Meiji Seika Kaisha, Ltd.

Meiji Seika Kabushiki Kaisha

Taisho Pharmaceutical Co., Ltd.

Meiji Seika Pharma Co., Ltd.

Other

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Sagami Chemical Research Center

Meiji Seiki Kaisha, Ltd.

Eiki Shitara

Tomoaki Miura

Takashi Ando

Takashi Tsuruoka

Tomio Takeuchi

Takashi Ida

Satoshi Yoshida

Kunio Atsumi

Kiyoaki Katano

Shokichi Ohuchi

Yasuo Yamamoto

Toshiro Sasaki

Masato Kashimura

Kazuhiro Aihara

Tomohiro Sugimoto

Kenichi Kanemoto

Dai Kubota

Kanako Yamamoto

Naoki Sasamoto

Hiroyuki Iida

Jun Kurosaka

Emiko Hatsushiba

Yasuko Isomura

Kenji Asai

Masaro Shimizu

Kazue Yaegashi

Midori Ishikawa

Takahiro Imai

Yuko Kano

Haruhisa Ogita

Mami Kawaguchi

Takahisa Maruyama

Shohei Yasuda

Takehiko Sawabe

Yoshio Nishimura

Ken Chikauchi

Katsuhiko Noguchi

Nobuyuki Hori

Tomohiro Ozawa

Takashi Watanabe

Katsuyoshi Iwamatsu

Masato Hayashi

Keiichi Ajito

Hiroko Ogino

Fukio Konno

Tomoya Machinami

Keiji Tamura

Naomi Osada

Naoto Ohkura

Yasuyuki Ichimaru

Yasunobu Ushiki

Kou Kumura

Madoka Kawamura

Akira Manaka

Kazumi Ota

Hiromi Watanabe

Jun Nagura

Shinichi Kitahara

Toshifumi Hasegawa

Mari Nakatani

Munenori Inoue

Tadashi Katoh

Shinya Ikeda

A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas). 

C-4&#x2033; position substituted macrolide derivative

A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci). 

10a-Azalide compound crosslinked at 10a- and 12-positions

[Object]: To provide a compound having a novel structure effective againstand erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.

10a-Azalide compound

The present invention relates to compounds of formula (I) and a process for producing the same. In formula (I), X represents a halogen atom, and Rrepresents group &#x2014;CORwherein Rrepresents group OM or C1-12 alkyloxy wherein M represents a hydrogen atom, an alkali metal, an alkaline earth metal, or quaternary ammonium. The use of this compound as a synthetic intermediate can realize the production of carbapenem derivatives having potent antimicrobial activity in an efficient and safe manner at low cost. 

Imidazothiazole derivatives and process for producing the same

The present invention relates to compounds represented by formula (1) and a process for producing the same. The use of these compounds can realize the production of carbapenem derivatives having potent antimicrobial activity and a wide antimicrobial spectrum in a safe and cost-effective manner. 

Intermediates of 2-substituted carbapenem derivatives and process for production thereof

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

A compound of the formula (I):and a compound of the formula (V):as well as a compound of the formula (X):which are each a novel siastatin B derivative having a potent inhibitory activity against a glycosidase, are now synthesized by new processes. The compound of the formula (I), the compound of the formula (V) and the compound of the formula (X) have a potent enzyme-inhibitory activity to a glycosidase, which is particularly N-acetyl-galactosaminidase, galactosidase, glucosidase and mannosidase.

Siastatin B derivatives having a glycosidase inhibitory activity and processes for producing the same

Carbapenem derivatives of quarternary salt type

2-n-substituted or unsubstituted-2-amino-5-methylpiperidine-3,4-diols and processes for the preparation thereof

A .gamma.-diketone compound represented by the following formula (I) and a pharmaceutically acceptable salt and solvate thereof having platelet aggregation inhibitory activity is disclosed: ##STR1## wherein B is --Z--(CH.sub.2).sub.q COOR.sup.7 and A is the following group (II) or (III): ##STR2##

.gamma.-diketone compounds with inhibitory activity against platelet

Compounds with platelet aggregation inhibitor activity

.gamma.-Diketone compounds with inhibitory activity against platelet

A compound represented by the general formula (I) and a pharmaceutically acceptable salt and solvate thereof having an effect for inhibiting the agglutination of platelets is disclosed: ##STR1## wherein R.sup.1 represents a group --W--(CH.sub.2).sub.i --COOR.sup.3,

Compound with platelet aggregation inhibitor activity

Growing community of inventors

Yokohama, Japan

Eiki Shitara