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    SILYL ETHERIFIED DERIVATIVES OF 5-AZACYTIDINES IN CARBOHYDRATE MOIETY
    1.
    发明申请
    SILYL ETHERIFIED DERIVATIVES OF 5-AZACYTIDINES IN CARBOHYDRATE MOIETY 有权

    公开(公告)号：US20170304337A1

    公开(公告)日：2017-10-26

    申请号：US15355315

    申请日：2016-11-18

    申请人： OHARA PHARMACEUTICAL CO., LTD.

    发明人： Magoichi SAKO ,  Shinpei SUGIYAMA

    IPC分类号： A61K31/706

    CPC分类号： A61K47/549 ,  A61K31/706 ,  A61K47/48023 ,  C07H19/12

    摘要： The present invention relates to a prodrug of 5-azacytidine or 2′-deoxy-5-azacytidine having remarkable stability against cytidine deaminase, a metabolic hydrolyzing enzyme in replacement of current injections (5-azacytidine or 2′-deoxy-5-azacytidine) which are clinically used as therapeutic agents for various myelomas including myelodysplastic syndrome. The present invention provides a compound represented by formula (1), or salt thereof, wherein, R is OR3 or a hydrogen atom, R1, R2, and R3 are each independently hydrogen atom or silyl group represented by formula (2): wherein, R1, R5, and R6 are each independently alkyl group which may have a substituent, aryl group which may have a substituent, or arylalkyl group which may have a substituent, with the provision that R1, R2, and R3 are not hydrogen atom simultaneously.

    Light-enabled drug delivery
    4.
    发明授权
    Light-enabled drug delivery 有权
    光启用药物递送

    公开(公告)号：US09364551B2

    公开(公告)日：2016-06-14

    申请号：US14347656

    申请日：2012-09-28

    申请人： Virginia Commonwealth University

    发明人： Matthew Hartman ,  Martin Michael Dcona ,  Deboleena Mitra

    IPC分类号： A61K38/00 ,  C07K2/00 ,  A61K47/48 ,  A61K41/00 ,  A61K31/704 ,  A61N5/06

    CPC分类号： A61K47/48023 ,  A61K31/704 ,  A61K41/0042 ,  A61K47/54 ,  A61K47/62 ,  A61K47/65 ,  A61N5/062

    摘要： Conjugates are provided which comprise a membrane permeable drug linked to a moiety that is not membrane permeable. Attachment of the moiety that is not membrane permeable prevents the drug from crossing cell membranes and entering cells. However, exposure to light either i) breaks the linkage, releasing the drug and allowing it to enter cells; or ii) converts the non-membrane permeable moiety to a membrane permeable form, allowing the entire conjugate to enter the cell, where the drug is released from the conjugate by cleavage. The membrane permeable drugs are thus delivered to cells at locations of interest, e.g. cancer cells in a tumor, in a temporally and spatially controlled manner.

    摘要翻译： 提供了缀合物，其包含连接到不透膜的部分的膜可渗透药物。 不透膜部分的附着防止药物穿过细胞膜并进入细胞。 然而，暴露于光，或者i）断开连接，释放药物并使其进入细胞; 或ii）将非膜可渗透部分转化为膜可渗透形式，允许整个缀合物进入细胞，其中药物通过切割从缀合物释放。 因此，膜渗透性药物被递送到感兴趣的位置的细胞，例如， 肿瘤中的癌细胞，以时间和空间方式控制。

    High penetration prodrug compositions of retinoids and retinoid-related compounds
    7.
    发明授权
    High penetration prodrug compositions of retinoids and retinoid-related compounds 有权
    类维生素A和类视黄醇相关化合物的高渗透前药组合物

    公开(公告)号：US09193672B2

    公开(公告)日：2015-11-24

    申请号：US12503739

    申请日：2009-07-15

    申请人： Chongxi Yu

    发明人： Chongxi Yu

    IPC分类号： A61K31/24 ,  A61K31/20 ,  A61K31/19 ,  A61K31/22 ,  A61K31/15 ,  A61K31/13 ,  C12Q1/02 ,  A61P17/00 ,  A61P27/02 ,  A61P35/04 ,  C07C219/10

