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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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公开(公告)号：US07919519B2
公开(公告)日：2011-04-05
申请号：US11726351
申请日：2007-03-21
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： A61K31/404 , A61K31/381 , A61K31/343 , C07D209/12 , C07D333/56 , C07D307/80
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.
摘要翻译： 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：US20120129828A1
公开(公告)日：2012-05-24
申请号：US12995387
申请日：2009-06-18
申请人： Victor J. Cee , Jian Lin , Xiang Y. Yu , Zhaoda Zhang
发明人： Victor J. Cee , Jian Lin , Xiang Y. Yu , Zhaoda Zhang
IPC分类号： A61K31/397 , C07D409/14 , C07D409/10 , C07D405/14 , A61K31/4025 , A61K31/4525 , A61K31/4535 , A61K31/55 , A61K31/343 , A61K31/4178 , A61P25/00 , A61P19/02 , A61P1/00 , A61P11/06 , A61P3/10 , A61P11/00 , A61P31/00 , A61P35/04 , A61P35/00 , A61P35/02 , A61P21/04 , C07D405/10
CPC分类号： C07D513/04 , A61K9/2018 , A61K9/2059 , A61K9/48
摘要： The present invention relates to compounds of Formula (I) that are have activity as S1P1 receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
摘要翻译： 本发明涉及具有作为S1P1受体调节剂的活性的式（I）化合物，更具体地涉及具体为S1P1受体激动剂的化合物。 本发明还涉及使用这些化合物来治疗与不适当的S1P1受体活性相关的疾病，例如自身免疫性疾病。
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公开(公告)号：US07842685B2
公开(公告)日：2010-11-30
申请号：US12456687
申请日：2009-06-18
申请人： Victor J. Cee , Michael J. Frohn , Brian Alan Lanman , Susana C. Neira , Anthony B. Reed , Kelvin K. C. Sham
发明人： Victor J. Cee , Michael J. Frohn , Brian Alan Lanman , Susana C. Neira , Anthony B. Reed , Kelvin K. C. Sham
IPC分类号： A61K31/397 , A61K31/4365 , C07D513/04
CPC分类号： C07D513/04 , A61K9/2018 , A61K9/2059 , A61K9/48
摘要： The present invention relates to compounds of Formula (I): that are have activity as S1P receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
摘要翻译： 本发明涉及式（I）化合物：其具有作为S1P受体调节剂的活性，更具体地涉及作为S1P1受体激动剂的具体化合物。 本发明还涉及使用这些化合物来治疗与不适当的S1P1受体活性相关的疾病，例如自身免疫性疾病。
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公开(公告)号：US20140187553A1
公开(公告)日：2014-07-03
申请号：US14006285
申请日：2012-03-21
申请人： Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L.M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
发明人： Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L.M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
IPC分类号： C07D413/14 , C07D487/04 , C07D417/04 , C07D471/04 , C07D417/14
CPC分类号： C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译： 本发明涉及式I和Ia的双环化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。
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公开(公告)号：US20100029611A1
公开(公告)日：2010-02-04
申请号：US12456687
申请日：2009-06-18
申请人： Victor J. Cee , Michael J. Frohn , Brian Alan Lanman , Susana C. Neira , Anthony B. Reed , Kelvin K.C. Sham
发明人： Victor J. Cee , Michael J. Frohn , Brian Alan Lanman , Susana C. Neira , Anthony B. Reed , Kelvin K.C. Sham
IPC分类号： A61K31/397 , C07D417/14 , A61K31/437 , C07D513/04 , A61P37/00
CPC分类号： C07D513/04 , A61K9/2018 , A61K9/2059 , A61K9/48
摘要： The present invention relates to compounds of Formula (I): that are have activity as S1P receptor modulating agents, more specifically to specifically compounds that are S1P1 receptor agonists. The invention also related to the use of such compounds to treat diseases associated with inappropriate S1P1 receptor activity such as autoimmune diseases.
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公开(公告)号：US09321756B2
公开(公告)日：2016-04-26
申请号：US14006285
申请日：2012-03-21
申请人： Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L. M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
发明人： Hui-Ling Wang , Victor J. Cee , Bradley J. Herberich , Claire L. M. Jackson , Brian Alan Lanman , Thomas Nixey , Liping H. Pettus , Anthony B. Reed , Bin Wu , Ryan Wurz , Andrew Tasker
IPC分类号： C07D413/14 , C07D487/04 , C07D417/04 , C07D471/04 , C07D417/14 , A61P35/00 , A61P35/02 , A61P35/04
CPC分类号： C07D413/14 , C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04
摘要： The invention relates to bicyclic compounds of formulas I and Ia, and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer.
摘要翻译： 本发明涉及式I和Ia的双环化合物及其盐。 在一些实施方案中，本发明涉及Pim-1和/或Pim-2和/或Pim-3蛋白激酶活性或酶功能的抑制剂或调节剂。 在另外的实施方案中，本发明涉及包含本文公开的化合物的药物组合物及其在预防和治疗Pim激酶相关病症和疾病，优选癌症中的用途。
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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：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：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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