Glycopeptide antibiotic monomer derivatives
    1.
    发明授权
    Glycopeptide antibiotic monomer derivatives 失效
    糖肽抗生素单体衍生物

    公开(公告)号:US08778874B2

    公开(公告)日:2014-07-15

    申请号:US11791446

    申请日:2005-11-24

    CPC分类号: C07K9/008 A61K38/00 A61K38/04

    摘要: Novel glycopeptide antibiotic derivatives. These derivatives are represented by the formula (aglycon part of glycopeptide antibiotic derivative)-(Sac-NH)—RA [wherein (aglycon part of glycopeptide antibiotic derivative) is the part formed by removing the sugar part from a known glycopeptide antibiotic derivative; (Sac-NH) part is an amino sugar part or a sugar chain part containing an amino sugar; and RA represents, e.g., the formula —X1—Ar1—X2—Y—X3—Ar2 (wherein X1, X2, and X3 each represents 1) a single bond or 2) a heteroatom or heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1—, —O—, etc.; Y represents —NR2CO— or —CONR2— (wherein R2 represents hydrogen or lower alkyl), etc.)]. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

    摘要翻译: 新型糖肽抗生素衍生物。 这些衍生物由式(糖肽抗生素衍生物的糖苷配基) - (Sac-NH)-RA [其中(糖肽抗生素衍生物的糖苷配基部分)是通过从已知的糖肽抗生素衍生物中除去糖部分而形成的部分) (Sac-NH)部分是含有氨基糖的氨基糖部分或糖链部分; RA表示例如式-X1-Ar1-X2-Y-X3-Ar2(其中X1,X2和X3各自表示1)单键或2)选自以下的杂原子或含杂原子的基团: 的-N =,-N =,-NR1-,-O-等; Y表示-NR2CO-或-CONR2-(其中R2表示氢或低级烷基)等)。 这些衍生物对万古霉素抗性细菌具有抗菌活性。

    Glycopeptide Antibiotic Monomer Derivatives
    2.
    发明申请
    Glycopeptide Antibiotic Monomer Derivatives 失效
    糖肽抗生素单体衍生物

    公开(公告)号:US20080097078A1

    公开(公告)日:2008-04-24

    申请号:US11791446

    申请日:2005-11-24

    IPC分类号: C07K7/64 C07K5/12

    CPC分类号: C07K9/008 A61K38/00 A61K38/04

    摘要: Novel glycopeptide antibiotic derivatives. These derivatives are represented by the formula (aglycon part of glycopeptide antibiotic derivative)-(Sac-NH)—RA [wherein (aglycon part of glycopeptide antibiotic derivative) is the part formed by removing the sugar part from a known glycopeptide antibiotic derivative; (Sac-NH) part is an amino sugar part or a sugar chain part containing an amino sugar; and RA represents, e.g., the formula —X1—Ar1—X2—Y—X3—Ar2 (wherein X1, X2, and X3 each represents 1) a single bond or 2) a heteroatom or heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1—, —O—, etc.; Y represents —NR2CO— or —CONR2— (wherein R2 represents hydrogen or lower alkyl), etc.)]. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

    摘要翻译: 新型糖肽抗生素衍生物。 这些衍生物由式(糖肽抗生素衍生物的糖苷配基部分) - (Sac-NH)-R A表示[其中(糖肽抗生素衍生物的糖苷配基部分)是通过除去糖部分而形成的部分 从已知的糖肽抗生素衍生物; (Sac-NH)部分是含有氨基糖的氨基糖部分或糖链部分; 并且R A表示例如式-X 1 -Ar 1 -x 2 -YX SUP >其中X 1,X 2和X 3各自表示 1)单键或2)选自-N-,-N-,-NR 1 - , - O - 等的杂原子或含杂原子的基团; Y表示-NR 2 CO-或-CONR 2 - (其中R 2表示氢或低级烷基)等)。 这些衍生物对万古霉素抗性细菌具有抗菌活性。

    Glycopeptide antibiotic derivative
    3.
    发明授权
    Glycopeptide antibiotic derivative 有权
    糖肽抗生素衍生物

