Meiji Seika Kaisha, Ltd.

Taisho Pharmaceutical Co., Ltd.

Sagami Chemical Research Center

Meiji Seika Pharma Co., Ltd.

Keiichi Ajito

Shuichi Gomi

Mikio Yamamoto

Seiji Shibahara

Akira Shimizu

Osamu Hara

Ken-ichi Kurihara

Kunio Atsumi

Tomoaki Miura

Dai Kubota

Shoichi Murakami

Minako Araake

Kou Kumura

Minoru Ishikawa

Nobue Kikuchi

Tsuneo Ishizuka

Takashi Watanabe

Kenichi Kurihara

Kiyoaki Katano

Tsuneo Okonogi

Mitsugu Hachisu

Kenichi Kanemoto

Eijirou Umemura

Kazutaka Ueda

Satomi Masaki

Yoshinari Wakiyama

Chizuko Kaji

Aiko Miyata

Satoshi Yoshida

Yasuo Sato

Shigeharu Inouye

Takuji Yoshida

Masato Kashimura

Yasuo Yamamoto

Eiki Shitara

Takashi Yaguchi

Kazuhiro Aihara

Shinji Miyadoh

Yuji Tabata

Tomohiro Sugimoto

Takayuki Usui

Kiyoshi Tanabe

Naoto Ohkura

Kanako Yamamoto

Shohei Yasuda

Naoki Sasamoto

Jun Kurosaka

Takehiko Sawabe

Rie Shinei

Kazuyuki Fujishima

Shinya Ikeda

Satomi Natsume

Yumiko Fujihira

Hideki Fushimi

Mari Nakatani

Tetsuro Hara

Munenori Inoue

Tadashi Katoh

Eriko Tanaka

Kuniaki Tatsuta

Naokazu Yahata

Kaori Miyajima

Takeshi Furuuchi

Shokichi Ouchi

A 10-azalide compound having a 4-membered ring structure crosslinked at the 10- and 12-positions, which is represented by the formula (I), and is effective on even, or erythromycin resistant bacteria (e.g., resistant pneunococci and streptococci). 

10a-azalide compound having 4-membered ring structure

This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, Rrepresents a halide, nitro, substituted Calkyl, optionally substituted amino, Calkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, Rrepresents a hydrogen atom or Calkyl, Rrepresents Calkyl, all of R, R, and Rrepresent a hydrogen atom, Rrepresents Calkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases. 

Lincomycin derivatives and antimicrobial agents comprising the same as active ingredient

An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while Rrepresents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while Rrepresents aryl or a five- or six-membered monocyclic heterocyclic group; Rrepresents a hydrogen atom or Calkyl; Rrepresents Calkyl or Ccycloalkyl-Calkyl; R, R, and Rrepresent a hydrogen atom; Rrepresents Calkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases. 

Lincosamide derivatives and antimicrobial agents comprising the same as active ingredient

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 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

Compounds represented by the general formula (1) or pharmaceutically acceptable salts thereof, effective in the prevention and/or treatment of infections with microbes: (1) (a) wherein Ris hydrogen or straight-chain Calkylcarbonyl; Ris hydrogen or Calkylcarbonyl; Ris hydrogen, Calkyl, Calkylcarbonyl, Calkenyl, Calkenylcarbonyl, Calkynyl, or an Ar&#x2014;B&#x2014; group (wherein Ar is aryl or a heterocyclic group; and B is Calkyl, Calkylcarbonyl, Calkenyl, Calkenylcarbonyl, or Calkynyl); R, R, Rand Rare each hydrogen, Calkyl, Calkenyl, Calkynyl, or an Ar&#x2014;B'&#x2014; group (wherein B&#x2032; is Calkyl, Calkenyl, or Calkynyl); X is oxygen or &#x2014;NR&#x2014; (wherein Ris hydrogen, Calkyl or Calkyl which may be substituted with Ar); and Ris hydrogen or a group represented by the general formula (a) (wherein Rand Rare each hydrogen or straight-chain or branched Calkylcarbonyl) 

Azalide and azalactam derivatives and method for producing the same

&OHgr;-amino-&agr;-hydroxycarboxylic acid derivatives having integrin &agr;&ngr;&bgr;3 antagonistic activity

3-modified leucomycin derivatives

Phenylpiperazine derivatives as integrin &agr;v&bgr;3 antagonists

Aminopiperidine derivates as integrin &agr;v&bgr;3 antagonists

Compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as abortifacients, oral contraceptive pills, carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for endometriosis, meningioma, and myeloma, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance.

Tetrahydronaphthofuranone derivatives and process for producing the same

16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.2 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.3 represents a hydrogen atom or a straight-chain aliphatic acyl group having 2 to 4 carbon atoms; and R.sup.4 represents a hydrogen atom or a straight-chain aliphatic or aromatic acyl group having 1 to 10 carbon atoms;

16-membered macrolide derivatives

16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 represents a straight-chain alkyl group having 1 to 3 carbon atoms; R.sup.2 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.3 represents a hydrogen atom or a COR.sup.6 group, wherein R.sup.6 is as defined above; R.sup.4 represents a straight-chain alkyl group having 1 to 4 carbon atoms or a substituted or unsubstituted allyl group; and R.sup.5 represents a substituted or unsubstituted, straight-chain or branched alkyl, alkenyl or aralkyl group having 1 to 10 carbon atoms; and pharmaceutically acceptable salts thereof are disclosed. These compounds show excellent and long-acting antimicrobial activities. A novel process for producing these 16-membered macrolide derivatives is further disclosed.

16-membered macrolide derivatives and process for producing the same

16-membered macrolide compounds wherein both of hydroxyl groups at the 3'- and 4'-positions form ether bonds together with two alkyl groups which are either the same or different from each other is useful as an antibacterial agent. The macrolide compounds represented by formula (I) are prepared by chemically modifying midecamycin A.sub.3 to obtain a synthesis intermediate of the formula (II), which is further chemically modified. ##STR1##

16-membered macrolide derivative having sustained antibacterial activity

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Kawasaki, Japan

Keiichi Ajito