公开(公告)号：US08952007B2

公开(公告)日：2015-02-10

申请号：US14101740

申请日：2013-12-10

Applicant: Gilead Sciences, Inc.

Inventor： Matthew Abelman ,  Nancy Chu ,  Robert H. Jiang ,  Kwan Leung ,  Jeff Zablocki

IPC: C07D215/227 ,  C07D401/06 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04

CPC classification number: C07D401/06 ,  C07D215/227 ,  C07D413/06 ,  C07D417/06 ,  C07D471/04

Abstract: The present invention relates to sodium channel inhibitors of Formula I: in which R1, R2, R3, R4, R5, R6, and R7 are as defined above, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes.

Abstract translation: 本发明涉及式I的钠通道抑制剂：其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如上所定义，并且用于治疗各种疾病状态，包括心血管疾病和糖尿病 。

公开(公告)号：US20140274884A1

公开(公告)日：2014-09-18

申请号：US14214477

申请日：2014-03-14

Applicant: Gilead Sciences, Inc.

Inventor： Kyla L. Bjornson ,  Kapil K. Karki ,  John O. Link ,  Hyung-jung Pyun ,  Adam J. Schrier ,  Kirk L. Stevens ,  James G. Taylor ,  Randall W. Vivian ,  Jeff Zablocki ,  Sheila Zipfel

IPC: C07K7/64

CPC classification number: C07K7/64 ,  A61K31/437 ,  A61K31/519 ,  C07D203/02 ,  C07D487/00 ,  C07D487/02 ,  C07D498/22

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein the various substituents are defined herein, methods of using said compounds, and pharmaceutical compositions containing said compounds.

Abstract translation: 式I化合物或其药学上可接受的盐，其中各种取代基在本文中定义，使用所述化合物的方法和含有所述化合物的药物组合物。

公开(公告)号：US08697863B2

公开(公告)日：2014-04-15

申请号：US13789469

申请日：2013-03-07

Applicant: Gilead Sciences, Inc.

Inventor： Elfatih Elzein ,  Dmitry Koltun ,  Xiaofen Li ,  Jeff Zablocki ,  Chandrasekar Venkataramani

IPC: A61K31/00 ,  C07D267/02

CPC classification number: C07D413/06 ,  A61K31/5513 ,  A61K31/553 ,  C07B59/002 ,  C07B2200/05 ,  C07D243/14 ,  C07D243/24 ,  C07D267/08 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Z1, Z2, Z3, Z4, X, Y, R2, R3 and R4 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

Abstract translation: 本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。 在具体实施方案中，化合物的结构由式I给出：其中Z 1，Z 2，Z 3，Z 4，X，Y，R 2，R 3和R 4如本文所述，用于制备和使用该化合物的方法， 含有该组合物的药物组合物。

公开(公告)号：US20140017198A1

公开(公告)日：2014-01-16

申请号：US13934090

申请日：2013-07-02

Applicant: Gilead Sciences, Inc.

Inventor： Kyla Bjornson ,  Eda Canales ,  Jeromy J. Cottell ,  Kapil Kumar Karki ,  Ashley Anne Katana ,  Darryl Kato ,  Tetsuya Kobayashi ,  John O. Link ,  Ruben Martinez ,  Barton W. Phillips ,  Hyung-Jung Pyun ,  Michael Sangi ,  Adam James Schrier ,  Dustin Siegel ,  James G. Taylor ,  Chinh Viet Tran ,  Teresa Alejandra Trejo Martin ,  Randall W. Vivian ,  Zheng-Yu Yang ,  Jeff Zablocki ,  Sheila Zipfel

IPC: C07D498/16 ,  C07D498/22 ,  A61K45/06 ,  A61K31/506 ,  A61K31/519 ,  A61K31/4985 ,  A61K31/4745

CPC classification number: A61K31/498 ,  A61K31/10 ,  A61K31/401 ,  A61K31/4745 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K38/00 ,  A61K38/06 ,  A61K38/21 ,  A61K45/06 ,  C07D241/36 ,  C07D403/14 ,  C07D498/16 ,  C07D498/22 ,  C07K5/08 ,  C07K5/0808 ,  C07K5/0812 ,  C07K5/0827 ,  A61K2300/00

Abstract: Compounds of Formula I are disclosed As well as pharmaceutically acceptable salts thereof. Methods of using said compounds and pharmaceutical compositions containing said compounds are also disclosed.

Abstract translation: 公开的式I化合物及其药学上可接受的盐。 还公开了使用所述化合物和含有所述化合物的药物组合物的方法。

公开(公告)号：US20130203819A1

公开(公告)日：2013-08-08

申请号：US13828984

申请日：2013-03-14

Applicant: Gilead Sciences, Inc.

Inventor： Britton Corkey ,  Gregory Notte ,  Jeff Zablocki

IPC: C07D409/14

CPC classification number: C07D409/14

Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, R, R1, R2 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).

Abstract translation: 本发明涉及式（I）的化合物：其中X1，X2，X3，X4，X5，R，R1，R2如上定义。 这些化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫性疾病，炎性疾病，心血管疾病，糖尿病，糖尿病肾病，心肾肾病，包括 肾脏疾病，纤维化疾病，呼吸系统疾病，COPD，特发性肺纤维化，急性肺损伤，急性和慢性肝病和神经变性疾病。 本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。