Polypeptide thin film from amphiphilic compounds
    1.
    发明授权
    Polypeptide thin film from amphiphilic compounds 失效
    来自两亲化合物的多肽薄膜

    公开(公告)号:US5095090A

    公开(公告)日:1992-03-10

    申请号:US507540

    申请日:1992-04-11

    IPC分类号: C07K14/00 C08G69/10

    摘要: A polypeptide thin film obtained by polymerizing a monomolecular film comprising a monomer mixture of(a) an amphiphilic compound having a hydrophobic moiety and a hydrophilic moiety having an amino acid ester structure per molecule, the conjugated acid of the elimination group of the ester having a pKa of not higher than 14, and(b) an amphiphilic compound having two amino groups per molecule or an amphiphilic compound having two ester structures per molecule, the conjugated acid of the elimination group of the ester having a pKa of not higher than 16,or a built-up film of the monomolecular film; and a process for preparing a material carrying the polypeptide thin film.

    摘要翻译: 通过使包含单体混合物(a)具有疏水部分的两亲性化合物和每分子具有氨基酸酯结构的亲水部分的单体混合物聚合获得的多肽薄膜,所述酯的消除基团的共轭酸具有 pKa不高于14,和(b)每分子具有两个氨基的两亲化合物或每分子具有两个酯结构的两亲化合物,所述酯的消除基团的共轭酸的pKa不高于16, 或单分子膜的叠层膜; 以及制备携带多肽薄膜的材料的方法。

    Polypeptide thin film
    2.
    发明授权
    Polypeptide thin film 失效
    多肽薄膜

    公开(公告)号:US5198224A

    公开(公告)日:1993-03-30

    申请号:US614484

    申请日:1990-11-16

    摘要: A polypeptide thin film produced by polymerizing a monomolecular film or a built-up film comprising an amphipatic phospholipid compound, wherein the amphipatic phospholipid compound has a hydrophobic portion and a hydrophilic portion having an amino acid ester structure in the molecule, the amino acid ester structure containing a splitting-off group with a pKa value of the conjugated acid thereof being 16 or below.

    摘要翻译: 通过聚合单分子膜或包含两性磷脂化合物的叠层膜制备的多肽薄膜,其中所述两性磷脂化合物在分子中具有疏水部分和具有氨基酸酯结构的亲水部分,所述氨基酸酯结构 含有共轭酸的pKa值为16以下的剥离基。

    Surface-modifiable liposome and process for producing surface-modified
liposome
    3.
    发明授权
    Surface-modifiable liposome and process for producing surface-modified liposome 失效
    表面改性脂质体和生产表面改性脂质体的方法

    公开(公告)号:US5190822A

    公开(公告)日:1993-03-02

    申请号:US687799

    申请日:1991-04-19

    摘要: A surface-modifiable liposome comprising a compound represented by formula (I) or (II): ##STR1## and a lipid capable of forming a liposome, wherein R.sub.1 represents a hydrophobic group;R.sub.2 and R.sub.3 represent each an organic group including a hydrogen atom) R.sub.2 and R.sub.3 optionally combined with each other to form a double bond or a ring;X and Y each represents an oxygen atom or a sulfur atom; R.sub.2 ' and R.sub.3 ' each represents a hydrogen atom or an organic group; W represents a linking group; n represents 0 or 1; and Z represents a hydrophilic group;and a process for producing a surface-modified liposome by using the surface-modifiable liposome.

    摘要翻译: 包含由式(I)或(II)表示的化合物:能够形成脂质体的脂质的表面改性脂质体,其中R1表示疏水基团; R2和R3各自表示包含氢原子的有机基团)R 2和R 3彼此相互结合以形成双键或环; X和Y各自表示氧原子或硫原子; R2'和R3'各自表示氢原子或有机基团; W表示连接基团; n表示0或1; Z表示亲水基团; 以及通过使用表面改性脂质体制造表面改性脂质体的方法。

    Polypeptide thin film
    4.
    发明授权
    Polypeptide thin film 失效
    多肽薄膜

    公开(公告)号:US5138026A

    公开(公告)日:1992-08-11

    申请号:US480699

    申请日:1990-02-15

    IPC分类号: C08G69/10

    摘要: A polypeptide thin film obtained by polymerizing a monomolecular film comprising an amphiphilic compound having a hydrophobic moiety and a hydrophilic moiety having an amino acid ester structure per molecule, the conjugated acid of the elimination group of said ester having a pKa of not higher than 14, or a built-up film of said monomolecular film; and a process for preparing a material on which said polypeptide thin film is carried.

    摘要翻译: 通过聚合包含具有疏水部分的两亲化合物和每分子具有氨基酸酯结构的亲水部分的单分子膜,所述酯的消除基团的共轭酸的pKa不高于14,获得的多肽薄膜, 或所述单分子膜的叠层膜; 以及制备其上携带所述多肽薄膜的材料的方法。

    PACLITAXEL ENHANCER COMPOUNDS
    9.
    发明申请
    PACLITAXEL ENHANCER COMPOUNDS 审中-公开
    PACLITAXEL增强化合物

    公开(公告)号:US20100280075A1

    公开(公告)日:2010-11-04

    申请号:US12692895

    申请日:2010-01-25

    摘要: Disclosed is a compound represented by the Structural Formula (I): Y is a covalent bond, a phenylene group or a substituted or unsubstituted straight chained hydrocarbyl group. In addition, Y, taken together with both >C═Z groups to which it is bonded, is a substituted or unsubstituted aromatic group. Preferably, Y is a covalent bond or —C(R7R8)—.R1 and R2 are independently an aryl group or a substituted aryl group, R3 and R4 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R5-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aryl group or a substituted aryl group.R7 and Rg are each independently —H, an aliphatic or substituted aliphatic group, or R7 is —H and Rg is a substituted or unsubstituted aryl group, or, R7 and R8, taken together, are a C2-C6 substituted or unsubstituted alkylene group.Z is ═O or ═S.Also disclosed are pharmaceutical compositions comprising the compound of the present invention and a pharmaceutically acceptable carrier or diluent.Also disclosed is a method of treating a subject with cancer by administering to the subject a compound of Structural Formula (I) in combination with Paclitaxel or an analog of Paclitaxel.

    摘要翻译: 公开了由结构式(I)表示的化合物:Y是共价键,亚苯基或取代或未取代的直链烃基。 此外,Y与它所键合的两个> C = Z基团一起是取代或未取代的芳族基团。 优选Y为共价键或-C(R 7 R 8) - 。 R 1和R 2独立地是芳基或取代的芳基,R 3和R 4独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R5-R6独立地是-H,脂族基团,取代的脂族基团,芳基或取代的芳基。 R7和Rg各自独立地为-H,脂族或取代的脂族基团,或R7为-H,Rg为取代或未取代的芳基,或者R7和R8一起为C2-C6取代或未取代的亚烷基 。 Z为═O或═S。 还公开了包含本发明化合物和药学上可接受的载体或稀释剂的药物组合物。 还公开了通过向受试者施用结合式(I)的化合物与紫杉醇或紫杉醇的类似物组合来治疗患有癌症的受试者的方法。