5,6,6a,7,8,9-HEXAHYDRO-2H-PYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
    71.
    发明申请
    5,6,6a,7,8,9-HEXAHYDRO-2H-PYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) 审中-公开
    (ADP-RIBOSE)聚合酶(PARP)的5,6,6a,7,8,9-HEXAHYDRO-2H-吡咯烷酮嗪抑制剂

    公开(公告)号:US20110190266A1

    公开(公告)日:2011-08-04

    申请号:US13021474

    申请日:2011-02-04

    Abstract: Provided herein are compounds having the structure set forth in Formula (I): wherein the variables Y, Z, A, B, R1, R2, R3, R1′, R2′, R3′, R4 and R5 are as defined herein and methods of their synthesis. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

    Abstract translation: 本文提供具有式(I)所示结构的化合物:其中变量Y,Z,A,B,R 1,R 2,R 3,R 1',R 2',R 3',R 4和R 5如本文所定义, 的合成。 本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗通过抑制PARP活性而改善的疾病,病症和病症的药物组合物。

    DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
    73.
    发明申请
    DIHYDROPYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) 有权
    聚(ADP-RIBOSE)聚合酶(PARP)的二氢吲哚哒嗪酮抑制剂

    公开(公告)号:US20100035883A1

    公开(公告)日:2010-02-11

    申请号:US12510096

    申请日:2009-07-27

    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions that are ameliorated by the inhibition of PARP activity.

    Abstract translation: 具有式(I)和式(II)所示结构的化合物:其中取代基Y,Z,A,B,R 1,R 2,R 3,R 4和R 5如本文所定义。 本文提供了聚(ADP-核糖)聚合酶活性的抑制剂。 本文还描述了包含本文所述的至少一种化合物和本文所述的化合物或药物组合物用于治疗通过抑制PARP活性而改善的疾病,病症和病症的药物组合物。

    Cascode protected negative voltage switching
    77.
    发明授权
    Cascode protected negative voltage switching 有权
    串联保护负压开关

    公开(公告)号:US07382591B2

    公开(公告)日:2008-06-03

    申请号:US11133648

    申请日:2005-05-20

    CPC classification number: G11C16/12 G11C16/30 Y10T307/964

    Abstract: A double cascode protected switchable voltage source may be used to selectively provide positive or negative voltage sources, for example, to a flash memory. The positive supply may be connected through a PMOS pass device to a first cascode protection device. A negative supply may be connected through an NMOS pass device and an NMOS cascode protection device to an output. The circuits may be designed so that exceeding snapback limits and gate aided drain breakdown are less likely.

    Abstract translation: 可以使用双共源共栅保护的可切换电压源来选择性地将正或负电压源例如提供给闪存。 正电源可以通过PMOS通道器件连接到第一共源共栅保护器件。 负电源可以通过NMOS通道器件和NMOS共源共栅保护器件连接到输出端。 这些电路可以被设计成使得超过回跳限制和栅极辅助漏极击穿不太可能。

    Semi-synthetic desmethyl-vancomycin-based glycopeptides with antibiotic activity
    78.
    发明申请
    Semi-synthetic desmethyl-vancomycin-based glycopeptides with antibiotic activity 审中-公开
    具有抗菌活性的半合成脱甲基万古霉素基糖肽

    公开(公告)号:US20070185015A1

    公开(公告)日:2007-08-09

    申请号:US11361682

    申请日:2006-02-24

    CPC classification number: C07K9/008 A61K38/00

    Abstract: Semi-synthetic glycopeptides that have antibacterial activity are based on modifications of the desmethyl-vancomycin scaffold, in particular, acylation of the amino substituent on the amino-substituted sugar moiety on this scaffold with certain acyl groups; and/or conversion of the acid moiety on the macrocyclic ring of this scaffolds to certain substituted amides. In addition, compounds of the invention include desmethyl-vancomycin scaffolds on which the acid moiety on the macrocyclic ring is converted to certain substituted amides and the amino substituent on the amino-substituted sugar moiety is alkylated with certain alkyl groups. Also provided are methods for synthesis of the compounds, pharmaceutical compositions containing the compounds, and methods of use of the compounds for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 具有抗菌活性的半合成糖肽基于脱甲基万古霉素支架的修饰,特别是在该支架上具有某些酰基的氨基取代的糖部分上的氨基取代基的酰化; 和/或将该支架的大环上的酸部分转化为某些取代的酰胺。 此外,本发明的化合物包括去甲基 - 万古霉素支架,大环上的酸部分转化为某些取代的酰胺,氨基取代的糖部分上的氨基取代基被某些烷基烷基化。 还提供了合成化合物的方法,含有化合物的药物组合物,以及用于治疗和/或预防疾病,特别是细菌感染的化合物的使用方法。

    Ketolide derivatives
    79.
    发明授权
    Ketolide derivatives 失效
    酮内酯衍生物

    公开(公告)号:US07163924B2

    公开(公告)日:2007-01-16

    申请号:US10831522

    申请日:2004-04-23

    CPC classification number: C07H17/08

    Abstract: Antimicrobial ketolide compounds are provided having the formula (A): as well as pharmaceutically acceptable salts, esters or prodrugs thereof, pharmaceutical compositions comprising such compounds, methods of treating bacterial infections by the administration of such compounds, and processes for the preparation of the compounds.

    Abstract translation: 提供具有式(A)的抗微生物酮内酯化合物:以及其药学上可接受的盐,酯或前药,包含这些化合物的药物组合物,通过施用这些化合物治疗细菌感染的方法,以及制备化合物的方法 。

    Cascode protected negative voltage switching
    80.
    发明申请
    Cascode protected negative voltage switching 有权
    串联保护负压开关

    公开(公告)号:US20060267414A1

    公开(公告)日:2006-11-30

    申请号:US11133648

    申请日:2005-05-20

    CPC classification number: G11C16/12 G11C16/30 Y10T307/964

    Abstract: A double cascode protected switchable voltage source may be used to selectively provide positive or negative voltage sources, for example, to a flash memory. The positive supply may be connected through a PMOS pass device to a first cascode protection device. A negative supply may be connected through an NMOS pass device and an NMOS cascode protection device to an output. The circuits may be designed so that exceeding snapback limits and gate aided drain breakdown are less likely.

    Abstract translation: 可以使用双共源共栅保护的可切换电压源来选择性地将正或负电压源例如提供给闪存。 正电源可以通过PMOS通道器件连接到第一共源共栅保护器件。 负电源可以通过NMOS通道器件和NMOS共源共栅保护器件连接到输出端。 这些电路可以被设计成使得超过回跳限制和栅极辅助漏极击穿不太可能。

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