公开(公告)号：WO2021126816A1

公开(公告)日：2021-06-24

申请号：PCT/US2020/065050

申请日：2020-12-15

Applicant: AMGEN INC.

Inventor： HENARY, Haby ,  LIPFORD, James, Russell ,  CEE, Victor, J.

IPC: A61K31/519 ,  A61K45/06 ,  A61P35/00

Abstract: A method of treating cancer comprising administering to a subject in need thereof the compound AMG510 in a daily dose of 180 mg, 270 mg, 360 mg, 540 mg, 720 mg, or 960 mg.

公开(公告)号：WO2020106640A1

公开(公告)日：2020-05-28

申请号：PCT/US2019/062051

申请日：2019-11-18

Applicant: AMGEN INC.

Inventor： SHIN, Youngsook ,  CEE, Victor, J. ,  TEGLEY, Christopher, M. ,  LANMAN, Brian, Alan ,  WURZ, Ryan, Paul ,  YANG, Kevin, C. ,  MA, Vu, Van ,  ERLANSON, Daniel ,  JEONG, Joon, Won ,  FUCINI, Raymond, V. ,  IWIG, Jeffrey

IPC: A61K31/404 ,  A61K31/4427 ,  A61K31/497 ,  A61K31/506 ,  A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：WO2019213526A1

公开(公告)日：2019-11-07

申请号：PCT/US2019/030606

申请日：2019-05-03

Applicant: AMGEN INC.

Inventor： WURZ, Ryan Paul ,  CEE, Victor, J. ,  AMEGADZIE, Albert ,  CHEN, Ning ,  LANMAN, Brian, Alan ,  BARTBERGER, Michael, D.

IPC: C07F9/6561 ,  A61K31/553 ,  A61K45/06

Abstract: Provided herein are KRAS G12C inhibitors, composition of the same, and methods of using the same. These inhibitors are useful for treating a number of disorders, including pancreatic, colorectal, and lung cancers.

公开(公告)号：WO2009154775A1

公开(公告)日：2009-12-23

申请号：PCT/US2009/003666

申请日：2009-06-18

Applicant: AMGEN INC. ,  CEE, Victor, J. ,  FROHN, Michael, J. ,  NIERA, Susana, C. ,  LANMAN, Brian, Alan ,  REED, Anthony, B. ,  SHAM, Kelvin, K., C.

Inventor： CEE, Victor, J. ,  FROHN, Michael, J. ,  NIERA, Susana, C. ,  LANMAN, Brian, Alan ,  REED, Anthony, B. ,  SHAM, Kelvin, K., C.

IPC: A61K31/00

CPC classification number: C07D513/04 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/48

Abstract: The present invention relates to compounds of Formula (I), that 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.

Abstract translation: 本发明涉及具有作为S1P受体调节剂的活性的式（I）化合物，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。

公开(公告)号：WO2010126895A1

公开(公告)日：2010-11-04

申请号：PCT/US2010/032593

申请日：2010-04-27

Applicant: AMGEN INC. ,  ANDREWS, Kristin ,  BO, Yunxin, Y. ,  BOOKER, Shon ,  CEE, Victor, J. ,  D'ANGELO, Noel ,  HERBERICH, Bradley, J. ,  HONG, Fang-Tsao ,  JACKSON, Claire, L., M. ,  LANMAN, Brian, A. ,  LIAO, Hongyu ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark, H. ,  PETTUS, Liping, H. ,  REED, Anthony, B. ,  SMITH, Adrian, L. ,  TADESSE, Seifu ,  TAMAYO, Nuria, A. ,  WU, Bin ,  WURZ, Ryan ,  YANG, Kevin

Inventor： ANDREWS, Kristin ,  BO, Yunxin, Y. ,  BOOKER, Shon ,  CEE, Victor, J. ,  D'ANGELO, Noel ,  HERBERICH, Bradley, J. ,  HONG, Fang-Tsao ,  JACKSON, Claire, L., M. ,  LANMAN, Brian, A. ,  LIAO, Hongyu ,  LIU, Longbin ,  NISHIMURA, Nobuko ,  NORMAN, Mark, H. ,  PETTUS, Liping, H. ,  REED, Anthony, B. ,  SMITH, Adrian, L. ,  TADESSE, Seifu ,  TAMAYO, Nuria, A. ,  WU, Bin ,  WURZ, Ryan ,  YANG, Kevin

IPC: C07D401/14 ,  C07D473/00 ,  A61K31/52 ,  A61P35/00

CPC classification number: C07D473/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

Abstract: The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; methods of treating diseases or conditions, such as cancer, using the compounds; and pharmaceutical compositions containing the compounds, wherein the variables are as defined herein.

Abstract translation: 本发明涉及式I化合物或其药学上可接受的盐; 使用该化合物治疗疾病或病症如癌症的方法; 和含有这些化合物的药物组合物，其中变量如本文所定义。

公开(公告)号：EP1751136A2

公开(公告)日：2007-02-14

申请号：EP05779977.7

申请日：2005-05-09

Applicant: AMGEN INC.

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: C07D401/04

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, 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.

公开(公告)号：WO2009154780A1

公开(公告)日：2009-12-23

申请号：PCT/US2009/003673

申请日：2009-06-18

Applicant: AMGEN INC. ,  EPIX PHARMACEUTICALS ,  CEE, Victor, J. ,  LIN, Jian ,  YU, Xiang, Y. ,  ZHANG, Zhaoda

Inventor： CEE, Victor, J. ,  LIN, Jian ,  YU, Xiang, Y. ,  ZHANG, Zhaoda

IPC: C07D307/78 ,  C07D405/04 ,  C07D405/10 ,  C07D409/10 ,  A61K31/343 ,  A61K31/397 ,  A61P25/00

CPC classification number: C07D513/04 ,  A61K9/2018 ,  A61K9/2059 ,  A61K9/48

Abstract: 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.

Abstract translation: 本发明涉及具有作为S1P受体调节剂的活性的式（I）化合物，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。

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。