公开(公告)号：US09676760B2

公开(公告)日：2017-06-13

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 ,  A61K31/5513 ,  C07D267/08 ,  C07D243/24 ,  C07D267/14 ,  C07D291/08 ,  C07D403/06 ,  C07D413/12 ,  C07D413/14 ,  C07D419/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  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：US20150080370A1

公开(公告)日：2015-03-19

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: 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。

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：US11229638B2

公开(公告)日：2022-01-25

申请号：US16641166

申请日：2018-08-20

Applicant: Gilead Sciences, Inc.

Inventor： Mark J. Bartlett ,  Britton Kenneth Corkey ,  Jennifer Leigh Cosman ,  Kristyna M. Elbel ,  Elfatih Elzein ,  Rao V. Kalla ,  Dmitry Koltun ,  Xiaofen Li ,  Eric Q. Parkhill ,  Thao Perry

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/4745 ,  C07D487/04 ,  A61P35/00 ,  A61K31/497 ,  A61K35/17 ,  A61K31/4985 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K35/26 ,  A61K39/395 ,  A61K45/06 ,  C07K16/28

Abstract: Compounds having the following Formula I and/or Formula II and methods of their use and preparation are 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：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：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。

公开(公告)号：US20130184255A1

公开(公告)日：2013-07-18

申请号：US13789469

申请日：2013-03-07

Applicant: Gilead Sciences, Inc.

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

IPC: C07D413/06 ,  C07D471/04

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：US20230040586A1

公开(公告)日：2023-02-09

申请号：US17355813

申请日：2021-06-23

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Byoung-Kwon Chun ,  Michael O. Clarke ,  Petr Jansa ,  Rao V. Kalla ,  Dmitry Koltun ,  Richard L. Mackman ,  Thao D. Perry ,  Dustin S. Siegel ,  Scott P. Simonovich

IPC: C07F9/6561 ,  A61K45/06

Abstract: Compounds and methods of using said compounds, singly or in combination with additional agents, and pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.