    CPC分类号： A61K47/48023 ,  A61K31/21 ,  A61K31/215 ,  A61K31/216 ,  A61K31/221 ,  A61K31/4453 ,  A61K47/54 ,  C07C219/10 ,  C07C2601/16 ,  C07C2602/10 ,  G01N33/502

    摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of retinoids and retinoid-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

    摘要翻译： 本发明提供了能够穿过具有高穿透效率的生物屏障的类视黄醇和类视黄醇相关化合物的新型高渗透组合物（HPC）或高渗透前药（HPP）的组合物。 HPP在穿过生物屏障后能够转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

    Silicon-Containing Fumaric Acid Esters
    9.
    发明申请
    Silicon-Containing Fumaric Acid Esters 有权
    含硅富马酸酯

    公开(公告)号：US20140336151A1

    公开(公告)日：2014-11-13

    申请号：US14363546

    申请日：2012-12-14

    申请人： Biogen Idec MA Inc.

    发明人： Jianhua Chao

    IPC分类号： A61K47/48 ,  C07F7/08 ,  C07F7/18

    CPC分类号： A61K47/48023 ,  A61K47/54 ,  C07F7/0836 ,  C07F7/1804 ,  C07F7/1896

    摘要： The present invention is directed to silicon-containing fumaric acid esters of the Formulae I-IV. The silicon-containing fumaric acid esters of Formulae I-IV are useful in transplantation medicine and for the treatment of autoimmune diseases and autoimmune-related diseases. (I), (II), (III) & (IV)

    摘要翻译： 本发明涉及式I-IV的含硅富马酸酯。 式I-IV的含硅富马酸酯可用于移植医学和用于治疗自身免疫疾病和自身免疫相关疾病。 （I），（II），（III）和（IV）

    HALOGENATED PHENOLS FOR DIAGNOSTICS, ANTIOXIDANT PROTECTION AND DRUG DELIVERY
    10.
    发明申请
    HALOGENATED PHENOLS FOR DIAGNOSTICS, ANTIOXIDANT PROTECTION AND DRUG DELIVERY 审中-公开
    用于诊断，抗氧化剂保护和药物输送的氢化酚

    公开(公告)号：US20140135397A1

    公开(公告)日：2014-05-15

    申请号：US14159893

    申请日：2014-01-21

    申请人： Keith R. Latham

    发明人： Keith R. Latham

    IPC分类号： A61K47/48

    CPC分类号： A61K47/48023 ,  A61K49/006 ,  A61K49/0438 ,  A61K51/0446 ,  C07C43/295 ,  C07C217/60 ,  C07C229/36 ,  C07C233/25 ,  C07C323/52 ,  C07D209/36 ,  C07D475/08 ,  C07D489/02 ,  C07D499/897 ,  C07J1/0022 ,  C07J5/0053 ,  G01N33/52 ,  Y10T436/145555

    摘要： The present invention provides compositions and methods for the targeted delivery, release and/or formation of a drug compound at a target site(s) within the body of an individual, such as a diseased and/or inflamed tissue in the body of the individual. These compositions may comprise a halogenated phenol ring cleavably linked to a core structure of a drug compound. Due to the variety of substituents that may be utilized in forming the different types of linkages, numerous examples of drug compounds linked to a halogenated phenol ring are proposed. The present invention further provides compositions comprising halogenated phenol starting compounds that do not undergo cleavage during a dehalogenation reaction to form a drug compound in a targeted tissue when administered to an individual. Methods of administering these non-cleaving compounds are further provided.

    摘要翻译： 本发明提供用于在个体体内的目标部位（例如个体体内的患病和/或发炎的组织）靶向递送，释放和/或形成药物化合物的组合物和方法 。 这些组合物可以包含与药物化合物的核心结构可分离连接的卤代苯酚环。 由于可用于形成不同类型的键的多种取代基，提出了与卤代酚环连接的药物化合物的许多实例。 本发明进一步提供包含卤代苯酚起始化合物的组合物，其在给予个体时在脱卤反应期间不会在靶组织中形成药物化合物时进行裂解。 还提供了施用这些非切割化合物的方法。