Taisho Pharmaceutical Co., Ltd.

Meiji Seika Pharma Co., Ltd.

Meiji Seika Kaisha, Ltd.

Masato Kashimura

Toshifumi Asaka

Shigeo Morimoto

Katsuo Hatayama

Tomohiro Sugimoto

Yoko Misawa

Yoshiaki Watanabe

Takaaki Ishii

Tetsuya Tanikawa

Takashi Adachi

Kaoru Sota

Tomoaki Miura

Kenichi Kanemoto

Kanako Yamamoto

Naoki Sasamoto

Jun Kurosaka

Akiko Matsuura

Eiki Shitara

Haruhisa Ogita

Tohru Matsunaga

Madoka Kawamura

Kou Kumura

Ken Chikauchi

Tomohiro Ozawa

Satoshi Yoshida

Nobuyuki Suzuki

Masato Hayashi

Keiichi Ajito

Kiyoshi Takayama

Keiji Tamura

Dai Kubota

Kazuto Sekiuchi

Yasunobu Ushiki

Takeshi Kuwada

Akira Manaka

Hiroaki Kamiyama

A macrolide compound represented by the formula (I) effective against erythromycin resistant bacteria (for example, resistant pneumococci, streptococci and mycoplasmas). 

C-4&#x2033; position substituted macrolide derivative

A 10-azalide compound having a 4-membered ring structure crosslinked at the 10- and 12-positions, which is represented by the formula (I), and is effective on even, or erythromycin resistant bacteria (e.g., resistant pneunococci and streptococci). 

10a-azalide compound having 4-membered ring structure

A novel 10a-azalide compound crosslinked at the 10a- and 12-positions, which is represented by the following formula, and is effective on even, or erythromycin resistant bacteria (e.g., resistant pneumococci and streptococci). 

10a-Azalide compound crosslinked at 10a- and 12-positions

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

[Object]: To provide a compound having a novel structure effective againstand erythromycin resistant bacteria (for example, resistant pneumococci and streptococci) as well as against conventional erythromycin sensitive bacteria. [Solution]: A novel 10a-azalide compound represented by the formula (I), a pharmaceutically acceptable salt thereof or a solvate thereof, or an intermediate for the preparation of the same. The compound of the present invention has superior antibacterial activity against, erythromycin resistant pneumococci and the like, and therefore, the compound can be used as a therapeutic agent of infectious diseases.

10a-Azalide compound

Erythromycin A derivatives represented by the general formulawherein Ris a 2-alkenyl group having 3 to 15 carbon atoms, an arylmethyl group, or an arylmethyl group substituted by 1 to 3 of a halogen atom, an alkoxy group 1 to 4 carbon atoms, a nitro group or an alkoxycarbonyl group having 2 to 6 carbon atoms, Ris a substituted silyl group and Ris a hydrogen atom or R, are disclosed. These compounds are useful as intermediates of the anti-bacterial agents.

Erythromycin A derivatives and method for preparing same

There is provided a preparation process useful for an efficient synthesis of 6-O-substituted ketolide derivatives by combining a characterized step of introduction of a substituent at the 6-position by selective cleavage of a C&mdash;O bond of the cyclic acetal at the 9-position side via 6,9-cyclic acetal 5-O-desosaminyl erythronolide derivative, a step of conversion into carbonyl groups at the 9- and 3-positions, and a step of 11,12-cyclic carbamation to lead to 6-O-substituted ketolide derivatives.

Process for producing erythromycin derivative

Erythromycin a derivatives and method for preparing same

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

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Saitama, Japan

Masato Kashimura