Use of synthetic polycationic amphiphilic substances with fatty acid or
hydrocarbon substituents as anti-sepsis agents
    1.
    发明授权
    Use of synthetic polycationic amphiphilic substances with fatty acid or hydrocarbon substituents as anti-sepsis agents 失效
    使用合成的阳离子两亲物质与脂肪酸或烃取代物作为抗脓毒剂

    公开(公告)号:US5998482A

    公开(公告)日:1999-12-07

    申请号:US188720

    申请日:1998-11-10

    IPC分类号: A61K31/16

    CPC分类号: A61K31/16

    摘要: The present invention describes the ability of synthetic cationic amphiphilic molecules to bind and sequester bacterial lipopolysaccharides and other microbial products that share structural and/or physical-chemical properties with those of LPS. Such cationic amphiphilic molecules have a molecular structure comprised of a linear or branched backbone derived from polymethylenes or alkylamines which bear at the termini two or more protonatable positively charged groups derived from primary-amino. imidazolinium, or N, N'-unsubstituted amidinium or guanidium functions. They also possess one or more lipophilic groups derived from fatty acids or hydrocarbon substituents, attached to the backbone via amide, ester, carbamate, or urethane linkages. The use of these compounds provide low cost, effective therapeutic method for the treatment of sepsis and septic shock.

    摘要翻译: 本发明描述了合成阳离子两亲分子结合和螯合细菌脂多糖和其它与LPS的结构和/或物理化学性质共享的微生物产物的能力。 这种阳离子两亲分子具有由衍生自聚亚甲基或烷基胺的直链或支链主链的分子结构,所述聚亚烷基或烷基胺在末端具有衍生自伯氨基的两个或多个可质子化带正电基团。 咪唑啉鎓或N,N'-未取代的脒鎓或胍的功能。 它们还具有一个或多个衍生自脂肪酸或烃取代基的亲油基团,其通过酰胺,酯,氨基甲酸酯或氨基甲酸酯键与骨架连接。 这些化合物的使用为治疗败血症和败血性休克提供了低成本,有效的治疗方法。

    TOLL-LIKE RECEPTOR-7 AND -8 MODULATORY 1H IMIDAZOQUINOLINE DERIVED COMPOUNDS
    2.
    发明申请
    TOLL-LIKE RECEPTOR-7 AND -8 MODULATORY 1H IMIDAZOQUINOLINE DERIVED COMPOUNDS 有权
    TOLL-LIKE受体-7和-8调节性1H缩水甘油衍生化合物

    公开(公告)号:US20120294885A1

    公开(公告)日:2012-11-22

    申请号:US13475284

    申请日:2012-05-18

    摘要: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

    摘要翻译: 本公开提供了新的咪唑并喹啉衍生的化合物,其衍生物,其类似物及其药学上可接受的盐,以及制备和使用这些化合物的方法。 本公开还提供TLR7激动剂和TLR7 / TLR8双重激动剂,探针,组织特异性分子,佐剂,免疫原性组合物,治疗组合物和自我佐剂疫苗,包括咪唑并喹啉衍生的化合物,其衍生物,其类似物和药学上可接受的盐 其中。 咪唑并喹啉衍生化合物的衍生物还包括咪唑并喹啉衍生化合物的树枝状大分子和二聚体,以及制备和使用树枝状和二聚咪唑并喹啉衍生化合物的方法。 本公开还提供了包含本发明的咪唑并喹啉衍生化合物的双重TLR2 / TLR7混合激动剂。

    Polyamines and their use as antibacterial and sensitizing agents
    6.
    发明申请
    Polyamines and their use as antibacterial and sensitizing agents 审中-公开
    多胺及其作为抗菌和敏化剂的用途

    公开(公告)号:US20070197658A1

    公开(公告)日:2007-08-23

    申请号:US11709425

    申请日:2007-02-22

    IPC分类号: A61K31/16 A61K31/13

    摘要: Polyamines with varying chain-lengths were evaluated for antimicrobial activity in order to test the hypothesis that these bis-cationic amphipathic compounds may also bind to and permeabilize intact Gram negative bacterial membranes. The compounds were found to possess significant antimicrobial activity and mediated via permeabilization of bacterial membranes. Homologated spermine, bis-acylated with C8 or C9 chains was found to profoundly sensitize E. coli to hydrophobic antibiotics such as rifampicin.

    摘要翻译: 评估具有不同链长度的多胺以测定抗微生物活性,以测试这些双阳离子两亲化合物也可以结合完整的革兰氏阴性细菌膜并使其透化的假说。 发现这些化合物具有显着的抗微生物活性并通过细菌膜的透化介导。 发现用C 8 N或C 9链双酰化的同系精胺使大肠杆菌对例如利福平的疏水性抗生素敏感。

    Toll-like receptor-7 and -8 modulatory 1H imidazoquinoline derived compounds
    8.
    发明授权
    Toll-like receptor-7 and -8 modulatory 1H imidazoquinoline derived compounds 有权
    Toll样受体-7和-8调节性1H咪唑并喹啉衍生化合物

    公开(公告)号:US08728486B2

    公开(公告)日:2014-05-20

    申请号:US13475284

    申请日:2012-05-18

    摘要: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

    摘要翻译: 本公开提供了新的咪唑并喹啉衍生的化合物,其衍生物,其类似物及其药学上可接受的盐,以及制备和使用这些化合物的方法。 本公开还提供TLR7激动剂和TLR7 / TLR8双重激动剂,探针,组织特异性分子,佐剂,免疫原性组合物,治疗组合物和自我佐剂疫苗,包括咪唑并喹啉衍生的化合物,其衍生物,其类似物和药学上可接受的盐 其中。 咪唑并喹啉衍生化合物的衍生物还包括咪唑并喹啉衍生化合物的树枝状大分子和二聚体,以及制备和使用树枝状和二聚咪唑并喹啉衍生化合物的方法。 本公开还提供了包含本发明的咪唑并喹啉衍生化合物的双重TLR2 / TLR7混合激动剂。