    公开(公告)号:US08933012B2

    公开(公告)日:2015-01-13

    申请号:US12224443

    申请日:2007-05-25

    CPC分类号: C07K9/008 A61K38/00 A61K38/04

    摘要: The present invention provides a novel glycopeptide antibiotic derivative.These derivatives are represented by the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein RA is —X1—Ar1—X2—Y—X3—Ar2 wherein X1, X2 and X3 are single bond; heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group; Y is —NR2CO—, —CONR2— (R2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R3 is alkylene; Ar1 and Ar2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond; RB is —NHNRXRY or —NRZORW wherein RX is hydrogen or lower alkyl; RY is hydrogen, optionally substituted lower alkyl, C(═NH)NH2, CSNH2, COCONH2, CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl; RZ is hydrogen or lower alkyl; RW is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl; RC is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—; and R is optionally substituted alkyl.

    摘要翻译: 本发明提供了一种新型糖肽抗生素衍生物。 这些衍生物由式(I)表示或其药学上可接受的盐或溶剂化物,其中RA为-X1-Ar1-X2-Y-X3-Ar2,其中X1,X2和X3为单键; 选自-N =,N-,-NR1-(R 1为氢或低级烷基), - O - , - S - , - SO-和-SO 2 - 的杂原子的基团,或其连接基 ; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-,-CONR 2 - (R 2是氢或低级烷基)或式(II)的基团,其中R 3是亚烷基; Ar1和Ar2是任选被取代并可具有不饱和键的碳环或杂环; RB是-NHNRXRY或-NRZORW,其中RX是氢或低级烷基; RY是氢,任选取代的低级烷基,C(= NH)NH 2,CSNH 2,COCONH 2,CN,任选取代的杂环基和任选取代的氨基甲酰基; RZ是氢或低级烷基; RW是氢,任选取代的低级烷基,任选取代的低级烯基,任选取代的杂环基,任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基,其中所述烷基可以被选自N =,N-,-NR1-(R 1是氢或低级烷基),-O - , - S - , - SO-和-SO 2 - ; R是任选取代的烷基。

    Glycopeptide Antibiotic Derivative
    4.
    发明申请
    Glycopeptide Antibiotic Derivative 有权
    糖肽抗生素衍生物

    公开(公告)号:US20090286717A1

    公开(公告)日:2009-11-19

    申请号:US12224443

    申请日:2007-05-25

    IPC分类号: A61K38/00 C07K9/00 A61P43/00

    CPC分类号: C07K9/008 A61K38/00 A61K38/04

    摘要: The present invention provides a novel glycopeptide antibiotic derivative.These derivatives are represented by the formula (I) or a pharmaceutically acceptable salt or solvate thereof, wherein RA is —X1—Ar1—X2—Y—X3—Ar2 wherein X1, X2 and X3 are single bond; heteroatom-containing group selected from the group consisting of —N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—, or a linkage thereof; or alkylene or alkenylene optionally substituted and optionally interrupted by one or more of said heteroatom-containing group; Y is —NR2CO—, —CONR2— (R2 is hydrogen or lower alkyl), or a group of the formula (II) wherein R3 is alkylene; Ar1 and Ar2 are a carbocycle or a heterocycle which is optionally substituted and may have an unsaturated bond; RB is —NHNRXRY or —NRZORW wherein RX is hydrogen or lower alkyl; RY is hydrogen, optionally substituted lower alkyl, C(═NH)NH2, CSNH2, COCONH2, CN, optionally substituted heterocyclic group, and optionally substituted carbamoyl; RZ is hydrogen or lower alkyl; RW is hydrogen, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted heterocyclic group, optionally substituted heterocyclic carbonyl or optionally substituted carbamoyl; RC is hydrogen or optionally substituted alkyl, wherein said alkyl may be interrupted by a heteroatom-containing group selected from N═, ═N—, —NR1— (R1 is hydrogen or lower alkyl), —O—, —S—, —SO— and —SO2—; and R is optionally substituted alkyl.

