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    • 5. 发明申请
    • COMPOSITIONS THAT INCLUDE A HYDROPHOBIC COMPOUND AND A POLYAMINO ACID CONJUGATE
    • 包含疏水化合物和聚氨基酸共混物的组合物
    • WO2008141107A3
    • 2009-04-23
    • PCT/US2008063114
    • 2008-05-08
    • NITTO DENKO CORPVAN SANGSONG YUCHENGWANG XINGHEHOU ZHENGFENG ZHONGLINGZHAO GANGYU LEI
    • VAN SANGSONG YUCHENGWANG XINGHEHOU ZHENGFENG ZHONGLINGZHAO GANGYU LEI
    • A61K47/48A61K49/00A61K49/12A61K49/18A61P35/00
    • B82Y5/00A61K47/645A61K47/6925A61K49/0056A61K49/085A61K49/146A61K49/1824
    • Various compositions that include a hydrophobic compound and a polyamino acid conjugate are prepared. The compositions described herein are useful for a variety of drug, biomolecule, and imaging agent delivery applications. The inventors have discovered novel compositions that include a polymer conjugate, a first hydrophobic drug, and a second hydrophobic drug. The polymer conjugates of the compositions described herein are capable of conjugating to a number of agents, such as imaging agents, targeting agents, stabilizing agents and/or drugs. In some embodiments, the polymers and the resulting conjugates preferentially accumulate in certain tissues (e.g. tumor tissues) and/or certain receptors, and thus are useful for delivering drugs (e.g., anticancer drugs) and/or imaging agents to specific parts of the body (e.g., tumors). In some embodiments, the polymers described herein and the resulting conjugates can form nanoparticles that effectively solubilize the drug in an aqueous system by dispersing it at a molecular level, thus increasing the functionality and/or bioavailability of the drug.
    • 制备包括疏水化合物和聚氨基酸缀合物的各种组合物。 本文描述的组合物可用于各种药物,生物分子和成像剂递送应用。 发明人已经发现了包括聚合物缀合物,第一疏水性药物和第二疏水性药物的新型组合物。 本文所述组合物的聚合物缀合物能够与许多试剂(例如成像剂,靶向剂,稳定剂和/或药物)共轭。 在一些实施方案中,聚合物和所得的缀合物优先积聚在某些组织(例如肿瘤组织)和/或某些受体中,因此可用于将药物(例如抗癌药物)和/或成像剂递送至身体的特定部位 (例如肿瘤)。 在一些实施方案中,本文所述的聚合物和所得的共轭物可以形成纳米颗粒,其通过将其分散在分子水平上来有效地将药物溶解在水性体系中,从而增加药物的功能性和/或生物利用度。
    • 10. 发明申请
    • HYDROPHILIC POLYMERS WITH PENDANT FUNCTIONAL GROUPS AND METHOD THEREOF
    • 具有辅助功能组的亲水聚合物及其方法
    • WO2006124205A2
    • 2006-11-23
    • PCT/US2006015447
    • 2006-04-24
    • NITTO DENKO CORPVAN SANGYU LEI
    • VAN SANGYU LEI
    • C08G69/26A61K47/595A61K47/60C08G69/02
    • A polymer comprising a recurring unit of the formula (I) as defined herein is described. In the formula (I), X is selected from the group consisting of -(CH2CH2O)m-CH2CH2- and -CH2CH2CH2O-(CH2CH2O)m-CH2CH2CH2-, wherein m is an integer in the range of 1 to 100; Y is selected from the group consisting of -C*HCH2-, -C*HCH2CH2-, -C*H-NHC(=O)-CH2CH2-, -C*H-NHC(=O)-CH2CH2CH2-, -CH2CH2N*CH2CH2-, -CH2CH2CH2N* CH2CH2CH2-, C2 to C20 alkyl, and C6 to C20 aryl, wherein C* and N* represent atoms to which Z is bonded; and Z is selected from the group consisting of -NHR1, -NH-C(=O)-(CH2)nC(=O)NR1R2, -NH-C(=O)-(CH2)nC(=O)OR1, -(CH2)nC(=O)NR1R2, -(CH2)nC(=O)OR1, -(CH2)nC(=O)SR1, and -(CH2)nNR1R2, wherein n is an integer in the range of 1 to 3, wherein R1 and R2 are each independently selected from the group consisting of hydrogen, C1 to C20 alkyl, C6 to C20 aryl, anticancer drugs, peptides, antibody fragment, lactose, galactose, mannose, transferrin, magnetic resonance imaging agents, succinimyl, and alkali metal.
    • 描述了包含如本文所定义的式(I)的重复单元的聚合物。 在式(I)中,X选自 - (CH 2 CH 2 O)m -CH 2 CH 2 - 和-CH 2 CH 2 CH 2 O-(CH 2 CH 2 O)m -CH 2 CH 2 CH 2 - ,其中m是1至100的整数; Y选自-C * HCH 2 - , - C * HCH 2 CH 2 - , - C * H-NHC(= O)-CH 2 CH 2 - , - C * H-NHC(= O)-CH 2 CH 2 CH 2 - , - CH 2 CH 2 N * CH 2 CH 2 - , - CH 2 CH 2 CH 2 N * CH 2 CH 2 CH 2 - ,C 2至C 20烷基和C 6至C 20芳基,其中C *和N *表示与Z键合的原子; 并且Z选自-NHR1,-NH-C(= O) - (CH2)nC(= O)NR1R2,-NH-C(= O) - (CH2)nC(= O)OR1, - (CH2)nC(= O)NR1R2, - (CH2)nC(= O)OR1, - (CH2)nC(= O)SR1和 - (CH2)nNR1R2,其中n是1 3,其中R1和R2各自独立地选自氢,C1至C20烷基,C6至C20芳基,抗癌药物,肽,抗体片段,乳糖,半乳糖,甘露糖,转铁蛋白,磁共振成像剂,琥珀酰基 ,和碱金属。