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公开(公告)号：US20120088749A1
公开(公告)日：2012-04-12
申请号：US13327951
申请日：2011-12-16
Applicant: Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
Inventor： Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
IPC: A61K31/397 , C07D401/10 , A61K31/4427 , A61P37/06 , A61P29/00 , A61P35/02 , A61P3/10 , A61P25/00 , A61P17/06 , A61P1/04 , A61P1/00 , C07D205/04 , A61P19/04
CPC classification number: C07D205/04 , C07D401/10
Abstract: The present invention relates to amides 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.
Abstract translation: 本发明涉及具有作为S1P受体调节剂的活性的酰胺和这些化合物用于治疗与不适当的S1P受体活性相关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US08080542B2
公开(公告)日：2011-12-20
申请号：US12234514
申请日：2008-09-19
Applicant: Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
Inventor： Susana C. Neira , Xiang Yu , Roland Burli , Victor Cee , Brian Lanman
IPC: A61K31/397 , C07D205/04
CPC classification number: C07D205/04 , C07D401/10
Abstract: The present invention relates to amides that have activity as SIP 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.
Abstract translation: 本发明涉及具有作为SIP受体调节剂的活性的酰胺和这些化合物用于治疗与不适当的S1P受体活性相关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20070185111A1
公开(公告)日：2007-08-09
申请号：US11655642
申请日：2007-01-18
Applicant: Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Brian Hodous , Hanh Nguyen , Philip Olivieri , Vinod Patel , Karina Romero , Laurie Schenkel
Inventor： Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Brian Hodous , Hanh Nguyen , Philip Olivieri , Vinod Patel , Karina Romero , Laurie Schenkel
IPC: A61K31/53 , A61K31/503 , C07D403/14
CPC classification number: C07D401/14 , C07D237/30 , C07D239/42 , C07D401/04 , C07D409/04 , C07D409/14 , C07D417/14 , C07D471/04 , C07D491/048 , C07D495/04 , C07D497/04
Abstract: The present invention relates to chemical compounds having a general formula I wherein A1, A2, C1, C2, D, L1, L2, Z and R1- 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.
Abstract translation: 本发明涉及具有通式I的化合物，其中A 1，A 2，C 1，C 2， 本文定义的SUP，D，L 1，L 2，Z和R 1 - 以及能够调节的合成中间体 各种蛋白激酶受体酶，从而影响与这些激酶的活性相关的各种疾病状态和病症。 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：US20060217380A1
公开(公告)日：2006-09-28
申请号：US11251490
申请日：2005-10-14
Applicant: Stuart Chaffee , Brian Albrecht , Brian Hodous , Matthew Martin , David McGowan , Erin DiMauro , Gade Reddy , Victor Cee , Philip Olivieri , Anthony Reed , Karina Romero
Inventor： Stuart Chaffee , Brian Albrecht , Brian Hodous , Matthew Martin , David McGowan , Erin DiMauro , Gade Reddy , Victor Cee , Philip Olivieri , Anthony Reed , Karina Romero
IPC: A61K31/517 , A61K31/5377 , A61K31/503
CPC classification number: 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
Abstract: 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.
Abstract translation: 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A 1，A 2，A 3，A 4，R 4， 本文定义了SUP> 1和R 2。 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：US20120122847A1
公开(公告)日：2012-05-17
申请号：US13157195
申请日：2011-06-09
Applicant: Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Zihao Hua , Matthew Martin , Issac Marx , Hanh Nho Nguyen , Philip Olivieri , Kathleen Panter , Karina Romero , Laurie Schenkel , Ryan White
Inventor： Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Zihao Hua , Matthew Martin , Issac Marx , Hanh Nho Nguyen , Philip Olivieri , Kathleen Panter , Karina Romero , Laurie Schenkel , Ryan White
IPC: A61K31/502 , A61P35/00 , C07D413/14 , A61K31/5377 , C07D471/04 , A61K31/55
CPC classification number: C07D471/04 , C07D401/12 , C07D401/14 , C07D487/04 , C07D493/04 , C07D495/04
Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n 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.
Abstract translation: 本发明涉及具有通式I的化合物，其中A1-8，D'，L1，L2，R1，R6-8和n定义在本文中，以及合成中间体，其能够调节各种蛋白激酶受体酶和 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：US07776857B2
公开(公告)日：2010-08-17
申请号：US12080669
申请日：2008-04-03
Applicant: Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Brian L. Hodous , Zihao Hua , Matthew Martin , Isaac Marx , Hanh Nho Nguyen , Philip Olivieri , Kathleen Panter , Karina Romero , Laurie Schenkel , Ryan White
Inventor： Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Brian L. Hodous , Zihao Hua , Matthew Martin , Isaac Marx , Hanh Nho Nguyen , Philip Olivieri , Kathleen Panter , Karina Romero , Laurie Schenkel , Ryan White
IPC: C07D237/30
CPC classification number: C07D471/04 , C07D401/12 , C07D401/14 , C07D487/04 , C07D493/04 , C07D495/04
Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n 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.