    摘要翻译: 本发明提供了一种新型糖肽抗生素衍生物。 这些衍生物由式(I)表示或其药学上可接受的盐或溶剂化物,其中RA为-X1-Ar1-X2-Y-X3-Ar2,其中X1,X2和X3为单键; 选自-N-,-N-,-NR1-(R 1为氢或低级烷基), - , - - , - S - , - SO - 和-SO 2 - 或其连接基团 ; 或任选被取代并任选被一个或多个所述含杂原子基团中断的亚烷基或亚烯基; Y是-NR 2 CO-,-CONR 2 - (R 2是氢或低级烷基)或式(II)的基团,其中R 3是亚烷基; Ar1和Ar2是任选被取代并可具有不饱和键的碳环或杂环; RB是-NHNRXRY或-NRZORW,其中RX是氢或低级烷基; RY是氢,任选取代的低级烷基,C(-NH)NH 2,CSNH 2,COCONH 2,CN,任选取代的杂环基和任选取代的氨基甲酰基; RZ是氢或低级烷基; RW是氢,任选取代的低级烷基,任选取代的低级烯基,任选取代的杂环基,任选取代的杂环羰基或任选取代的氨基甲酰基; RC是氢或任选取代的烷基,其中所述烷基可以被选自N-,-N-,-NR1-(R 1是氢或低级烷基),-O - , - S - , - SO-和-SO 2 - ; R是任选取代的烷基。

    Glycosylated glycopeptide antibiotic derivatives
    5.
    发明授权
    Glycosylated glycopeptide antibiotic derivatives 有权
    糖基化糖肽抗生素衍生物

    公开(公告)号:US08481696B2

    公开(公告)日:2013-07-09

    申请号:US12810507

    申请日:2008-12-25

    CPC分类号: C07K9/008 A61K38/00

    摘要: The present invention provides novel glycopeptides antibiotic derivatives comprising a sugar residue (I) represented by the formula: (wherein n is an integer of 1 to 5: Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl)) is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

    摘要翻译: 本发明提供新的糖肽抗生素衍生物,其包含由下式表示的糖残基(I):其中n为1〜5的整数:Sug各自独立地为单糖,(Sug)n为通过结合形成的二价糖残基 相同或不同的1至5个单糖; RA1为任选取代的低级烷基,任选取代的低级烯基或任选取代的环烷基; RE为OH或NHAc(Ac为乙酰基))与第四个氨基酸残基的芳香环结合 在糖肽骨架中。 这些衍生物对万古霉素抗性细菌具有抗菌活性。

    GLYCOSYLATED GLYCOPEPTIDE ANTIBIOTIC DERIVATIVES
    6.
    发明申请
    GLYCOSYLATED GLYCOPEPTIDE ANTIBIOTIC DERIVATIVES 有权
    谷氨酰胆碱抗生素衍生物

    公开(公告)号:US20100286364A1

    公开(公告)日:2010-11-11

    申请号:US12810507

    申请日:2008-12-25

    IPC分类号: C07K9/00 C12P21/06

    CPC分类号: C07K9/008 A61K38/00

    摘要: The present invention provides novel glycopeptides antibiotic derivatives.These glycopeptide antibiotic derivatives are characterized in that a sugar residue (I) represented by the formula: (wherein n is an integer of 1 to 5; Sugs are each independently a monosaccharide, (Sug)n is a divalent sugar residue formed by binding of same or different 1 to 5 monosaccharides; RA1 is optionally substituted lower alkyl, optionally substituted lower alkenyl, or optionally substituted cycloalkyl; and RE is OH or NHAc (Ac is acetyl)) is bound to an aromatic ring of the fourth amino acid residue in the glycopeptide skeleton. These derivatives have antibacterial activity against vancomycin-resistant bacteria.

    摘要翻译: 本发明提供新型糖肽抗生素衍生物。 这些糖肽抗生素衍生物的特征在于由下式表示的糖残基(I)(其中n为1〜5的整数; Sug各自独立地为单糖,(Sug)n为通过结合形成的二价糖残基 相同或不同的1至5个单糖; RA1为任选取代的低级烷基,任选取代的低级烯基或任选取代的环烷基; RE为OH或NHAc(Ac为乙酰基))与第四个氨基酸残基的芳环结合 糖肽骨架。 这些衍生物对万古霉素抗性细菌具有抗菌活性。

