Meiji Seika Kaisha, Ltd.

Meiji Seiki Kaisha, Ltd.

Takahisa Maruyama

Yuko Kano

Kazuhiro Aihara

Takashi Ida

Kunio Atsumi

Takashi Ando

Toshiro Sasaki

Katsuyoshi Iwamatsu

Yumiko Sambongi

Yasuo Yamamoto

Eiki Shitara

Kiyoshi Tanabe

Hideo Kitagawa

Takehiko Sawabe

Hiromasa Takizawa

Yoshihisa Akiyama

Toshiki Fujita

Hisashi Suzuki

Hiromi Takata

Kastuyoshi Iwamatsu

Nobuyoshi Baba

2-Ethenylthio-type carbapenem derivatives of formula (I) or pharmaceutically acceptable salts thereof are provided. The compounds according to the present invention have potent antimicrobial activity and a wide antimicrobial spectrum against pneumococci including penicillin resistant(PRSP),including &#x3b2;-lactamase-negative, ampicillin-resistant(BLNAR), and(). 

2-thioethenyl substituted carbapenem derivatives

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: 

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

Carbapenem derivatives of quarternary salt type

Carbapenum derivatives

Disclosed is a novel carbapenem derivative having a substituted imidazo&lsqb;5,1-b&rsqb;thiazole group at the 2-position on the carbapenem ring have high anti microbial activities against &bgr;-lactamase producing bacteria, MRSA, resistant- , PRSP, enterococci, and influenza, and high stabilities to DHP-1. According to the present invention, there is provided a compound represented by the formula (I), or a pharmacologically acceptable salt thereof or an ester at the 3-position on the carbapenem ring thereof:

Disclosed is a novel carbapenem derivative having a substituted imidazo&lsqb;5,1-b&rsqb;thiazole group at the 2-position on the carbapenem ring have high anti-microbial activities against &bgr;-lactamase producing bacteria, MRSA, resistant- , PRSP, enterococci, and influenza, and high stabilities to DHP-1. According to the present invention, there is provided a compound represented by the formula (I), or a pharmacologically acceptable salt thereof or an ester at the 3-position on the carbapenem ring thereof:

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Yokohama, Japan

Takahisa Maruyama