公开(公告)号：US09949932B2

公开(公告)日：2018-04-24

申请号：US15178164

申请日：2016-06-09

Applicant: Gilead Connecticut, Inc.

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

IPC: C07D487/04 ,  A61K9/00 ,  B01J2/00 ,  B01J2/16 ,  A61K9/20 ,  C07C309/66 ,  A61K31/5377 ,  A61K47/10 ,  A61K47/38 ,  B29B9/10 ,  B29C43/00 ,  B29C43/02 ,  A61K9/28

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：US20180099971A1

公开(公告)日：2018-04-12

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

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：US09382256B2

公开(公告)日：2016-07-05

申请号：US14445970

申请日：2014-07-29

Applicant: Gilead Connecticut, Inc.

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

IPC: A61K31/495 ,  C07D487/04 ,  A61K9/20 ,  C07C309/66 ,  A61K31/5377 ,  A61K9/28

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.

Abstract translation: 公开了包含具有下式的化合物或其药学上可接受的盐，或其水合物和至少一种药学上可接受的聚合物的药物组合物。 式I化合物或其水合物的药学上可接受的盐可以是甲磺酸盐，包括例如单甲磺酸酯或双甲磺酸盐或其水合物。 还公开了用于药物组合物的方法。

公开(公告)号：US20140357627A1

公开(公告)日：2014-12-04

申请号：US14300189

申请日：2014-06-09

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: C07D498/04 ,  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.

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：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：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：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：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：US09657023B2

公开(公告)日：2017-05-23

申请号：US14446011

申请日：2014-07-29

Applicant: Gilead Connecticut, Inc.

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

IPC: C07D487/04 ,  C07C309/04

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：US20160168155A1

公开(公告)日：2016-06-16

申请号：US14907767

申请日：2014-07-29

Applicant: GILEAD CONNECTICUT, INC.

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

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.

Abstract translation: 提供式（I）化合物的双甲磺酸盐或其水合物的多晶型物。 双甲磺酸盐也可以描述为式（IA）的化合物：本文还提供其组合物，其制备方法和这些多晶型物的方法。