    Ratchet-type tensioner
    8.
    发明授权
    Ratchet-type tensioner 有权
    棘轮式张紧器

    公开(公告)号:US08821326B2

    公开(公告)日:2014-09-02

    申请号:US13474792

    申请日:2012-05-18

    IPC分类号: F16H7/08

    摘要: In a ratchet-type tensioner having a plunger with rack teeth formed thereon and a piston with ratchet teeth that engage the rack teeth, the ratchet teeth can be disengaged from the rack teeth by insertion of a tool through a tool insertion hole in the tensioner housing and exerting a prying action on the toothed end of the piston to move the piston away from the plunger. Alternatively if an oblique camming surface is formed on the toothed end of the piston, the ratchet teeth can be disengaged from the rack teeth by pushing the tool inward against the oblique camming surface. The piston and the hole in which it slides are shaped to prevent rotation of the piston. The ratchet teeth on the piston and the rack teeth on the plunger can be oblique to allow setback of the plunger when excessive force is exerted on the plunger.

    摘要翻译: 在具有形成有齿条齿的柱塞的棘轮式张紧器和具有与齿条齿接合的棘轮齿的活塞的棘轮式张紧器中,通过将工具插入到张紧器壳体中的工具插入孔中,棘轮齿可以与齿条齿脱离 并且在活塞的齿端上施加撬动作用以将活塞移离柱塞。 或者,如果在活塞的齿端上形成倾斜的凸轮表面,则可以通过将工具向内推靠在倾斜凸轮表面上而将棘轮齿与齿条齿脱离。 活塞及其滑动的孔被成形以防止活塞旋转。 活塞上的棘齿和柱塞上的齿条齿可以倾斜,以便在柱塞上施加过大的力时允许柱塞的遏制。

    Ring-type tensioner
    9.
    发明授权
    Ring-type tensioner 有权
    环型张紧器

    公开(公告)号:US08740736B2

    公开(公告)日:2014-06-03

    申请号:US13477345

    申请日:2012-05-22

    IPC分类号: F16H7/22 F16H7/08

    摘要: In a ring-type tensioner, an expansible elastic ring disposed in a groove formed in the wall of a plunger-accommodating hole cooperates with teeth formed on the plunger to restrict axial movement of the plunger. The ring and the groove in the wall of the plunger-accommodating hole have flat radial surfaces for mutual engagement. However the ring also has oblique plunger-tooth engaging surfaces. The ring has manipulable end parts that can be locked in fixed relation to each other by a tool to secure the plunger against axial movement. The tool can also be inserted into a gap between the manipulable end parts to expand the ring and thereby release the plunger.

    摘要翻译: 在环形张紧器中,设置在形成在柱塞容纳孔的壁中的槽中的可膨胀弹性环与形成在柱塞上的齿配合以限制柱塞的轴向运动。 柱塞容纳孔的壁中的环和槽具有相互接合的平坦的径向表面。 然而,该环也具有倾斜的柱塞 - 齿啮合表面。 环具有可操纵的端部,其可以通过工具彼此固定地相互锁定,以将柱塞固定在轴向运动上。 工具也可以插入到可操纵的端部之间的间隙中以使环膨胀,从而释放柱塞。

    Sunroff apparatus
    10.
    发明授权
    Sunroff apparatus 有权
    Sunroff装置

    公开(公告)号:US08740296B2

    公开(公告)日:2014-06-03

    申请号:US13991381

    申请日:2011-12-06

    IPC分类号: B60J7/057 B60J7/053 B60J7/047

    摘要: To provide a sunroof apparatus including a front panel and a rear panel closing a roof opening formed in a roof of a vehicle, capable of keeping a large distance in a back-and-forth direction between the supporting portions supporting the front and rear portions of the rear panel in a fully closed state of closing the roof opening by the front panel and the rear panel.In a fully closed state of panels, a rear forward supporting portion supporting the front portion of the rear panel is provided in a rear portion of a front slider and a rear backward supporting portion supporting the rear portion of the rear panel is provided in a rear slider.

    摘要翻译: 为了提供一种天窗装置,其包括前面板和后面板,其封闭形成在车辆顶部中的屋顶开口,能够在支撑前后部分的支撑部分之间沿前后方向保持大的距离 后面板处于完全关闭状态,通过前面板和后面板关闭屋顶开口。 在完全关闭状态的面板中,在前滑块的后部设有支撑后面板前部的后向前支撑部分,并且后支撑部分后支撑部分设置在后面板的后部 滑块