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公开(公告)号：US5958957A
公开(公告)日：1999-09-28
申请号：US842801
申请日：1997-04-16
IPC分类号： C07D231/20 , C07D249/14 , C07D257/04 , C07D271/10 , C07D271/113 , C07D277/34 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/38 , A61K31/14 , C07D271/07
CPC分类号： C07D271/113 , C07D231/20 , C07D249/14 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, 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 phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
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公开(公告)号：US6063800A
公开(公告)日：2000-05-16
申请号：US253443
申请日：1999-02-19
IPC分类号： C07D231/20 , C07D249/14 , C07D257/04 , C07D271/10 , C07D271/113 , C07D277/34 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/38 , A61K31/425 , C07D209/82 , C07D277/04
CPC分类号： C07D271/113 , C07D231/20 , C07D249/14 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, 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 phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 --A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
摘要翻译： 本发明涉及新型有机化合物，其制备方法，含有它们的组合物，其用于治疗人和动物疾病的用途，其用于蛋白质或糖蛋白的纯化及其在诊断中的用途。 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（PTPases）和具有Src-同源性-2结构域的蛋白质。 新型有机化合物是式（I）（L）n-Ar1-R1-A（I）的化合物，其中（L）n，n，Ar1，R1和A如申请中所定义。
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公开(公告)号：US6080770A
公开(公告)日：2000-06-27
申请号：US253419
申请日：1999-02-19
IPC分类号： C07D231/20 , C07D249/14 , C07D257/04 , C07D271/10 , C07D271/113 , C07D277/34 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/38 , A61K31/41 , C07D249/04 , C07D403/06
CPC分类号： C07D271/113 , C07D231/20 , C07D249/14 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, 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 phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I) ##STR1## wherein (L).sub.n, Ar.sub.1, R.sub.1 and A are as defined in the application.
摘要翻译： 本发明涉及新型有机化合物，其制备方法，含有它们的组合物，其用于治疗人和动物疾病的用途，其用于蛋白质或糖蛋白的纯化及其在诊断中的用途。 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（PTPases）和具有Src-同源性-2结构域的蛋白质。 新型有机化合物是式（I）的化合物，其中（L）n，Ar 1，R 1和A如本申请中所定义。
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公开(公告)号：US5972978A
公开(公告)日：1999-10-26
申请号：US252883
申请日：1999-02-19
IPC分类号： C07D231/20 , C07D249/14 , C07D257/04 , C07D271/10 , C07D271/113 , C07D277/34 , C07D285/08 , C07D285/12 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/38 , A61K31/41 , C07D285/10
CPC分类号： C07D271/113 , C07D231/20 , C07D249/14 , C07D257/04 , C07D277/34 , C07D285/08 , C07D285/125 , C07D285/135 , C07D417/06 , C07F9/3834 , C07F9/3882
摘要： The present invention relates to novel organic compounds, to methods for their preparation, to compositions containing them, 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 phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings. The novel organic compounds are compounds of formula (I)(L).sub.n --Ar.sub.1 --R.sub.1 A (I)wherein(L).sub.n, n, Ar.sub.1, R.sub.1 and A are as defined in the application.
摘要翻译： 本发明涉及新型有机化合物，其制备方法，含有它们的组合物，其用于治疗人和动物疾病的用途，其用于蛋白质或糖蛋白的纯化及其在诊断中的用途。 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（PTPases）和具有Src-同源性-2结构域的蛋白质。 新的有机化合物是式（I）（L）n-Ar1-R1A（I）的化合物，其中（L）n，n，Ar1，R1和A如本申请中所定义。
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公开(公告)号：US06613903B2
公开(公告)日：2003-09-02
申请号：US09901367
申请日：2001-07-09
申请人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Moller , Ole Hvilsted Olsen , Frank Urban Axe , Farid Bakir , Yu Ge , Daniel Dale Holsworth , Luke Milburn Judge , Michael James Newman , Roy Teruyuki Uyeda , Barry Zvi Shapira
发明人： Henrik Sune Andersen , Thomas Kruse Hansen , Jesper Lau , Niels Peter Hundahl Moller , Ole Hvilsted Olsen , Frank Urban Axe , Farid Bakir , Yu Ge , Daniel Dale Holsworth , Luke Milburn Judge , Michael James Newman , Roy Teruyuki Uyeda , Barry Zvi Shapira
IPC分类号： C07D47102
CPC分类号： C07D495/04 , A61K31/4365
摘要： The present invention provides novel thienopyridines, novel compositions, methods of their use, and methods of their manufacture, where such compounds of Formula 1 are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) including PTP1B, T cell PTP, wherein X, R1, R2, R3, and R4 are defined more fully in the description. The compounds are useful in the treatment of type 1 diabetes, type 2 diabetes, impaired glucose tolerance, insulin resistance, obesity, and other diseases.
