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：US20150038505A1

公开(公告)日：2015-02-05

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.

Abstract translation: 提供了式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。

公开(公告)号：US20150038504A1

公开(公告)日：2015-02-05

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: C07D487/04 ,  A61K9/20 ,  C07C309/66

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：US20130338142A1

公开(公告)日：2013-12-19

申请号：US13918848

申请日：2013-06-14

Applicant: Gilead Connecticut, Inc.

Inventor： Peter A. BLOMGREN ,  Kevin S. CURRIE ,  Randall HALCOMB ,  Jeffrey E. KROPF ,  Seung H. LEE ,  Jiayao LI ,  Jennifer R. LO ,  Scott A. MITCHELL ,  Aaron SCHMITT ,  Qiaoyin WU ,  Jin-Min XIONG ,  Jianjun XU ,  Zhongdong ZHAO ,  Jayaraman CHANDRASEKHAR ,  Eric LANSDON

IPC: C07D487/04 ,  C07D498/10 ,  C07D513/04 ,  C07D498/04

CPC classification number: C07D487/04 ,  C07D498/04 ,  C07D498/10 ,  C07D513/04 ,  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 an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.

Abstract translation: 本文提供了某些咪唑并嗪及其药物组合物。 治疗患有对抑制Syk活性有反应的某些疾病和病症的患者的方法，其包括给予这些患者一定量的有效减少疾病或病症的体征或症状的咪唑并吡嗪化合物。

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：US09918939B2

公开(公告)日：2018-03-20

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: A61K31/537 ,  A61K9/20 ,  C07C309/66 ,  C07D487/04 ,  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：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：US20170020821A1

公开(公告)日：2017-01-26

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: A61K9/20 ,  B29B9/10 ,  B29C43/02 ,  A61K31/5377 ,  B29C43/00

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: 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。 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：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：