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    • 5. 发明专利
      DK0919553T3  未知
    • DK0919553T3
    • 2005-06-06
    • DK97930766
    • 1997-07-11
    • DAIICHI SEIYAKU CO
    • TAKEMURA MAKOTO , KIMURA YOUICHI , TAKAHASHI HISASHI , ISHIDA YOHHEI
    • C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , C07D207/24 , C07D207/26 , C07D401/04 , C07D207/09 , C07D207/16 , C07D489/08 , C07D513/08
    • The present invention is to provide an antimicrobial agent having high safety as well as potent antimicrobial activity on broad range of microorganisms. A compound represented by the following formula, its salt and their hydrates: wherein R and R each independently represents a hydrogen atom or an alkyl group; n represents an integer of 1 to 3; R represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cycloalkyl group, an aryl group, a heteroaryl group, an alkoxyl group or an alkylamino group; R represents a hydrogen atom or an alkylthio group; R represents a hydrogen atom, an amino group, a hydroxyl group, a thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; X represents a halogen atom or a hydrogen atom; and A represents a nitrogen atom or a partial structure represented by formula (II): wherein X represents a hydrogen atom, an amino group, a halogen atom, a cyano group, a halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; and Y represents a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl, an alkoxymethyl group or a phenylalkyl group.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 6. 发明专利
      AT289999T  未知
    • AT289999T
    • 2005-03-15
    • AT97930766
    • 1997-07-11
    • DAIICHI SEIYAKU CO
    • TAKEMURA MAKOTO , KIMURA YOUICHI , TAKAHASHI HISASHI , ISHIDA YOHHEI
    • C07D471/04 , A61K31/4375 , A61K31/47 , A61K31/4709 , C07D207/24 , C07D207/26 , C07D401/04 , C07D489/08 , C07D513/08 , C07D207/09 , C07D207/16
    • The present invention is to provide an antimicrobial agent having high safety as well as potent antimicrobial activity on broad range of microorganisms. A compound represented by the following formula, its salt and their hydrates: wherein R and R each independently represents a hydrogen atom or an alkyl group; n represents an integer of 1 to 3; R represents an alkyl group, an alkenyl group, a halogenoalkyl group, a cycloalkyl group, an aryl group, a heteroaryl group, an alkoxyl group or an alkylamino group; R represents a hydrogen atom or an alkylthio group; R represents a hydrogen atom, an amino group, a hydroxyl group, a thiol group, a halogenomethyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; X represents a halogen atom or a hydrogen atom; and A represents a nitrogen atom or a partial structure represented by formula (II): wherein X represents a hydrogen atom, an amino group, a halogen atom, a cyano group, a halogenomethyl group, a halogenomethoxyl group, an alkyl group, an alkenyl group, an alkynyl group or an alkoxyl group; and Y represents a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidinyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl, an alkoxymethyl group or a phenylalkyl group.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 7. 发明专利
      CA2111974C CARBAPENEM DERIVATIVES 未知
    • CARBAPENEM DERIVATIVES
    • CA2111974C
    • 2001-07-24
    • CA2111974
    • 1992-06-19
    • DAIICHI SEIYAKU CO
    • NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
    • A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20 , C07F7/10
    • Prior art carbapenem derivatives including thienamycin have disadvantages in that they are physico- chemically unstable and apt to be decomposed by DHP and the like enzyme in the kidney, thereby causing side-effects such as renal toxicity. In addition, 1-b-methylcarbapenem compounds which exhibit stable and strong antibacterial activity are still unsatisfactory in terms of their stability and antibacterial activity against DHP. The present invention provides an antibiotic which shows strong antibacterial activity against various bacterial strains including Pseudomonas aeruginosa and is excellent in terms of safety and stable against hydrolases such as DHP. A compound represented by formula (I): (I) wherein R1 represents a lower alkyl group or a hydroxy lower alkyl group which may have a protecting group; R1 represents a hydrogen atom or a lower alkyl group; R3 represents a carboxyl group which may be esterified; R4 represents an amino group-protecting group, a hydrogen atom or a lower - 76 - alkyl group; R5 and R6, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a hydroxy lower alkyl group or a halogen atom, and R5 and R6 may together form an alkylene group having 2 to 6 carbon atoms; R7 represents a hydrogenatom, a lower alkyl group, a carboxyl group, a carbamoyl group, a carboxyl group which may have a protecting group, or a partial structure represented by -CON71R72 where R71 and R72, which may be the same or different, each represents a hydrogen atom or a lower alkyl group; R8 represents a hydrogen atom, a lower alkyl group or a hydroxy lower alkyl group, and R7 and R8 may together form an alkylene group having 2 to 6 carbon atoms; R9 and R10, which may be the same or different, each represents an amino group-protecting group, a hydrogen atom or a lower alkyl group; Z represents a single bond, an oxygen atom, a sulfur atom, or a partial structure represented by - CR11R12-, -NR13CO-, -CONR14- or -NR15- where R11 and R12, which may be the same or different, each represents a hydrogen atom, a hydroxyl group, a lower alkyl group, a hydroxy lower alkyl group or a halogen atom, and R11 and R12 may together form an alkylene group having 2 to 6 carbon atoms, R13 and R14, which may be the same or different, each represents a hydrogen atom or a lower alkyl group and R15 represents an amino group-protecting group, a hydrogen atom or a lower alkyl group; and each of m and n represents an integer of 0 to 6, and a salt thereof. - 77 -
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明专利
      FI935698A  未知
    • FI935698A
    • 1994-02-04
    • FI935698
    • 1993-12-17
    • DAIICHI SEIYAKU CO
    • NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
    • A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20 , C07D
    • Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 10. 发明专利
      FI935698A0  未知
    • FI935698A0
    • 1993-12-17
    • FI935698
    • 1993-12-17
    • DAIICHI SEIYAKU CO
    • NISHI TOSHIYUKI , KODA HIROKO , SUGITA KAZUYUKI , ISHIDA YOHHEI , TAKEMURA MAKOTO , HAYANO TAKESHI
    • A61K31/40 , A61K31/397 , A61K31/4025 , A61K31/496 , A61P31/04 , C07D20060101 , C07D477/00 , C07D477/20 , C07D
    • Known carbapenem derivatives such as thienamycin have disadvantages that they are physicochemically unstable and readily decomposed by enzymes such as DHP of the kidney to bring about adverse effects such as nephrotoxicity, while 1- beta - methylcarbapenem compounds are stable and have potent antibacterial activities but are yet unsatisfactory as regards the stability and antibacterial activity against DHP. Under these circumstances the invention provides an antibiotic represented by general formula (I) which has a potent antibacterial activity against various bacteria including Pseudomonas aeruginosa and is excellent in safety and stable against hydrolases such as DHP, and a salt thereof (I), wherein R represents lower alkyl or optionally protected hydroxy lower alkyl; R , R and R represent each hydrogen or lower alkyl; R represents optionally esterified carboxy R , R , R and R represent each an amino-protective group, hydrogen or lower alkyl; R , R , R and R represent each hydrogen, hydroxyl, lower alkyl, hydroxy lower alkyl or halogen, or alternatively R and R and/or R and R may combine together to form alkylene; R represents hydrogen, lower alkyl, carboxyl, carbamoyl or -CONR R ; R and R represent each hydrogen or lower alkyl; R represents hydrogen, lower alkyl or hydroxy lower alkyl, or alternatively R may combine with R to form alkylene; Z represents a single bond, oxygen, sulfur, -CR R -, -NR CO-, -CONR - or -NR -; and m and n represent each an integer of 0 to 6.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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