Toyo Jozo Kabushiki Kaisha

Eiichi Honda

Hideo Sakakibara

Tatsuro Fujiwara

Takao Hirano

Yukio Suzuki

Masao Yaso

Susumu Watanabe

Eiichi Hayashi

Tetsu Saito

Kensuke Shibata

Tetsuo Matsuda

Noriyasu Takayanagi

Osamu Okegawa

Hiroyuki Kinoshita

Kazuyo Ohta

A compound of the formula ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkoxy or halogen, and A is lower alkylene, or a pharmacologically acceptable salt thereof, has sympatholytic .alpha.-receptor blocking activity and is useful for the treatment of hypertension.

1-Substituted alkyl-2-oxo-1,2-dihydroquinoxaline derivatives

Compounds of the formula ##STR1## wherein R.sub.1 is lower alkyl, lower alkoxycarbonyl-lower alkyl, phenyl, phenyl substituted by one or more lower alkyl or halogen, phenyl-lower alkyl optionally substituted in its side chain by lower alkyl or lower alkoxycarbonyl, thienylmethyl or thiazolyl, R.sub.2 is hydrogen or lower alkyl, or ##STR2## constitutes a 3-7-membered nitrogen-containing heterocyclic ring in which R.sub.1 and R.sub.2 are connected, R.sub.3 is hydrogen or hydroxyl, and X is oxygen or sulfur, or a non-toxic salt thereof. These compounds have stronger antibacterial activity as compared with known clinically used macrolide antibiotics such as erythromycin, oleandomycin, josamycin and leucomycin, and also have strong antibacterial activity against all macrolide antibiotic-resistant strains such as macrolide-resistant A group strains (clinical isolates or erythromycin, oleandomycin and 16-membered macrolide antibiotic resistant strains). These compounds are also stable in vivo and hence may be used for treatment of infectious diseases and also are useful for feed additives and growth stimulants.

23-O-substituted carbamoyl-23-demycinosyldesmycosin

A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or hydroxy and at least one of R.sub.1 and R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof, has strong antimicrobial and antibacterial activity..

Deoxydesmycosin

A compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or hydroxyl and at least one of R.sub.1 and R.sub.2 is hydrogen, or a pharmaceutically acceptable salt thereof, has antibacterial activity against Gram positive bacteria and against macrolide-resistant A group bacteria.

19-Deformyl-deoxy-desmycosin

Deformyltylosin derivatives of the formula ##STR1## wherein A is ##STR2## --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, R.sub.1 is hydrogen, lower alkanoyl or aryl-lower alkanoyl, X.sub.1 and X.sub.2 are hydrogen or are connected to form a valence bond, Y.sub.1 and Y.sub.2 are hydrogen or are connected to form a valence bond, Q.sub.1 is hydrogen or methyl, Q.sub.2 is hydrogen or ##STR3## R.sub.2 is hydrogen or lower alkanoyl, R is hydrogen or ##STR4## R.sub.3 is hydrogen or C.sub.2-5 alkanoyl, and R.sub.4 is hydrogen or C.sub.2-6 alkanoyl, and when R.sub.3 is not hydrogen, then R.sub.4 is not hydrogen, or a pharmaceutically acceptable salt thereof, have strong antibacterial activities as compared to the known antibiotic tylosin, and also have enhanced antibacterial activities against all macrolide antibiotic-resistant strains such as A, B and C group strains, and have higher blood levels as compared with tylosin.

Deformyltylosin derivatives

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Mishima, Japan

Eiichi Honda