Fujisawa Pharmaceutical Company, Ltd.

Wakunaga Pharmaceutical Co., Ltd.

Masayoshi Murata

Takao Takaya

Hideo Tsutsumi

Keiji Matsuda

Kohji Hattori

Hisashi Takasugi

Takashi Nakajima

Yoshikazu Inoue

Akiteru Yoshioka

Toshiyuki Chiba

Kiyotaka Ito

Nobuyoshi Yasuda

Fumiyuki Shirai

Satoru Kuroda

Hiroaki Ohtake

Akira Yamada

Chiyoshi Kasahara

Kenichi Washizuka

Kazuo Sakane

Keiji Hemmi

Hiroshi Kayakiri

Akira Yazaki

Satoshi Inoue

Kiyoshi Taniguchi

Masahiro Neya

Hitoshi Sawada

Naoaki Fujii

Hitoshi Hamashima

Minoru Sakurai

Motohiro Hino

Yasuyo Tomishima

Tatsuya Zenkoh

Takeshi Terasawa

Masashi Imanishi

David Barrett

Hideo Tsutumi

Yoshihiro Murakami

Yutaka Nakajima

Hohji Hattori

The present invention relates to a compound formula (I) wherein X is bond or &mdash;O&mdash;CH &mdash;, (II) or (III) R is hydrogen or an amino protective group, a is phenyl, indolyl or carbazolyl, each of which may be substituted with one or two substituent(s), and B is hydrogen; halogen; lower alkyl; lower alkoxycarbonyl; cyclo(lower)alkyl; or a heterocyclic group, naphthyl, 1,2,3,4-tetrahydronaphthyl, benzyl or phenyl, each of which may be substituted with one or two substituent(s), or a salt thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiures or urinary incontinence.

Aminoalcohol derivatives

Endothelin antagonists

Substituted 3-pyrrolidinylthio-carbapenems as antimicrobial agents

Novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and processes for their preparation are disclosed. These novel compounds have antimicrobial activity, and are useful as a medicament in the treatment of infectious diseases in human beings and animals.

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

Certain tricyclic pyrido[3,2,1-ij]cinnoline-8-carboxylates, useful as

The invention relates to carbapenem derivatives useful as antimicrobial agents, more particularly to intermediate compounds for the preparations thereof of the formula ##STR1##

Processes for preparing carbapenem derivatives

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

Novel carbapenem compounds of the formula: ##STR1## in which R.sup.1 is carboxy or protected carboxy,

Carbapenem compounds

The present invention concerns intermediates in the preparation of novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof. The novel 3-pyrrolidinylthio-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof show antimicrobial activity.

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

The invention relates to compounds of the formula: ##STR1## in which R.sup.4 is an unsaturated, 5 or 6-membered heteromonocyclic group,

Intermediates for the preparation of compounds of antimicrobial activity

Novel 3-pyrrolidinylthio-1-azabiycyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds and pharmaceutically acceptable salts thereof have antimicrobial activity and are useful as medicaments in the treatment of infectious diseases caused by pathogenic microorganisms.

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

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

3-thio pyrrolidines are intermediates for carbapenams.

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

Growing community of inventors

Osaka, Japan

Masayoshi Murata