公开(公告)号：WO2008057280A1

公开(公告)日：2008-05-15

申请号：PCT/US2007/022712

申请日：2007-10-25

Applicant: AMGEN INC. ,  HODOUS, Brian, L. ,  GEUNS-MEYER, Stephanie, D. ,  OLIVIERI, Philip, R. ,  PATEL, Vinod, F. ,  TEMPEST, Paul

Inventor： HODOUS, Brian, L. ,  GEUNS-MEYER, Stephanie, D. ,  OLIVIERI, Philip, R. ,  PATEL, Vinod, F. ,  TEMPEST, Paul

IPC: C07D261/06 ,  C07D401/04 ,  C07D413/04

CPC classification number: C07D401/04 ,  C07D263/32 ,  C07D413/04

Abstract: The present invention relates to compounds of Formulas I and II, wherein B 1 , B 2 , B 3 , B 4 , C 1 , C 2 , ring D, L 1 , L 2 and R 1-4 are defined herein, synthetic intermediates, and pharmaceutical compositions, comprising such compounds. The compounds and compositions are capable of modulating various protein kinase receptors such as Tie-2 and Aurora and, therefore, influencing kinase related disease states and conditions. The compounds, for example, are capable of treating cancer caused by unregulated angiogenesis, and inflammation as well as other proliferative disorders.

Abstract translation: 本发明涉及式I和II的化合物，其中B 1，B 2，B 3，B 4， C 1，C 1，C 2，环D，L 1，L 2和R 2， 1-4本文中定义的合成中间体和包含这些化合物的药物组合物。 化合物和组合物能够调节各种蛋白激酶受体如Tie-2和Aurora，因此影响激酶相关的疾病状态和状况。 该化合物例如能够治疗由不受调节的血管发生，炎症以及其它增殖性疾病引起的癌症。

公开(公告)号：WO2005070891A2

公开(公告)日：2005-08-04

申请号：PCT/US2005/002326

申请日：2005-01-24

Applicant: AMGEN INC

Inventor： POTASHMAN, Michele ,  KIM, Tae-seong ,  BELLON, Steven ,  BOOKER, Shon ,  CHENG, Yuan ,  KIM, Joseph, L. ,  TASKER, Andrew ,  XI, Ning ,  XU, Shimin ,  HARMANGE, Jean-Christophe ,  BORG, George ,  WEISS, Matthew ,  HODOUS, Brian, L. ,  GRACEFFA, Russell ,  BUCKNER, Willian, H. ,  MASSE, Craig, E. ,  CHOQUETTE, Deborah ,  MARTIN, Matthew, W. ,  GERMAIN, Julie ,  DIPIETRO, Lucian, V. ,  CHAFFEE, Stuart, C. ,  NUNES, Joseph, J. ,  BUCHANAN, John, L. ,  HABGOOD, Gregory, J. ,  MCGOWAN, David, C. ,  WHITTINGTON, Douglas, A.

IPC: C07D215/00

CPC classification number: C07D213/64 ,  C07D213/81 ,  C07D215/233 ,  C07D215/38 ,  C07D215/48 ,  C07D215/54 ,  C07D237/34 ,  C07D239/34 ,  C07D239/47 ,  C07D239/84 ,  C07D239/94 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutically compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract translation: 所选化合物对于预防和治疗诸如HGF介导的疾病等疾病是有效的。 本发明包括新颖的化合物，类似物，前药和药学上可接受的盐，用于预防和治疗涉及癌症等的疾病和其它疾病或病症的药物组合物和方法。 本发明还涉及制备这些化合物的方法以及在这些方法中有用的中间体。

公开(公告)号：WO2008124083A3

公开(公告)日：2008-10-16

申请号：PCT/US2008/004432

申请日：2008-04-03

Applicant: AMGEN INC. ,  CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  DU, Bingfan ,  HODOUS, Brian, L. ,  MARTIN, Mathew, W. ,  NGUYEN, Hanh, Nho ,  OLIVIERI, Philip, R. ,  PANTER, Kathleen ,  ROMERO, Karina ,  SCHENKEL, Laurie ,  WHITE, Ryan

Inventor： CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  DU, Bingfan ,  HODOUS, Brian, L. ,  MARTIN, Mathew, W. ,  NGUYEN, Hanh, Nho ,  OLIVIERI, Philip, R. ,  PANTER, Kathleen ,  ROMERO, Karina ,  SCHENKEL, Laurie ,  WHITE, Ryan

IPC: C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D409/04 ,  C07D471/04 ,  C07D487/04 ,  C07D493/04 ,  C07D495/04 ,  A61K31/502 ,  A61P35/00

Abstract: The present invention relates to chemical compounds having a general formula (I), wherein A 1-8 , D , , L 1 , L 2 , R 1 , R 6-8 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.

公开(公告)号：WO2007100646A1

公开(公告)日：2007-09-07

申请号：PCT/US2007/004700

申请日：2007-02-22

Applicant: AMGEN INC. ,  CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  HODOUS, Brian, L. ,  NGUYEN, Hanh Nho ,  OLIVIERI, Philip R. ,  PATEL, Vinod, F. ,  ROMERO, Karina

Inventor： CEE, Victor, J. ,  DEAK, Holly, L. ,  GEUNS-MEYER, Stephanie, D. ,  HODOUS, Brian, L. ,  NGUYEN, Hanh Nho ,  OLIVIERI, Philip R. ,  PATEL, Vinod, F. ,  ROMERO, Karina

IPC: C07D401/14 ,  C07D417/14 ,  C07D413/14 ,  C07D403/12 ,  A61K31/444 ,  A61K31/4427 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D403/12 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to chemical compounds having a general formula I "INSERT STRUCTURE HERE" wherein A, B, C 1 , C 2 , D, L 1 , L 2 and R 3-4 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“INSERT STRUCTURE HERE”的化合物，其中A，B，C 1，C 2，D，L 1， / SUP>，L 2和R 3〜4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 与这种激酶的活动相关的状态和条件。 例如，这些化合物能够调节Tie-2和Aurora激酶，从而分别影响血管生成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。

公开(公告)号：WO2005113494A2

公开(公告)日：2005-12-01

申请号：PCT/US2005/016346

申请日：2005-05-09

Applicant: AMGEN INC. ,  GEUNS-MEYER, Stephanie, D. ,  HODOUS, Brian, L. ,  CHAFFEE, Stuart, C. ,  TEMPEST, Paul, A. ,  OLIVIERI, Philip, R. ,  JOHNSON, Rebecca, E. ,  ALBRECHT, Brian, K. ,  PATEL, Vinod, F. ,  CEE, Victor, J. ,  KIM, Joseph, L. ,  BELLON, Steven ,  ZHU, Xiaotian ,  CHENG, Yuan ,  XI, Ning ,  ROMERO, Karina ,  NGUYEN, Hanh, Nho ,  DEAK, Holly, L.

Inventor： GEUNS-MEYER, Stephanie, D. ,  HODOUS, Brian, L. ,  CHAFFEE, Stuart, C. ,  TEMPEST, Paul, A. ,  OLIVIERI, Philip, R. ,  JOHNSON, Rebecca, E. ,  ALBRECHT, Brian, K. ,  PATEL, Vinod, F. ,  CEE, Victor, J. ,  KIM, Joseph, L. ,  BELLON, Steven ,  ZHU, Xiaotian ,  CHENG, Yuan ,  XI, Ning ,  ROMERO, Karina ,  NGUYEN, Hanh, Nho ,  DEAK, Holly, L.

IPC: C07D1/04

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, H 1-5 and R 1-4 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，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。