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    • 5. 发明授权
    • pH 또는 환원 조건 민감성 리포좀 및 그 제조방법
    • 对于PH或还原条件敏感的脂肪酶及其制备方法
    • KR100853172B1
    • 2008-08-20
    • KR1020070033349
    • 2007-04-04
    • 포항공과대학교 산학협력단
    • 김기문박경민이돈욱정민선정현태고영호
    • C07D487/04A61K9/127
    • C07D487/04
    • A liposome formed by self-assembling of a cucurbituril derivative having a functional group which is sensitively cut off under acidic or reducing condition is provided to be stable in blood, be disintegrated after being absorbed into cells, allow a drug to be acted on a tissue of a desired target portion with preventing side effects of a systemic drug by encapsulating a target-oriented material into the cucurbituril derivative, thereby being used as a desirable drug delivery system. A liposome is formed by self-assembling of a cucurbituril derivative represented by a formula(1). In the formula(1), X is O, S or NH; each A1 and A2 is respectively OR^1, OR^2, or SR^1, SR^2. or NHR^1, NHR^2, wherein each R^1 and R^2 is independently a hydrophilic functional group which makes the compound of the formula(1) have amphiphilic property to form a liposome and is selected from the group consisting of C5-20 alkyl, C5-20 alkenyl, C5-20 alkynyl, C5-20 carbonylalkyl, C5-20 thioalkyl, C5-20 alkylthiol, C5-20 hydroxyalkyl, C5-20 alkylsilyl, C5-20 aminoalkyl, C5-20 cycloalkyl, C5-20 heterocycloalkyl, C5-20 arylalkyl and C5-20 heteroarylalkyl(wherein the alkyl, alkenyl or alkynyl is substituted by at least one hetero-atom selected from the group consisting of O, N and S, provided that a number of carbon atoms is higher than a number of substituted hetero-atoms, and the hydrophilic functional group is an amino acid or a peptide consisting of 2-10 amino acids, which may be substituted or unsubstituted with hexose or pentose); and n is an integer from 4 to 20. A method for preparing the liposome comprises the steps of: (a) drying a solution after dissolving the cucurbituril derivative of the formula(1) in an organic solvent; and (b) adding water to a dried compound obtained from the step(a) and dispersing it.
    • 提供通过在酸性或还原条件下敏感切断的具有官能团的葫芦素衍生物自组装形成的脂质体,使其在血液中稳定,在被细胞吸收后分解,使药物作用于组织 的预期目标部分,通过将目标取向材料包封在葫芦巴衍生物中,从而用作期望的药物递送系统,从而防止全身药物的副作用。 通过式(1)表示的葫芦素衍生物的自组装形成脂质体。 在式(1)中,X是O,S或NH; 每个A1和A2分别为OR ^ 1,OR ^ 2或SR ^ 1,SR ^ 2。 或NHR 1,NHR 2,其中每个R 1和R 2独立地是使式(1)的化合物具有两亲性以形成脂质体的亲水官能团,并且选自C5 -20烷基,C5-20烯基,C5-20炔基,C5-20羰基烷基,C5-20硫代烷基,C5-20烷基硫醇,C5-20羟基烷基,C5-20烷基甲硅烷基,C5-20氨基烷基,C5-20环烷基,C5 -20杂环烷基,C5-20芳基烷基和C5-20杂芳基烷基(其中烷基,烯基或炔基被至少一个选自O,N和S的杂原子取代,条件是碳原子数为 高于多个取代的杂原子,并且亲水性官能团是由2-10个氨基酸组成的氨基酸或肽,其可以被己糖或戊糖取代或未取代); n是4〜20的整数。脂质体的制造方法包括以下步骤:(a)将式(1)的葫芦巴衍生物溶解在有机溶剂中后,使其溶解; 和(b)向由步骤(a)获得的干燥化合物中加入水并将其分散。