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    6-o-substituted ketolide having antibacterial activity
    1.
    发明专利
    6-o-substituted ketolide having antibacterial activity 审中-公开
    具有抗生素活性的6-O-取代的硬脂酸乙酯

    公开(公告)号：JP2013047243A

    公开(公告)日：2013-03-07

    申请号：JP2012228250

    申请日：2012-10-15

    Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: C07H17/08 ,  A61K31/7048 ,  A61K31/7056 ,  A61P31/04

    CPC classification number: C07H17/08 ,  Y02P20/55

    Abstract: PROBLEM TO BE SOLVED: To provide new semi-synthesized macrolides having antibacterial activity, a pharmaceutical composition including these compounds, and a medical treatment method of remedy.SOLUTION: There is provided a 6-O-substituted erythromycin ketolide derivative expressed by formula (IV-A), where in formula, Rc is hydrogen or a hydroxy-protective group; R is a substituted methyl group; A, B, D and E are each selected from hydrogen, a 1-6C alkyl which may be substituted by a substituent, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, hydroxy, 1-6C alkoxy, and halogen of Br, Cl, F or I, or the like, under conditions that at least two of A, B, D and E are both hydrogen.

    Abstract translation: 要解决的问题：提供具有抗菌活性的新的半合成大环内酯类，包括这些化合物的药物组合物和补救药物治疗方法。 解决方案：提供由式（IV-A）表示的6-O-取代的红霉素酮内酯衍生物，其中在式中，Rc是氢或羟基保护基; R是取代的甲基; A，B，D和E各自选自氢，可被取代基取代的1-6C烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环烷基，羟基，1-6C烷氧基和Br的卤素， Cl，F或I等，在A，B，D和E中的至少两个都是氢的条件下。 版权所有（C）2013，JPO＆INPIT

    6-o-substituted ketolide having bacterial activity
    2.
    发明专利
    6-o-substituted ketolide having bacterial activity 有权
    具有细菌活性的6-O-取代的硬脂酸乙酯

    公开(公告)号：JP2011016808A

    公开(公告)日：2011-01-27

    申请号：JP2010175066

    申请日：2010-08-04

    Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: C07H17/08 ,  A61K31/7048 ,  A61P31/04 ,  C07B61/00

    CPC classification number: C07H17/08 ,  Y02P20/55

    Abstract: PROBLEM TO BE SOLVED: To provide a new semisynthesized macrolide having antibacterial activity.SOLUTION: The antibacterial compound having formula (II) or the like, and pharmaceutically acceptable salts, esters or prodrugs thereof, are provided. Pharmaceutical compositions each containing such a compound; methods for treating bacterial infections by administering such a compound; and a method for producing the compound; are also provided.

    Abstract translation: 要解决的问题：提供具有抗菌活性的新的半合成大环内酯。提供具有式（II）等的抗菌化合物及其药学上可接受的盐，酯或前药。 各含有这种化合物的药物组合物; 通过施用这种化合物治疗细菌感染的方法; 和该化合物的制造方法。 也提供。

    6-o-substituted ketolide having antibacterial activity
    4.
    发明专利
    6-o-substituted ketolide having antibacterial activity 有权
    具有抗生素活性的6-O-取代的硬脂酸乙酯

    公开(公告)号：JP2009221214A

    公开(公告)日：2009-10-01

    申请号：JP2009124819

    申请日：2009-05-25

    Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: C07H17/08 ,  A61K31/7048 ,  A61P31/04

    CPC classification number: C07H17/08 ,  Y02P20/55

    Abstract: PROBLEM TO BE SOLVED: To provide novel semi-synthetic macrolides having antibacterial activity and pharmaceutical compositions containing these compounds and to provide medical methods for treating bacterial infection. SOLUTION: Antimicrobial compounds having formula (III) as well as pharmaceutically acceptable salts, esters or prodrugs thereof are provided herein. COPYRIGHT: (C)2010,JPO&INPIT

    Abstract translation: 要解决的问题：提供具有抗菌活性的新型半合成大环内酯类和含有这些化合物的药物组合物，并提供用于治疗细菌感染的医学方法。 解决方案：本文提供了具有式（III）的抗微生物化合物及其药学上可接受的盐，酯或前药。 版权所有（C）2010，JPO＆INPIT

    6-o-substituted ketolide possessing antibacterial activity
    5.
    发明专利
    6-o-substituted ketolide possessing antibacterial activity 审中-公开
    6-O-取代的胶原蛋白抗菌活性

    公开(公告)号：JP2009084282A

    公开(公告)日：2009-04-23

    申请号：JP2008253261

    申请日：2008-09-30

    Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: C07H17/08 ,  A61K31/7048 ,  A61P31/00

    CPC classification number: C07H17/08 ,  Y02P20/55

    Abstract: PROBLEM TO BE SOLVED: To provide a new antibacterial compound with enhanced activity. SOLUTION: Antibacterial compounds represented by formula (II) or the like, pharmaceutically acceptable salts, esters or prodrugs thereof, medicinal compositions including the same, treatment methods for bacterial infections by administration of such compounds and a method for producing the compound are provided. COPYRIGHT: (C)2009,JPO&INPIT

