公开(公告)号：US20140371201A1

公开(公告)日：2014-12-18

申请号：US14302337

申请日：2014-06-11

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  Alessandro BOEZIO ,  Christiane BOEZIO ,  John R. BUTLER ,  Margaret Yuhua CHU-MOYER ,  Erin F. DIMAURO ,  Thomas DINEEN ,  Russell GRACEFFA ,  Angel GUZMAN-PEREZ ,  Hongbing HUANG ,  Charles KREIMAN ,  Daniel LA ,  Isaac E. MARX ,  Benjamin Charles MILGRIM ,  Hanh Nho NGUYEN ,  Emily PETERSON ,  Karina ROMERO ,  Brian SPARLING

IPC: C07D471/04 ,  C07D401/12 ,  C07D215/227 ,  C07D417/12 ,  C07C53/18 ,  C07D413/12 ,  C07D413/14

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav1.7。 该化合物可用于治疗与钠通道活性相关的疾病，例如疼痛障碍和瘙痒。 还提供含有本发明化合物的药物组合物。

公开(公告)号：US20160046626A1

公开(公告)日：2016-02-18

申请号：US14920833

申请日：2015-10-22

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  Alessandro BOEZIO ,  Christiane BOEZIO ,  John R. BUTLER ,  Margaret Yuhua CHU-MOYER ,  Erin F. DIMAURO ,  Thomas DINEEN ,  Russell GRACEFFA ,  Angel GUZMAN-PEREZ ,  Hongbing HUANG ,  Charles KREIMAN ,  Daniel LA ,  Isaac E. MARX ,  Benjamin Charles MILGRAM ,  Hanh Nho NGUYEN ,  Emily Anne PETERSON ,  Karina R. VAIDA ,  Brian SPARLING

IPC: C07D471/04 ,  C07D417/12 ,  C07D413/14 ,  C07D413/12 ,  C07D401/12

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, and pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases associated with the activity of sodium channels such as pain disorders and itch. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物及其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav1.7。 该化合物可用于治疗与钠通道活性相关的疾病，例如疼痛障碍和瘙痒。 还提供含有本发明化合物的药物组合物。

公开(公告)号：US20140066430A1

公开(公告)日：2014-03-06

申请号：US14045715

申请日：2013-10-03

Applicant: Amgen Inc.

Inventor： Victor J. CEE ,  Holly L. DEAK ,  Bingfan DU ,  Stephanie D. GEUNS-MEYER ,  Brian L. HODOUS ,  Hanh Nho NGUYEN ,  Philip R. Olivieri ,  Vinod F. Patel ,  Karina ROMERO ,  Laurie Schenkel

IPC: C07D401/14 ,  C07D491/048 ,  C07D417/14 ,  C07D409/14 ,  C07D471/04 ,  C07D495/04

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 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.

Abstract translation: 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。

公开(公告)号：US20160137636A1

公开(公告)日：2016-05-19

申请号：US14898070

申请日：2014-06-11

Applicant: AMGEN INC.

Inventor： Matthew WEISS ,  Erin F. DIMAURO ,  Thomas DINEEN ,  Russell GRACEFFA ,  Angel GUZMAN-PEREZ ,  Hongbing HUANG ,  Charles KREIMAN ,  Isaac E. MARX ,  Hanh Nho NGUYEN ,  Emily Anne PETERSON ,  Holly L. DEAK

IPC: C07D417/14 ,  C07D413/14 ,  C07D401/14 ,  C07D403/12 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

CPC classification number: C07D417/14 ,  C07C53/18 ,  C07D215/227 ,  C07D215/36 ,  C07D241/44 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav1.7。 该化合物可用于治疗可通过抑制钠通道（例如疼痛障碍）治疗的疾病。 还提供含有本发明化合物的药物组合物。

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：US20130150339A1

公开(公告)日：2013-06-13

申请号：US13707096

申请日：2012-12-06

Applicant: Amgen Inc.

Inventor： Christiane BOEZIO ,  Howard BREGMAN ,  James R. COATS ,  Erin F. DIMAURO ,  Thomas DINEEN ,  Bingfan DU ,  Russell GRACEFFA ,  Charles KREIMAN ,  Daniel LA ,  Isaac E. MARX ,  Nagasree CHAKKA ,  Hanh Nho NGUYEN ,  Emily Anne PETERSON ,  Matthew WEISS ,  Katrina W. COPELAND ,  Holly L. DEAK ,  Alessandro BOEZIO

IPC: C07D498/04 ,  C07D471/04 ,  C07D401/14 ,  C07D417/12 ,  C07D417/14

CPC classification number: C07D498/04 ,  C07D239/42 ,  C07D277/52 ,  C07D285/08 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: The present invention provides compounds of Formula I, or pharmaceutically acceptable salts thereof, that are inhibitors of voltage-gated sodium channels, in particular Nav 1.7. The compounds are useful for the treatment of diseases treatable by inhibition of sodium channels such as pain disorders. Also provided are pharmaceutical compositions containing compounds of the present invention.

Abstract translation: 本发明提供式I化合物或其药学上可接受的盐，其是电压门控钠通道的抑制剂，特别是Nav 1.7。 该化合物可用于治疗可通过抑制钠通道（例如疼痛障碍）治疗的疾病。 还提供含有本发明化合物的药物组合物。