Stabilized nucleic acid dark quencher-fluorophore probes
    3.
    发明授权
    Stabilized nucleic acid dark quencher-fluorophore probes 有权
    稳定的核酸暗猝灭剂 - 荧光团探针

    公开(公告)号:US08466266B2

    公开(公告)日:2013-06-18

    申请号:US12416901

    申请日:2009-04-01

    IPC分类号: C07C245/02

    摘要: The present invention provides a new class of solids supports for synthesis of modified oligomers of nucleic acids, and nucleic acid probes that have a format expediently synthesized on the new supports. Exemplary solid supports include at least one quencher bound through a linker to the solid support. Various exemplary embodiments include a moiety that stabilizes a duplex, triplex or higher order aggregation (e.g., hybridization) of nucleic acids of which the oligomer of the invention is a component. Other components of the solid support include moieties that stabilize aggregations of nucleic acids, e.g., intercalators, minor groove binding moieties, bases modified with a stabilizing moiety (e.g., alkynyl moieties, and fluoroalkyl moieties), and conformational stabilizing moieties, such as those described in commonly owned U.S. Patent Application Publication No. 2007/0059752.

    摘要翻译: 本发明提供了用于合成核酸修饰低聚物的新类固体支持物,以及具有在新载体上方便合成的形式的核酸探针。 示例性的固体支持物包括通过连接体与固体支持物结合的至少一种猝灭剂。 各种示例性实施方案包括稳定其本发明的低聚物是组分的核酸的双链体,三链体或更高级聚集(例如杂交)的部分。 固体支持物的其它组分包括稳定核酸聚集的部分,例如嵌入剂,小槽结合部分,用稳定部分修饰的碱基(例如炔基部分和氟烷基部分)和构象稳定部分,例如描述的那些 在共同拥有的美国专利申请公开No.2007 / 0059752中。

    Diazeniumdiolate Cyclohexyl Derivatives
    4.
    发明申请
    Diazeniumdiolate Cyclohexyl Derivatives 有权
    二氮烯二硫代环己基衍生物

    公开(公告)号:US20130059823A1

    公开(公告)日:2013-03-07

    申请号:US13698444

    申请日:2011-05-16

    摘要: A compound having the structure (I) or a pharmaceutically acceptable salt thereof, wherein R3 is hydrogen, deuterium, —OH, —OC1-6alkyl, or halogen; R8 is hydrogen, deuterium, or C1-6alkyl; R11 and R12 are independently hydrogen, —C1-6alkyl, —OH, —OC1-6alkyl, or halogen; R13 and R14 are independently —C1-6alkyl, —(CH2)1-2OH, or —OC1-6alkyl, or, together with the nitrogen atom to which they are attached, form a 4- to 7-membered heterocyclic ring containing one nitrogen atom and 0 or 1 oxygen atoms, wherein said ring is unsubstituted or mono-, di- or tri-substituted with halogen or —C1-6alkyl; R15 is (CR1R2)nC(O)OR16, wherein n is 0, 1 or 2, —C(O)NHCH(R17)OR16, or —C(O)NHCH(R17)C(O)NHCH(R18)C(O)OR16; R16 is hydrogen, C1-6alkyl, or (CH2)1-2N+R19R20R21; R1, R2, R4, R5, R6, R7, R9, R10, R17, R18, R19, R20, and R21 are independently hydrogen or —C1-6alkyl; and stereoisomers thereof, and pharmaceutically acceptable salts thereof, and pharmaceutically acceptable salts of stereoisomers thereof.

    摘要翻译: 具有结构(I)的化合物或其药学上可接受的盐,其中R 3是氢,氘,-OH,-OC 1-6烷基或卤素; R8是氢,氘或C1-6烷基; R 11和R 12独立地是氢,-C 1-6烷基,-OH,-OC 1-6烷基或卤素; R 13和R 14独立地为C 1-6烷基, - (CH 2)1-2 OH或-OC 1-6烷基,或者与它们所连接的氮原子一起形成含有一个氮的4-至7-元杂环 原子和0或1个氧原子,其中所述环是未取代的或被卤素或-C 1-6烷基单取代,二取代或三取代; R15是(CR1R2)nC(O)OR16,其中n是0,1或2,-C(O)NHCH(R17)OR16或-C(O)NHCH(R17)C(O)NHCH(R18) (O)OR16; R16是氢,C1-6烷基或(CH2)1-2N + R19R20R21; R 1,R 2,R 4,R 5,R 6,R 7,R 9,R 10,R 17,R 18,R 19,R 20和R 21独立地为氢或-C 1-6烷基; 其立体异构体及其药学上可接受的盐及其立体异构体的药学上可接受的盐。

    MULTICOMPONENT ASSEMBLIES HAVING ENHANCED BINDING PROPERTIES FOR DIAGNOSIS AND THERAPY
    5.
    发明申请
    MULTICOMPONENT ASSEMBLIES HAVING ENHANCED BINDING PROPERTIES FOR DIAGNOSIS AND THERAPY 有权
    具有增强结合特性的多组分组合用于诊断和治疗

    公开(公告)号:US20100041827A1

    公开(公告)日:2010-02-18

    申请号:US12603438

    申请日:2009-10-23

    CPC分类号: A61K49/223 A61K47/6925

    摘要: An organized mobile multicomponent conjugate (OMMC) and method of using to enhance binding of weakly binding compounds to a target. A lamellar structure containing at least two binding compounds is assembled under conditions in which the binding compounds self-regulate in or on the lamellar structure, forming a cooperative ensemble that is capable of binding with enhanced affinity to a complementary affinity site on a target. Each binding compound is bound to the lamellar surface, and may be connected by a linker. The OMMC may contain an effector molecule, such as a diagnostic or therapeutic agent, for administration to a patent who is then diagnosed or treated using the effector molecule.

