公开(公告)号：US20160166580A1

公开(公告)日：2016-06-16

申请号：US14906248

申请日：2014-07-29

Applicant: GILEAD CONNECTICUT, INC.

Inventor： Melissa Jean Casteel ,  Bei Li ,  Rowchanak Pakdaman ,  Diana Sperger ,  Dimitrios Stefanidis

IPC: A61K31/5377 ,  A61K47/10 ,  A61K47/38

CPC classification number: A61K9/2095 ,  A61K9/2027 ,  A61K9/2866 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/003 ,  B29C43/02 ,  B29K2995/0056 ,  C07C309/66 ,  C07D487/04

Abstract: Disclosed are pharmaceutical compositions comprising a compound having the formula: or a pharmaceutically acceptable salt thereof, or a hydrate of thereof, and at least one pharmaceutically acceptable polymer. The pharmaceutically acceptable salt of the compound of Formula I, or a hydrate thereof, can be a mesylate salt, including, for example, a mono-mesylate or a bis-mesylate salt, or a hydrate thereof. Also disclosed are methods of use for the pharmaceutical composition.

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：US20140336169A1

公开(公告)日：2014-11-13

申请号：US14274618

申请日：2014-05-09

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 ,  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：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。

公开(公告)号：US20140057896A1

公开(公告)日：2014-02-27

申请号：US14059626

申请日：2013-10-22

Applicant: GENENTECH, INC. ,  GILEAD CONNECTICUT, 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 ,  C07D495/04 ,  C07D487/04 ,  C07D471/14 ,  A61K31/501 ,  A61K31/5386 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/497 ,  A61K31/5025 ,  A61K31/551 ,  A61K45/06 ,  A61K31/506

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.

Abstract translation: 提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

公开(公告)号：US10266539B2

公开(公告)日：2019-04-23

申请号：US15788583

申请日：2017-10-19

Applicant: Gilead Connecticut, Inc.

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

IPC: 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：US10093684B2

公开(公告)日：2018-10-09

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: A61K31/4985 ,  C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  A61K9/00

Abstract: Certain imidazopyrazines of Formula I 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：US20180179229A1

公开(公告)日：2018-06-28

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

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：US20170073356A1

公开(公告)日：2017-03-16

申请号：US15281923

申请日：2016-09-30

Applicant: GILEAD CONNECTICUT, INC. ,  GENENTCH 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 ,  C07C69/65 ,  C07F5/04 ,  C07D209/52 ,  C07D495/04 ,  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 intro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 提供式I的吡啶酮和氮杂 - 吡啶酮化合物，包括其可用于抑制Btk激酶的立体异构体，互变异构体及其药学上可接受的盐，以及用于治疗免疫疾病如Btk激酶介导的炎症。 公开了使用式I化合物进行体外，原位和体内诊断以及哺乳动物细胞或相关病理学条件下的这些疾病的治疗的方法。

公开(公告)号：US09567348B2

公开(公告)日：2017-02-14

申请号：US14629390

申请日：2015-02-23

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

IPC: A61K31/437 ,  C07D239/70 ,  C07D519/00 ,  C07D487/04 ,  C07D471/04

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

Abstract: Certain pyrazolo[1,5-a]pyrimidines: 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）的某些咪唑并嗪：及其药物组合物。 治疗响应于抑制Syk活性的患者的方法，其包括给予这些患者一定数量的至少一种有效减少疾病或病症体征或症状的式（I）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。