Shionogi Company Limited

Eiji Kondo

Naoki Tsuji

Kentaro Tanaka

Yoshimi Kawamura

Kouichi Matsumoto

Jun'ichi Shoji

Koichi Matsumoto

Takao Konishi

Takashi Mitsugi

Tadashi Yoshida

Tamio Fujiwara

Teruo Hattori

Yoshiyuki Hayashi

Junichi Shoji

Ryonosuke Muneyuki

Toshiyuki Kamigauchi

Masaru Shin

Shinzo Matsuura

Kenzo Koizumi

Mikao Mayama

Yoshiharu Wakisaka

Takashi Fujiwara

Goro Kuwajima

Masaaki Kobayashi

Junichiro Asaka

Glycopeptide antibiotics PA-45052 which are produced by Nocardia orientalis PA-45052, show potent activity against gram-positive bacteria, especially against methicillin-resistant bacteria, and stimulate growth of animals.

Glycopetide antibiotic PA-45052-B

An anti-mycoplasma agent comprising tropolone, its derivatives, represented by the formula: ##STR1## (wherein R.sub.1 is hydroxy, aliphatic acyloxy, arylacyloxy, arysulfonyloxy, carboxyalkyloxy or its ester, benzoylalkyloxy, alkenyloxy, 1,3-dihydro-3-oxo-1-isobenzofuranyloxy, (2-oxo-5-methyl-1,3-dioxol-4-yl)methyloxy or thiocyanato and R.sub.2 is hydrogen, halogen, hydroxy, alkyl or alkoxy) and their salts as an active ingredient, which has potent activity especially against tylosin-resistant mycoplasma both in vitro and in vivo and is effectively used in treating the diseases caused thereby.

Anti-mycoplasma agent

The compounds of the formula: ##STR1## wherein R is ##STR2## or H, wherein X is NH.sub.2 and Y is CH.sub.3 ; or X is OH and Y is H, and their pharmaceutically acceptable salts. The compounds have a potent activity against gram-positive bacteria, especially, methicillin-resistant bacteria.

Novel glycopeptide antibiotics

The whole DNA sequence coding for flagellin of E. coli (hag gene) cloned in phage .lambda. was determined. The hag gene is introduced into pBR322 and the region of the hag gene concerning the antigencity of flagella is lacked, into which linkers are inserted. Where the vector in which foreign DNA is inserted in the linker is introduced in E. coli forming no flagella, the E. coli can form flagella and possesses motility. The flagella comprises flagellin fused with foreign peptide encoded by the foreign DNA. Namely, the foreign peptide is excreted outside of bacteria. This system can be utilized in determination of epitope and preparation of antigen as well as excretion of peptide.

DNA encoding flagellin and vector having the same

Antibiotics DO-248-A and DO-248-B of the following Formula I: ##STR1## wherein R is ethyl or isopropyl, have antibacterial activity against acid-fast bacteria. DO-248-A, DO-248-B, or their pharmaceutically acceptable salts are, as an active ingredient of anti-fast-acid drugs, orally or parenterally administered to human beings or animal. DO-248-A and DO-248-B are prepared by incubating an antibiotic DO-248-A- and/or DO-248-B-producing microorganism belonging to genus Streptoverticillium in a medium and recovering antibiotic DO-248-A and/or DO-248-B from the culture broth.

Antibiotics DO-248-A and B and process for preparing the same

Antibiotics PA-41746-A.sub.2, PA-41746-E and PA-41746-F produced by fermentation of Streptomyces pluracidomyceticus on a conventional culture medium, having .beta.-lactamase inhibitory activities and excellent antimicrobial activities, and useful as drugs for treatment of infections in humans or animals, or as disinfectants.

Carbapenem-type antibiotics

A new antibiotic having .beta.-lactamase inhibitory activity, PA-39504-X.sub.1 of the formula: ##STR1## being useful as a medicament and a veterinary drug for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces argenteolus PA-39504 or Streptomyces tokunonensis PA-31088 in a suitable medium and recovering PA-39504-X.sub.1 from the cultured broth.

Antibiotic PA-39504-X.sub.1 and production thereof

New antibiotics having .beta.-lactamase inhibitory activity, PA-41746-B and C of the formula ##STR1## wherein R is carboxymethylsulfinyl (PA-41746-B) or formylsulfinyl (PA-41746-C) and the pharmaceutically acceptable salts being useful as a medicament, a veterinary drug and a disinfectant for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces pluracidomyceticus in a suitable medium and isolating PA-41746-B and/or PA-41746-C from the culture broth.

Antibiotics PA-41746-B and C

A new antibiotic having .beta.-lactamase inhibitory activity, PA-39504-X.sub.3 of the formula: ##STR1## and the pharmaceutically acceptable slats being useful as a drug, a animal drug and a disinfectant for inhibiting the growth of gram-positive and gram-negative pathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces argenteolus PA-39504 or Streptomyces tokunonensis PA-31088 in a suitable medium and isolating PA-39504-X.sub.3 from the cultured broth.

Antibiotic PA-39504-X.sub.3 and production thereof

A new process for preparing thienamycin, a known antibiotic useful as a medicament and veterinary drug, characterized by cultivating Streptomyces penemifaciens sp. nov. in a suitable medium and recovering thienamycin from the fermentation broth.

Process for preparing thienamycin

A process for producing 6-aminopenicillanic acid and 6-aminopenicillanic acid S-oxide by means of enzymes produced by microbes belonging to Arthrobacter genus, especially Arthrobacter cremorum and Arthrobacter flagellum.

Process for producing 6-aminopenicillanic acid and 6-aminopenicillanic

Penicillins and cephalosporins can be synthesized by the action of an acylase on a penicillin or cephalosporin nucleus amine as substrate and an ester (I) of the following formula as the acyl source: ##STR1## (wherein RCO is an acyl group in penicillin or cephalosporin side chains;

Enzymatic synthesis of .beta.-lactam antibacterials

A new antibiotic having .beta.-lactamase inhibitory activity, PA-31088-IV, being useful as a medicament and a veterinary drug for inhibiting the growth of gram-positive and gram-negative phathogenic microorganisms and a process for preparing the same, being characterized by cultivating Streptomyces tokunonensis sp. nov. in a suitable medium and recovering PA-31088-IV from the cultured broth.

Antibiotic PA-31088-IV and production thereof

Penicillin or cephalosporin antibiotics represented by following formula: ##STR1## where ##STR2## is an acyl group derived from an .alpha.-amino acid, N-ammonium salt of .alpha.-amino acid, or N--(C.sub.1 to C.sub.10) acyl-.alpha.-amino acid; COOM is carboxy or carboxylate salt group! Are prepared by treating an amino compound selected from a group consisting of 6-aminopenicillanic acid, 7-aminocephalosporanic acid, 7-aminodeacetoxycephalosporanic acid, and their salts with an ester represented by following formula:

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Osaka, Japan

Eiji Kondo