Meiji Seika Kaisha, Ltd.

Hashimoto Forming Industry Company Limited

Meiji Seika Kabushiki Kaisha

Riken Corporation

Kabushiki Kaisha Yakult Honsha

Japanese Foundation for Cancer Research

Meiji Seiki Kaisha, Ltd.

Yuko Kano

Kazuhiro Aihara

Kunio Atsumi

Katsuyoshi Iwamatsu

Takashi Ida

Toshiro Sasaki

Takahisa Maruyama

Takashi Ando

Atsushi Tamura

Yumiko Toyooka

Hiromasa Takizawa

Yumiko Sambongi

Seiji Shibahara

Tatsuya Tamura

Eiki Shitara

Yasuo Yamamoto

Sohjiro Shiokawa

Masaki Tsushima

Kiyoshi Tanabe

Hideo Kitagawa

Takehiko Sawabe

Yoshihisa Akiyama

Toshio Ohkura

Toshiki Fujita

Takashi Watanabe

Toshiaki Kudo

Kazuko Kobayashi

Kenichi Fushihara

Hisashi Suzuki

Hiromi Takata

Hiroyuki Seimiya

Kenichi Washizuka

Yoko Yashiroda

Fumiyuki Shirai

Minoru Yoshida

Nobuko Yoshimoto

Eijiro Umemura

Fumihito Setsu

Miyuki Ishii

Masayuki Okue

Kastuyoshi Iwamatsu

Nobuyoshi Baba

Tsubasa Chikada

Takehiro Fukami

Yasuko Kouda

Takeshi Tsumura

Provided are 2-(piperidin-1-yl)pyrimidin-4(3H)-ones or pharmaceutically acceptable salts thereof, each characterized by having a 1,8-diazaspiro[4.5]deca-3-ene, 1-oxa-8-azaspiro[4.5]deca-3-ene, 2,8-diazaspiro[4.5]deca-3-ene, 2-oxa-8-azaspiro[4.5]deca-3-ene, 2,9-diazaspiro[5.5]undeca-3-ene, 1-oxa-9-azaspiro[5.5]undeca-3-ene, 1,9-diazaspiro[5.5]undeca-4-ene, or 3,9-diazaspiro[5.5]undeca-1-ene structure represented by the following general formula (1): 

Compound or pharmaceutically acceptable salt thereof

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:

The carbapenem derivatives represented by the following formula (I) is disclosed. These compounds have strong anti-bacterial activities against bacteria including methicillin resistant,, penicillin resistant,, Enterococci, influenza, and &bgr;-lactamase producing bacteria, and have high stabilities to DHP-1

Compounds of formula (I) and compounds of formula (II) which have potent antimicrobial activity against a wide range of bacteria including Gram-positive bacteria and Gram-negative bacteria as well as heve potent antimicrobial activity against various &bgr;-lactamase-producing bacteria, MRSA, and resistant Pseudomonas aeruginosa and are very stable against DHP-1.

Imidazo&lsqb;5,1-b&rsqb;thiazol-3-yl carbapenem antimicrobials

An apparatus producing an elongated member having a main body portion and terminal portions extending form ends thereof includes bending an elongated strip between circumferential faces of first forming rolls and second forming rolls having parallel central rotational axes. The circumferential faces of the first forming rolls include annular main body portion bending sections that form the main body portion in the strip and adjacent transition portion bending sections that form adjacent transition portions in the strip, thereby forming an intermediate stage elongated member. The transition portions have a cross-section that changes continuously from the annular cross-section of the main body portion to a different cross-section of the terminal portions. The intermediate elongated member is further formed by annular main body portion and transition portion bending sections of the second forming rolls corresponding to the respective bending sections of the first forming rolls in circumferential length but having a different axial dimension such that the intermediate stage elongated member approaches a shape of the fully-formed elongated member.

Apparatus for producing rigid elongated member for use in vehicles

A method of producing an elongated member having a main body portion and terminal portions extending form ends thereof includes bending an elongated strip between circumferential faces of first forming rolls and second forming rolls having parallel central rotational axes. The circumferential faces of the first forming rolls include annular main body portion bending sections that form the main body portion in the strip and adjacent transition portion bending sections that form adjacent transition portions in the strip, thereby forming an intermediate stage elongated member. The transition portions have a cross-section that changes continuously from the annular cross-section of the main body portion to a different cross-section of the terminal portions. The intermediate elongated member is further formed by annular main body portion and transition portion bending sections of the second forming rolls corresponding to the respective bending sections of the first forming rolls in circumferential length but having a different axial dimension such that the intermediate stage elongated member approaches a shape of the fully-formed elongated member.

Rigid elongated member for use in vehicles and producing method and

Cephem derivatives

A cephalosporin derivative having a quaternary salt type substituent group at the 3-position, represented by formula (I): ##STR1## wherein X is a carbon atom or a nitrogen atom; Y is a sulfur atom, an oxygen atom or a nitrogen atom substituted with a substituted or unsubstituted lower alkyl group; R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group; R.sup.2 is a lower alkyl group, a substituted lower alkyl group, a lower alkylene group or a substituted lower alkylene group; and A is an unsaturated six-membered heterocyclic ring containing at least one nitrogen atom, or a pharmaceutically acceptable salt thereof is disclosed. The derivatives have excellent antibacterial activities and can be used as a drug for the treatment of various bacterial infections.

Cephalosporin derivatives

Growing community of inventors

Yokohama, Japan

Yuko Kano