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公开(公告)号：US08450317B2
公开(公告)日：2013-05-28
申请号：US12768268
申请日：2010-04-27
申请人： Jennifer A. Kowalski , Daniel Richard Marshall , Anthony S. Prokopowicz, III , Sabine Schlyer , Robert Sibley , Ronald John Sorcek , Di Wu , Frank Wu , Erick Richard Roush Young
发明人： Jennifer A. Kowalski , Daniel Richard Marshall , Anthony S. Prokopowicz, III , Sabine Schlyer , Robert Sibley , Ronald John Sorcek , Di Wu , Frank Wu , Erick Richard Roush Young
IPC分类号： C07D239/34 , C07D239/42 , A61K31/506
CPC分类号： C07D471/04 , C07D209/48 , C07D213/26 , C07D213/56 , C07D213/65 , C07D213/74 , C07D217/00 , C07D231/10 , C07D233/90 , C07D235/04 , C07D239/34 , C07D239/42 , C07D277/30 , C07D295/185 , C07D307/68 , C07D317/68 , C07D319/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D491/08
摘要： The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1至R 5，A，B，D和X如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。
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公开(公告)号：US06844435B2
公开(公告)日：2005-01-18
申请号：US10271222
申请日：2002-10-15
申请人： Roger John Snow , Donghong A. Gao , Daniel R. Goldberg , Abdelhakim Hammach , Daniel Kuzmich , Tina Marie Morwick , Neil Moss , Anthony S. Prokopowicz, III , Robert D. Selliah , Hidenori Takahashi
发明人： Roger John Snow , Donghong A. Gao , Daniel R. Goldberg , Abdelhakim Hammach , Daniel Kuzmich , Tina Marie Morwick , Neil Moss , Anthony S. Prokopowicz, III , Robert D. Selliah , Hidenori Takahashi
IPC分类号： A61K31/517 , A61P1/04 , A61P3/10 , A61P9/00 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/08 , A61P25/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D487/04 , C07D235/14
CPC分类号： C07D487/04 , A61K31/517
摘要： Disclosed are novel compounds of formula (I): wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.
摘要翻译： 公开了式（I）的新化合物：其中Ar1，X，Y，P，Q和Het在本文中定义，其可用作某些蛋白酪氨酸激酶的抑制剂，因此可用于治疗由不适当的细胞增殖引起的疾病， 包括自身免疫性疾病，慢性炎症性疾病，过敏性疾病，移植排斥和癌症，以及由脑缺血引起的病症，例如中风。 还公开了包含这些化合物的药物组合物，制备这些化合物的方法和用于这些方法的新型中间体化合物。
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公开(公告)号：US08318723B2
公开(公告)日：2012-11-27
申请号：US12377283
申请日：2007-08-15
IPC分类号： A61K31/55 , A61K31/4965
CPC分类号： C07D401/10 , C07D213/74 , C07D241/20 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.
摘要翻译： 本发明提供式（I）化合物的用途和制备方法，其中A，X，Y，R 1，R 2和R 3在本文中定义。 本发明的化合物抑制参与炎症过程和异常细胞增殖的特异性丝氨酸/苏氨酸激酶，因此可用于治疗相关疾病和病理状况，例如Pim激酶介导的疾病和涉及炎症的病理状况，包括Chron氏病，炎性肠 疾病，类风湿性关节炎和慢性炎症性疾病，或包括各种癌症在内的异常细胞增殖。
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公开(公告)号：US20100280028A1
公开(公告)日：2010-11-04
申请号：US12768268
申请日：2010-04-27
申请人： Jennifer A. KOWALSKI , Daniel Richard MARSHALL , Anthony S. PROKOPOWICZ, III , Sabine SCHLYER , Robert SIBLEY , Ronald John SORCEK , Di WU , Frank WU , Erick Richard Roush YOUNG
发明人： Jennifer A. KOWALSKI , Daniel Richard MARSHALL , Anthony S. PROKOPOWICZ, III , Sabine SCHLYER , Robert SIBLEY , Ronald John SORCEK , Di WU , Frank WU , Erick Richard Roush YOUNG
IPC分类号： A61K31/5377 , C07D403/14 , A61K31/506 , C07D413/14 , A61K31/497 , C07D241/04 , A61K31/4965 , C07D401/12 , A61P29/00 , A61P9/00 , A61P37/00
CPC分类号： C07D471/04 , C07D209/48 , C07D213/26 , C07D213/56 , C07D213/65 , C07D213/74 , C07D217/00 , C07D231/10 , C07D233/90 , C07D235/04 , C07D239/34 , C07D239/42 , C07D277/30 , C07D295/185 , C07D307/68 , C07D317/68 , C07D319/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D491/08
摘要： The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 to R5, A, B, D and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，其中R 1至R 5，A，B，D和X如本文所定义。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。
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公开(公告)号：US07550473B2
公开(公告)日：2009-06-23
申请号：US10933635
申请日：2004-09-03