    摘要翻译: 有组织的移动多组分缀合物(OMMC)和用于增强弱结合化合物与靶标的结合的方法。 包含至少两种结合化合物的层状结构在其中结合化合物在层状结构中或其上层板自调节的条件下组装,形成能够以增强的亲和力与靶上的互补亲和位点结合的合作整体。 每个结合化合物结合到层状表面,并且可以通过连接体连接。 OMMC可以含有效应分子,例如诊断或治疗剂,用于给予专利,然后使用效应分子进行诊断或治疗。

    Preparation of 3,3'-diamino-4,4'-azoxyfurazan, 3,3'-4,4'-azofurazan, and pressed articles
    7.
    发明申请
    Preparation of 3,3'-diamino-4,4'-azoxyfurazan, 3,3'-4,4'-azofurazan, and pressed articles 审中-公开
    制备3,3'-二氨基-4,4'-氮杂氧呋喃,3,3'-4,4'-氮呋喃和压制物

    公开(公告)号:US20090306355A1

    公开(公告)日:2009-12-10

    申请号:US12156904

    申请日:2008-06-04

    IPC分类号: C07C291/08 C07C245/02

    CPC分类号: C07D271/08

    摘要: A method for preparing essentially pure 3,3′-diamino-4,4′-azoxyfurazan (“DAAF”) that involves reacting an aqueous solution that includes 3,4-diaminofurazan (“DAF”) with OXONE™ (i.e. 2KHSO5.KHSO4.K2SO4) in the presence of a chemical buffer or a material that produces a chemical buffer during the reaction between DAF and the OXONE™. The essentially pure product particles can be used without further purification in preparing pressed articles of that consist of essentially pure DAAF. When sodium hypochlorite is used instead of OXONE, the product is 3,3′-diamino-4,4′-azofurazan (“DAAzF”).

    摘要翻译: 一种制备基本上纯的3,3'-二氨基-4,4'-氮杂氧杂呋咱(“DAAF”)的方法,其包括使包含3,4-二氨基呋咱(“DAF”)的水溶液与OXONE TM(即2KHSO5 在一种化学缓冲液或在DAF和OXONE TM之间的反应期间产生化学缓冲剂的材料的存在下.KHSO4.K2SO4)。 基本上纯的产物颗粒可以在不经进一步纯化的情况下用于制备由基本上纯的DAAF组成的压制制品。 当使用次氯酸钠代替OXONE时,产物是3,3'-二氨基-4,4'-氮呋喃(“DAAzF”)。

    STABILIZED NUCLEIC ACID DARK QUENCHER-FLUOROPHORE PROBES
    8.
    发明申请
    STABILIZED NUCLEIC ACID DARK QUENCHER-FLUOROPHORE PROBES 有权
    稳定的核酸深色探针 - 荧光探针

    公开(公告)号:US20090259030A1

    公开(公告)日:2009-10-15

    申请号:US12416901

    申请日:2009-04-01

    摘要: The present invention provides a new class of solids supports for synthesis of modified oligomers of nucleic acids, and nucleic acid probes that have a format expediently synthesized on the new supports. Exemplary solid supports include at least one quencher bound through a linker to the solid support. Various exemplary embodiments include a moiety that stabilizes a duplex, triplex or higher order aggregation (e.g., hybridization) of nucleic acids of which the oligomer of the invention is a component. Other components of the solid support include moieties that stabilize aggregations of nucleic acids, e.g., intercalators, minor groove binding moieties, bases modified with a stabilizing moiety (e.g., alkynyl moieties, and fluoroalkyl moieties), and conformational stabilizing moieties, such as those described in commonly owned U.S. Patent Application Publication No. 2007/0059752.

    摘要翻译: 本发明提供了用于合成核酸修饰低聚物的新类固体支持物,以及具有在新载体上方便合成的形式的核酸探针。 示例性的固体支持物包括通过连接体与固体支持物结合的至少一种猝灭剂。 各种示例性实施方案包括稳定其本发明的低聚物是组分的核酸的双链体,三链体或更高级聚集(例如杂交)的部分。 固体支持物的其它组分包括稳定核酸聚集的部分,例如嵌入剂,小槽结合部分,用稳定部分修饰的碱基(例如炔基部分和氟烷基部分)和构象稳定部分,例如描述的那些 在共同拥有的美国专利申请公开No.2007 / 0059752中。

    Ink jet printing composition comprising a dye containing hydrazine or hydrazide
    9.
    发明授权
    Ink jet printing composition comprising a dye containing hydrazine or hydrazide 失效
    包含含有肼或酰肼的染料的喷墨印刷组合物

    公开(公告)号:US07141106B2

    公开(公告)日:2006-11-28

    申请号:US10469309

    申请日:2002-02-27

    IPC分类号: C09D11/02 C07C245/02 B41J2/01

    CPC分类号: C09D11/32 C09B43/16 C09B69/00

    摘要: A composition comprising: (a) a liquid medium; and (b) a compound comprising one or more chromophoric groups and one or more hydrazine or hydrazide groups; wherein the liquid medium comprises water and an organic solvent, an organic solvent free from water, or a low melting point solid. The composition is useful for ink jet printing.

    摘要翻译: 一种组合物,其包含:(a)液体介质; 和(b)包含一个或多个发色基团和一个或多个肼或酰肼基团的化合物; 其中液体介质包括水和有机溶剂,不含水的有机溶剂或低熔点固体。 该组合物可用于喷墨印刷。