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公开(公告)号：US07868177B2
公开(公告)日：2011-01-11
申请号：US11709994
申请日：2007-02-21
申请人： Victor J. Cee , Holly L. Deak , Stephanie D. Geuns-Meyer , Brian L. Hodous , Hanh Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero
发明人： Victor J. Cee , Holly L. Deak , Stephanie D. Geuns-Meyer , Brian L. Hodous , Hanh Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero
IPC分类号： C07D401/14 , C07D403/14 , A61K31/4427 , A61K31/506 , A61K31/53 , A61P19/02 , A61P35/00
CPC分类号： C07D403/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to chemical compounds having a general formula I wherein A, B, C1, C2, D, L1, L2 and R3-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Tie-2 and Aurora kinase enzymes thereby influencing angiogenesis and the process of cell cycle and cell proliferation, respectively, to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of various protein kinases.
摘要翻译： 本发明涉及具有通式I的化合物，其中A，B，C1，C2，D，L1，L2和R3-4在本文中定义，合成中间体能够调节各种蛋白激酶受体酶， 从而影响与这种激酶的活性有关的各种疾病状态和状况。 例如，化合物能够调节Tie-2和Aurora激酶，从而分别影响血管发生和细胞周期和细胞增殖过程，以治疗癌症和癌症相关疾病。 本发明还包括药物组合物，包括该化合物，以及治疗与各种蛋白激酶活性有关的疾病状态的方法。
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公开(公告)号：US07880000B2
公开(公告)日：2011-02-01
申请号：US11126000
申请日：2005-05-09
申请人： Stephanie D. Geuns-Meyer , Brian L. Hodous , Stuart C. Chaffee , Paul A. Tempest , Philip R. Olivieri , Rebecca E. Johnson , Brian K. Albrecht , Vinod F. Patel , Victor J. Cee , Joseph L. Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nho Nguyen , Holly L. Deak
发明人： Stephanie D. Geuns-Meyer , Brian L. Hodous , Stuart C. Chaffee , Paul A. Tempest , Philip R. Olivieri , Rebecca E. Johnson , Brian K. Albrecht , Vinod F. Patel , Victor J. Cee , Joseph L. Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nho Nguyen , Holly L. Deak
IPC分类号： C07D401/14 , C07D403/14 , A61K31/53 , A61K31/4427 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D213/73 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other poliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
摘要翻译： 本发明涉及具有通式I的化合物，其中A，B，D，E，G，H1-5和R1-4在本文中定义，以及能够调节各种蛋白激酶受体酶的合成中间体， 从而影响与这些激酶的活性相关的各种疾病状态和状况。 例如，这些化合物能够调节激酶，从而影响血管生成过程并治疗血管生成相关疾病和其它包括癌症和炎症的复发性疾病。 本发明还包括药物组合物，包括该化合物，以及治疗与蛋白激酶活性有关的疾病状态的方法。
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公开(公告)号：US08022221B2
公开(公告)日：2011-09-20
申请号：US12378426
申请日：2009-02-12
申请人： Victor J. Cee , Holly L. Deak , Bingfan Du , Stephanie D. Geuns-Meyer , Brian L. Hodous , Hanh Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero , Laurie Schenkel
发明人： Victor J. Cee , Holly L. Deak , Bingfan Du , Stephanie D. Geuns-Meyer , Brian L. Hodous , Hanh Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero , Laurie Schenkel
IPC分类号： C07D401/14 , C07D403/14 , A61K31/53 , A61K31/4427 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
摘要翻译： 本发明涉及具有通式I的化合物，其中A1，A2，C1，C2，D，L1，L2，Z和R3，R4，R6，R7和R8如本文所定义，其能够调节极光激酶蛋白 活动，从而影响与Aurora激酶蛋白活性相关的各种疾病状态和病症。 例如，化合物能够影响细胞周期和细胞增殖的过程，以治疗癌症和与癌症有关的疾病。 本发明还包括药物组合物，制备本发明化合物的方法，合成中间体和治疗与Aurora激酶活性有关的病症的方法。
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公开(公告)号：US08476434B2
公开(公告)日：2013-07-02
申请号：US12952156
申请日：2010-11-22
申请人： Stephanie D. Geuns-Meyer , Brian L. Hodous , Stuart C. Chaffee , Paul Tempest , Ning Xi , Phillip R. Olivieri , Joseph L. Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Brian K. Albrecht , Vinod F. Patel , Victor J. Cee , Karina Romero , Hanh Nho Nguyen , Holly L. Deak , Rebecca E. Johnson
发明人： Stephanie D. Geuns-Meyer , Brian L. Hodous , Stuart C. Chaffee , Paul Tempest , Ning Xi , Phillip R. Olivieri , Joseph L. Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Brian K. Albrecht , Vinod F. Patel , Victor J. Cee , Karina Romero , Hanh Nho Nguyen , Holly L. Deak , Rebecca E. Johnson
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , A61K31/4427 , A61K31/506 , A61K31/54 , A61P19/02 , A61P35/00
CPC分类号： C07D213/73 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A, B, D, E, G, H1-5 and R1-4 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of these kinases. For example, the compounds are capable of modulating kinase enzymes thereby influencing the process of angiogenesis and treating angiogenesis-related diseases and other proliferative disorders, including cancer and inflammation. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of protein kinases.
