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公开(公告)号：US20030207841A1
公开(公告)日：2003-11-06
申请号：US10430705
申请日：2003-05-05
发明人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
IPC分类号： A61K031/7076 , A61K031/7072 , A61K031/675 , C07H019/04 , A61K031/522 , A61K031/513 , C07D473/18
摘要： A compound of the formula (1): 1 wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphate group, or nullP(R3)R4, wherein R3 and R4 are the same or different and represent a hydroxyl group, an amino group, an alkoxy group having from 1 to 4 carbon atoms, a cyanoalkoxy group having from 1 to 5 carbon atoms or an amino group substituted by an alkyl group having from 1 to 4 carbon atoms; A represents an alkylene group having from 1 to 4 carbon atoms and B represents a purin-9-yl group, a 2-oxo-pyrimidin-1-yl group, a substituted purin-9-yl group or a substituted 2-oxo-pyrimidin-1-yl group having a substituent null selected from the group consisting of a hydroxyl group which may be protected, an alkoxy group having from 1 to 4 carbon atoms, a mercapto group which may be protected, an alkylthio group having from 1 to 4 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, an amino group which may be protected, a mono- or di-alkylamino group which may be substituted by an alkyl group having from 1 to 4 carbon atoms, an alkyl group having from 1 to 4 carbon atoms and a halogen atom; or a salt thereof.
摘要翻译： 式（1）的化合物：其中R 1和R 2相同或不同，表示氢原子，羟基保护基，磷酸基或-P（R 3） 4>，其中R 3和R 4相同或不同，表示羟基，氨基，具有1至4个碳原子的烷氧基，具有1至5个碳原子的氰基烷氧基或 被具有1至4个碳原子的烷基取代的氨基; A表示具有1至4个碳原子的亚烷基，B表示嘌呤-9-基，2-氧代 - 嘧啶-1-基，取代的嘌呤-9-基或取代的2-氧代 - 具有选自可被保护的羟基，具有1至4个碳原子的烷氧基，可被保护的巯基的取代基的嘧啶-1-基，具有1至4个碳原子的烷硫基， 4个碳原子，具有1至4个碳原子的烷氧基，可被保护的氨基，可以被具有1至4个碳原子的烷基取代的一烷基或二烷基氨基，烷基 具有1至4个碳原子和卤素原子; 或其盐。
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公开(公告)号：US20030069204A1
公开(公告)日：2003-04-10
申请号：US10096006
申请日：2002-03-12
发明人： Masatoshi Inukai , Masakatsu Kaneko , Toshio Takatsu , Hitoshi Hotoda , Masatoshi Arai , Shunichi Miyakoshi , Masaaki Kizuka , Yasumasa Ogawa
IPC分类号： A61K031/7072 , C07H019/067 , A61K031/554 , C07D417/14
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. 1 (wherein R1 is a hydrogen atom or a methyl group; R2a is a hydrogen atom, a protecting group for a hydroxy group, or a methyl group; R3 is a hydrogen atom or a protecting group for a hydroxy group; R4a is a hydrogen atom, a hydroxy group or a protected hydroxy group; R5 is a hydrogen atom or a protecting group for a hydroxy group; and X is a methylene group or a sulfur atom). The invention also includes compounds which are related to the aforeidentified compounds.
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为氢原子或保护基 对于羟基; R 4是氢原子，羟基或被保护的羟基; R 5是氢原子或羟基的保护基; X是亚甲基或硫 原子）。 本发明还包括与前述化合物有关的化合物。
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公开(公告)号：US20030171330A1
公开(公告)日：2003-09-11
申请号：US10080191
申请日：2002-02-19
发明人： Hitoshi Hotoda , Masakatsu Kaneko , Masatoshi Inukai , Yasunori Muramatsu , Yukio Utsui , Satoshi Ohya
IPC分类号： A61K031/7072 , C07H019/073 , A61K031/513 , C07D47/14
CPC分类号： C07H19/06
摘要： A compound of formula (I) 1 wherein R1 and R2 represent a hydrogen atom or an aryl, a heterocyclic, an alkyl or an alkenyl, which are optionally substituted, R3 represents a hydrogen atom or a hydroxyl and X1 and X2 represent an oxygen atom, a sulfur atom or a nitrogen containing group, a pharmaceutically acceptable derivative thereof or a salt thereof. A pharmaceutical composition comprising the compound for the prevention or treatment of a bacterial infection. A method for the prevention or treatment of a bacterial infection in a warm-blooded animal comprising administering a pharmacologically effective amount of the compound.
摘要翻译： 式（I）的化合物，其中R 1和R 2表示氢原子或任选被取代的芳基，杂环，烷基或链烯基，R 3表示氢原子或羟基 X 1和X 2表示氧原子，硫原子或含氮基团，其药学上可接受的衍生物或其盐。 一种药物组合物，其包含用于预防或治疗细菌感染的化合物。 一种预防或治疗温血动物细菌感染的方法，包括施用药理学有效量的化合物。
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公开(公告)号：US20020147332A1
公开(公告)日：2002-10-10
申请号：US09925673
申请日：2001-08-09
发明人： Masakatsu Kaneko , Koji Morita , Takeshi Imanishi
IPC分类号： C07H019/04 , C07H019/06
摘要： A compound of the formula (1): 1 wherein R1 and R2 are the same or different and represent a hydrogen atom, a hydroxyl protecting group, a phosphate group, or nullP(R3)R4, wherein R3 and R4 are the same or different and represent a hydroxyl group, an amino group, an alkoxy group having from 1 to 4 carbon atoms, a cyanoalkoxy group having from 1 to 5 carbon atoms or an amino group substituted by an alkyl group having from 1 to 4 carbon atoms; A represents an alkylene group having from 1 to 4 carbon atoms and B represents a purin-9-yl group, a 2-oxo-pyrimidin-1-yl group, a substituted purin-9-yl group or a substituted 2-oxo-pyrimidin-1-yl group having a substituent null selected from the group consisting of a hydroxyl group which may be protected, an alkoxy group having from 1 to 4 carbon atoms, a mercapto group which may be protected, an alkylthio group having from 1 to 4 carbon atoms, an alkoxy group having from 1 to 4 carbon atoms, an amino group which may be protected, a mono- or di-alkylamino group which may be substituted by an alkyl group having from 1 to 4 carbon atoms, an alkyl group having from 1 to 4 carbon atoms and a halogen atom; or a salt thereof.
摘要翻译： 式（1）的化合物：其中R 1和R 2相同或不同，表示氢原子，羟基保护基，磷酸基或-P（R 3）R 4，其中R 3和R 4相同或不同 并且表示羟基，氨基，具有1至4个碳原子的烷氧基，具有1至5个碳原子的氰基烷氧基或被具有1至4个碳原子的烷基取代的氨基; A表示具有1至4个碳原子的亚烷基，B表示嘌呤-9-基，2-氧代 - 嘧啶-1-基，取代的嘌呤-9-基或取代的2-氧代 - 具有选自可被保护的羟基，具有1至4个碳原子的烷氧基，可被保护的巯基的取代基的嘧啶-1-基，具有1至4个碳原子的烷硫基， 4个碳原子，具有1至4个碳原子的烷氧基，可被保护的氨基，可以被具有1至4个碳原子的烷基取代的一烷基或二烷基氨基，烷基 具有1至4个碳原子和卤素原子; 或其盐。
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