Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai

Microbial Chemistry Research Foundation

Meiji Seika Pharma Co., Ltd.

Bristol-Myers Company

The University of Tokyo

Daishiro Ikeda

Shinichi Kondo

Tomio Takeuchi

Hamao Umezawa

Akio Fujii

Teruya Nakamura

Hironobu Iinuma

Takeshi Murakami

Yoshiaki Takahashi

Nobuto Minowa

Yoshihiko Kobayashi

Toshiaki Miyake

Shoichi Murakami

Shigeru Hoshiko

Mitsuhiro Abe

Yukiko Hiraiwa

Kazushige Sasaki

Yoshihisa Akiyama

Masaki Tsushima

Seiji Shibahara

Shuichi Gomi

Atsushi Tamura

Toshiaki Kudo

Takayuki Usui

Yoko Ikeda

Hiroyuki Inoue

Yoshikazu Takahashi

Masafumi Matsuo

Yoshiro Okami

Yoshiyuki Koyama

Hamao Umezawa, Deceased

Ryoichi Matsuda

Kazuo Umezawa

Manabu Kawada

Atsushi Nishida

Yoshiaki Nonomura

Masataka Shiozuka

Keiichi Ajito

Sonoko Hirose

Akira Wagatsuma

Toshio Nishizuka

A readthrough inducing agent for inducing readthrough of a premature stop codon generated by nonsense mutations, the readthrough inducing agent comprising a compound having a structure expressed by the following Structural Formula (A), and a drug for treating a genetic disease caused by nonsense mutations, the drug comprising the readthrough inducing agent. 

Readthrough inducing agent and drug for treating genetic disease caused by nonsense mutation

This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them. 

Aminoglycoside antibiotics

A compound having a structure expressed by the following Structural Formula (1): 

Compound ceramidastin, method for producing the same, and use of the same

Desalaninebenanomicin A derivatives and processes for the preparation

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

As a new antifungal and antiviral antibiotic is provided benanomicin A 4''-O-sulfate or a salt thereof having formula (I) ##STR1## wherein M.sup.1 denotes a mono-valent alkali metal atom or a di-valent alkaline earth metal atom or a hydrogen atom and A denotes an organic base; n is zero when M.sup.1 is an alkali metal atom or alkaline earth metal atom but n is 1 or zero when M.sup.1 is a hydrogen atom, and M.sup.2 denotes a hydrogen atom or an alkali metal atom or an alkaline earth metal atom. This new compound is useful as antifungal agent to treat fungal infections in mammals and as antiviral agent to inhibitingly treat HIV.

Antifungal and antiviral antibiotic, benanomicin A 4''-O-sulfate or its

As new compounds are now provided 14-O-(3,4-disubstituted benzoyl)adriamycins which are of low cytotoxicity and exhibit a high activity inhibitory to the reverse transcriptase of human immunodeficiency virus (HIV) and which can inhibit propagation of HIV.

Anthracycline derivatives having inhibitory activity against reverse

N-[4-(3-Aminopropyl)aminobutyl]-2-(.omega.-guanidino-fatty acid-amido)-2-substituted-ethanamides represented by the general formula ##STR1## wherein Y represents --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH or ##STR2## R represents a hydrogen atom, an alkyl group of 1 to 4 carbon atoms which may have a hydroxyl group as substituent, or a benzyl group, and n is an integer of from 1 to 8, provided that when Y is ##STR3## and n is 4, R represents the groups other than the hydrogen atom; salt thereof having antitumor activity in experimental animal tumors and a process for the preparation thereof is provided.

N-(4-(3-aminopropyl)aminobutyl)-2-(.omega.-gua

As new 2'-deamino-2'-hydroxyistamycin B.sub.o derivatives are provided four compounds, namely 2'-deamino-2'-hydroxyistamycin B; 2'-deamino-2'-hydroxy-3-O-demethylistamycin B; 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxyistamycin B.sub.o ; and 4-N-(.beta.-alanyl)-2'-deamino-2'-hydroxy-3-O-demethylistamycin B.sub.o which all exhibit high antibacterial activity and low acute toxicity in combination. These new compounds are useful as antibacterial agent.

2'-deamino-2'-hydroxyistamycin B.sub.o derivatives of low toxicity

The novel compound N-[(3-aminoproypl)aminobutyl]-Z-(F-guandino-3-hydroxyheptanamido)-2-methox yethanamide or a pharmaceutically acceptable salt thereof which has antitumor activity in experimental animals.

11-O-methylspergualin

N-[4-(3-Aminopropyl)aminobutyl]-2-(.omega.-guanidino-fatty acid-amido)-2-substituted-ethanamides represented by the general formula ##STR1## wherein Y represents --(CH.sub.2 --CH.sub.2 --, --CH.dbd.CH or ##STR2## R represents a hydrogen atom, an alkyl group of 1 to 4 carbon atoms which may have a hydroxyl group as substituent, or a benzyl group, and n is an integer of from 1 to 8, provided that when Y is ##STR3## and n is 4, R represents the groups other than the hydrogen atom; a salt thereof having antitumor activity in experimental animal tumors and a process for the preparation thereof is provided.

N-[4-(3-aminopropyl)-aminobutyl]-2-(.omega.-gua

N-[4-[(3-aminopropyl)amino]butyl]-2,2-dihydroxyethanamide is an immunostimulant in animals and an intermediate for synthesis of the antibiotic BMG162-aF2.

N-[4-[(3-aminopropyl)amino]butyl]-2,2-dihydroxyethanamide

Growing community of inventors

Tokyo, Japan

Daishiro Ikeda