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    Processes of synthesizing dihydropyridophthalazinone derivatives
    1.
    发明授权
    Processes of synthesizing dihydropyridophthalazinone derivatives 有权
    合成二氢吡啶并酞嗪酮衍生物的方法

    公开(公告)号：US08765945B2

    公开(公告)日：2014-07-01

    申请号：US13023140

    申请日：2011-02-08

    Applicant: Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Quan Jiang ,  Lei Lu

    Inventor： Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Quan Jiang ,  Lei Lu

    IPC: C07D237/36

    CPC classification number: C07D405/06 ,  C07D249/08 ,  C07D401/04 ,  C07D403/06 ,  C07D471/06

    Abstract: Provided herein are processes for synthesizing dihydropyridophthalazinone derivatives, such as for example, 5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one and its stereoisomers, which are potent poly(ADP-ribose)polymerase (PARP) inhibitors as well as novel synthetic intermediate compounds.

    Abstract translation: 本文提供了合成二氢吡啶并二氮杂萘酮衍生物的方法，例如5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基） 9-二氢-2H-吡啶并[4,3,2-de]酞嗪-3（7H） - 酮及其立体异构体，它们是有效的聚（ADP-核糖）聚合酶（PARP）抑制剂以及新的合成中间体化合物。

    Crystalline (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt
    2.
    发明授权
    Crystalline (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt 有权
    结晶（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H-吡啶 [4,3,2-de]酞嗪-3（7H） - 酮甲苯磺酸盐

    公开(公告)号：US08735392B2

    公开(公告)日：2014-05-27

    申请号：US13277607

    申请日：2011-10-20

    Applicant: Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Shichun Peng

    Inventor： Bing Wang ,  Daniel Chu ,  Yongbo Liu ,  Shichun Peng

    IPC: A01N43/58 ,  A61K31/495

    CPC classification number: C07D471/06

    Abstract: Provided herein are (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt forms, including crystalline forms, and methods of their preparation. Pharmaceutical compositions comprising a (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt are also provided, as are methods of using (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one tosylate salt to treat a disease or condition, such as a cancer.

    Abstract translation: 本文提供的是（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H- - 吡啶并[4,3,2-de]酞嗪-3（7H） - 酮甲磺酸盐形式，包括晶型，及其制备方法。 包含（8S，9R）-5-氟-8-（4-氟苯基）-9-（1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢 - 还提供了使用（8S，9R）-5-氟-8-（4-氟苯基）-9（7H） - 酮的方法，使用2-吡啶并[4,3,2- - （1-甲基-1H-1,2,4-三唑-5-基）-8,9-二氢-2H-吡啶并[4,3,2-de]酞嗪-3（7H） - 酮甲苯磺酸盐 治疗疾病或病症，如癌症。

    NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    3.
    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：US20100105607A1

    公开(公告)日：2010-04-29

    申请号：US12603435

    申请日：2009-10-21

    Applicant: Daniel Chu ,  Tao Ye ,  Bing Wang

    Inventor： Daniel Chu ,  Tao Ye ,  Bing Wang

    IPC: A61K38/08 ,  C07K9/00 ,  A61P31/04

    CPC classification number: C07K9/006

    Abstract: Semi-synthetic glycopeptides having antibacterial activity are described, in particular, the semi-synthetic glycopeptides described herein are made by chemical modification of the a glycopeptide (Compound A, Compound B, Compound H or Compound C) or the 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; conversion of the amide group in amino acid-3 on these scaffolds to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring of these scaffolds to certain substituted amides. 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）或通过水解二糖而制备的单糖 在酸性介质中母体糖肽的氨基酸-4部分得到氨基酸-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; 这些支架上氨基酸-3中的酰胺基转化为各种酰基酰胺，酰基磺酰胺，酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将这些支架的大环上的酸部分转化为某些取代的酰胺。 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)
    4.
    发明申请
    BENZOXAZOLE CARBOXAMIDE INHIBITORS OF POLY(ADP-RIBOSE)POLYMERASE (PARP) 有权
    聚（ADP-RIBOSE）聚合酶（PARP）的苯并噻唑羧酰胺抑制剂

    公开(公告)号：US20090197863A1

    公开(公告)日：2009-08-06

    申请号：US12355692

    申请日：2009-01-16

    Applicant: Daniel Chu ,  Bing Wang

    Inventor： Daniel Chu ,  Bing Wang

    IPC: A61K31/422 ,  C07D263/54 ,  A61K31/423 ,  A61K31/496 ,  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。

    NOVEL SEMI-SYNTHETIC GLYCOPEPTIDES AS ANTIBACTERIAL AGENTS
    5.
    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：US20120252741A1

    公开(公告)日：2012-10-04

    申请号：US13440692

    申请日：2012-04-05

    Applicant: Daniel Chu ,  Tao Ye ,  Bing Wang

    Inventor： Daniel Chu ,  Tao Ye ,  Bing Wang

    IPC: A61K38/14 ,  A61P31/04 ,  C07K1/06 ,  C07K9/00

    CPC classification number: C07K9/006

    Abstract: Provided herein are semi-synthetic glycopeptides having antibacterial activity. The semi-synthetic glycopeptides described herein are made by chemical modification of a glycopeptide 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 with certain acyl groups; conversion of the amide group in amino acid-3 to various acylamide, acylsulfonamide, acylsulfonylurea derivatives; aminomethylation with substituent containing sulfonamide or acylsulfonamide group on amino acid-7 through Mannich reaction; and conversion of the acid moiety on the macrocyclic ring to certain substituted amides. Also provided herein are pharmaceutical compositions comprising the semi-synthetic glycopeptides, and methods of use of the semi-synthetic glycopeptides for the treatment and/or prophylaxis of diseases, especially bacterial infections.

    Abstract translation: 本文提供具有抗菌活性的半合成糖肽。 本文所述的半合成糖肽通过在酸性介质中水解母体糖肽的氨基酸-4的二糖部分而使糖肽进行化学修饰来制备，得到氨基酸-4单糖; 单糖转化为氨基糖衍生物; 用某些酰基酰化氨基酸4氨基取代的糖部分上的氨基取代基; 氨基酸-3中的酰胺基转化为各种酰基酰胺，酰基磺酰胺，酰基磺酰脲衍生物; 通过曼尼希反应在氨基酸-7上氨基甲基化与含有磺酰胺或酰基磺酰胺基团的取代基; 并将大环上的酸部分转化为某些取代的酰胺。 本文还提供了包含半合成糖肽的药物组合物，以及使用半合成糖肽来治疗和/或预防疾病，特别是细菌感染的方法。

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