公开(公告)号：USRE47301E1

公开(公告)日：2019-03-19

申请号：US15653860

申请日：2017-07-19

Applicant: Gilead Sciences, Inc.

Inventor： Jeff Zablocki ,  Elfatih Elzein ,  Robert Seemayer ,  Travis Lemons

IPC: A01N43/04 ,  A61K31/70 ,  C07H19/00 ,  C07H19/167 ,  C07H19/173 ,  C07H19/16

Abstract: Disclosed is a synthesis suitable for large scale manufacture of an A2A-adenosine receptor agonist, and also relates to polymorphs of that compound, and to methods of isolating a specific polymorph.

公开(公告)号：US20180065938A1

公开(公告)日：2018-03-08

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 ,  A61K45/06 ,  A61K31/517 ,  C07D471/04 ,  A61K31/519 ,  C07D495/04 ,  C07D487/04

CPC classification number: C07D239/95 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61P31/18 ,  A61P35/00 ,  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：US20170290827A1

公开(公告)日：2017-10-12

申请号：US15488035

申请日：2017-04-14

Applicant: Gilead Sciences, Inc.

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

IPC: A61K31/498 ,  C07D403/14 ,  C07D241/36 ,  A61K31/401 ,  A61K31/10

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.

公开(公告)号：US09598435B2

公开(公告)日：2017-03-21

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: C07D267/08 ,  C07D498/04 ,  A61K31/553 ,  A61K31/5513 ,  C07D243/24 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D243/14 ,  C07B59/00 ,  C07D413/04 ,  C07D417/14

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：US20160376261A1

公开(公告)日：2016-12-29

申请号：US15239422

申请日：2016-08-17

Applicant: Gilead Sciences, Inc.

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

IPC: C07D413/04 ,  C07D453/02 ,  C07D417/14 ,  C07D413/14 ,  C07D471/04

CPC classification number: C07D413/04 ,  C07D413/14 ,  C07D417/14 ,  C07D453/02 ,  C07D471/04

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, R4a, R4b, and R5 are described herein.

Abstract translation: 其中R1a，R1b，R2a，R2b，R3，R4a，R4b和R5如本文所述。

公开(公告)号：US20160362421A1

公开(公告)日：2016-12-15

申请号：US15188701

申请日：2016-06-21

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 ,  C07D403/06 ,  C07D413/14 ,  C07D417/06 ,  C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D237/32 ,  C07D417/12 ,  C07D401/06 ,  C07D265/22 ,  C07D279/08 ,  C07D217/26 ,  C07D405/12 ,  C07D253/08

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: 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：US20160347744A1

公开(公告)日：2016-12-01

申请号：US15152231

申请日：2016-05-11

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: C07D413/06 ,  A61K31/553

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: 其中Z 1，Z 2，Z 3，Z 4，X，Y，R 2，R 3和R 4如本文所述，用于制备和使用化合物的方法和含有该化合物的药物组合物。

公开(公告)号：US20160289229A1

公开(公告)日：2016-10-06

申请号：US15059070

申请日：2016-03-02

Applicant: Gilead Sciences, Inc.

Inventor： Evangelos Aktoudianakis ,  Gregory Chin ,  Richard L. Mackman ,  Samuel E. Metobo ,  Michael R. Mish ,  Hyung-jung Pyun ,  Jeff Zablocki

IPC: C07D471/04

CPC classification number: A61K31/517 ,  C07D239/84 ,  C07D401/04 ,  C07D471/04

Abstract: The present disclosure relates generally to toll like receptor modulator compounds, such as diamino pyrido[3,2 D]pyrimidine compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR-8), and methods of making and using them.

Abstract translation: 本公开内容一般涉及诸如二氨基吡啶并[3,2 D]嘧啶化合物等受体调节剂化合物和除其他外调节toll样受体（例如TLR-8）的药物组合物，以及制备和 使用它们。

公开(公告)号：US09416128B2

公开(公告)日：2016-08-16

申请号：US14573854

申请日：2014-12-17

Applicant: Gilead Sciences, Inc.

Inventor： Rao Kalla ,  Thao Perry ,  Jeff Zablocki

IPC: C07D413/06 ,  C07D417/06

CPC classification number: C07D417/06 ,  C07D413/06

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 n, R1, R2, R2′, R3, R4, R5, R6 and R7 are as described herein, and 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n，R 1，R 2，R 2'，R 3，R 4，R 5，R 6和R 7如本文所述，以及该化合物的制备和使用方法 以及含有该组合物的药物组合物。

公开(公告)号：US09079901B2

公开(公告)日：2015-07-14

申请号：US14217011

申请日：2014-03-17

Applicant: Gilead Sciences, Inc.

Inventor： Tetsuya Kobayashi ,  Dmitry Koltun ,  Gregory Notte ,  Eric Parkhill ,  Jeff Zablocki

IPC: C07D401/14 ,  A61K31/437 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

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 R1, R2, R3, R4, and R5 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R 1，R 2，R 3，R 4和R 5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。