Taisho Pharmaceutical Co., Ltd.

Masami Goi

Yoshiaki Watanabe

Kaoru Sota

Hiroshi Fukushima

Chihiro Yokoo

Akira Onodera

Mitsuo Murata

Takashi Adachi

Shigeo Morimoto

Minoru Taguchi

Toshifumi Asaka

Kazuya Kameo

Takehiro Amano

Kazunori Hanada

Jiro Sawada

Kiyoshi Oguma

Masaharu Tamai

Kazuto Sekiuchi

Jozi Nakagami

Morihiro Mitsukuchi

Tomomichi Yoshida

Tadashi Eguchi

Masahiro Hasegawa

A process for preparing erythromycin A oxime or a salt thereof which comprises reacting erythromycin A with hydroxylamine using an acid, is disclosed. Erythromycin A oxime and the salts thereof are useful as intermediates for the synthesis of macrolide antibiotics.

Process for preparing erythromycin A oxime or a salt thereof

Cephalosporin derivatives represented by the general formula ##STR1## wherein R is a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R' is a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, or R and R' together with the nitrogen atom to which they are attached form a tetrahydropyridinyl group, a morpholinyl group or pyrroridinyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

Cephalosporin derivatives

Cephalosporin derivatives represented by the general formula ##STR1## wherein X represents a halogen atom, a hydroxyl group, a cyano group, a trifluoromethyl group, an amino group, a lower alkylcarbonylamino group, a lower alkoxy group, a lower alkylthio group, a lower alkoxycarbonyl group, a carbamoyl group, a substituted carbamoyl group, a carbamoyloxy group, a lower alkylcarbonyl group, a lower alkenyl group, an ethynyl group, a thiocyanate group, an .alpha.-carboxyaminomethyl group, a phenyl group, a pyridinyl group or an aminothiazolyl group, and n is an integer of 1 to 3, and the non-toxic salts thereof, are disclosed. These compounds are useful as antibacterial agents.

Cephalosporin derivatives represented by the general formula ##STR1## Wherein X represents a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, an allyl group, a cycloalkyl group having 5 or 6 carbon atoms or a benzyl group, and the non-toxic salts thereof are disclosed. These compounds are useful as antibacterial agents.

A method for the selective methylation of a hydroxy group at the 6-position of an erythromycin A derivative which comprises converting an erythromycin A derivative into an erythromycin A 9-oxime derivative, and reacting the resulting ethythromycin A 9-oxime derivative with an methylating agent.

Method for selective methylation of erythromycin A derivatives

The epoxysuccinamic acid compounds of the present invention are prepared by reaction of monoesters of epoxysuccinic acid or monoesters of epoxysuccinic acid chloride with amino compounds. These epoxysuccinamic acid compounds have excellent anti-inflammatory activity, thiol protease inhibitory activity, muscular dystrophy inhibitory activity and anti-hypertensive activity without acceleration of vascular permeability.

Epoxysuccinamic acid compounds

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Saitama, Japan

Masami Goi