Depsipeptide for therapy of kidney cancer
    1.
    发明授权
    Depsipeptide for therapy of kidney cancer 有权
    用于治疗肾癌的多肽

    公开(公告)号:US08673888B2

    公开(公告)日:2014-03-18

    申请号:US10508958

    申请日:2003-03-27

    CPC分类号: A61K38/15

    摘要: The present invention provides a therapeutic agent of kidney cancer, which comprises FK228 of the formula (I) or a salt thereof. FK228 or a salt thereof, which is an active ingredient in the present invention, shows a superior antitumor activity in vivo against kidney cancer.

    摘要翻译: 本发明提供了包含式(I)的FK228或其盐的肾癌治疗剂。 作为本发明中的活性成分的FK228或其盐显示出对肾癌的体内优异的抗肿瘤活性。

    Attenuated human-bovine chimeric parainfluenza virus(PIV) vaccines
    4.
    发明授权
    Attenuated human-bovine chimeric parainfluenza virus(PIV) vaccines 有权
    减毒的人 - 牛嵌合副流感病毒(PIV)疫苗

    公开(公告)号:US07201907B1

    公开(公告)日:2007-04-10

    申请号:US09586479

    申请日:2000-06-01

    IPC分类号: A61K39/12 A61K39/155

    摘要: Chimeric human-bovine parainfluenza viruses (PIVs) are infectious and attenuated in humans and other mammals and useful individually or in combination in vaccine formulations for eliciting an anti-PIV immune response or as vectors for introducing heterologous genes into a host. Also provided are isolated polynucleotide molecules and vectors incorporating a chimeric PIV genome or antigenome which includes a partial or complete human or bovine PIV “background” genome or antigenome combined or integrated with one or more heterologous gene(s) or genome segment(s) of a different PIV. Chimeric human-bovine PIV of the invention include a partial or complete “background” PIV genome or antigenome derived from or patterned after a human or bovine PIV virus combined with one or more heterologous gene(s) or genome segment(s) of a different PIV virus to form the human-bovine chimeric PIV genome or antigenome.

    摘要翻译: 嵌合人 - 牛副流感病毒(PIV)在人类和其他哺乳动物中具有感染性和减毒性,并且在疫苗制剂中单独使用或组合用于引发抗PIV免疫应答或作为将异源基因导入宿主的载体。 还提供了分离的多核苷酸分子和掺入嵌合PIV基因组或抗原组的载体,其包括部分或完整的人或牛PIV“背景”基因组或反基因组,其与一个或多个异源基因或基因组片段组合或整合, 不同的PIV。 本发明的嵌合人牛PIV包括部分或完整的“背景”PIV基因组或反义基因组,其衍生自或构图在人或牛PIV病毒与一个或多个异源基因或不同基因组的基因组片段组合 PIV病毒形成人 - 牛嵌合PIV基因组或抗原组。

    Formulation of boronic acid compounds
    6.
    发明申请
    Formulation of boronic acid compounds 有权
    制备硼酸化合物

    公开(公告)号:US20020169114A1

    公开(公告)日:2002-11-14

    申请号:US10056567

    申请日:2002-01-25

    发明人: Shanker Lal Gupta

    IPC分类号: A61K038/14 C07K009/00

    摘要: The present invention provides stable compounds prepared from boronic acid and lyophilized compounds thereof of the formula (1): 1 in which Z1 and Z2 are moieties derived from sugar. The invention also provides methods for preparing such compounds. Lyophilizing a mixture comprising a boronic acid compound and a moiety derived from sugar produces a stable composition that readily releases the boronic acid compound upon reconstitution in aqueous media.

    摘要翻译: 本发明提供由硼酸制备的稳定化合物及其式(1)的冻干化合物:其中Z 1和Z 2为衍生自糖的部分。 本发明还提供了制备这些化合物的方法。 冻干包含硼酸化合物和衍生自糖的部分的混合物产生稳定的组合物,其在水性介质中重构后容易释放硼酸化合物。

    Redox-stable, non-phosphorylated cyclic peptide inhibitors of SH2 domain binding to target protein, conjugates thereof, compositions and methods of synthesis and use
    8.
    发明授权
    Redox-stable, non-phosphorylated cyclic peptide inhibitors of SH2 domain binding to target protein, conjugates thereof, compositions and methods of synthesis and use 有权
    与靶蛋白结合的SH2结构域的氧化还原稳定的非磷酸化环肽抑制剂,其结合物,组合物和合成和使用方法

