Meiji Seika Kaisha, Ltd.

Meiji Seika Kabushiki Kaisha

Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Merck + Co., Inc.

Other

Koichi Shudo

Nimura Genetic Solutions Co., Ltd.

Forest Research Institute Malaysia

Meiji Seika Kaburhiki Kaisha

Seiji Shibahara

Tsuneo Okonogi

Shinichi Kondo

Yasushi Murai

Shigeharu Inouye

Katsuyoshi Iwamatsu

Kunio Atsumi

Atsushi Tamura

Tomoya Machinami

Takashi Tsuruoka

Shunzo Fukatsu

Taro Niida

Kiyoaki Katano

Shuichi Gomi

Mitsugu Hachisu

Fumiya Hirano

Toshiaki Kudo

Yasukatsu Yuda

Tadashi Wakazawa

Tomio Takeuchi

Yasuo Sato

Keiichi Ajito

Shigeharu Inoue

Fukio Konno

Hiroko Ogino

Masaki Tsushima

Takayuki Usui

Motohiro Nishio

Burton G Christensen

Akira Shimizu

Takashi Yoshida

Yuichi Yamamoto

Kenji Sakagami

Osamu Hara

Yoko Ikeda

Minako Araake

Tamako Tomomoto

Ken-ichi Kurihara

Tsuneo Ishizuka

Nobue Kikuchi

Takaaki Aoyagi

Nobuto Minowa

Daishiro Ikeda

Yuko Kano

Ken Nishihata

Toshio Yoneta

Sohjiro Shiokawa

Shigeharu Inoye

Naoki Yamazaki

Yuji Matsuhashi

Kazue Yasufuku

Aiko Miyata

Shinsuke Kato

Takako Taniguchi

Arthur A Patchett

Masaru Shimura

Takashi Shomura

Masao Koyama

Kenichi Kurihara

Toru Sasaki

Masaji Sezaki

Shigeo Seki

Hironobu Iinuma

Katsuharu Iinuma

Hiroo Hoshino

Keiichi Numata

Yoshiyuki Koyama

Satoru Nakabayashi

Haruo Yamamoto

Osamu Sakanaka

Masahiro Onodera

Yumiko Okada

Michiaki Iwata

Shokichi Ohuchi

Osamu Makabe

Toshio Nishizuka

Tsutomu Tsuruoka

Susumu Nishimura

Yasuyuki Ichimaru

Keiichi Imamura

Masayuki Takagi

Shinjiro Sumi

Makoto Ohyama

Osamu Itoh

Kozo Nagaoka

Tadaaki Okada

Masaaki Izumi

Eijiro Umemura

Szu Ting Ng

Chin Jye Tan

Yasuo Fukagawa

Yamazaki Naoki

Kunimoto Hotta

Shinsuke Katoh

Satoshi Nimura

Nobuko Okada

Tetsuro Hara

Seven novel antibiotic substances can be produced by cultivation of a microbial strain which has been isolated from a soil sample and which is designated assp. A 34030 (deposited under an access number FERM BP-10505 in terms of Budapest Treaty). These seven antibiotic substances are named as bispolide A1, bispolide A2, bispolide A3, bispolide B1, bispolide B2a, bispolide B2b and bispolide B3, respectively. These bispolides are each novel compounds which have a chemical structure as collectively represented by the general formula (III) shown below:  These bispolides have each a high antibacterial activity against a variety of bacteria, particularly Gram-positive bacteria and their antibiotic-resistant strains, and hence these bispolides each are effective and useful for therapeutically treating bacterial infections of Gram-positive bacteria in humans and animals.

Antibiotics, bispolides A1, A2, and A3 as well as bispolides B1, B2a, B2b and B3 and processes for producing said antibiotics

D-.beta.-lysylmethanediamine derivatives and preparation thereof

Cephalosporin derivative

Derivatives of cyclodepsipeptide PF 1022

Cephem derivatives

A benzoxazole derivative of the formula (1) or (2) which has an alicyclic diamine group at the 2-position: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X.sup.-, m and n are defined herein. The compound shows excellent 5-HT.sub.3 receptor antagonism and is useful as an antiemetic agent, a peristalsis controlling agent, an analgesic agent, an antianxiety agent and a schizophrenia treating agent.

Benzoxazole derivatives

As new dibekacin derivatives and new arbekacin derivatives are now provided 2'-amino-2'-deoxydibekacin, 2'-amino-5,2'-dideoxydibekacin, 2'-amino-2'-deoxyarbekacin, 2'-amino-5,2'-dideoxyarbekacin, 2'-amino-5,2'-dideoxy-5-epi-fluoroarbekacin and 2'-amino-5,2'-dideoxy-5-epi-aminoarbekacin which all exhibit high antibacterial activity against a wide variety of gram-positive and gram-negative bacteria, including resistant bacteria such as methicillin-resistant Staphylococcus aureus and which are of low toxicity to mammals and are useful as antibacterial agent for treatment of bacterial infections.

Dibekacin derivatives and arbekacin derivatives active against resistant

An aminothiazolyl- or aminothiadiazolyl-cephalosporin derivative represented by the following general formula (I) which has a condensed-ring thio group as a 3-positioned substituent group that contains a thiazolylthio group, an oxazolylthio group or a heterocyclic ring thereof as one of the ring components. The compound according to the present invention has excellent activities to inhibit growth of various bacteria, especially Gram-positive bacteria including methicillin-resistant Staphylococcus aureus (MRSA), and therefore, the antibacterial agent comprising, as an active ingredient, the inventive compound can be used as a therapeutic drug for the treatment of various bacterial infections. ##STR1##

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

The invention relates to derivatives of pyrrolidin-2-ylcarbonylheterocyclic compound of the general formula ##STR1## in which R.sup.1 represents C.sub.1-6 alkyl, C.sub.1-20 cycloalkyl, aryl or heteroaryl,

Derivatives of pyrrolidin-2-ylcarbonylheterocyclic compounds

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

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

As new antibacterial agent are provided cephalosporin derivatives having a general formula (I): ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkyl group or a substituted lower alkyl group, R.sup.2 is a hydrogen atom or an ester-forming group easily cleavable by an esterase present in the digestive tracts, R.sup.3 and R.sup.4 may be the same and each is independently a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkenyl group, hydroxyl group, amino group or a lower alkoxy group, and a pharmaceutically acceptable salt thereof. The cephalosporin derivative of formula (I) is useful as an orally or injectably administrable cephalosporin derivative which exhibits in combination a high antibacterial activity and a favorable characteristic capable of giving a high concentration of this compound in blood when administered.

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

Growing community of inventors

Yokohama, Japan

Seiji Shibahara