公开(公告)号：US09505785B2

公开(公告)日：2016-11-29

申请号：US14059626

申请日：2013-10-22

Applicant: GILEAD CONNECTICUT, INC. ,  GENENTECH, INC.

Inventor： Antonio J. M. Barbosa ,  Peter A. Blomgren ,  Kevin S. Currie ,  Ravi Krishnamoorthy ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Scott A. Mitchell ,  Daniel Ortwine ,  Aaron C. Schmitt ,  Xiaojing Wang ,  Jianjun Xu ,  Wendy Young ,  Honglu Zhang ,  Zhongdong Zhao ,  Pavel E. Zhichkin

IPC: C07D519/00 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07D471/14

CPC classification number: C07D519/00 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07C69/65 ,  C07D209/52 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07F5/04

Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US10344040B2

公开(公告)日：2019-07-09

申请号：US15905363

申请日：2018-02-26

Applicant: GILEAD CONNECTICUT, INC. ,  GENENTECH INC.

Inventor： Antonio J. M. Barbosa ,  Peter A. Blomgren ,  Kevin S. Currie ,  Ravi Krishnamoorthy ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Scott A. Mitchell ,  Daniel Ortwine ,  Aaron C. Schmitt ,  Xiaojing Wang ,  Jianjun Xu ,  Wendy Young ,  Honglu Zhang ,  Zhongdong Zhao ,  Pavel E. Zhichkin

IPC: C07D487/04 ,  C07D519/00 ,  C07D495/04 ,  C07D498/04 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07D471/14 ,  C07C69/65 ,  C07D209/52 ,  C07F5/04

Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US10053469B2

公开(公告)日：2018-08-21

申请号：US15281923

申请日：2016-09-30

Applicant: GILEAD CONNECTICUT, INC. ,  GENENTECH INC.

Inventor： Antonio J. M. Barbosa ,  Peter A. Blomgren ,  Kevin S. Currie ,  Ravi Krishnamoorthy ,  Jeffrey E. Kropf ,  Seung H. Lee ,  Scott A. Mitchell ,  Daniel Ortwine ,  Aaron C. Schmitt ,  Xiaojing Wang ,  Jianjun Xu ,  Wendy Young ,  Honglu Zhang ,  Zhongdong Zhao ,  Pavel E. Zhichkin

IPC: C07D519/00 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07D471/14 ,  C07C69/65 ,  C07D209/52 ,  C07F5/04

CPC classification number: C07D519/00 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/551 ,  A61K45/06 ,  C07C69/65 ,  C07D209/52 ,  C07D471/14 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07F5/04

Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US08748607B2

公开(公告)日：2014-06-10

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: C07D497/00

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

Abstract: Certain imidazopyrazines having the structure of formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are as defined herein, 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: 具有式（I）结构的某些咪唑并吡嗪或其药学上可接受的盐，其中R1，R2，R3，R4和R5如本文所定义，及其药物组合物在本文中提供。 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：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：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.