摘要翻译： 本发明涉及具有通式I的化合物，其中A，B，D，E，G，H1-5和R1-4在本文中定义，以及能够调节各种蛋白激酶受体酶的合成中间体， 从而影响与这些激酶的活性相关的各种疾病状态和状况。 例如，化合物能够调节激酶，从而影响血管发生过程并治疗血管生成相关疾病和其它增殖性疾病，包括癌症和炎症。 本发明还包括药物组合物，包括该化合物，以及治疗与蛋白激酶活性有关的疾病状态的方法。
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公开(公告)号：US20090163501A1
公开(公告)日：2009-06-25
申请号：US12378426
申请日：2009-02-12
申请人： Victor J. Cee , Holly L. Deak , Bingfan Du , Stephanie D. Genus-Meyer , Brain L. Hodous , Han Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero , Laurie Schenkel
发明人： Victor J. Cee , Holly L. Deak , Bingfan Du , Stephanie D. Genus-Meyer , Brain L. Hodous , Han Nho Nguyen , Philip R. Olivieri , Vinod F. Patel , Karina Romero , Laurie Schenkel
IPC分类号： A61K31/502 , C07D251/20 , C07D413/14 , C07D237/30 , A61K31/53 , A61K31/5377 , A61P35/00
CPC分类号： C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
摘要翻译： 本发明涉及具有通式I的化合物，其中A1，A2，C1，C2，D，L1，L2，Z和R3，R4，R6，R7和R8如本文所定义，其能够调节极光激酶蛋白 活动，从而影响与Aurora激酶蛋白活性相关的各种疾病状态和病症。 例如，化合物能够影响细胞周期和细胞增殖的过程，以治疗癌症和与癌症有关的疾病。 本发明还包括药物组合物，制备本发明化合物的方法，合成中间体和治疗与Aurora激酶活性有关的病症的方法。
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公开(公告)号：US07776869B2
公开(公告)日：2010-08-17
申请号：US11251490
申请日：2005-10-14
申请人： Stuart C. Chaffee , Brian K. Albrecht , Brian L. Hodous , Matthew W. Martin , David C. McGowan , Erin F. DiMauro , Gade Reddy , Victor J. Cee , Philip R. Olivieri , Anthony Reed , Karina Romero
发明人： Stuart C. Chaffee , Brian K. Albrecht , Brian L. Hodous , Matthew W. Martin , David C. McGowan , Erin F. DiMauro , Gade Reddy , Victor J. Cee , Philip R. Olivieri , Anthony Reed , Karina Romero
IPC分类号： C07D239/38 , C07D239/42 , A61K31/505 , A61K31/506 , A61P35/00
CPC分类号： C07D213/74 , C07D213/81 , C07D215/14 , C07D239/42 , C07D241/42 , C07D401/06 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症，癌症和相关病症的化合物。 化合物具有通式I，其中A1，A2，A3，A4，R1和R2如本文所定义。 因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US20100160283A1
公开(公告)日：2010-06-24
申请号：US12716187
申请日：2010-03-02
申请人： Stuart C. Chaffee , Brian K. Albrecht , Brian L. Hodous , Matthew W. Martin , David C. McGowan , Erin F. DiMauro , Gade Reddy , Victor J. Cee , Philip R. Olivieri , Anthony Reed , Karina Romero
发明人： Stuart C. Chaffee , Brian K. Albrecht , Brian L. Hodous , Matthew W. Martin , David C. McGowan , Erin F. DiMauro , Gade Reddy , Victor J. Cee , Philip R. Olivieri , Anthony Reed , Karina Romero
IPC分类号： A61K31/397 , A61P35/00 , C07D239/28 , A61K31/505 , C07D403/12 , A61K31/496 , C07D413/12 , A61K31/5377 , C07D417/12 , A61K31/541
CPC分类号： C07D213/74 , C07D213/81 , C07D215/14 , C07D239/42 , C07D241/42 , C07D401/06 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/06 , C07D409/06 , C07D413/12 , C07D417/12 , C07D471/04
摘要： The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation, cancer and related conditions. The compounds have a general Formula I wherein A1, A2, A3, A4, R1 and R2 are defined herein. Accordingly, the invention also comprises pharmaceutical compositions comprising the compounds of the invention, methods for the prophylaxis and treatment of kinase mediated diseases using the compounds and compositions of the invention, and intermediates and processes useful for the preparation of compounds of the invention.
