Semi-Synthetic Desmethyl-Vancomycin-Based Glycopeptides With Antibiotic Activity
    62.
    发明申请
    Semi-Synthetic Desmethyl-Vancomycin-Based Glycopeptides With Antibiotic Activity 审中-公开
    具有抗生素活性的半合成去甲基 - 万古霉素基糖肽

    公开(公告)号:US20090131304A1

    公开(公告)日:2009-05-21

    申请号:US12268364

    申请日:2008-11-10

    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。

    Antimicrobial derivatives
    64.
    发明申请
    Antimicrobial derivatives 审中-公开
    抗微生物衍生物

    公开(公告)号:US20050101548A1

    公开(公告)日:2005-05-12

    申请号:US10940900

    申请日:2004-09-13

    CPC classification number: C07H17/08

    Abstract: Antimicrobial compounds are provided having the formula (Q): as well as tautomers, stereoisomers, 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(Q)的抗微生物化合物:以及互变异构体,立体异构体,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; 和化合物的制备方法。

    Guanidino compounds
    67.
    发明授权
    Guanidino compounds 失效
    胍基化合物

    公开(公告)号:US06716840B2

    公开(公告)日:2004-04-06

    申请号:US10118730

    申请日:2002-04-08

    Abstract: Compounds having the general structure I are provided: X and Y are independently selected from the group consisting of CH2, N, NR9, C═O, C═S, S═O, SO2, S, O, (CR6R7)n, C(═O)—(CR6R7)n, and C(═S)—(CR6R7)n, where n is 1, 2, or 3. W is selected from the group consisting of and L is selected from the group consisting of N, O, S, S═O, SO2, C(O), NC(O), NC(S), OC(O), OC(S), C(NR10), C(NOR10), and a covalent bond. Z1, Z2, and Z3 are independently selected from the group consisting of substituted carbon and nitrogen. Compounds of formula I are agonists of the melanocortin-4 receptor (“MC-4r”) and therefore may have useful properties for controlling diseases related to MC-4r action in humans, such as obesity and type II diabetes.

    Abstract translation: 提供具有通式结构I的化合物:X和Y独立地选自CH 2,N,NR 9,C = O,C = S,S = O,SO 2,S,O, (R 6 R 7)n,C(= O) - (CR 6 R 7)n和C(= S) - (CR 6 R 7)n,其中n为1 W选自N,O,S,S = O,SO 2,C(O),NC(O),NC(S),OC (O),OC(S),C(NR 10),C(NOR 10))和共价键。 Z 1,Z 2和Z 3独立地选自取代的碳和氮。 式I化合物是黑皮质素-4受体(“MC-4r”)的激动剂,因此可能具有控制人类MC-4r作用相关疾病如肥胖和II型糖尿病的有用性质。

    ROSIN CORE ROLLED SMOKING PRODUCT METHOD AND DEVICES

    公开(公告)号:US20220264934A1

    公开(公告)日:2022-08-25

    申请号:US17179809

    申请日:2021-02-19

    Abstract: The embodiments disclose an apparatus for producing rosin core rolled smoking products, including a modular rosin core rolled smoking product apparatus assembly for automatically producing at least one rosin core rolled smoking product, at least one interchangeable packing and shaping subassembly for automatically packing and shaping user selected smoking materials, at least one interchangeable injection subassembly for automatically injecting a user selected rosin core material between two layers of smoking materials, at least one interchangeable insertion subassembly for inserting at least one tip coupled to the rosin core rolled smoking product, at least one paper wrapper application roller for rolling and adhering a paper wrapper around the at least one rosin core rolled smoking product, and a rosin core rolling apparatus app for remotely regulating the modular rosin core rolled smoking product apparatus assembly functions and operations.

    Benzoxazole carboxamide inhibitors of poly(ADP-ribose)polymerase (PARP)
    69.
    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

    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。

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