公开(公告)号：EP1209166A1

公开(公告)日：2002-05-29

申请号：EP00953494.2

申请日：2000-08-18

申请人： Sankyo Company, Limited

发明人： HOTODA, Hitoshi Sankyo Company, Limited ,  KANEKO, Masakatsu Sankyo Company, Limited ,  INUKAI, Masatoshi Sankyo Company, Limited ,  MURAMATSU, Yasunori Sankyo Company, Limited ,  UTSUI, Yukio Sankyo Company, Limited ,  OHYA, Satoshi Sankyo Company, Limited

IPC分类号： C07H19/067 ,  C07H19/073 ,  A61K31/7072 ,  A61P31/06 ,  A61P31/08

CPC分类号： C07H19/06

摘要： The present invention relates to a compound of formula (I) (wherein R 1 and R 2 represent an aryl group, a heterocyclic group, an alkyl group, an alkenyl group and the like which are optionally substituted, R 3 represents a hydrogen atom or a hydroxyl group, and X 1 and X 2 represent an oxygen atom or a sulfur atom, or a nitrogen atom which may be substituted), a pharmaceutically acceptable derivative thereof or a salt thereof.
The present invention also relates to a pharmaceutical composition comprising a compound described above as an active ingredient for the prevention or treatment of bacterial infections.
The present invention includes the use of a compound described above in order to prepare a medicament effective in the prevention or treatment of bacterial infections.
The present invention is concerned with a method for the prevention or treatment of bacterial infections in warm-blooded animals comprising administering a pharmacologically effective amount of a compound described above to them.

摘要翻译： 本发明涉及式（I）的化合物（其中R 1和R 2表示任选被取代的芳基，杂环基，烷基，烯基等，R 3表示氢原子或羟基 ，X1和X2代表氧原子或硫原子或可被取代的氮原子），其药学上可接受的衍生物或其盐。 本发明还涉及包含上述化合物作为用于预防或治疗细菌感染的活性成分的药物组合物。 本发明包括使用上述化合物以制备有效预防或治疗细菌感染的药物。 本发明涉及一种预防或治疗温血动物细菌感染的方法，该方法包括向其中施用药理学有效量的上述化合物。

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.

公开(公告)号：EP1209166B1

公开(公告)日：2004-03-31

申请号：EP00953494.2

申请日：2000-08-18

申请人： Sankyo Company, Limited

发明人： HOTODA, Hitoshi Sankyo Company, Limited ,  KANEKO, Masakatsu Sankyo Company, Limited ,  INUKAI, Masatoshi Sankyo Company, Limited ,  MURAMATSU, Yasunori Sankyo Company, Limited ,  UTSUI, Yukio Sankyo Company, Limited ,  OHYA, Satoshi Sankyo Company, Limited

IPC分类号： C07H19/067 ,  C07H19/073 ,  A61K31/70

CPC分类号： C07H19/06

摘要： Compounds of general formula (I) or pharmacologically acceptable derivatives or salts thereof; compositions for the prevention or treatment of bacterial infections, containing the compounds, the derivatives or the salts as the active ingredient; use of the same in preparing preventive or therapeutic drugs for bacterial infections; and preventive or therapeutic methods of bacterial infections by administering them to warm-blooded animals in pharmacologically effective doses, wherein R and R are each an optionally substituted, aryl, heterocyclic, alkyl or alkenyl group or the like; R is hydrogen or hydroxyl; and X and X are each oxygen, sulfur, or optionally substituted nitrogen.