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1. 发明申请

US20090281100A1 Benzimidazole quinolinones and uses thereof 审中-公开
标题翻译：苯并咪唑喹啉酮及其用途
公开(公告)号：US20090281100A1
公开(公告)日：2009-11-12
申请号：US12317493
申请日：2008-12-23
申请人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, JR. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
发明人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, JR. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
IPC分类号： A61K31/5377 , A61K31/497 , A61K31/4709
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并具有本文所述的变量。这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。

2. 发明授权

US07470709B2 Benzimidazole quinolinones and uses thereof 失效
标题翻译：苯并咪唑喹啉酮及其用途
公开(公告)号：US07470709B2
公开(公告)日：2008-12-30
申请号：US10644055
申请日：2003-08-19
申请人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, Jr. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
发明人： Paul A. Barsanti , Dirksen Bussiere , Stephen D. Harrison , Carla C. Heise , Johanna M. Jansen , Elisa Jazan , Timothy D. Machajewski , Christopher McBride , William R. McCrea, Jr. , Simon Ng , Zhi-Jie Ni , Sabina Pecchi , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Cynthia M. Shafer , Joel B. Silver , Allan S. Wagman , Marion Wiesmann , Kelly Wayman
IPC分类号： A61K31/47
CPC分类号： C07D401/04 , A61K31/4375 , A61K31/4709 , A61K31/496 , A61K31/52 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D453/02 , C07D453/06 , C07D471/04
摘要： Methods of inhibiting various enzymes and treating various conditions are provided that include administering to a subject a compound of Structure I or IB, a pharmaceutically acceptable salt thereof, a tautomer thereof, or a pharmaceutically acceptable salt of the tautomer. Compounds having the Structure I and IB have the following structures and have the variables described herein. Such compounds may be used to prepare medicaments for use in inhibiting various enzymes and for use in treating conditions mediated by such enzymes.
摘要翻译：提供了抑制各种酶和治疗各种病症的方法，其包括向受试者施用结构I或IB的化合物，其药学上可接受的盐，其互变异构体或互变异构体的药学上可接受的盐。具有结构I和IB的化合物具有以下结构并具有本文所述的变量。这些化合物可用于制备用于抑制各种酶的药物，并用于治疗由这些酶介导的病症。

3. 发明授权

US07037918B2 Inhibitors of glycogen synthase kinase 3 失效
公开(公告)号：US07037918B2
公开(公告)日：2006-05-02
申请号：US10309535
申请日：2002-12-03
申请人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
发明人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
IPC分类号： A61K31/505 , A61K31/535 , A61K31/47 , A61K31/475 , A61K31/52
CPC分类号： C07D213/74 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12
摘要： New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

4. 发明授权

US06489344B1 Inhibitors of glycogen synthase kinase 3 失效
标题翻译：糖原合酶激酶抑制剂3
公开(公告)号：US06489344B1
公开(公告)日：2002-12-03
申请号：US09336098
申请日：1999-06-18
申请人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
发明人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Sean P. Brown , Dane A. Goff , Kirk W. Johnson , Keith B. Pfister , Savithri Ramurthy , Paul A. Renhowe , Lynn Seely , Sharadha Subramanian , Allan S. Wagman , Xiaohui A. Zhou
IPC分类号： C07D40104
CPC分类号： C07D213/74 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D417/12
摘要： New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.
摘要翻译：提供了新的嘧啶或吡啶类化合物，体外抑制糖原合成酶激酶（GSK3）活性和体内GSK3介导的病症治疗的组合物和方法。本发明的方法，化合物和组合物可以单独使用或与其它药理活性剂组合用于治疗由GSK3活性介导的病症，例如治疗糖尿病，阿尔茨海默病和其他神经变性疾病，肥胖症，动脉粥样硬化心血管疾病，原发性高血压，多囊卵巢综合征，X综合征，缺血，创伤性脑损伤，双相情感障碍，免疫缺陷或癌症。

5. 发明授权

US07045519B2 Inhibitors of glycogen synthase kinase 3 失效
公开(公告)号：US07045519B2
公开(公告)日：2006-05-16
申请号：US09949035
申请日：2001-09-06
申请人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Kirk Johnson , Keith B. Pfister , Savithri Ramurthy , Lynn Seely , Allan S. Wagman , Manoj C. Desai , Barry H. Levine
发明人： John M. Nuss , Stephen D. Harrison , David B. Ring , Rustum S. Boyce , Kirk Johnson , Keith B. Pfister , Savithri Ramurthy , Lynn Seely , Allan S. Wagman , Manoj C. Desai , Barry H. Levine
IPC分类号： A61K31/506 , C07D403/04
CPC分类号： C07D213/74 , C07D213/75 , C07D213/80 , C07D213/85 , C07D239/42 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.

