公开(公告)号：EP1095947A1

公开(公告)日：2001-05-02

申请号：EP99929772.4

申请日：1999-07-09

申请人： Sankyo Company Limited

发明人： INUKAI, Masatoshi Sankyo Company, Limited ,  KANEKO, Masakatsu Sankyo Company, Limited ,  TAKATSU, Toshio Sankyo Company, Limited ,  HOTODA, Hitoshi Sankyo Company, Limited ,  KIZUKA, Masaaki Sankyo Company, Limited ,  ARAI, Masatoshi Sankyo Company, Limited ,  MIYAKOSHI, Shunichi Sankyo Company, Limited ,  OGAWA, Yasumasa Sankyo Company, Limited

IPC分类号： C07H19/067

CPC分类号： C07H19/06 ,  C12P17/16 ,  C12P17/162 ,  C12P17/167 ,  C12P19/38 ,  C12P19/40 ,  Y02P20/55

摘要： The present invention relates to ester, ether and N-alkylcarbamoyl derivatives of compound (Ia) and pharmaceutically acceptable salts thereof. These compounds exhibit excellent antibacterial activity and are useful for the treatment or prevention of bacterial infections.
(wherein R 1 is a hydrogen atom or a methyl group; R 2 a is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R 3 is a hydrogen atom or a protecting group for a hydroxy group; R 4 a is a hydrogen atom, a hydroxy group or a protected hydroxy group; R 5 is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom).

摘要翻译： 本发明涉及化合物（Ia）的酯，醚和N-烷基氨基甲酰基衍生物及其药学上可接受的盐。 这些化合物表现出优异的抗菌活性，可用于治疗或预防细菌感染。 （其中R 1为氢原子或甲基; R 2为氢原子，羟基保护基或甲基; R 3为氢原子或 羟基的保护基; R 4是氢原子，羟基或保护的羟基; R 5是氢原子或羟基的保护基; X是亚甲基 或硫原子）。

公开(公告)号：EP1095947B1

公开(公告)日：2007-03-14

申请号：EP99929772.4

申请日：1999-07-09

申请人： Sankyo Company Limited

发明人： INUKAI, Masatoshi Sankyo Company, Limited ,  KANEKO, Masakatsu Sankyo Company, Limited ,  TAKATSU, Toshio Sankyo Company, Limited ,  HOTODA, Hitoshi Sankyo Company, Limited ,  KIZUKA, Masaaki Sankyo Company, Limited ,  ARAI, Masatoshi Sankyo Company, Limited ,  MIYAKOSHI, Shunichi Sankyo Company, Limited ,  OGAWA, Yasumasa Sankyo Company, Limited

IPC分类号： C07H19/067 ,  A61K31/70 ,  A61P31/04 ,  C12P19/38 ,  C12R1/545

CPC分类号： C07H19/06 ,  C12P17/16 ,  C12P17/162 ,  C12P17/167 ,  C12P19/38 ,  C12P19/40 ,  Y02P20/55

摘要： Pharmacologically acceptable esters, ethers and carbamoyl N-alkylates derived from compounds represented by general formula (Ia), and pharmacologically acceptable salts of the same, which exhibit an excellent antibacterial activity and are useful in the treatment or prevention of infectious diseases, wherein R is hydrogen or methyl; R a is hydrogen, a hydroxyl-protecting group or methyl; R is hydrogen or a hydroxyl-protecting group; R a is hydrogen or optionally protected hydroxyl; R is hydrogen or a hydroxyl-protecting group; and X is methylene or sulfur.