Taisho Pharmaceutical Co., Ltd.

Toshifumi Asaka

Masato Kashimura

Shigeo Morimoto

Yoshiaki Watanabe

Katsuo Hatayama

Yoko Misawa

Takaaki Ishii

Kaoru Sota

Tetsuya Tanikawa

Takashi Adachi

Tomohiro Sugimoto

Akiko Matsuura

Jiro Sawada

Chihiro Yokoo

Kiyoshi Takayama

Haruhisa Ogita

Akira Onodera

Kazuto Sekiuchi

Masami Goi

Madoka Kawamura

Tohru Matsunaga

Morihiro Mitsukuchi

Yoko Takahashi

Jozi Nakagami

Tadashi Eguchi

Compounds represented by formula (I) and the formula (IV) have an inhibitory activity of MMP-9 production, therefore, are useful as a medicine agent with fewer side effects than conventional MMP enzyme activity inhibitors, as a prophylactic and therapeutic drug for oncogenic angiogenesis, chronic rheumatoid arthritis, vascular intimal thickening after a percutaneous coronary transluminal angioplasty, vascular atherosclerosis, hemorrhagic apoplexy, acute myocardial infarction, chronic heart failure, aneurysm, lung cancer metastasis, adult respiratory distress syndrome, asthma, interstitial pulmonary fibrosis, chronic rhinosinusitis, bronchitis or chronic obstructive pulmonary disease (COPD).

Macrolide derivatives

An erythromycin A derivative represented by Formula

Erythromycin A derivatives

An erythromycin A derivative represented by the formula:

Erythromycin a derivatives

An erythromycin A derivative represented by the formula (I): ##STR1## �wherein R.sup.1 is a group represented by the formula: --OCOCH.sub.2 Y (wherein Y is a pyridyl group, a quinolyl group, a p-nitrophenyl group or a group represented by the formula: --NR.sup.4 R.sup.5 (wherein R.sup.4 and R.sup.5 may be the same or different, and are each a hydrogen atom, a methyl group, a pyridylmethyl, a quinolylmethyl group or a benzyloxycarbonyl group)) or a cladinosyloxy group, R.sup.2 is a hydrogen atom, or R.sup.1 and R.sup.2 together form an oxo group, R.sup.3 is a hydrogen atom, an acetyl group, an ethylsuccinyl group or a nicotinoyl group! or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only Gram-positive bacteria but also some Gram-negative bacteria, in particular, Haemophilus influenzae which is a serious factor of infectious diseases in the respiratory organs.

5-O-desosaminylerythronolide a derivatives

5-O-desosaminylerythronolide derivatives

5-O-desosaminylerythronolide a derivative

6-0-methylerythromycin A derivatives

2'-position modified compound of erythromycin or its derivative

A 6-O-methylerythromycin A oxime derivative represented by the formula ##STR1## wherein X is a substituted benzyl group, a substituted phenyl group, an .alpha.-methylbenzyl group, an .alpha.-methylphenethyl group, a diphenylmethyl group, a trityl group, a dibenzosuberanyl group, or a group of the formula --(CH.sub.2).sub.n --R, and Y is a hydrogen atom, a substituted phenyl group or a 2-aminothiazol-4-ylmethylcarbonyl group, and a pharmaceutically acceptable salt thereof are disclosed. These compounds have antibacterial activity against erythromycin resistant bacteria.

6-O-methylerythromycin A oxime derivatives

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Tokyo, Japan

Toshifumi Asaka