公开(公告)号：US10092583B2

公开(公告)日：2018-10-09

申请号：US15387557

申请日：2016-12-21

Applicant: Gilead Connecticut, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Scott A. Mitchell ,  Aaron C. Schmitt ,  Jianjun Xu ,  Zhongdong Zhao

IPC: A61K31/69 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/4985

Abstract: Certain imidazopyridines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

公开(公告)号：US09796718B2

公开(公告)日：2017-10-24

申请号：US14882278

申请日：2015-10-13

Applicant: Gilead Connecticut, Inc.

Inventor： Scott A. Mitchell ,  Kevin S. Currie ,  Peter A. Blomgren ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Jianjun Xu ,  Douglas G. Stafford ,  James P. Harding ,  Antonio J. M. Barbosa, Jr. ,  Zhongdong Zhao ,  David M. Armistead ,  Soumya Mitra

IPC: A61K31/4985 ,  C07D487/04 ,  A61K31/495 ,  C07D519/00 ,  C07D498/04 ,  C12Q1/48 ,  C07D471/04 ,  C07D491/107 ,  G01N33/573

CPC classification number: C07D487/04 ,  A61K31/495 ,  C07D471/04 ,  C07D491/107 ,  C07D498/04 ,  C07D519/00 ,  C12Q1/485 ,  G01N33/573 ,  G01N2333/91205

Abstract: Provided are imidazopyrazine compounds, particularly including 6-(benzo[d]thiazol-5-yl)-N-(3,4-dimethoxyphenyl)imidazo[1,2-a]pyrazin-8-amine, structure below, and methods and formulations for their use in inhibiting Spleen Tyrosine Kinase in treating conditions including B-cell lymphomas or leukemias and inflammatory conditions:

公开(公告)号：US20170095490A1

公开(公告)日：2017-04-06

申请号：US15387557

申请日：2016-12-21

Applicant: Gilead Connecticut, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Scott A. Mitchell ,  Aaron C. Schmitt ,  Jianjun Xu ,  Zhongdong Zhao

IPC: A61K31/69 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/506 ,  A61K31/498 ,  A61K31/538 ,  A61K31/517 ,  A61K31/5383 ,  A61K31/437

CPC classification number: A61K31/69 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  C12Q1/485

Abstract: Certain imidazopyridines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

公开(公告)号：US20150266902A1

公开(公告)日：2015-09-24

申请号：US14629390

申请日：2015-02-23

Applicant: Gilead Connecticut, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Peter A. Blomgren ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Jianjun Xu ,  Douglas G. Stafford

IPC: C07D519/00 ,  C07D471/04 ,  C07D487/04

CPC classification number: C07D519/00 ,  A61K9/0053 ,  C07D471/04 ,  C07D487/04 ,  G01N2333/9121

Abstract: Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Abstract translation: 本文提供了某些咪唑并嗪及其药物组合物。 治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 还提供了用于确定样品中Syk激酶的存在或不存在的方法。

公开(公告)号：US08962835B2

公开(公告)日：2015-02-24

申请号：US13862194

申请日：2013-04-12

Applicant: Gilead Connecticut, Inc.

Inventor： Scott A. Mitchell ,  Kevin S. Currie ,  Peter A. Blomgren ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Jianjun Xu ,  Douglas G. Stafford

IPC: C07D241/36 ,  C07D487/04 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K9/0053 ,  C07D471/04 ,  C07D487/04 ,  G01N2333/9121

Abstract: Certain imidazopyrazines of Formula (I): or pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are provided. Also provided are methods for determining the presence or absence of Syk kinase in a sample.

Abstract translation: 本文提供了式（I）的某些咪唑并吡嗪或其药学上可接受的盐及其药物组合物。 治疗患有某些对抑制Syk活性有作用的疾病和病症的患者的方法，其包括给予这些患者一定量的至少一种有效减少疾病或病症体征或症状的化学实​​体。 还提供了用于确定样品中Syk激酶的存在或不存在的方法。