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    CELL-PENETRATING, GUANIDINIUM-RICH OLIGOPHOSPHOTRIESTERS FOR DRUG AND PROBE DELIVERY
    44.
    发明申请
    CELL-PENETRATING, GUANIDINIUM-RICH OLIGOPHOSPHOTRIESTERS FOR DRUG AND PROBE DELIVERY 审中-公开
    用于药物和探针递送的细胞渗透，富含胍类化合物的寡核苷酸

    公开(公告)号：WO2017083637A1

    公开(公告)日：2017-05-18

    申请号：PCT/US2016/061515

    申请日：2016-11-11

    Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITY

    Inventor： MCKINLAY, Colin J. ,  WENDER, Paul A. ,  WAYMOUTH, Robert M.

    IPC: A61K47/48 ,  A61K48/00 ,  C07H21/00

    CPC classification number: A61K48/00 ,  C07F9/091 ,  C07F9/65512

    Abstract: Guanidinium-rich oligophosphotriesters transporter compounds and methods of making and using the same are provided. Also provided are pharmaceutical compositions that include the subject transporter compounds, where the transporter can be joined to a cargo of interest, and is formulated with a pharmaceutically acceptable excipient. Formulations may be provided in a unit dose, where the dose provides an amount of the compound effective to afford a desired therapeutic effect. Methods of using the subject transporter compounds to deliver a cargo moiety to a cell are provided, where the method can include contacting a target cell with the transporter compound. The subject methods can be performed in vitro or in vivo.

    Abstract translation: 提供了含胍丰富的寡磷酸三酯转运蛋白化合物及其制备和使用方法。 还提供了包含主题转运蛋白化合物的药物组合物，其中转运蛋白可以连接到感兴趣的货物上，并且与药学上可接受的赋形剂一起配制。 制剂可以以单位剂量提供，其中剂量提供有效提供所需治疗效果的量的化合物。 提供了使用主题转运蛋白化合物将货物部分递送至细胞的方法，其中该方法可以包括使靶细胞与转运蛋白化合物接触。 主题方法可以在体外或体内进行。

    HYDROPHOBIC TAXANE DERIVATIVES
    46.
    发明申请
    HYDROPHOBIC TAXANE DERIVATIVES 审中-公开
    疏水性TAXANE衍生物

    公开(公告)号：WO1996021658A1

    公开(公告)日：1996-07-18

    申请号：PCT/US1996000351

    申请日：1996-01-11

    Applicant: THE LIPOSOME COMPANY, INC.

    Inventor： THE LIPOSOME COMPANY, INC. ,  MAYHEW, Eric ,  FRANKLIN, J., Craig ,  BHATIA, Suresh ,  HARMON, Paul, A. ,  JANOFF, Andrew, S.

    IPC: C07D305/14

    CPC classification number: B82Y5/00 ,  A61K9/127 ,  C07D305/14 ,  C07F9/65512

    Abstract: This invention provides a taxane derivative of formula (I), wherein a hydrophobic organic moiety is attached to a taxane. R and R is each independently H or a hydrophobic organic moiety, as long as at least one of R and R is not H. Attachment of a hydrophobic organic moiety to the taxane so as to obtain a taxane derivative generally stabilizes the association of the derivative with a lipid, including a liposomal lipid, carrier in the plasma of animals to which the derivative-carrier association is administered. Also provided herein is a composition containing the taxane derivative and a pharmaceutically acceptable medium; desirably, the medium also contains a lipid carrier, and the derivative is associated with the carrier. Further provided herein is a method of administering taxane derivatives to animals, for example, animals afflicted with cancers.

    Abstract translation: 本发明提供式（I）的紫杉烷衍生物，其中疏水性有机部分连接于紫杉烷。 R和R 1各自独立地为H或疏水性有机部分，只要R和R 1中的至少一个不为H.将疏水性有机部分连接到紫杉烷以获得一般的紫杉烷衍生物 稳定衍生物与携带衍生物 - 载体缔合的动物血浆中的脂质（包括脂质体脂质）载体的缔合。 本文还提供含有紫杉烷衍生物和药学上可接受的介质的组合物; 理想地，培养基还含有脂质载体，并且该衍生物与载体相关。 本文还提供了将紫杉烷衍生物施用于动物，例如患有癌症的动物的方法。

    CHEMILUMINESCENT 3-(SUBSTITUTED ADAMANT-2'-YLIDENE) 1,2-DIOXETANES
    47.
    发明申请
    CHEMILUMINESCENT 3-(SUBSTITUTED ADAMANT-2'-YLIDENE) 1,2-DIOXETANES 审中-公开
    亮氨酸3-（取代的ADAMANT-2'-YLIDENE）1,2-二氧化物

    公开(公告)号：WO1992004341A1

    公开(公告)日：1992-03-19

    申请号：PCT/US1991006096

    申请日：1991-08-30

    Applicant: TROPIX, INC. ,  BRONSTEIN, Irena ,  EDWARDS, Brooks ,  JUO, Rouh-Rong

    Inventor： TROPIX, INC.

