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    • 4. 发明授权
    • Piperazine derivatives useful as CCR5 antagonists
    • 哌嗪衍生物可用作CCR5拮抗剂
    • US07825121B2
    • 2010-11-02
    • US11255643
    • 2005-10-21
    • Ragulan RamanathanAnima GhosalMichael W. MillerSwapan K. ChowdhuryKevin B. Alton
    • Ragulan RamanathanAnima GhosalMichael W. MillerSwapan K. ChowdhuryKevin B. Alton
    • A61K31/497A01N43/54C07D403/00C07D239/00
    • C07D401/14C07D401/06C07H17/02
    • The use of CCR5 antagonists of the formula or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, pyridyl, thiophenyl or naphthyl; R1 is hydrogen or alkyl; R2 is substituted phenyl, substituted heteroaryl, naphthyl, fluorenyl, diphenylmethyl or optionally substituted phenyl- or heteroaryl-alkyl; R3 is hydrogen, alkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, or optionally substituted phenyl, phenylalkyl, naphthyl, naphthylalkyl, heteroaryl or heteroarylalkyl; R4, R5 and R7 are hydrogen or alkyl; R6 is hydrogen, alkyl or alkenyl; for the treatment of HIV, solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis is disclosed, as well as novel compounds, pharmaceutical compositions comprising them, and the combination of CCR5 antagonists of the invention in combination with antiviral agents useful in the treatment of HIV or agents useful in the treatment of inflammatory diseases.
    • 使用下式的CCR5拮抗剂或其药学上可接受的盐,其中R是任选取代的苯基,吡啶基,噻吩基或萘基; R1是氢或烷基; R 2是取代的苯基,取代的杂芳基,萘基,芴基,二苯基甲基或任选取代的苯基或杂芳基 - 烷基; R 3是氢,烷基,烷氧基烷基,环烷基,环烷基烷基或任选取代的苯基,苯基烷基,萘基,萘基烷基,杂芳基或杂芳基烷基; R4,R5和R7是氢或烷基; R6是氢,烷基或烯基; 公开了用于治疗HIV,实体器官移植排斥,移植物抗宿主病,关节炎,类风湿性关节炎,炎症性肠病,特应性皮炎,牛皮癣,哮喘,过敏或多发性硬化的新型化合物,以及包含它们的药物组合物 ,以及本发明的CCR5拮抗剂与可用于治疗HIV的抗病毒剂或可用于治疗炎性疾病的药剂的组合。
    • 7. 发明授权
    • Electrospray ionization mass spectrometer with new features
    • 具有新功能的电喷雾电离质谱仪
    • US4977320A
    • 1990-12-11
    • US467978
    • 1990-01-22
    • Swapan K. ChowdhuryViswanatham KattaBrian T. Chait
    • Swapan K. ChowdhuryViswanatham KattaBrian T. Chait
    • H01J49/04H01J49/10
    • H01J49/0404H01J49/044H01J49/0468H01J49/165
    • An electrospray ion source is designed for ready and simple plugging into commercial mass analyzers for mass spectrometric analysis of organic molecules. The electrospray is carried out is the ambient air and the ions and other charged species enter the mass analyuzer through a long metal capillary tube and three stages of differential pumping. The use of the long tube allows (a) convenient injection of the ions into the mass analyzer (b) optimization of the spray by direct visualization in the air (c) efficient and controlled heat transfer to the droplets and (d) efficient pumping of the region between the capillary exit and the skinner. Desolvation of the solvated ions is carried out using a combination of controlled heat transfer to the charged droplets during the transit through the tube and collisional activation in a region of reduced pressure. Desolvation with this system does not involve use of a strong countercurrent flow of heated gas. The system also may be used to obtain the collisional activated fragmentation spectra of molecule ions. The use of a metal capillary tube avoids complications from charging that arise from the use of dielectric capilliary tubes.
    • 电喷雾离子源设计用于准备和简单的插入商业质量分析仪,用于有机分子的质谱分析。 进行电喷雾是环境空气,离子和其他带电物质通过长金属毛细管进入质量分析仪和三级差动泵送。 使用长管允许(a)方便地将离子注入质量分析器中(b)通过在空气中直接可视化来优化喷雾(c)有效和可控制的热传递到液滴,以及(d)有效泵送 毛细管出口与皮肤之间的区域。 溶剂化离子的去溶剂使用在通过管的运输过程中受控的热传递到带电液滴和在减压区域中的碰撞活化的组合来进行。 该系统的去溶剂不涉及使用强逆流的加热气体。 该系统也可用于获得分子离子的碰撞激活的碎裂光谱。 使用金属毛细管避免了使用电介质毛细管引起的充电并发症。