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    NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    11.
    发明申请
    NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS 审中-公开
    新型半合成糖苷作为抗菌剂

    公开(公告)号：US20110015119A1

    公开(公告)日：2011-01-20

    申请号：US12552221

    申请日：2009-09-01

    Applicant: Daniel Chu ,  Tao Ye ,  Bing Wang

    Inventor： Daniel Chu ,  Tao Ye ,  Bing Wang

    IPC: A61K38/12 ,  C07K7/50 ,  A61P31/04

    CPC classification number: C07K9/008 ,  A61K38/00 ,  A61K45/06

    Abstract: Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide (Compound A, Compound B, Compound H or Compound C) or monosaccharide made by hydrolyzing the disaccharide moiety of the amino acid-4 of the parent glycopeptide in acidic medium to give the amino acid-4 monosaccharide; conversion of the monosaccharide to the amino-sugar derivative; acylation of the amino substituent on the amino acid-4 amino-substituted sugar moiety on these scaffolds with certain acyl groups; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. Key reaction is the treatment of properly protected intermediate compound with isocyanate. Also provided are methods for the 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: 具体描述了具有抗菌活性的半合成糖肽，特别是本文所述的半合成糖肽通过化学修饰糖肽（化合物A，化合物B，化合物H或化合物C）或通过水解二糖部分 在酸性介质中母体糖肽的氨基酸-4得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 在这些支架上的氨基酸4氨基取代的糖部分上的氨基取代基被某些酰基酰化; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 关键反应是用异氰酸酯处理适当保护的中间体化合物。 还提供了合成化合物的方法，含有该化合物的药物组合物，以及该化合物用于治疗和/或预防疾病，特别是细菌感染的方法。

    Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP)
    13.
    发明授权
    Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP) 有权
    聚（ADP-核糖）聚合酶（PARP）的苯并恶唑甲酰胺抑制剂

    公开(公告)号：US08088760B2

    公开(公告)日：2012-01-03

    申请号：US12355692

    申请日：2009-01-16

    Applicant: Daniel Chu ,  Bing Wang

    Inventor： Daniel Chu ,  Bing Wang

    IPC: A61K31/422 ,  A61K31/423 ,  A61K31/496 ,  C07D263/54 ,  C07D413/02 ,  A61P35/00

    CPC classification number: C07D263/57 ,  C07D413/04 ,  C07D413/10 ,  C07D455/02 ,  C07D487/04 ,  C07D487/08

    Abstract: A compound having the structure set forth in Formula (I) or Formula (II): wherein the variables Y, R1, R2, R3, and R4 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）或式（II）所示结构的化合物：其中变量Y，R1，R2，R3和R4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。

    5,6,6a,7,8,9-HEXAHYDRO-2H-PYRIDOPHTHALAZINONE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP)
    15.
    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

    Applicant: Daniel Chu ,  Bing Wang

    Inventor： Daniel Chu ,  Bing Wang

    IPC: A61K31/397 ,  C07D487/06 ,  A61K31/5025 ,  C07D413/14 ,  A61K31/5377 ,  A61P9/00 ,  A61P35/00 ,  A61P25/28

    CPC classification number: A61K31/397 ,  A61K31/5025 ,  A61K31/5377 ,  C07D413/14 ,  C07D487/06

    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)
    16.
    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

    Applicant: Bing Wang ,  Daniel Chu

    Inventor： Bing Wang ,  Daniel Chu

    IPC: A61K31/5025 ,  C07D471/06 ,  A61P35/00 ,  A61P25/00

    CPC classification number: A61K31/5025 ,  A61K31/282 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/5377 ,  A61K33/24 ,  A61N5/10 ,  A61N2005/1098 ,  C07D471/06

    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。

    Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP)
    20.
    发明授权
    Dihydropyridophthalazinone inhibitors of poly(ADP-ribose)polymerase (PARP) 有权
    聚（ADP-核糖）聚合酶（PARP）的二氢吡喃并酞嗪酮抑制剂

    公开(公告)号：US08012976B2

    公开(公告)日：2011-09-06

    申请号：US12510096

    申请日：2009-07-27

    Applicant: Bing Wang ,  Daniel Chu

    Inventor： Bing Wang ,  Daniel Chu

    IPC: C07D237/36 ,  A01N43/60 ,  A61K31/50

    CPC classification number: A61K31/5025 ,  A61K31/282 ,  A61K31/4745 ,  A61K31/495 ,  A61K31/5377 ,  A61K33/24 ,  A61N5/10 ,  A61N2005/1098 ,  C07D471/06

    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。

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