公开(公告)号：US09403782B2

公开(公告)日：2016-08-02

申请号：US14808296

申请日：2015-07-24

Applicant: Gilead Sciences, Inc.

Inventor： Britton Kenneth Corkey ,  Elfatih Elzein ,  Michael Graupe ,  Juan Guerrero ,  Robert H. Jiang ,  Rao V. Kalla ,  Tetsuya Kobayashi ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Gregory Notte ,  Eric Q. Parkhill ,  Thao Perry ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC: C07D237/30 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D413/06 ,  C07D413/14 ,  A61K31/502 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/4427 ,  A61P25/08 ,  C07D253/08 ,  C07D498/04 ,  C07D263/58 ,  C07D237/32 ,  C07D239/88 ,  C07D239/90 ,  C07D265/22 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D417/06 ,  C07D417/14 ,  C07D217/26 ,  C07D413/12 ,  C07D498/10

CPC classification number: C07D498/10 ,  C07D217/26 ,  C07D237/32 ,  C07D239/88 ,  C07D239/90 ,  C07D253/08 ,  C07D263/58 ,  C07D265/22 ,  C07D279/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  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 Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.

公开(公告)号：US20160096846A1

公开(公告)日：2016-04-07

申请号：US14872787

申请日：2015-10-01

Applicant: Gilead Sciences, Inc.

Inventor： Britton Kenneth Corkey ,  Elfatih Elzein ,  Michael Graupe ,  Juan Guerrero ,  Robert H. Jiang ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Eric Q. Parkhill ,  Thao Perry ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC: C07D498/04 ,  C07D413/04 ,  C07D413/14 ,  C07D413/06 ,  C07D471/04 ,  C07B59/00 ,  C07D419/06 ,  C07D243/14 ,  C07D403/06 ,  C07D487/04 ,  C07D417/14 ,  C07D267/14 ,  C07D291/08

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.

公开(公告)号：US09296782B2

公开(公告)日：2016-03-29

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: A61K6/00 ,  C07K1/00 ,  C07K5/08 ,  C07D498/16 ,  A61K31/4985 ,  C07D498/22 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/519 ,  A61K45/06 ,  C07K5/087 ,  C07K5/083 ,  A61K38/21 ,  A61K38/06 ,  A61K38/00

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：US20160031868A1

公开(公告)日：2016-02-04

申请号：US14774019

申请日：2014-03-27

Applicant: GILEAD SCIENCES, INC.

Inventor： Evangelos Aktoudianakis ,  Gregory Chin ,  Britton Kenneth Corkey ,  Jinfa Du ,  Kristyna Elbel ,  Robert H. Jiang ,  Tetsuya Kobayashi ,  Ruben Martinez ,  Samuel E. Metobo ,  Michael Mish ,  Sophie Shevick ,  David Sperandio ,  Hai Yang ,  Jeff Zablocki

IPC: C07D413/14

CPC classification number: C07D413/14 ,  C07D413/04 ,  C07D417/14

Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, a bromodomain-containing protein, including bromodomain-containing protein 4 (BRD4), and to compositions and formulations containing such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I) wherein R1a, R1b, R2a, R2b, R3, and X are described herein.

Abstract translation: 本申请涉及可用作含溴结构域的蛋白质（包括含溴结构域蛋白质的蛋白质4（BRD4））的抑制剂或其它方式调节其含有活性的蛋白质的化学化合物，以及含有这些化合物的组合物和制剂，以及 使用和制造这些化合物。 化合物包括其中R1a，R1b，R2a，R2b，R3和X在本文中描述的式（I）的化合物。

公开(公告)号：US20150329558A1

公开(公告)日：2015-11-19

申请号：US14808296

申请日：2015-07-24

Applicant: Gilead Sciences, Inc.

