeatedly over long periods of the time while maintaining at high levels the reactivity of the microorganism enclosed therein.

Immobilization of microorganisms in a polymer gel

A secalonic acid derivative of the formula (I); ##STR1## wherein R is ##STR2## wherein R.sub.1 and R.sub.2 each independently is a hydrogen atom or a C.sub.1-4 alkyl group; R.sub.3 is a hydrogen atom, a C.sub.1-4 alkyl group, an aryl group, a C.sub.1-5 alkoxy group, a halogen atom, a cyano group, a carboxyl group, a sulfonic acid group, a carboxylic acid amide group or a sulfonic acid amide group; and R.sub.4 is a saturated or unsaturated C.sub.1-22 alkyl group, an aryl group or an aryl alkyl group, and may have a substituent; and the pharmaceutically acceptable salts thereof.

Secalonic acid derivatives and method for preparing thereof

A dried, sterilized column containing a carrier-fixed .gamma.-globulin capable of specifically combining with various harmful substances found in blood of patients suffering from certain diseases and acting as an antibody. The .gamma.-globulin fixed column according to the present invention has a prolonged storage stability, and an excellent activity and safety even after the storage for a prolonged period of time as compared with unsterilized columns. Therefore, the .gamma.-globulin fixed column according to the present invention may be advantageously used for medical instrument applications.

Dried, sterilized, gamma-globulin-fixed column and a process for

AI-77 compounds, pharmaceutically acceptable salts thereof, and a process for the preparation thereof are described, said compounds having the formulae ##STR1## wherein: X is NR.sub.6 or O; Y is NHR.sub.5 or combine with Z to provide a link for bonding C and C; Z is H or combines with Y to provide a link for bonding C and C; R.sub.1, R.sub.3 and R.sub.5 are each H, R', --CH.sub.2 R, or --COR; R.sub.6 is H or R; R.sub.7 is H, R or CH.sub.2 R; R is a hydrocarbon group consisting of a saturated or unsaturated straight or branched aliphatic group of C.sub.1 to C.sub.17, an aromatic group of C.sub.6 to C.sub.10, a cage type group of C.sub.7 to C.sub.10, a monocyclic aliphatic group of C.sub.3 to C.sub.8, an aromatic-aliphatic group of C.sub.7 to C.sub.15, a heterocyclic hydrocarbon of C.sub.1 to C.sub.9, wherein the above hydrocarbons can be substituted with one or more groups selected from halogen, oxo, carboxyl, hydroxyl, a saturated or unsaturated straight or branched aliphatic group of C.sub.1 to C.sub.5, an aromatic group of C.sub.6 to C.sub.10, a monocyclic aliphatic group of C.sub.3 to C.sub.8, an aromatic-aliphatic group of C.sub.7 to C.sub.11, alkoxy of C.sub.1 to C.sub.5, thioalkoxyl of C.sub.1 to C.sub.5, carboalkoxyl of C.sub.1 to C.sub.6, acyl of C.sub.1 to C.sub.5, acyloxy of C.sub.2 to C.sub.6 and a heterocyclic group of C.sub.1 to C.sub.9 ; R' is the same as R exclusive of those groups wherein unsaturated carbon or tertiary carbon is directly bonded to O or N; R.sub.2 is H, or combines with T.sub.1 to provide a link for bonding C and O in a lactone ring; T.sub.1 is OH or combines with R.sub.2 to provide a link for bonding C and O in a lactone ring; R.sub.4 is H or combines with T.sub.2 to provide a link for bonding C and O in a lactone ring; and T.sub.2 is OH or combines with R.sub.4 to provide a link for bonding C and O in a lactone ring; and pharmaceutically acceptable salts thereof.

AI-77 Compounds and pharmaceutically acceptable salts thereof

A process for producing L-tryptophan or a derivative thereof is disclosed, wherein an indole compound is reacted with serine, or with pyruvic acid and ammonium ion, in the presence of a culture or treated culture of a microorganism of genus Aeromonas or genus Klebsiella having the ability to produce L-tryptophan or a derivative thereof from an indole compound and serine, or from an indole compound, pyruvic acid and/or its salt, and ammonium ion.

Process for producing L-tryptophan or derivatives thereof using

A process for producing L-tryptophan or a derivative thereof is disclosed, wherein an indole compound is reacted with serine, or with pyruvic acid and/or its salt and ammonium ion, in the presence of a culture or treated culture of a particular microorganism of genus Enterobacter having a special ability to produce L-tryptophan or a derivative thereof from an indole compound and serine, or from an indole compound, pyruvic acid and/or its salt, and ammonium ion.

Process for producing L-tryptophan or derivatives thereof using a

A plasminogen activator having a molecular weight of 45,000 to 68,000 is formed as a single fraction in the cells of human kidney or lung, and is separated and recovered with good efficiency without reducing its molecular weight. The pH of a solution to be contacted with said cells and the concentration of dissolved oxygen should be maintained within suitable ranges in order to form the plasminogen activator having a molecular weight of 45,000 to 68,000 as a single fraction. Furthermore, by properly adjusting the residence time of the solution with the cells, the activator can be formed over a long period of more than 40 days. To separate the activator, the pH of the solution in the separating step is maintained preferably at 4 to 12. By causing a metal chelating agent to be present in the solution in the separating step, the plasminogen activator can be obtained without reducing its molecular weight.

Production of plasminogen activator

Novel 7.alpha.-methoxycephalosporin derivatives having a high antimicrobial activity. They are useful for the medical treatment of diseases infected by gram-positive bacteria and gram-negative bacteria. More particularly, they show an antimicrobial activity against bacteria such as Eschericha coli Proteus, Citrobacter and Enterobacter which bacteria have resistance to the conventionally employed cephalosporins, and they are effective for the medical treatment of diseases infected by these bacteria. Such 7.alpha.-methoxycephalosporin derivatives are prepared by a relatively simple method.

Growing community of inventors

Yokohama, Japan

Mitsuru Shibukawa