Modulators of proteins with phosphotyrosine recognition units
    33.
    发明授权
    Modulators of proteins with phosphotyrosine recognition units 失效
    具有磷酸酪氨酸识别单元的蛋白质的调节剂

    公开(公告)号:US6150532A

    公开(公告)日:2000-11-21

    申请号:US210076

    申请日:1998-12-11

    摘要: The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganism, eukaryoic cells, whole animals and human being. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.

    摘要翻译: 本发明涉及具有式(A1)所示的一般结构的新型蛋白质酪氨酸磷酸酶调节化合物,其制备方法,包含该化合物的组合物,其用于治疗人和动物病症的用途,用于其纯化 的蛋白质或糖蛋白,以及它们在诊断中的用途。 本发明涉及在体外系统,微生物,真核细胞,整个动物和人中调节具有磷酸酪氨酸识别单元的分子的活性,包括蛋白酪氨酸磷酸酶(PTP酶)和具有Src-同源性-2结构域的蛋白质。 R'和R“独立地选自氢,卤素,氰基,硝基,三卤代甲基,烷基,芳基烷基。 R“选自氢,烷基,取代的烷基,芳基,芳基烷基。 X是芳基。 Y选自氢或其中(*)表示与X连接的潜在点。

    Modulators of proteins with phosphotryrosine recognition units
    34.
    发明授权
    Modulators of proteins with phosphotryrosine recognition units 失效
    具有磷酸基酪氨酸识别单元的蛋白质调节剂

    公开(公告)号:US5753687A

    公开(公告)日:1998-05-19

    申请号:US766114

    申请日:1996-12-16

    摘要: Y--X--C(R').dbd.C(R")COOR'" (A1) The present invention relates to novel protein tyrosine phosphatase modulating compounds having the general structure shown in Formula (A1), to methods for their preparation, to compositions comprising the compounds, to their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention relates to modulation of the activity of molecules with phosphotyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryoic cells, whole animals and human beings. R' and R" are independently selected from the group consisting of hydrogen, halo, cyano, nitro, trihalomethyl, alkyl, arylalkyl. R'" is selected from the group consisting of hydrogen, alkyl, substituted alkyl, aryl, arylalkyl. X is aryl. Y is selected from hydrogen or ##STR1## wherein (*) indicates a potential point of attachment to X.

    摘要翻译: YXC(R')= C(R“)COOR”'(A1)本发明涉及具有式(A1)所示的一般结构的新的蛋白质酪氨酸磷酸酶调节化合物及其制备方法, 该化合物用于治疗人和动物疾病,用于蛋白质或糖蛋白的纯化及其在诊断中的应用。 本发明涉及在体外系统,微生物,真核细胞,整个动物和人类中调节具有磷酸酪氨酸识别单元的分子的活性,包括蛋白酪氨酸磷酸酶(PTP酶)和具有Src同源性-2结构域的蛋白质。 R'和R“独立地选自氢,卤素,氰基,硝基,三卤代甲基,烷基,芳基烷基。 R“选自氢,烷基,取代的烷基,芳基,芳基烷基。 X是芳基。 Y选自氢或 其中(*)表示与X的连接点。

    Rage Fusion Proteins And Method Of Use
    35.
    发明申请
    Rage Fusion Proteins And Method Of Use 有权
    愤怒的融合蛋白和使用方法

    公开(公告)号:US20080075733A1

    公开(公告)日:2008-03-27

    申请号:US11629437

    申请日:2005-08-03

    CPC分类号: C07K14/705 A61K38/00

    摘要: Disclosed are RAGE fusion proteins comprising RAGE polypeptide sequences linked to a second, non-RAGE polypeptide. The RAGE fusion protein may utilize a RAGE polypeptide domain comprising a RAGE ligand binding site and an interdomain linker directly linked to an immunoglobulin CH2 domain. Such fusion proteins may provide specific, high affinity binding to RAGE ligands. Also disclosed is the use of the RAGE fusion proteins as therapeutics for RAGE-mediated pathologies.

    摘要翻译: 公开了包含与第二非RAGE多肽连接的RAGE多肽序列的RAGE融合蛋白。 RAGE融合蛋白可以利用包含RAGE配体结合位点的RAGE多肽结构域和直接连接到免疫球蛋白H 2结构域的域间连接。 这样的融合蛋白可以提供与RAGE配体的特异的高亲和力结合。 还公开了RAGE融合蛋白作为RAGE介导的病理学的治疗剂的用途。

    Fluorescence polarization assay
    36.
    发明申请
    Fluorescence polarization assay 审中-公开
    荧光偏振测定

    公开(公告)号:US20070154954A1

    公开(公告)日:2007-07-05

    申请号:US10592553

    申请日:2005-03-18

    IPC分类号: G01N33/567 C12M1/34

    摘要: Disclosed are methods and systems that use fluorescence polarization to identify compounds that have the ability to bind to, and/or modulate, the activity of the Receptor for Advanced Glycated Endproducts (RAGE). Compounds identified using the methods and systems of the present invention may comprise small organic molecule RAGE antagonists. The small organic molecule RAGE antagonists identified using the methods and systems of the present invention may be used to treat RAGE-mediated diseases, such as, but not limited to, diabetes or Alzheimer's disease.

    摘要翻译: 公开了使用荧光偏振来鉴定具有结合和/或调节高级糖基化产物(RAGE)受体活性的能力的化合物的方法和系统。 使用本发明的方法和系统鉴定的化合物可以包含小的有机分子RAGE拮抗剂。 使用本发明的方法和系统鉴定的小有机分子RAGE拮抗剂可用于治疗RAGE介导的疾病,例如但不限于糖尿病或阿尔茨海默氏病。

    Bis-heteroaryl alkanes as therapeutic agents
    37.
    发明申请

    公开(公告)号:US20060128784A1

    公开(公告)日:2006-06-15

    申请号:US11345065

    申请日:2006-02-01

    IPC分类号: A61K31/405

    摘要: This invention provides compounds which are useful as inhibitors of protein tyrosine phosphatases (PTPases). As inhibitors of PTPases the compounds of the invention are useful for the management, treatment, control and adjunct treatment of diseases in mammals mediated by PTPase activity. Such diseases include type I diabetes, type II diabetes, immune dysfunction, AIDS, autoimmunity, glucose intolerance, obesity, cancer, psoriasis, allergic diseases, infectious diseases, inflammatory diseases, diseases involving the modulated synthesis of growth hormone or the modulated synthesis of growth factors or cytokines which affect the production of growth hormone, or Alzheimer's disease.