摘要翻译： 本发明提供新颖的噻吩并吡啶类，其新颖的组合物，使用方法及其制备方法，其中式1化合物是包括PTP1B，T细胞PTP在内的蛋白酪氨酸磷酸酶（PTPase）的药理学有用的抑制剂，其中X， R2，R3和R4在说明书中更全面地定义。 该化合物可用于治疗1型糖尿病，2型糖尿病，葡萄糖耐量降低，胰岛素抵抗，肥胖症等疾病。
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公开(公告)号：US20130071351A1
公开(公告)日：2013-03-21
申请号：US13608542
申请日：2012-09-10
IPC分类号： A61K38/20 , A61K39/395
CPC分类号： A61K38/20 , A61K31/655 , A61K39/39533 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K2300/00
摘要： The invention provides combination treatments with IL-21, analogues and derivatives thereof. In particular, a combination comprising IL-21 and a monoclonal antibody and methods for using the combination in treating cancer are described.
摘要翻译： 本发明提供了与IL-21，其类似物和衍生物的组合治疗。 特别地，描述了包含IL-21和单克隆抗体的组合以及在治疗癌症中使用该组合的方法。
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公开(公告)号：US20100135901A1
公开(公告)日：2010-06-03
申请号：US12637109
申请日：2009-12-14
CPC分类号： A61K38/20 , A61K31/655 , A61K39/39533 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K2300/00
摘要： The invention provides combination treatments with IL-21, analogues and derivatives thereof.
摘要翻译： 本发明提供了与IL-21，其类似物和衍生物的组合治疗。
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公开(公告)号：US06492495B1
公开(公告)日：2002-12-10
申请号：US09361096
申请日：1999-07-26
IPC分类号： C07K1600
摘要： A novel protein tyrosine phosphatase designated PTP-S31 and its subfamily are identified, as are nucleic acid molecule coding therefor. Included in this;family are PTP-S31 proteins or glycoproteins having one, two, or three identified amino acid changes in previously defined consensus sequences in the catalytic phosphatase domains of known protein tyrosine phosphatases. The PTP-S31 proteins or glycoproteins may be produced by recombinant means. Antibodies to PTP-S31 proteins or glycoproteins and nucleic acid constructs coding therefor, and methods for screening molecules which can bind to PTP-S31 proteins or glycoproteins and inhibit or stimulate their enzymatic activity, are provided.
摘要翻译： 鉴定了称为PTP-S31及其亚家族的新型蛋白酪氨酸磷酸酶，编码该核酸分子的核酸分子也是如此。 包括在这个家族中的PTP-S31蛋白或糖蛋白在已知蛋白酪氨酸磷酸酶的催化磷酸酶结构域中具有一个，两个或三个鉴定的氨基酸变化。 PTP-S31蛋白或糖蛋白可以通过重组方法产生。 提供了针对PTP-S31蛋白或糖蛋白的抗体及其编码的核酸构建体，以及用于筛选可结合PTP-S31蛋白或糖蛋白并抑制或刺激其酶活性的分子的方法。
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公开(公告)号：US20080206192A1
公开(公告)日：2008-08-28
申请号：US12112452
申请日：2008-04-30
CPC分类号： A61K38/20 , A61K31/655 , A61K39/39533 , A61K39/3955 , A61K39/39558 , A61K45/06 , A61K2300/00
摘要： The invention provides combination treatments with IL-21, analogues and derivatives thereof.
摘要翻译： 本发明提供了与IL-21，其类似物和衍生物的组合治疗。
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公开(公告)号：US5952212A
公开(公告)日：1999-09-14
申请号：US449609
申请日：1995-05-24
IPC分类号： G01N33/53 , A61K38/00 , A61K38/46 , A61K39/395 , A61P43/00 , C07K14/47 , C07K16/40 , C12N1/21 , C12N9/16 , C12N9/18 , C12N15/09 , C12N15/55 , C12P21/08 , C12Q1/42 , C12Q1/68 , C12R1/19 , G01N33/573 , C12N9/12
摘要： A novel protein tyrosine phosphatase designated PTP-S31 and its subfamily are identified, as are nucleic acid molecule coding therefor. Included in this family are PTP-S31 proteins or glycoproteins having one, two, or three identified amino acid changes in previously defined consensus sequences in the catalytic phosphatase domains of known protein tyrosine phosphatases. The PTP-S31 proteins or glycoproteins may be produced by recombinant means. Antibodies to PTP-S31 proteins or glycoproteins and nucleic acid constructs coding therefor, and methods for screening molecules which can bind to PTP-S31 proteins or glycoproteins and inhibit or stimulate their enzymatic activity, are provided.
摘要翻译： 鉴定了称为PTP-S31及其亚家族的新型蛋白酪氨酸磷酸酶，编码该核酸分子的核酸分子也是如此。 该家族包括PTP-S31蛋白或糖蛋白，其在已知蛋白酪氨酸磷酸酶的催化磷酸酶结构域中具有一个，两个或三个鉴定的氨基酸变化。 PTP-S31蛋白或糖蛋白可以通过重组方法产生。 提供了针对PTP-S31蛋白或糖蛋白的抗体及其编码的核酸构建体，以及用于筛选可结合PTP-S31蛋白或糖蛋白并抑制或刺激其酶活性的分子的方法。
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