6. 发明申请

US20090074886A1 GSK-3 INHIBITORS 审中-公开
标题翻译： GSK-3抑制剂
公开(公告)号：US20090074886A1
公开(公告)日：2009-03-19
申请号：US12325828
申请日：2008-12-01
申请人： Christina N. Bennett , Kurt D. Hankenson , Stephen D. Harrison , Kenneth A. Longo , Ormond A. MacDougald , Allan S. Wagman
发明人： Christina N. Bennett , Kurt D. Hankenson , Stephen D. Harrison , Kenneth A. Longo , Ormond A. MacDougald , Allan S. Wagman
IPC分类号： A61K33/06 , A61K31/505 , A61K38/16 , A61K31/675 , A61P19/08 , A61K31/663 , A61K31/56
CPC分类号： A61K31/535 , A61K31/505 , A61K31/506 , A61K33/06 , A61K38/29 , A61K45/06 , A61K2300/00
摘要： This invention relates to methods of treating or preventing bone loss by administering to a human or animal subject pyrimidine and pyridine derivatives that inhibit the activity of glycogen synthase kinase 3 (GSK3), to pharmaceutical compositions containing the compounds, and to the use of the compounds and compositions alone or in combination with other pharmaceutically active agents.
摘要翻译：本发明涉及通过向人或动物施用抑制糖原合酶激酶3（GSK3）的活性的嘧啶和吡啶衍生物，含有该化合物的药物组合物以及使用该化合物来治疗或预防骨丢失的方法单独或与其它药物活性剂组合的组合物。

7. 发明申请

US20080182313A1 GSK3 polypeptides 失效
标题翻译： GSK3多肽
公开(公告)号：US20080182313A1
公开(公告)日：2008-07-31
申请号：US12074543
申请日：2008-03-03
申请人： Stephen D. Harrison , John A. Hall , Maria Calderon-Cacia , Ziyang Zhong , Eric Y. Fang , Doris G. Coit , Steve H. Nguyen , Angelica Medina-Selby
发明人： Stephen D. Harrison , John A. Hall , Maria Calderon-Cacia , Ziyang Zhong , Eric Y. Fang , Doris G. Coit , Steve H. Nguyen , Angelica Medina-Selby
IPC分类号： C12N9/12 , C07H21/04 , C12N15/00
CPC分类号： C12N9/1205 , C12Q1/485 , C12Y207/01037 , G01N2500/00
摘要： The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.
摘要翻译：本发明提供能够结晶的截短的GSK 3多肽，包括GSK3α和GSK3β多肽，以及这些多肽用于鉴定和优化GSK 3抑制剂的用途。还提供了具有与野生型GSK 3不同的至少一个取代的氨基酸的GSK 3多肽，其中取代的氨基酸不能被磷酸化。本发明用于提供鉴定和优化用于治疗由GSK 3活性（包括阿尔茨海默病，2型糖尿病和炎症）介导的疾病的化合物的方法。

8. 发明授权

US07361484B2 GSK3 polypeptides 失效
标题翻译： GSK3多肽
公开(公告)号：US07361484B2
公开(公告)日：2008-04-22
申请号：US11704724
申请日：2007-02-08
申请人： Stephen D. Harrison , John A. Hall , Maria Calderon-Cacia , Ziyang Zhong , Eric Y. Fang , Doris G. Coit , Steve H. Nguyen , Angelica Medina-Selby
发明人： Stephen D. Harrison , John A. Hall , Maria Calderon-Cacia , Ziyang Zhong , Eric Y. Fang , Doris G. Coit , Steve H. Nguyen , Angelica Medina-Selby
IPC分类号： C12Q1/48 , G01N33/53 , G01N33/00 , G01N33/563 , C12P21/06 , C12P21/08 , C12N9/12 , C12N5/02 , C12N5/06 , C12N15/00 , C07K14/00
CPC分类号： C12N9/1205 , C12Q1/485 , C12Y207/01037 , G01N2500/00
摘要： The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3α and GSK3β polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.
摘要翻译：本发明提供能够结晶的截短的GSK3多肽，包括GSK3α和GSK3β多肽，以及使用这些多肽来鉴定和优化GSK3抑制剂。还提供了具有与野生型GSK3不同的至少一个取代的氨基酸的GSK3多肽，其中取代的氨基酸不能被磷酸化。本发明用于提供鉴定和优化用于治疗由GSK3活性介导的疾病（包括阿尔茨海默病，2型糖尿病和炎症）的化合物的方法。

