发明公开
- 专利标题： ERYTHROMYCIN A DERIVATIVES
- 专利标题（中）： DORIVATE VON ERYTHROMYCIN-A
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申请号： EP97943199.6申请日： 1997-10-14
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公开(公告)号： EP0945459A1公开(公告)日： 1999-09-29
- 发明人: ASAKA, Toshifumi , KASHIMURA, Masato , MATSUURA, Akiko , SUGIMOTO, Tomohiro , TANIKAWA, Tetsuya , ISHII, Takaaki
- 申请人： TAISHO PHARMACEUTICAL CO. LTD
- 申请人地址： 24-1 Takata 3-chome Toshima-ku Tokyo 171 JP
- 专利权人： TAISHO PHARMACEUTICAL CO. LTD
- 当前专利权人： TAISHO PHARMACEUTICAL CO. LTD
- 当前专利权人地址： 24-1 Takata 3-chome Toshima-ku Tokyo 171 JP
- 代理机构： Weisert, Annekäte, Dipl.-Ing. Dr.-Ing.
- 优先权： JP31580596 19961127
- 国际公布： WO9823628 19980604
- 主分类号： C07H17/08
- IPC分类号： C07H17/08
摘要：
An erythromycin A derivative represented by Formula (I):
[wherein n is an integer of from 1 to 4, R 1 is a group represented by the formula:
a group represented by the formula:
a pyridylacetyl group, a cycloalkylmethyl group having 4 to 8 carbon atoms or a 1,2-bis(ethoxycarbonyl)vinyl group, R 2 is the same group as defined for R 1 , a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkanoyl group having 2 to 6 carbon atoms or an alkoxycarbonyl group having 2 to 6 carbon atoms, R 1 and R 2 together form a group of the formula: =CH-R 14 , or R 1 and R 2 together with the nitrogen atom to which they are attached form a group represented by the formula:
R 15 and R 16 are each a hydrogen atom or when W is a carbon atom, R 15 and R 16 together with the carbon atoms to which they are attached form a benzene ring or a naphthalene ring, R 3 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a cinnamyl group, R 4 is a hydrogen atom, an acetyl group, an ethylsuccinyl group or a nicotinoyl group, A is a group represented by the formula:
-OC(=O)-R 17 , -OC(=O)-CH 2 -R 17 , -OC(=O)-NH-R 17 , -O-R 17 or -OC(=O)-O-R 17 , and R 5 and R 6 are each a hydrogen atom or an alkyl group having 1 to 5 carbon atoms] or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only against known erythromycin-sensitive bacteria but also erythromycin-resistant bacteria.
[wherein n is an integer of from 1 to 4, R 1 is a group represented by the formula:
a group represented by the formula:
a pyridylacetyl group, a cycloalkylmethyl group having 4 to 8 carbon atoms or a 1,2-bis(ethoxycarbonyl)vinyl group, R 2 is the same group as defined for R 1 , a hydrogen atom, an alkyl group having 1 to 5 carbon atoms, an alkanoyl group having 2 to 6 carbon atoms or an alkoxycarbonyl group having 2 to 6 carbon atoms, R 1 and R 2 together form a group of the formula: =CH-R 14 , or R 1 and R 2 together with the nitrogen atom to which they are attached form a group represented by the formula:
R 15 and R 16 are each a hydrogen atom or when W is a carbon atom, R 15 and R 16 together with the carbon atoms to which they are attached form a benzene ring or a naphthalene ring, R 3 is a hydrogen atom, an alkyl group having 1 to 5 carbon atoms or a cinnamyl group, R 4 is a hydrogen atom, an acetyl group, an ethylsuccinyl group or a nicotinoyl group, A is a group represented by the formula:
-OC(=O)-R 17 , -OC(=O)-CH 2 -R 17 , -OC(=O)-NH-R 17 , -O-R 17 or -OC(=O)-O-R 17 , and R 5 and R 6 are each a hydrogen atom or an alkyl group having 1 to 5 carbon atoms] or a pharmaceutically acceptable salt thereof has a strong antibacterial activity against not only against known erythromycin-sensitive bacteria but also erythromycin-resistant bacteria.
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