Meiji Seika Kaisha, Ltd.

Meiji Seiki Kaisha, Ltd.

Takehiko Sawabe

Kazuhiro Aihara

Kunio Atsumi

Takashi Ando

Eiki Shitara

Yuko Kano

Takahisa Maruyama

Takashi Ida

Takashi Watanabe

Yasuo Yamamoto

Keiichi Ajito

Hisashi Suzuki

Hiromi Takata

Kazumi Ota

Toshiki Fujita

Toshifumi Hasegawa

Shinichi Kitahara

Nobuyoshi Baba

An objective of the present invention is to provide compounds that are effective against various resistant bacteria which cause current clinical problems, for example, pneumococci including penicillin resistant(PRSP),including bata-lactamase-nonproducing ampicillin-resistant(BLNAR), and(Branhamella) catarrhalis. The present invention provides 2-ethenylthio-based carbapenem derivatives represented by the formula (I) or pharmaceutically acceptable salts thereof that are effective, for example, against pneumococci including penicillin resistant(PRSP),including beta-lactamase-nonproducing ampicillin-resistant(BLNAR), and(Branhamella) catarrhalis: 

2-thioethenyl substituted carbapenem derivatives

The present invention relates to a compound represented by formula (1) or a salt thereof: wherein R represents a group that is easily removable upon hydrolysis in vivo. This compound is usable in the production of prodrug-type carbapenem antibacterial agents for oral administration. The use of this compound in the process of production of the antibacterial agents can realize enhanced production efficiency and reduced production cost.

Malonic acid monoesters and process for producing the same

This invention relates to crystals of compounds of formula (I), wherein TBS represents t-butyldimethylsilyl, and Ph represents phenyl, or its salt or solvate. Compounds of formula (I) are synthesis intermediates of 2-substituted-1&#x3b2;-methyl carbapenem compounds useful as antimicrobial agents. The crystals of the present invention have excellent handleability and can realize the production of carbapenem compounds having excellent antimicrobial activity in a simpler manner with improved yield and purity. 

Crystalline carbapenem intermediate

An objective of the present invention is to provide carbapenem derivatives which have strong antibiotic activity also against MRSA, PRSP, Influenzavirus, and &#x3b2;-lactamase producing bacteria and are stable to DHP-1. The carbapenem derivatives according to the present invention are compounds represented by formulae (I) and (II) or pharmaceutically acceptable salts thereof:wherein Rrepresents H or methyl, Rand Reach independently represent H; halogen; substituted or unsubstituted alkyl; cycloalkyl; substituted or unsubstituted alkylcarbonyl; carbamoyl; substituted or unsubstituted aryl; substituted or unsubstituted alkylthio; morpholinyl; alkylsulfonyl; or formyl, n is 0 (zero) to 4, and Hy represents a substituted or unsubstituted monocyclic or bicyclic heterocyclic group.

Carbapenem derivatives

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Yokohama, Japan

Takehiko Sawabe