Fujisawa Pharmaceutical Company, Ltd.

Anges Mg, Inc.

Toshiyuki Chiba

Takao Takaya

Hisashi Takasugi

Kiyoshi Tsuji

Masayoshi Murata

Fumiyuki Shirai

Zenzaburo Tozuka

Hiroaki Ohtake

Ryuichi Morishita

Akira Yamada

Hideo Tsutsumi

Kohji Hattori

Takeshi Nakai

Satoru Kuroda

Kazuhiro Maeda

Ikuo Kawamura

Toshio Ogiwara

Toshiko Sugimoto

Takashi Masugi

Motohiro Hino

Kenichi Washizuka

Kiyosha Tsuji

Administration of a decoy, i.e. a compound which specifically antagonizes the nucleic acid domain to which NF-&#x3ba;B is bound, is effective in the treatment and prevention of diseases caused by the transcriptional regulatory factor NF-&#x3ba;B, such as ischemic diseases, inflammatory diseases, autoimmune diseases, cancer metastasis and invasion, and cachexia.

Remedy and preventive for diseases caused by NF-&#x3ba;B

Administration of a decoy, i.e. a compound which specifically antagonizes the nucleic acid domain to which NF-&kgr;B is bound, is effective in the treatment and prevention of diseases caused by the transcriptional regulatory factor NF-&kgr;B, such as ischemic diseases, inflammatory diseases, autoimmune diseases, cancer metastasis and invasion, and cachexia.

Remedy for diseases associated with NF-&kgr;B

1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds

Preparation of optically active 3-substituted azetidinones of the formula (I) ##STR1## in which R.sup.1 is a hydroxy-protective group wherein an allylic alcohol of the formula (II) ##STR2## is acylated, then subjected to asymmetric enzymatic hydrolysis yielding the R-allylic alcohol. The hydroxyl group is protected and then stereoselectively reacted with an amine which is subsequently cyclized to yield the desired 3-substituted azetidinone. Two new species of microorganisms have been isolated, Pimelobacter sp. No. 1254 and Bacillus megaterium No. 1253 which exhibit stereoselective esterase activity.

Enzymatic process for preparing optically active 3-substituted

1-Azabicyclo[3.2.0]hept-2-ene-2-carboxyic acids having antimicrobial activity have been prepared.

The invention relates to novel intermediate compounds for preparation of compounds of high antimicrobial activity, said intermediate compounds being of one of the formulas: ##STR1## wherein R.sup.1 is carboxy or protected carboxy,

3-alkenyl-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds

The invention relates to the preparation of 3,4-disubstituted-2-azetidinone compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or amido-protective group, R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl, R.sup.3 is lower alkyl, and R.sup.4 is 1-(lower)alkyl-1-hydroxy(C.sub.2 -C.sub.6)alkyl, 1-(lower)alkyl-1-(protected hydroxy)-(C.sub.2 -C.sub.6)alkyl or 2-thioxothiazolidin-3-yl, useful as an intermediate for the production of antimicrobial agents by reacting a compound a compound of the formula: ##STR2## in which R.sup.5 is acyl, or salts thereof, with a compound of the formula:

3,4-disubstituted-2-azetidinone derivatives and processes for

The invention relates to an antimicrobial compound of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,

3-Alkenyl-1-azabicyclo(3.2.0)hept-2-ene-2-carboxylic acid compounds

7-substituted 3-cephem or cepham compounds characterized by the grouping, in the 7-position thereof, of the formula:

Cephem and cepham compounds and processes for preparation thereof

The invention relates to a method of producing an azetidinone derivative of the formula: ##STR1## which comprises reacting a compound of the formula ##STR2## with a compound of the formula ##STR3## and then subjecting the resulting compound to hydrolysis, the substituents above being as defined in the specification.

Azetidinone derivatives and processes for production thereof

Compounds of the formula: ##STR1## wherein R.sup.2 is cyclo(lower)alkyl or lower alkynyl having 2 to 6 carbon atoms, and

New cephem and cepham compounds and processes for preparation thereof

A compound of the formula: ##STR1## wherein R.sup.2 is halo(lower)alkyl, and

New cepham compounds and processes for the production thereof

The invention relates to novel cephem compounds, of high antimicrobial activity, of the formula ##STR1## wherein R.sup.1 is amino or protected amino,

Cephem compounds and processes for preparation thereof

Cephem and cepham compounds

Thiazole intermediates for cephalosporins have been prepared.

Growing community of inventors

Osaka, Japan

Toshiyuki Chiba