公开(公告)号：US20140336182A1

公开(公告)日：2014-11-13

申请号：US13893182

申请日：2013-05-13

Applicant: Amgen Inc.

Inventor： Victor J. CEE ,  Holly L. DEAK ,  Bingfan DU ,  Stephanie D. GEUNS-MEYER ,  Zihao HUA ,  Matthew W. MARTIN ,  Isaac MARX ,  Hanh Nho NGUYEN ,  Philip R. OLIVIERI ,  Kathleen PANTER FABER ,  Karina ROMERO ,  Laurie SCHENKEL ,  Ryan WHITE

IPC: C07D495/04 ,  C07D491/048 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D495/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D491/048

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。

公开(公告)号：US20130165445A1

公开(公告)日：2013-06-27

申请号：US13757438

申请日：2013-02-01

Applicant: AMGEN INC.

Inventor： Ryan WHITE ,  Jason HUMAN

IPC: C07D487/04

CPC classification number: C07D487/04

Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-5 and 7-8, D′, L1, L2, R1, R3, R6-8, n and o are defined herein, and synthetic intermediates, which are capable of modulating the activity of Aurora kinase proteins and, thereby, influencing various disease states and conditions related to the activities of Aurora kinases. 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, 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A1-5和7-8，D'，L1，L2，R1，R3，R6-8，n和o如本文所定义，和合成中间体，其能够 调节极光激酶蛋白的活性，从而影响与极光激酶活性相关的各种疾病状态和状况。 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，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。