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Title:
ERYTHROMYCIN A DERIVATIVES
Document Type and Number:
WIPO Patent Application WO/1998/018808
Kind Code:
A1
Abstract:
Erythromycin A derivatives represented by general formula (I) or pharmaceutically acceptable salts thereof having potent antibacterial activities not only on gram-positive bacteria but also some erythromycin-tolerant bacteria, wherein R?1� represents -O-CO-CH�2?Y (wherein Y represents phenyl, nitrophenyl or pyridyl) or cladinosyloxy; R?2� represents hydrogen, or R?1� and R?2� form together oxo; R?3� represents hydrogen, acetyl, ethylsuccinyl or nicotinoyl; R?4� represents -CH�2?CH�m?CH�m+1? (wherein m is 0 or 1), -CH�2?CHC(CH�3?)�2?, -CH�2?CH�n?CH�n?Ph (wherein n is 1 or 2; and Ph represents phenyl), -CH�2?CH(OH)CH(OH)Ph (wherein Ph is as defined above) or fluoromethyl; R?5� represents =O or =NOR?8� (wherein R?8� represents hydrogen or benzyl optionally substituted by 1 to 5 halogen atoms); R?6� represents hydroxy; and R?7� represents hydroxy or hydrogen, or R?6� and R?7� form together a cyclic carbonate.

Inventors:
ASAKA TOSHIFUMI (JP)
MATSUURA AKIKO (JP)
KASHIMURA MASATO (JP)
Application Number:
PCT/JP1997/003684
Publication Date:
May 07, 1998
Filing Date:
October 14, 1997
Export Citation:
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Assignee:
TAISHO PHARMACEUTICAL CO LTD (JP)
ASAKA TOSHIFUMI (JP)
MATSURA AKIKO (JP)
KASHIMURA MASATO (JP)
International Classes:
C07H17/08; (IPC1-7): C07H17/08; A61K31/70
Domestic Patent References:
WO1997042204A11997-11-13
WO1997042206A11997-11-13
Foreign References:
JPS572298A1982-01-07
Attorney, Agent or Firm:
Asamura, Kiyoshi (Room 331 2-1, Ohtemachi 2-chom, Chiyoda-ku Tokyo 100, JP)
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