    Abstract translation: 要解决的问题：提供具有增强活性的新型抗菌化合物。 解决方案：由式（II）等表示的抗菌化合物，其药学上可接受的盐，酯或前药，包含它们的药物组合物，通过施用这些化合物的细菌感染的治疗方法和制备该化合物的方法是： 提供。 版权所有（C）2009，JPO＆INPIT

    6-o-substituted ketolide having antibacterial activity
    7.
    发明专利
    6-o-substituted ketolide having antibacterial activity 有权
    具有抗生素活性的6-O-取代的硬脂酸乙酯

    公开(公告)号：JP2009062378A

    公开(公告)日：2009-03-26

    申请号：JP2008253259

    申请日：2008-09-30

    Applicant: Abbott Lab ,  アボット・ラボラトリーズAbbott Laboratories

    Inventor： OR YAT SUN ,  MA ZHENKUN ,  CLARK RICHARD F ,  CHU DANIEL T ,  PLATTNER JACOB J

    IPC: C07H17/08 ,  A61K31/7048 ,  A61P31/04

    CPC classification number: C07H17/08 ,  Y02P20/55

    Abstract: PROBLEM TO BE SOLVED: To provide a new class 6-O-substituted erythromycin derivative having increased acid stability to erythromycin A and 6-O-methylerythromycin A, and enhanced activity to gram-negative bacteria and macrolide-resisting gram-positive bacteria. SOLUTION: Provided are an antibacterial compound having structural formula (V) and the like as well as pharmaceutically permissible salts, esters or prodrugs thereof; pharmaceutical compositions comprising the compound; a therapeutic method of bacterial infection by administering the compound; and a production method of the compound. COPYRIGHT: (C)2009,JPO&INPIT

    Abstract translation: 要解决的问题：提供一种具有增加的对红霉素A和6-O-甲基红霉素A的酸稳定性的新型6-O-取代的红霉素衍生物，并且对革兰氏阴性细菌和抗大肠杆菌抗性革兰氏阳性的活性增强 菌。 解决方案：提供具有结构式（V）等的抗菌化合物及其药学上可允许的盐，酯或前药; 包含该化合物的药物组合物; 通过施用该化合物的细菌感染的治疗方法; 和该化合物的制造方法。 版权所有（C）2009，JPO＆INPIT

    INHIBITORS OF TRANSPEPTIDASE
    8.
    发明申请
    INHIBITORS OF TRANSPEPTIDASE 审中-公开
    运输抑制剂

    公开(公告)号：WO1982001875A1

    公开(公告)日：1982-06-10

    申请号：PCT/US1981000109

    申请日：1981-01-19

    Applicant: ABBOTT LAB

    Inventor： ABBOTT LAB ,  CHU DANIEL T

    IPC: C07D487/04

    CPC classification number: C07D477/24

    Abstract: New ss-lactams of the general structure: (FORMULA) wherein R represents H or an acyl moiety known from the penicillin or cephalosporin art, R' is hydrogen, lower alkoxy, lower alkoxyalkyl, lower alkyl, phenylthio or lower alkylmercapto, R' is lower alkyl, the broken line represents an optional double bond, and acyloxymethyl esters thereof. All compounds are effective antibacterials.

    Abstract translation: 一般结构的新型β-内酰胺：其中R表示H或由青霉素或头孢菌素领域已知的酰基部分，其中R'为氢，低级烷氧基，低级烷氧基烷基，低级烷基，苯硫基或低级烷基巯基，R'为 低级烷基，虚线表示任选的双键，和其酰氧基甲基酯。 所有化合物都是有效的抗菌剂。

    3-DESCLADINOSE 6-O-SUBSTITUDED ERYTHROMYCIN DERIVATIVES
    9.
    发明申请
    3-DESCLADINOSE 6-O-SUBSTITUDED ERYTHROMYCIN DERIVATIVES 审中-公开
    3-DESCLADINOSE 6-O-取代的红霉素衍生物

    公开(公告)号：WO9911651A3

    公开(公告)日：1999-05-06

    申请号：PCT/US9818125

    申请日：1998-09-01

    Applicant: ABBOTT LAB

    Inventor： OR YAT SUN ,  LI LEPING ,  RUPP MICHAEL J ,  CHU DANIEL T

    IPC: A61K31/7042 ,  A61K31/7048 ,  A61K31/7056 ,  A61P31/04 ,  C07H17/08 ,  A61K31/70

    CPC classification number: C07H17/08

    Abstract: Novel multicyclic erythromycin compounds and pharmaceutically acceptable salts and esters thereof having antibacterial activity having a formula selected from the group consisting of (I), (II), (III), (IV) and (V), compositions comprising a therapeutically eff ective amount of a compound of the invention in combination with a pharmaceutically acceptable carrier, as well as a method for treating bacterial infections by administering to a mammal a pharmaceutical composition containing a therapeutically effective amount of a compound of formulas (I)-(V).

    Abstract translation: 具有选自（I），（II），（III），（IV）和（V）组的式的具有抗菌活性的新型多环红霉素化合物及其药学上可接受的盐和酯包含治疗有效量 的本发明化合物与药学上可接受的载体的组合，以及通过向哺乳动物施用含有治疗有效量的式（I） - （V）化合物的药物组合物来治疗细菌感染的方法。

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