Rage antagonists as agents to reverse amyloidosis and diseases associated therewith
    23.
    发明申请
    Rage antagonists as agents to reverse amyloidosis and diseases associated therewith 审中-公开
    愤怒的拮抗剂作为逆转淀粉样变性的药物和与之相关的疾病

    公开(公告)号:US20050026811A1

    公开(公告)日:2005-02-03

    申请号:US10850238

    申请日:2004-05-20

    摘要: Disclosed are RAGE antagonist compounds that have the ability to reverse pre-existing amyloidosis. Treatment with the RAGE antagonist compounds described herein may be used to reduce plaque size and improve cognition for subjects in the later stages of Alzheimer's disease. Additionally, the RAGE antagonists described herein may be used to reduce the onset of plaque formation and thereby prevent loss of cognition and other symptoms associated with Alzheimer's Disease and other diseases of amyloid deposition.

    摘要翻译: 公开了具有逆转预先存在的淀粉样变性的能力的RAGE拮抗剂化合物。 本文所述的RAGE拮抗剂化合物的治疗可用于减少斑块大小并改善阿尔茨海默病后期受试者的认知。 此外,本文所述的RAGE拮抗剂可用于减少斑块形成的发作,从而防止与阿尔茨海默病和其他淀粉样蛋白沉积疾病相关的认知和其它症状的丧失。

    Modulators of proteins with phosphotyrosine recognition units
    24.
    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:US5965558A

    公开(公告)日:1999-10-12

    申请号:US960637

    申请日:1997-10-29

    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 phosphotyrosine recognition units
    29.
    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
    30.
    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。