Abstract translation: 本发明涉及具有通式I的化合物，其中A1-8，D'，L1，L2，R1，R6-8和n定义在本文中，以及合成中间体，其能够调节各种蛋白激酶受体酶和 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：US20070213325A1
公开(公告)日：2007-09-13
申请号：US11709994
申请日：2007-02-21
Applicant: Victor Cee , Holly Deak , Stephanie Geuns-Meyer , Brian Hodous , Hanh Nho Nguyen , Philip Olivieri , Vinod Patel , Karina Romero
Inventor： Victor Cee , Holly Deak , Stephanie Geuns-Meyer , Brian Hodous , Hanh Nho Nguyen , Philip Olivieri , Vinod Patel , Karina Romero
IPC: A61K31/541 , A61K31/5377 , A61K31/506 , A61K31/53 , C07D403/02 , C07D413/02 , C07D417/02
CPC classification number: C07D403/12 , C07D401/14 , C07D413/14 , C07D417/14
Abstract: 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.
Abstract translation: 本发明涉及具有通式I的化合物，其中A，B，C 1，C 2，D，L 1，L 本文定义了本发明的第二和第三和第三十四种以及合成中间体，其能够调节各种蛋白激酶受体酶，从而影响各种疾病状态和与 这种激酶的活性。 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：US20080027036A1
公开(公告)日：2008-01-31
申请号：US11726351
申请日：2007-03-21
Applicant: Roland Burli , Victor Cee , Jennifer Golden , Brian Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
Inventor： Roland Burli , Victor Cee , Jennifer Golden , Brian Lanman , Susana Neira , Ashis Saha , Nili Schutz , Xiang Yu , Dilara McCauley , Mercedes Lobera , Yael Marantz , Jian Lin , Srinivasa Cheruku , Pini Orbach , Anurag Sharadendu , Robert Penland , Kimberley Gannon , Sharon Shacham , Silvia Noiman , Oren Becker , Zhaoda Zhang
IPC: A61K31/397 , A61K31/343 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/5377 , A61P1/00 , A61P19/02 , A61P29/00 , A61P3/10 , A61P35/00 , A61P37/00 , A61P43/00 , C07D205/12 , C07D213/00 , C07D217/00 , C07D221/00 , C07D235/02 , C07D239/70 , C07D257/04 , C07D263/52 , C07D277/00 , C07D295/00 , C07D307/77
CPC classification number: 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
Abstract: 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.
Abstract translation: 本发明涉及具有作为S1P受体调节剂的活性的通式（I）的化合物，以及这些化合物用于治疗与不适当的S1P受体活性有关的疾病的用途。 这些化合物可用作免疫调节剂，例如用于治疗或预防诸如自身免疫性疾病和相关免疫疾病（包括系统性红斑狼疮），炎症性肠病如克罗恩病和溃疡性结肠炎，I型糖尿病，葡萄膜炎，牛皮癣，重症肌无力，类风湿 关节炎，非肾小球性肾病，肝炎，白塞病，肾小球性肾炎，慢性血小板减少性紫癜，溶血性贫血，肝炎和韦格纳肉芽肿; 并处理其他条件。
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公开(公告)号：US20060009453A1
公开(公告)日：2006-01-12
申请号：US11126000
申请日：2005-05-09
Applicant: Stephanie Geuns-Meyer , Brian Hodous , Stuart Chaffee , Paul Tempest , Philip Olivieri , Rebecca Johnson , Brian Albrecht , Vinod Patel , Victor Cee , Joseph Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nguyen , Holly Deak
Inventor： Stephanie Geuns-Meyer , Brian Hodous , Stuart Chaffee , Paul Tempest , Philip Olivieri , Rebecca Johnson , Brian Albrecht , Vinod Patel , Victor Cee , Joseph Kim , Steven Bellon , Xiaotian Zhu , Yuan Cheng , Ning Xi , Karina Romero , Hanh Nguyen , Holly Deak
IPC: A61K31/53 , A61K31/506 , C07D43/14
CPC classification number: C07D213/73 , C07D239/42 , C07D401/04 , C07D401/14 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D471/04
Abstract: 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.
Abstract translation: 本发明涉及具有通式I的化合物，其中A，B，D，E，G，H 1-5和R 1-4如本文所定义， 和合成中间体，其能够调节各种蛋白激酶受体酶，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：US20090069297A1
公开(公告)日：2009-03-12
申请号：US12080669
申请日：2008-04-03
Applicant: Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Brian L. Hodous , Zihao Hua , Mathew Martin , Isaac Marx , Hanh Nho Nguyen , Philip Olivieri , Kathleen Panter , Karina Romero , Laurie Schenkel , Ryan White
Inventor： Victor Cee , Holly Deak , Bingfan Du , Stephanie Geuns-Meyer , Brian L. Hodous , Zihao Hua , Mathew Martin , Isaac Marx , Hanh Nho Nguyen , Philip Olivieri , Kathleen Panter , Karina Romero , Laurie Schenkel , Ryan White
IPC: A61K31/502 , C07D237/30 , A61K31/55 , A61P35/00 , C07D403/14
CPC classification number: C07D471/04 , C07D401/12 , C07D401/14 , C07D487/04 , C07D493/04 , C07D495/04
Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D′, L1, L2, R1, R6-8 and n 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.
Abstract translation: 本发明涉及具有通式I的化合物，其中A1-8，D'，L1，L2，R1，R6-8和n定义在本文中，以及合成中间体，其能够调节各种蛋白激酶受体酶和 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。
