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    Modulators of proteins with phosphotyrosine recognition units
    3.
    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

    申请人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    发明人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    IPC分类号： A61K31/495 ,  C07D241/38 ,  C07D263/34 ,  C07D263/44 ,  C07D263/48 ,  C07D413/04

    CPC分类号： A61K31/495 ,  C07D241/42 ,  C07D471/04

    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
    4.
    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

    申请人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    发明人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    IPC分类号： A61K31/415 ,  C07D233/54 ,  C07D233/56 ,  C07D233/66

    CPC分类号： A61K31/415 ,  C07D233/54 ,  C07D233/56 ,  C07D233/66

    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。

    Binding compentent oligomers containing unsaturated 3',5' and 2',5' linkages
    5.
    发明授权
    Binding compentent oligomers containing unsaturated 3',5' and 2',5' linkages 失效
    含有不饱和3'，5'和2'，5'键的结合性低聚物

    公开(公告)号：US5434257A

    公开(公告)日：1995-07-18

    申请号：US142785

    申请日：1993-10-26

    申请人： Mark D. Matteucci ,  Xiaodong Cao

    发明人： Mark D. Matteucci ,  Xiaodong Cao

    IPC分类号： C07H19/06 ,  C07H21/00 ,  C12N15/113 ,  C12Q1/68 ,  C07H19/00

    CPC分类号： C07H21/00 ,  C07H19/06 ,  C12N15/113 ,  C12Q1/68 ,  C12N2310/319

    摘要： Oligonucleotide analogs having one or more substitute linkages of the formula 2'/3'--S--CH.sub.2 --CH.dbd.5' or 2'/3'--O--CH.sub.2 --CH.dbd.5' between adjacent nucleomonomers are disclosed. The substitute linkage replace the usual phosphodiester linkage found in unmodified nucleic acids. The oligonucleotide analogs are easy to synthesize, stable in vivo, resistant to endogenous nucleases and are able to hybridize to target nucleic acid sequences in a sequence specific manner.

    摘要翻译： 公开了具有相邻核单体之间的式2'/ 3'-S-CH2-CH = 5'或2'/ 3'-O-CH2-CH = 5'的一个或多个取代键的寡核苷酸类似物。 替代连接取代未修饰核酸中常见的磷酸二酯连接。 寡核苷酸类似物易于合成，体内稳定，对内源性核酸酶具有抗性，并且能够以序列特异性方式与靶核酸序列杂交。

    Modulators of proteins with phosphotyrosine recognition units
    7.
    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

    申请人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    发明人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    IPC分类号： A61K31/495 ,  C07D241/38 ,  C07D263/34 ,  C07D263/44 ,  C07D263/48 ,  C07D413/04

    CPC分类号： A61K31/495 ,  C07D241/42 ,  C07D471/04

    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。

    Protein tyrosine phosphatase-inhibiting compounds
    8.
    发明授权
    Protein tyrosine phosphatase-inhibiting compounds 失效
    蛋白酪氨酸磷酸酶抑制化合物

    公开(公告)号：US06388076B1

    公开(公告)日：2002-05-14

    申请号：US09645785

    申请日：2000-08-24

    申请人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    发明人： Adnan Mjalli ,  Sepehr Sarshar ,  Xiaodong Cao ,  Farid Bakir

    IPC分类号： C07D47104

    CPC分类号： C07D471/04

    摘要： Y—X—C(R′)═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 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连接的潜在点。