    公开(公告)号:US07259142B2

    公开(公告)日:2007-08-21

    申请号:US11224819

    申请日:2005-09-13

    IPC分类号: A61K38/12

    CPC分类号: C07K7/06 A61K38/00 C07K7/56

    摘要: A compound of formula: in which (i) aa1 is Adi and aa4 is Glu or (ii) each of aa1 and aa4 is Adi, L is sulfur, sulfoxide, oxygen or methylene, which compound (and its conjugates) bind to an SH2 domain in a protein comprising an SH2 domain, is non-phosphorylated, is redox-stable in vivo, is characterized by an IC50 in vivo of less than about 4.0 μM with respect to the SH2 domain in Grb2, and, upon binding to the SH2 domain of Grb2, has a turn conformation. A conjugate comprising a compound as described above and a carrier agent, a composition comprising (i) a compound or a conjugate as described above and (ii) a carrier, a method of inhibiting binding of an SH2 domain in a protein comprising an SH2 domain to a target protein in an animal, wherein the SH2 domain is contacted with a target protein-binding inhibiting effective amount of a compound or a conjugate as described above, and a method of synthesizing such conjugates.

    摘要翻译: 下式化合物:其中(i)aa 1是Adi,aa 4是Glu或(ii)aa 1和a a各自独立地选自 Ad1,L是硫,亚砜,氧或亚甲基,该化合物(及其缀合物)与包含SH2结构域的蛋白质中的SH2结构域结合,未被磷酸化,是氧化还原稳定的 在体内,相对于Grb2中的SH2结构域,其体内IC 50小于约4.0μM,并且在结合到Grb2的SH2结构域时具有转向构象。 包含如上所述的化合物和载体的缀合物,包含(i)如上所述的化合物或缀合物和(ii)载体的组合物,抑制包含SH2结构域的蛋白质中SH2结构域结合的方法 涉及一种动物中的靶蛋白,其中SH2结构域与靶蛋白结合抑制有效量的上述化合物或结合物接触,以及合成这种缀合物的方法。

    Methods for the indentification of textual and physical structured query fragments for the analysis of textual and biopolymer information

    公开(公告)号:US20020177138A1

    公开(公告)日:2002-11-28

    申请号:US09991013

    申请日:2001-11-14

    发明人: Robert J. Boissy

    摘要: We disclose a combinatorial, hierarchical process that uses nullprocess-patternsnull in one preferred embodiment to identify, classify, and compare substrings within strings; and in another preferred embodiment to identify, classify, compare, generate, and separate fragments derived from one or more physical samples of polynucleotides. These substrings (and their physical polynucleotide counterparts) are called nullpartitionnull fragments, and the process-pattern-defined derivatives that some, but not all, nullpartitionnull fragments may yield are called nullstructured query fragmentsnull (SQFs). A process-pattern is both: (i) an ordered set of short nulltargetnull (one from each major search class) sites that must be present (and whose higher-ranked members of the same major search class must not have any sites) within the relevant search area of a partition fragment, and (ii) a step-wise delimitation process (where each step has a defined polarity and occurs after a target is found) that restricts the region of a partition fragment where the next class-specific, pre-emptive target-search takes place. In one preferred embodiment, the computer software disclosed herein locates the process-patterns and SQFs of interest within the partition fragments in the string(s) under study (e.g., a set of polynucleotide sequence data), stores the results, and provides for access to this data by database query and analysis tools. These computational analyses are emulated by another preferred embodiment using physical samples of polynucleotides and the laboratory methods disclosed herein. In the latter, sequence-specific, double-stranded cleavage effectors utilize as substrates and generate as products progressively expanding sets of asymmetrically end-immobilized DNA, a process that ultimately yields extremely large numbers of individually distinguishable SQFs (called nullrangednull SQFs) with lengths between 100-700 nucleotides. In almost all cases, the known process-pattern and observed length of an experimentally obtained ranged SQF provide sufficient information for the computer software disclosed herein to map the ranged SQF automatically to its partition fragment (and location) within a set of polynucleotide sequence data that characterizes the physical sample(s) of polynucleotides under study.