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    • 7. 发明申请
    • CHEMICALLY MODIFIED SMALL MOLECULES
    • 化学改性的小分子
    • US20140303403A1
    • 2014-10-09
    • US14248245
    • 2014-04-08
    • Nektar Therapeutics
    • Michael D. BENTLEYTacey X. ViegasRichard R. GoodinLin ChengXuan Zhao
    • C07C41/24
    • A61K9/007A61K31/167A61K31/485A61K47/60C07C41/24
    • Methods of modifying the rate of systemic absorption of a drug administered to a subject by a pulmonary route, the method comprising covalently conjugating a hydrophilic polymer to a drug, wherein the drug has a half-life of elimination from the lung of less than about 180 minutes, to form a drug-polymer conjugate, wherein the drug-polymer conjugate has a net hydrophilic character and a weight average molecular weight of from about 50 to about 20,000 Daltons, and wherein the half-life of elimination from the lung of the drug-polymer conjugate is at least about 1.5-fold greater than the half-life of elimination from the lung of the drug, wherein the half-life of elimination from the lung is measured by bronchoalveolar lavage followed by assaying residual lung material.
    • 通过肺途径改变施用于受试者的药物的全身吸收速率的方法,所述方法包括将亲水性聚合物与药物共价共轭,其中所述药物具有从肺中消除的半衰期小于约180 分钟,以形成药物 - 聚合物缀合物,其中药物 - 聚合物缀合物具有净亲水特性和约50至约20,000道尔顿的重均分子量,并且其中从药物的肺中消除的半衰期 - 聚合物缀合物比从药物肺消除的半衰期大至少约1.5倍,其中通过支气管肺泡灌洗测量肺部消除的半衰期,然后测定残留的肺部材料。
    • 8. 发明申请
    • Dehalogenation process
    • 脱卤过程
    • US20060252968A1
    • 2006-11-09
    • US11417159
    • 2006-05-04
    • Ivan WlassicsVito Tortelli
    • Ivan WlassicsVito Tortelli
    • C07C41/24
    • C07C17/23C07C41/24C07C41/48C07C43/17C07D317/42C07C21/20C07C43/313
    • A process for obtaining vinyl compounds by dehalogenation of halofluorinated compounds having a linear, branched or cyclic structure, said halofluorinated compounds containing in the molecule at least one group: wherein Y1 and Y2, equal to or different from each other, are selected from Cl, Br, I; wherein the halofluorinated compounds are dehalogenated in the presence of a transition metal, or of transition metal couples, by operating in a biphasic system of solvents immiscible among each other, formed of a (per)fluorinated solvent and a dipolar aprotic or protic solvent (co-solvent), wherein the ratio moles co-solvent/equivalents of the halofluorinated compound ranges from 0.5 to 10, preferably from 0.5 to 5, still more preferably from 1 to 3.
    • 一种通过使具有直链,支链或环状结构的卤代氟化化合物脱卤获得乙烯基化合物的方法,所述卤代氟化物在分子中含有至少一个基团:其中Y 1和Y 2, 彼此相同或不同,选自Cl,Br,I; 其中所述卤代氟化合物在过渡金属或过渡金属偶存在下通过在彼此不混溶的溶剂的双相体系中操作而脱卤,由(一个)氟化溶剂和偶极非质子或质子溶剂(共 - 溶剂),其中所述卤化氟化合物的共溶剂/当量的摩尔比为0.5至10,优选0.5至5,还更优选1至3。