申请人： Mario G. Cardozo , Derek Cogan , Charles Lawrence Cywin , George Dahmann , Darren DiSalvo , John David Ginn , Anthony S. Prokopowicz, III , Denice M. Spero , Erick Richard Roush Young
发明人： Mario G. Cardozo , Derek Cogan , Charles Lawrence Cywin , George Dahmann , Darren DiSalvo , John David Ginn , Anthony S. Prokopowicz, III , Denice M. Spero , Erick Richard Roush Young
IPC分类号： C07D239/42 , A61K31/505
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D471/04 , H01L51/0089
摘要： Disclosed are novel compounds of formula (I): wherein R1, R2 and R3 are as defined herein, which are useful as inhibitors of PKC-theta and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC-theta, including immunological disorders and type II diabetes. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
摘要翻译： 公开了式（I）的新化合物：其中R 1，R 2和R 3如本文所定义，其可用作PKC-θ的抑制剂，因此可用于治疗通过该活性介导或维持的多种疾病和病症 的PKC-θ，包括免疫学障碍和II型糖尿病。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗各种疾病和病症的方法，制备这些化合物的方法和可用于这些方法的中间体。
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公开(公告)号：US07125996B2
公开(公告)日：2006-10-24
申请号：US10955129
申请日：2004-09-30
申请人： Anthony S. Prokopowicz, III , Martha Priscilla Brown , Jessi Marie Wildeson , Scott Jakes , Mark E. Labadia
发明人： Anthony S. Prokopowicz, III , Martha Priscilla Brown , Jessi Marie Wildeson , Scott Jakes , Mark E. Labadia
IPC分类号： C07D239/30 , C07D233/96 , A61K31/506 , C09K11/06
CPC分类号： C07D405/12 , C09B11/24 , C09B55/003 , C12Q1/485 , G01N33/533 , G01N33/573 , G01N33/582 , G01N2500/02
摘要： The invention provides methods relating to a novel screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.
摘要翻译： 本发明提供了可应用于蛋白激酶基因家族的广泛成员的新型筛选测定形式的方法。 该测定使用本文所述的一系列标记的可被抑制剂代替的活性位点探针。 用于抑制剂化合物的K 基于用于激酶的探针的KⅢ和抑制剂的剂量反应而衍生。 本发明还提供适用于筛选方法的活性位点探针。
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公开(公告)号：US06489328B2
公开(公告)日：2002-12-03
申请号：US09921510
申请日：2001-08-02
申请人： Roger John Snow , Donghong A. Gao , Daniel R. Goldberg , Abdelhakim Hammach , Daniel Kuzmich , Tina Marie Morwick , Neil Moss , Anthony S. Prokopowicz, III , Robert D. Selliah , Hidenori Takahashi
发明人： Roger John Snow , Donghong A. Gao , Daniel R. Goldberg , Abdelhakim Hammach , Daniel Kuzmich , Tina Marie Morwick , Neil Moss , Anthony S. Prokopowicz, III , Robert D. Selliah , Hidenori Takahashi
IPC分类号： C07D48704
CPC分类号： C07D487/04 , A61K31/517
摘要： Disclosed are novel compounds of formula (I): wherein Ar1, X, Y, P, Q and Het are defined herein, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are pharmaceutical compositions comprising these compounds, processes for preparing these compounds and novel intermediate compounds useful in these processes.
摘要翻译： 公开了式（I）的新化合物：其中Ar1，X，Y，P，Q和Het在本文中定义，其可用作某些蛋白酪氨酸激酶的抑制剂，因此可用于治疗由不适当的细胞增殖引起的疾病， 包括自身免疫性疾病，慢性炎症性疾病，过敏性疾病，移植排斥和癌症，以及由脑缺血引起的病症，例如中风。 还公开了包含这些化合物的药物组合物，制备这些化合物的方法和用于这些方法的新型中间体化合物。
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公开(公告)号：US20100210627A1
公开(公告)日：2010-08-19
申请号：US12377283
申请日：2007-08-15
IPC分类号： A61K31/55 , C07D241/20 , A61K31/4965 , A61P35/02 , A61P35/00 , A61P19/02 , A61P25/28 , A61P9/10 , C07D401/12 , A61K31/497 , C07D403/02 , A61K31/551 , C07D413/02 , A61K31/5377
CPC分类号： C07D401/10 , C07D213/74 , C07D241/20 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04
摘要： The invention provides compounds according to formula (I) their use and methods for preparation wherein A, X, Y, R1, R2 and R3 are defined herein. The compounds of the invention inhibit specific serine/threonine kinases involved in inflammatory processes and aberrant cell proliferation, and are thus useful for treating associated diseases and pathological conditions such as Pim kinase-mediated diseases and pathological conditions involving inflammation, including Chron's disease, inflammatory bowel disease, rheumatoid arthritis, and chronic inflammatory disease, or aberrant cell proliferation including various cancers.
摘要翻译： 本发明提供式（I）化合物的用途和制备方法，其中A，X，Y，R 1，R 2和R 3在本文中定义。 本发明的化合物抑制参与炎症过程和异常细胞增殖的特异性丝氨酸/苏氨酸激酶，因此可用于治疗相关疾病和病理状况，例如Pim激酶介导的疾病和涉及炎症的病理状况，包括Chron氏病，炎性肠 疾病，类风湿性关节炎和慢性炎性疾病，或包括各种癌症在内的异常细胞增殖。
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公开(公告)号：US07588899B2
公开(公告)日：2009-09-15
申请号：US11492654
申请日：2006-07-25
申请人： Anthony S. Prokopowicz, III , Martha Priscilla Brown , Jessi Marie Wildeson , Scott Jakes , Mark E. Labadia
发明人： Anthony S. Prokopowicz, III , Martha Priscilla Brown , Jessi Marie Wildeson , Scott Jakes , Mark E. Labadia
CPC分类号： C07D405/12 , C09B11/24 , C09B55/003 , C12Q1/485 , G01N33/533 , G01N33/573 , G01N33/582 , G01N2500/02
摘要： The invention provides methods relating to a screening assay format that can be applied to broad members of the protein kinase gene family. The assay uses a series of labeled, active site probes described herein that can be displaced by an inhibitor agent. The Kd for the inhibitor compound is derived based on the Kd of the probe for the kinase and the dose response of the inhibitor agent. The invention also provides active site probes suitable for use with the screening method.
摘要翻译： 本发明提供了可应用于蛋白激酶基因家族的广泛成员的筛选测定形式的方法。 该测定使用本文所述的一系列标记的可被抑制剂代替的活性位点探针。 抑制剂化合物的Kd基于激酶的探针的Kd和抑制剂的剂量反应而衍生。 本发明还提供适用于筛选方法的活性位点探针。
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公开(公告)号：US06770639B2
公开(公告)日：2004-08-03
申请号：US10292026
申请日：2002-11-12
申请人： Roger John Snow , Mario Cardozo , Daniel Goldberg , Abdelhakim Hammach , Tina Morwick , Neil Moss , Usha R. Patel , Anthony S. Prokopowicz, III , Hidenori Takahashi , Matt Aaron Tschantz , Xiao-Jun Wang
发明人： Roger John Snow , Mario Cardozo , Daniel Goldberg , Abdelhakim Hammach , Tina Morwick , Neil Moss , Usha R. Patel , Anthony S. Prokopowicz, III , Hidenori Takahashi , Matt Aaron Tschantz , Xiao-Jun Wang
IPC分类号： A61K3133
CPC分类号： C07D471/04 , C07D217/24 , C07D235/30 , C07D513/04
摘要： Disclosed are novel compounds of formula (I): wherein Ar1, Ra, R4, R5, X and Y are defined below, which are useful as inhibitors of certain protein tyrosine kinases and are thus useful for treating diseases associated with such kinases, for example, diseases resulting from inappropriate cell proliferation, which include autoimmune diseases, chronic inflammatory diseases, allergic diseases, transplant rejection and cancer, as well as conditions resulting from cerebral ischemia, such as stroke. Also disclosed are processes for preparing these compounds, novel intermediates useful in these processes and compositions comprising compounds of the formula (I).
摘要翻译： 公开了式（I）的新化合物：其中Ar1，Ra，R4，R5，X和Y定义如下，其可用作某些蛋白酪氨酸激酶的抑制剂，因此可用于治疗与这种激酶相关的疾病，例如 由不适当的细胞增殖引起的疾病，包括自身免疫性疾病，慢性炎性疾病，过敏性疾病，移植排斥和癌症，以及脑缺血症如中风引起的疾病。 还公开了制备这些化合物的方法，可用于这些方法的新型中间体和包含式（I）化合物的组合物。
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