9. 发明授权

US06465231B2 GSK3 polypeptides 有权
标题翻译： GSK3多肽
公开(公告)号：US06465231B2
公开(公告)日：2002-10-15
申请号：US09916109
申请日：2001-07-25
申请人： Stephen D. Harrison , John A. Hall , Maria Calderon-Cacia , Ziyang Zhong , Eric Y. Fang , Doris G. Coit , Steve H. Nguyen , Angelica Medina-Selby
发明人： Stephen D. Harrison , John A. Hall , Maria Calderon-Cacia , Ziyang Zhong , Eric Y. Fang , Doris G. Coit , Steve H. Nguyen , Angelica Medina-Selby
IPC分类号： C12N912
CPC分类号： C12N9/1205 , C12Q1/485 , C12Y207/01037 , G01N2500/00
摘要： The invention provides truncated GSK3 polypeptides capable of crystallization, including GSK3&agr; and GSK3&bgr; polypeptides, and use of these polypeptides to identify and optimize GSK3 inhibitors. Also provided are GSK3 polypeptides having at least one substituted amino acid that differs from wild-type GSK3, wherein the substituted amino acid is incapable of being phosphorylated. The invention finds use in providing methods of identifying and optimizing compounds useful for treating diseases mediated by GSK3 activity, including Alzheimer's disease, type 2 diabetes, and inflammation.
摘要翻译：本发明提供能够结晶的截短的GSK3多肽，包括GSK3α和GSK3β多肽，以及使用这些多肽来鉴定和优化GSK3抑制剂。还提供了具有与野生型GSK3不同的至少一个取代的氨基酸的GSK3多肽，其中取代的氨基酸不能被磷酸化。本发明用于提供鉴定和优化用于治疗由GSK3活性介导的疾病（包括阿尔茨海默病，2型糖尿病和炎症）的化合物的方法。

10. 发明授权

US06512102B1 Compositions and methods of diagnosis and treatment using casein kinase I 失效
标题翻译：使用酪蛋白激酶I的组合物和诊断和治疗方法
公开(公告)号：US06512102B1
公开(公告)日：2003-01-28
申请号：US09472112
申请日：1999-12-23
申请人： Licen Xu , Stephen D. Harrison , Lewis T. Williams
发明人： Licen Xu , Stephen D. Harrison , Lewis T. Williams
IPC分类号： C07H2104
CPC分类号： C12N15/1137 , A61K31/00 , A61K38/45 , A61K48/00
摘要： The invention is generally directed to compositions and methods for affecting signal transduction using the casein kinase I (CKI) gene or gene product. The invention is more specifically directed to affecting the Wnt signal pathway using the CKI gene or gene product. The invention is particularly directed to using the CKI gene or gene product to treat and diagnose cancer, particularly breast and colon cancer. CKI&egr; is the preferred species. The field of the invention is compositions and methods for modulating signal transduction using the (CKI) gene or gene products and variants thereof. The invention is more specifically directed to modulating the Wnt signal pathway using the CKI gene or gene product. The invention is particularly directed to using the CKI gene or gene product to treat and diagnose disorders mediated by the Wnt signal pathway, especially hyperproliferative disorders, particularly breast and colon cancer.
摘要翻译：本发明一般涉及使用酪蛋白激酶I（CKI）基因或基因产物影响信号转导的组合物和方法。本发明更具体地涉及使用CKI基因或基因产物影响Wnt信号通路。本发明特别涉及使用CKI基因或基因产物来治疗和诊断癌症，特别是乳腺癌和结肠癌。 CKIepsi是首选品种。本发明的领域是使用（CKI）基因或其基因产物及其变体调节信号转导的组合物和方法。本发明更具体地涉及使用CKI基因或基因产物调节Wnt信号通路。本发明特别涉及使用CKI基因或基因产物来治疗和诊断由Wnt信号通路介导的疾病，特别是过度增殖性疾病，特别是乳腺癌和结肠癌。

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