摘要翻译： 本发明包括一类新的可用于预防和治疗蛋白激酶介导的疾病，包括炎症，癌症和相关病症的化合物。 化合物具有通式I，其中A1，A2，A3，A4，R1和R2如本文所定义。 因此，本发明还包括含有本发明化合物的药物组合物，使用本发明化合物和组合物预防和治疗激酶介导的疾病的方法，以及可用于制备本发明化合物的中间体和方法。
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公开(公告)号：US07560551B2
公开(公告)日：2009-07-14
申请号：US11655642
申请日：2007-01-18
申请人： Victor J. Cee , Hanh Nho Nguyen , Karina Romero
发明人： Victor J. Cee , Hanh Nho Nguyen , Karina Romero
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/14 , C07D417/14 , A61K31/502 , A61K31/506 , A61P19/02 , A61P35/00
CPC分类号： C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R1-8 are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
摘要翻译： 本发明涉及具有通式I的化合物，其中A1，A2，C1，C2，D，L1，L2，Z和R1-8在本文中定义，合成中间体能够调节各种蛋白激酶受体酶 从而影响与这种激酶的活性相关的各种疾病状态和状况。 例如，化合物能够调节Aurora激酶，从而影响细胞周期和细胞增殖的过程，以治疗癌症和与癌症有关的疾病。 本发明还包括药物组合物，包括该化合物，以及治疗与Aurora激酶活性有关的疾病状态的方法。
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公开(公告)号：US08686155B2
公开(公告)日：2014-04-01
申请号：US13171355
申请日：2011-06-28
IPC分类号： C07D401/14 , C07D403/14 , A61K31/4427 , A61K31/506 , A61K31/53 , A61K31/496 , A61K31/4155 , A61K31/4164 , A61K31/42 , A61K31/425 , A61P35/00
CPC分类号： C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
摘要： The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R3, R4, R6, R7 and R8 are defined herein, which are capable of modulating Aurora kinase protein activity, thereby influencing various disease states and conditions related to the activities of Aurora kinase proteins. For example, the compounds are capable of influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, processes of preparing compounds of the invention, synthetic intermediates and methods of treatment of conditions related to the activity of Aurora kinase.
摘要翻译： 本发明涉及具有通式I的化合物，其中A1，A2，C1，C2，D，L1，L2，Z和R3，R4，R6，R7和R8如本文所定义，其能够调节极光激酶蛋白 活动，从而影响与Aurora激酶蛋白活性相关的各种疾病状态和病症。 例如，化合物能够影响细胞周期和细胞增殖的过程，以治疗癌症和与癌症有关的疾病。 本发明还包括药物组合物，制备本发明化合物的方法，合成中间体和治疗与Aurora激酶活性有关的病症的方法。
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公开(公告)号：US20110212940A1
公开(公告)日：2011-09-01
申请号：US13034895
申请日：2011-02-25
申请人： Roland Burli , Victor J. Cee , Jennifer Golden , Brian Alan Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert C. Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
发明人： Roland Burli , Victor J. Cee , Jennifer Golden , Brian Alan Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa R. Cheruku , Pini Orbach , Anurag Sharadendu , Robert C. Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
IPC分类号： A61K31/397 , C07D405/10 , A61K31/4525 , C07D405/14 , A61K31/443 , C07D413/14 , A61K31/427 , C07D409/14 , A61K31/4725 , A61K31/4025 , C07D307/80 , A61K31/343 , A61K31/5377 , C07D413/10 , A61K31/41 , A61P35/00 , A61P37/06 , A61P29/00 , A61P3/10 , A61P25/00 , A61P17/06 , A61P35/02 , A61P11/00 , A61P11/06 , A61P17/02 , A61P9/00 , A61P9/10 , A61P13/12 , A61P1/16 , A61P7/06
CPC分类号： C07D307/79 , C07D307/80 , C07D307/81 , C07D403/10 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of the general formula (I) that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds may be used as immunomodulators, e.g., for treating or preventing diseases such as autoimmune and related immune disorders including systemic lupus erythematosus, inflammatory bowel diseases such as Crohn's disease and ulcerative colitis, type I diabetes, uveitis, psoriasis, myasthenia gravis, rheumatoid arthritis, non-glomerular nephrosis, hepatitis, Behçet's disease, glomerulonephritis, chronic thrombocytopenic purpura, hemolytic anemia, hepatitis and Wegner's granuloma; and for treating other conditions.
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