Inventor： Britton Kenneth Corkey ,  Elfatih Elzein ,  Michael Graupe ,  Juan Guerrero ,  Robert H. Jiang ,  Rao V. Kalla ,  Tetsuya Kobayashi ,  Dmitry Koltun ,  Xiaofen Li ,  Ruben Martinez ,  Gregory Notte ,  Eric Q. Parkhill ,  Thao Perry ,  Chandrasekar Venkataramani ,  Jeff Zablocki

IPC: C07D498/10 ,  C07D401/04 ,  C07D403/04 ,  C07D413/06 ,  C07D263/58 ,  C07D403/06 ,  C07D417/06 ,  C07D403/12 ,  C07D401/12 ,  C07D237/32 ,  C07D253/08 ,  C07D413/14

CPC classification number: C07D498/10 ,  C07D217/26 ,  C07D237/32 ,  C07D239/88 ,  C07D239/90 ,  C07D253/08 ,  C07D263/58 ,  C07D265/22 ,  C07D279/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/08 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  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 Q, R1, X1, X2, Y and R2 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Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用化合物的方法以及含有该化合物的药物组合物。

公开(公告)号：US08912190B2

公开(公告)日：2014-12-16

申请号：US13677058

申请日：2012-11-14

Applicant: Gilead Sciences, Inc.

Inventor： Dmitry Koltun ,  Eric Parkhill ,  Jeff Zablocki

IPC: A61K31/495 ,  C07D241/36 ,  A61K31/498 ,  C07D241/44

CPC classification number: A61K31/498 ,  C07D241/44

Abstract: The present invention relates to compounds that are late 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 R1, 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: 本发明涉及晚期钠通道抑制剂及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的化合物。 在具体实施方案中，化合物的结构由式（I）给出：其中R 1，R 2，R 3和R 4如本文所述，用于制备和使用化合物的方法以及含有该化合物的药物组合物。

公开(公告)号：US08664399B2

公开(公告)日：2014-03-04

申请号：US13706879

申请日：2012-12-06

Applicant: Gilead Sciences, Inc.

Inventor： Matthew Abelman ,  Robert H. Jiang ,  Jeff Zablocki

IPC: C07D413/04 ,  C07D215/54 ,  C07D215/14 ,  C07D401/06

CPC classification number: C07D215/54 ,  C07D215/14 ,  C07D215/18 ,  C07D215/38 ,  C07D401/06 ,  C07D413/04

Abstract: The present invention relates to sodium channel inhibitors of Formula (I): in which R1, R2, R3, R4, R5, X, Y, and Z are as defined herein, and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

公开(公告)号：US20130324525A1

公开(公告)日：2013-12-05

申请号：US13960636

申请日：2013-08-06

Applicant: Gilead Sciences, Inc.

Inventor： Matthew Abelman ,  Robert H. Jiang ,  Jeff Zablocki

IPC: C07D487/04 ,  C07D213/80 ,  C07D311/74 ,  C07D407/04 ,  C07D491/147 ,  C07D409/04

CPC classification number: C07D213/80 ,  A61K31/435 ,  C07D211/90 ,  C07D215/54 ,  C07D311/74 ,  C07D311/94 ,  C07D401/04 ,  C07D405/04 ,  C07D407/04 ,  C07D409/04 ,  C07D471/04 ,  C07D487/04 ,  C07D491/147

Abstract: The present invention relates to novel heterocyclic compounds 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 Q1, Q2, R2, R3, R4, R5, and R6 are as described herein.The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.

公开(公告)号：US10370342B2

公开(公告)日：2019-08-06

申请号：US15692093

申请日：2017-08-31

Applicant: Gilead Sciences, Inc.

Inventor： Gregory Chin ,  Richard L. Mackman ,  Michael R. Mish ,  Jeff Zablocki

IPC: C07D239/95 ,  A61K31/517 ,  A61P31/18 ,  A61P35/00 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.

公开(公告)号：US10259811B2

公开(公告)日：2019-04-16

申请号：US16044054

申请日：2018-07-24

Applicant: Gilead Sciences, Inc.

Inventor： Zhimin Du ,  Juan Arnaldo Guerrero ,  Joshua Aaron Kaplan ,  John Edward Knox, Jr. ,  Devan Naduthambi ,  Barton W. Phillips ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  William J. Watkins ,  Jeff Zablocki

IPC: C07D471/04 ,  C07D519/00 ,  C07D473/00 ,  C07D487/04

Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed: