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：US09212191B2

公开(公告)日：2015-12-15

申请号：US14300189

申请日：2014-06-09

Applicant: Gilead Connecticut, Inc.

Inventor： Scott A. Mitchell ,  Kevin S. Currie

IPC: A61K31/4985 ,  C07D487/04 ,  C07D498/04 ,  A61K31/495 ,  C07D519/00 ,  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-(2,3-dihydro-1H-pyrido-[2,3-b][1,4]oxazin-7-yl)-N-(4-morpholinophenyl)imidazo[1,2-a]pyrazine-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:

Abstract translation: 提供咪唑并吡嗪化合物，特别是包括6-（2,3-二氢-1H-吡啶并[2,3-b] [1,4]恶嗪-7-基）-N-（4-吗啉代苯基）咪唑并[ 2-a]吡嗪-8-胺，以下结构，以及用于抑制脾脏酪氨酸激酶用于治疗包括B细胞淋巴瘤或白血病和炎性病症的病症的方法和制剂：

公开(公告)号：US09120811B2

公开(公告)日：2015-09-01

申请号：US14274618

申请日：2014-05-09

Applicant: Gilead Connecticut, Inc.

Inventor： Scott A. Mitchell ,  Kevin S. Currie

IPC: C07D231/56 ,  C07D413/14 ,  C07D487/04 ,  C07D498/04 ,  A61K31/495 ,  C07D519/00 ,  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, including 6-(1H-indazol-6-yl)-N-(4 -moirpholinophenyl)imidazo-[1,2-a]pyrazine-8-amine: and methods for using the imidazopyrazine compounds for treating diseases and disorders responsive to the inhibition of Syk activity, including leukemia and lymphoma.

Abstract translation: 提供咪唑并吡嗪化合物，包括6-（1H-吲唑-6-基）-N-（4-咪唑啉基苯基）咪唑并[1,2-a]吡嗪-8-胺：和咪唑并吡嗪化合物用于治疗疾病的方法 以及对抑制Syk活性（包括白血病和淋巴瘤）有反应的病症。

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。

公开(公告)号：US20190117679A1

公开(公告)日：2019-04-25

申请号：US16124113

申请日：2018-09-06

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 ,  A61K31/506 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/437 ,  C07D498/04 ,  C07D487/04 ,  C12Q1/48 ,  C07D519/00 ,  A61K31/444

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：US20160031894A1

公开(公告)日：2016-02-04

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: C07D487/04 ,  G01N33/573 ,  C12Q1/48

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

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.

公开(公告)号：US08796270B2

公开(公告)日：2014-08-05

申请号：US13862147

申请日：2013-04-12

Applicant: Gilead Connecticut, Inc.

Inventor： Scott A. Mitchell

IPC: A61K31/495

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

Abstract: An imidazopyridine having the structure or a pharmaceutically acceptable salt 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: 本文提供具有结构或其药学上可接受的盐的咪唑并吡啶及其药物组合物。 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。