    IPC: C07D321/00

    CPC classification number: C12Q1/34 ,  C07C43/1788 ,  C07C43/196 ,  C07C2603/74 ,  C07D321/00 ,  C07F9/12 ,  C07F9/65512

    Abstract: Enzymatically cleavable chemiluminescent 1,2-dioxetane compounds capable of producing light energy when decomposed, substantially stable at room temperature before a bond by which an enzymatically cleavable labile substituent thereof is intentionally cleaved, are disclosed. These compounds can be represented by formula (I) wherein X and X each represent, individually, hydrogen, a hydroxyl group, a halo substituent, an unsubstituted lower alkyl group, a hydroxy (lower) alkyl group, a halo (lower) alkyl group, a phenyl group, a halophenyl group, an alkoxyphenyl group, a hydroxyalkoxy group, a cyano group, a carboxyl or substituted carboxyl group or an amide group, with at least one of X and X being other than hydrogen; and R1 and R2 individually or together, represent an organic substituent that does not interfere with the production of light when the dioxetane compound is enzymatically cleaved and that satisfies the valence of the dioxetane compound's 4-carbon atom, with the provisos that if R1 and R2 represent individual substituents the R2 substituent is aromatic, heteroaromatic, or an unsaturated substituent in conjugation with an aromatic ring, and that at least one of R1 and R2 is, or R1 and R2 taken together are, an enzymatically cleavable labile group-substituted fluorescent chromophore group that produces a luminescent substance when the enzymatically cleavable labile substituent thereof is removed by an enzyme. The corresponding dioxetanes which, instead of being substituted at the 5' or 7', or at the 5' and 7' positions, instead contain a 4' methylene group, are also disclosed, as are intermediates for all these 3-substituted adamant-2'-ylidenedioxetanes, and their use as reporter molecules in assays.

    Abstract translation: 公开了能够在分解时产生光能的酶促切割的化学发光的1,2-二氧杂环丁烷化合物，在其中有可能切割其可酶切的不稳定取代基的键之间在室温下基本稳定。 这些化合物可以由式（I）表示，其中X和X 1各自表示氢，羟基，卤素取代基，未取代的低级烷基，羟基（低级）烷基，卤代（低级） ）烷基，苯基，卤代苯基，烷氧基苯基，羟基烷氧基，氰基，羧基或取代的羧基或酰胺基，X和X 1中的至少一个不同于氢 ; R1和R2分别或一起表示当二氧杂环丁烷化合物被酶解时不干扰光的产生并且满足二氧杂环丁烷化合物的4-碳原子的化合价的有机取代基，条件是如果R1和R2 代表各个取代基，R 2取代基是芳族的，杂芳族的，或与芳香环共轭的不饱和取代基，R1和R2中的至少一个是或R1和R2一起是可酶切割的不稳定基团取代的荧光发色团 当其酶促切割不稳定取代基被酶除去时产生发光物质的组。 也公开了相对于在5'或7'或5'和7'位置取代含有4'亚甲基的二氧杂环丁烷，以及所有这些3-取代的金刚烷基 - 2'-亚基二氧杂环丁烷，以及它们在测定中作为报道分子的用途。

    IMPROVED METHODS OF USING CHEMILUMINESCENT 1,2-DIOXETANES
    48.
    发明申请
    IMPROVED METHODS OF USING CHEMILUMINESCENT 1,2-DIOXETANES 审中-公开
    改进使用亮氨酸1,2-二氧化物的方法

    公开(公告)号：WO1990000168A1

    公开(公告)日：1990-01-11

    申请号：PCT/US1989002792

    申请日：1989-06-28

    Applicant: TROPIX, INC.

    Inventor： TROPIX, INC. ,  BRONSTEIN, Irena, Y. ,  VOYTA, John, C.

    IPC: C07D305/04

    CPC classification number: C07C43/196 ,  C07C69/00 ,  C07C2603/00 ,  C07C2603/74 ,  C07D321/00 ,  C07F9/12 ,  C07F9/65512 ,  C07F9/65742 ,  C07H15/203 ,  C07H15/26 ,  C12Q1/34 ,  G01N21/76 ,  G01N33/533 ,  G01N33/535 ,  G01N33/581 ,  G01N33/582 ,  G01N33/76 ,  Y10S435/968 ,  Y10S435/973

    Abstract: Processes are disclosed in which light of different wavelengths is simultaneously released from two or more enzymatically decomposable chemiluminescent 1,2-dioxetane compounds, said compounds being configured, by means of the inclusion of a different light emitting fluorophore in each of them, to each emit light of said different wavelengths, by decomposing each of said compounds by means of a different enzyme. Such processes can be used in multi-channel assays, immunoassays, chemical assays and nucleic acid probe assays, to detect the presence or determine the concentration of chemical or biological substances, and in multi-channel chemical/physical probe procedures for studying the microstructures of macromolecules.

    Abstract translation: 公开了其中不同波长的光从两种或更多种可酶促分解的化学发光的1,2-二氧杂环丁烷化合物同时释放的方法，所述化合物通过在其每一种中包含不同的发光荧光团来配置，每种发射 通过用不同的酶分解每个所述化合物，所述不同波长的光。 这种方法可用于多通道测定，免疫测定，化学测定和核酸探针测定，以检测化学或生物物质的存在或确定浓度，以及用于研究化学或生物物质的微结构的多通道化学/物理探针程序 大分子。

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