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：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：US20130267496A1

公开(公告)日：2013-10-10

申请号：US13901523

申请日：2013-05-23

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 ,  C07D498/04 ,  C07D498/08 ,  C07D471/04 ,  C07D491/107

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D491/107 ,  C07D498/04 ,  C07D498/08 ,  C07D519/00

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：US20130237521A1

公开(公告)日：2013-09-12

申请号：US13868971

申请日：2013-04-23

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 ,  C07D471/04 ,  C07D498/04 ,  C07D491/107

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.

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：US20180086769A1

公开(公告)日：2018-03-29

申请号：US15719399

申请日：2017-09-28

Applicant: Gilead Connecticut, Inc.

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

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

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：US20170217967A1

公开(公告)日：2017-08-03

申请号：US15484844

申请日：2017-04-11

Applicant: Gilead Connecticut, Inc.

Inventor： Tim G. Elford ,  Peter Chee-Chu Fung ,  Michael Laird Hurrey ,  Dimitrios Stefanidis ,  Dragos Vizitiu

IPC: C07D487/04

CPC classification number: C07D487/04 ,  C07C309/04

Abstract: Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

公开(公告)号：US20170121350A1

公开(公告)日：2017-05-04

申请号：US15404120

申请日：2017-01-11

Applicant: Gilead Connecticut, Inc.

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

IPC: C07D519/00 ,  C07D471/04 ,  A61K9/00 ,  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.

公开(公告)号：US08765761B2

公开(公告)日：2014-07-01

申请号：US13868967

申请日：2013-04-23

Applicant: Gilead Connecticut, Inc.

Inventor： Scott A. Mitchell ,  Kevin S. Currie

IPC: A61K31/495

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

Abstract: An imidazopyrazine 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：US20130310363A1

公开(公告)日：2013-11-21

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: C07D487/04

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。