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    • 2. 发明授权
    • Compositions and methods for double-targeting virus infections and targeting cancer cells
    • 用于双向靶向病毒感染和靶向癌细胞的组合物和方法
    • US08138200B2
    • 2012-03-20
    • US12629387
    • 2009-12-02
    • Louis S. KuceraRonald A. FlemingKhalid S. IshaqGregory L. KuceraSusan L. Morris-Natschke
    • Louis S. KuceraRonald A. FlemingKhalid S. IshaqGregory L. KuceraSusan L. Morris-Natschke
    • A01N43/42A61K31/44
    • C07H19/06A61K31/66A61K31/675C07F9/10C07H19/10C07H19/16Y02A50/463
    • The invention includes compositions and methods useful for treatment of a virus infection in a mammal by double-targeting the virus (i.e. targeting the virus at more than one stage of the virus life cycle) and thereby inhibiting virus replication. The compositions of the invention include compounds which comprise a phosphocholine moiety covalently conjugated with one or more antiviral agents (e.g. nucleoside analogue, protease inhibitor, etc.) to a lipid backbone. The invention also includes pharmaceutical compositions and kits for use in treatment of a virus infection in mammals. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to treat the infection, to a mammal infected with a virus. Additionally, the invention includes compositions and methods useful for combating a cancer in a mammal and for facilitating delivery of a therapeutic agent to a mammalian cell. The compositions of the invention include compounds which comprise an alkyl lipid or phospholipid moiety covalently conjugated with an anticancer agent (e.g. a nucleoside analogue). The invention also includes pharmaceutical compositions and kits for combating a cancer and for facilitating delivery of a therapeutic agent to a mammalian cell. The methods of the invention comprise administering a compound of the invention, a pharmaceutically acceptable salt thereof, or a pharmaceutical composition of the invention, in an amount effective to combat a cancer or to facilitate delivery of a therapeutic agent to a mammalian cell.
    • 本发明包括通过双重靶向病毒(即在病毒生命周期的多于一个阶段靶向病毒)并因此抑制病毒复制而用于治疗哺乳动物病毒感染的组合物和方法。 本发明的组合物包括包含与一种或多种抗病毒剂(例如核苷类似物,蛋白酶抑制剂等)共价结合到脂质主链的磷酸胆碱部分的化合物。 本发明还包括用于治疗哺乳动物病毒感染的药物组合物和试剂盒。 本发明的方法包括将治疗感染的本发明化合物,其药学上可接受的盐或本发明的药物组合物给予感染病毒的哺乳动物。 另外,本发明包括可用于对抗哺乳动物中的癌症并促进治疗剂递送至哺乳动物细胞的组合物和方法。 本发明的组合物包括包含与抗癌剂(例如核苷类似物)共价缀合的烷基脂质或磷脂部分的化合物。 本发明还包括用于对抗癌症并促进治疗剂递送至哺乳动物细胞的药物组合物和试剂盒。 本发明的方法包括给予本发明的化合物,其药学上可接受的盐或本发明的药物组合物,其量有效地抵抗癌症或促进治疗剂递送至哺乳动物细胞。
    • 7. 发明授权
    • Blood-pool carrier for lipophilic imaging agents
    • 用于亲脂显像剂的血液池载体
    • US07582279B2
    • 2009-09-01
    • US10692311
    • 2003-10-23
    • Raymond E. CounsellMarc A. LonginoJamey P. Weichert
    • Raymond E. CounsellMarc A. LonginoJamey P. Weichert
    • A61K51/00A61M36/14
    • A61K49/0461A61K9/1075A61K9/1275A61K49/0433A61K49/1806A61K51/0406A61K51/0478A61K51/1217B82Y5/00Y10S514/938Y10S977/829Y10S977/905Y10S977/927Y10S977/93
    • A surface-modified lipoprotein-like oil-in-water emulsion useful as a blood-pool selective delivery vehicle for lipophilic imaging agents or lipophilic derivatives of water-soluble imaging agents. The blood-pool selective delivery vehicle remains in the blood for several hours, shows very little early hepatic sequestration, and is cleared from the blood within 24 hours. The mean diameter of the oil phase is less than 150 nm which minimizes sequestration by the reticuloendothelial system. The surface of the oil phase is modified with a polyethyl glycol-modified phospholipid to prevent normal interactions with the receptor sites of the hepatocytes. In radiographic imaging, radioactive or stable, synthetic or semi-synthetic polyhalogenated triglycerides, such as 2-oleoylglycerol-1,3-bis[7-(3-amino-2,4,6-triiodophenyl)heptanoate], or lipid soluble derivatives of traditional water-soluble contrast agents, such as aliphatic esters of iopanoic, diatrizoic, and acetrizoic acid, may be incorporated into the lipophilic core of a lipoprotein-like emulsion particle.
    • 用作脂溶性成像剂或水溶性成像剂的亲脂性衍生物的血液池选择性递送载体的表面改性脂蛋白样水包油乳液。 血液池选择性输送载体在血液中保持数小时,显示出非常少的早期肝脏螯合,并在24小时内从血液中清除。 油相的平均直径小于150nm,其最小化网状内皮系统的螯合。 用聚乙二醇修饰的磷脂修饰油相的表面以防止与肝细胞的受体位点的正常相互作用。 放射摄影成像中,放射性或稳定的合成或半合成多卤甘油三酸酯如2-油酰甘油-1,3-双[7-(3-氨基-2,4,6-三碘苯基)庚酸酯]或脂溶性衍生物 的传统的水溶性造影剂,如碘,脂肪族和代谢酸的脂肪族酯可以并入脂蛋白样乳液颗粒的亲脂性核心中。