公开(公告)号：EP0945459A1

公开(公告)日：1999-09-29

申请号：EP97943199.6

申请日：1997-10-14

申请人： TAISHO PHARMACEUTICAL CO. LTD

发明人： ASAKA, Toshifumi ,  KASHIMURA, Masato ,  MATSUURA, Akiko ,  SUGIMOTO, Tomohiro ,  TANIKAWA, Tetsuya ,  ISHII, Takaaki

IPC分类号： C07H17/08

CPC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.

摘要翻译： 由式（I）表示的红霉素A衍生物：其中n是1至4的整数，R 1是由下式表示的基团：CHEM>由下式表示的基团： 吡啶基乙酰基，具有4-8个碳原子的环烷基甲基或1,2-双（乙氧基羰基）乙烯基，R 2是与R 1所定义的相同的基团，氢原子，具有 1至5个碳原子，具有2至6个碳原子的烷酰基或具有2至6个碳原子的烷氧基羰基，R 1和R 2一起形成下式的基团：= CH-R 14 或R 1和R 2与它们所连接的氮原子一起形成由下式表示的基团： R 15和R 16各自为氢原子或当W为 碳原子，R 15和R 16与它们所连接的碳原子一起形成苯环或萘环，R 3是氢原子，具有1至5个碳原子的烷基 或肉桂基，R 4是氢 原子，乙酰基，乙基琥珀酰基或烟酰基，A是下式表示的基团：-OC（= O）-R 17，-OC（= O）-CH 2 -R 17， OC（= O）-NH-R 17，-OR 17或-OC（= O）-OR 17，R 5和R 6各自为氢原子或烷基 具有1至5个碳原子或其药学上可接受的盐对抗已知的红霉素敏感细菌而且对红霉素抗性细菌具有很强的抗菌活性。

公开(公告)号：EP0553353A1

公开(公告)日：1993-08-04

申请号：EP91917071.2

申请日：1991-10-08

申请人： TAISHO PHARMACEUTICAL CO. LTD

发明人： ASAKA, Toshifumi ,  MISAWA, Yoko ,  KASHIMURA, Masato ,  MORIMOTO, Shigeo ,  WATANABE, Yoshiaki ,  HATAYAMA, Katsuo

IPC分类号： C07H17/08 ,  A61K31/71

CPC分类号： C07H17/08

摘要： Modified erythromycin having remarkably alleviated bitterness and improved bioabsorbability, comprising a compound prepared by introducing a group represented by the formula: -O-CO-O-[(CH₂) m -O] n -R (wherein R represents C₁ to C₁₂ alkyl, m represents an integer of 2 to 4, and n represents an integer of 1 to 7), into the 2'-position of an erythromycin, or its salt.

摘要翻译： 改进的红霉素具有显着缓解的苦味和改善的生物吸收性，包括通过引入由下式表示的基团制备的化合物：-O-CO-O - [（CH2）mO] nR（其中R表示C1至C12烷基，m表示整数 2〜4，n表示1〜7的整数），进入红霉素或其盐的2'-位。