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    • 4. 发明授权
    • Methods for targeted drug delivery
    • 靶向药物递送方法
    • US07186399B2
    • 2007-03-06
    • US10302369
    • 2002-11-22
    • Gregory M. LanzaSamuel A. Wickline
    • Gregory M. LanzaSamuel A. Wickline
    • A61K5/055
    • A61K51/1217A61K49/18A61K49/1812G01N33/586
    • A method for ligand-based binding of lipid encapsulated particles to molecular epitopes on a surface in vivo or in vitro comprises sequentially administering (a) a site specific ligand activated with a biotin activating agent; (b) an avidin activating agent; and (c) lipid encapsulated particles activated with a biotin activating agent, whereby the ligand is conjugated to the particles through an avidin-biotin interaction and the resulting conjugate is bound to the molecular epitopes on such surface. The conjugate is effective for imaging by x-ray, ultrasound, magnetic resonance or positron emission tomography. Compositions for use in ultrasonic imaging of natural or synthetic surfaces and for enhancing the acoustic reflectivity thereof are also disclosed.
    • 在体内或体外,脂质包封的颗粒与表面上的分子表位的基于配体的结合的方法包括顺序施用(a)用生物素活化剂活化的位点特异性配体; (b)抗生物素蛋白活化剂; 和(c)用生物素活化剂活化的脂质包封的颗粒,由此配体通过抗生物素蛋白 - 生物素相互作用与颗粒缀合,并且所得到的缀合物结合到这种表面上的分子表位。 该共轭物通过X射线,超声,磁共振或正电子发射断层扫描成像是有效的。 还公开了用于天然或合成表面的超声成像和增强其声反射率的组合物。
    • 5. 发明授权
    • Chelating agents
    • 螯合剂
    • US6004529A
    • 1999-12-21
    • US833995
    • 1997-04-11
    • Shi-Bao YuJasbir Singh
    • Shi-Bao YuJasbir Singh
    • C07D233/14A61K49/00A61K49/04A61K49/08A61K51/00A61K51/04A61P35/00C07C323/59C07C323/60C07D213/52C07D213/53C09K3/00C07C319/00C07D213/04A61K5/055
    • A61K49/103A61K49/04A61K51/0478
    • The invention provides a complexant compound of formula IR.sup.3 S (CR.sup.1.sub.2).sub.n N(R.sup.2).sub.i (CR.sup.1.sub.2).sub.n X(CR.sup.1.sub.2).sub.n N(R.sup.2).sub.i (CR.sup.1.sub.2).sub.n SR.sup.3(I)(wherein each n, which may be the same or different, is an integer 2, 3 or 4 (preferably 2); each i, which may be the same or different, represents 0 or 1; each R.sup.3, which may be the same or different, is H or a thiol protecting group, preferably a protecting group; X is O, S, N, NR.sup.4 or a substituted phosphorus (eg. oxo substituted phosphorus), preferably S or N; each R.sup.4, which may be the same or different, is hydrogen or an optionally substituted organic group; each R.sup.1, which may be the same or different, is hydrogen or an optionally substituted organic group, or a moiety CR.sup.1.sub.2 may represents a carbonyl group or two, three or four R.sup.1 s on two different carbons together with those carbons and any intervening atoms may represent an optionally substituted saturated or unsaturated homocyclic or heterocyclic ring; and preferably, at least one CR.sup.1.sub.2 moiety is other than CH.sub.2 or CH(CH.sub.3)) or a salt or complex thereof, wherein optionally at least one of the R.sup.1, R.sup.2, R.sup.3 and R.sup.4 moieties is coupled directly or indirectly to a vector moiety.
    • 本发明提供式IR3S(CR12)nN(R2)i(CR12)nX(CR12)nN(R2)i(CR12)nSR3(I)的络合物,其中每个n可以相同或不同, 整数2,3或4(优选2);每个i可以相同或不同,表示0或1;每个R 3可以相同或不同,是H或硫醇保护基,优选保护基 基团; X是O,S,N,NR 4或取代的磷(例如氧代取代的磷),优选S或N;每个可以相同或不同的R 4是氢或任选取代的有机基团;每个R 1 可以相同或不同的是氢或任选取代的有机基团,或者部分CR 12可以表示羰基或两个不同碳上的两个,三个或四个R 1与那些碳原子一起并且任何中间原子可以代表任选地 取代的饱和或不饱和的杂环或杂环;并且优选地,至少一个CR 12部分不是CH 2或CH(CH 3))或 其盐或其复合物,其中任选地,R 1,R 2,R 3和R 4部分中的至少一个直接或间接连接到载体部分。