公开(公告)号：US20200255418A1

公开(公告)日：2020-08-13

申请号：US16741101

申请日：2020-01-13

Applicant: Gilead Sciences, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Morin Mae Frick ,  Elizabeth M. Horstman ,  Joshua A. Kaplan ,  Jeffrey E. Kropf ,  William J. Watkins

IPC: C07D413/14

Abstract: The present disclosure relates generally to compounds that bind to FXR and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

公开(公告)号：US11939318B2

公开(公告)日：2024-03-26

申请号：US18062363

申请日：2022-12-06

Applicant: Gilead Sciences, Inc.

Inventor： Brian P. Bestvater ,  Joshua A. Kaplan ,  Barton W. Phillips ,  Kin S. Yang ,  Anna Zagorska

IPC: C07D401/14 ,  C07D401/04 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D401/04 ,  C07D413/14

Abstract: The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).

公开(公告)号：US20230012262A1

公开(公告)日：2023-01-12

申请号：US17319507

申请日：2021-05-13

Applicant: Gilead Sciences, Inc.

Inventor： Brian P. Bestvater ,  Zhimin Du ,  Julie Farand ,  Joshua A. Kaplan ,  Barton W. Phillips ,  Doris T. Tang ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  Kin S. Yang ,  Anna Zagorska

IPC: C07D401/14 ,  C07D405/14 ,  C07D409/14

Abstract: The present disclosure relates generally to compounds that bind to Lysophosphatidic Acid Receptor 1 (LPAR1) and act as antagonists of LPAR1. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of LPAR1, including fibrosis and liver diseases such as non-alcoholic steatohepatitis (NASH), interstitial lung disease (ILD), or chronic kidney disease (CKD).

公开(公告)号：US20220204491A1

公开(公告)日：2022-06-30

申请号：US17534951

申请日：2021-11-24

Applicant: Gilead Sciences, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Morin Mae Frick ,  Elizabeth M. Horstman ,  Joshua A. Kaplan ,  Jeffrey E. Kropf ,  William J. Watkins

IPC: C07D413/14 ,  A61P1/16

Abstract: The present disclosure relates generally to compounds that bind to FXR and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

公开(公告)号：US20200061024A1

公开(公告)日：2020-02-27

申请号：US16403247

申请日：2019-05-03

Applicant: GILEAD SCIENCES, INC.

Inventor： Jinfa Du ,  Joshua A. Kaplan ,  Thorsten A. Kirschberg ,  Tetsuya Kobayashi ,  Scott E. Lazerwith ,  Rick Andrew Lee ,  Jonathan William Medley ,  Michael L. Mitchell ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun ,  Sophia L. Shevick ,  Neil H. Squires ,  William J. Watkins

IPC: A61K31/403 ,  A61K31/4192 ,  A61K31/38 ,  A61K31/16 ,  A61K31/03 ,  A61P31/20 ,  C07D519/00 ,  C07D487/04

Abstract: This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.

公开(公告)号：US10253019B2

公开(公告)日：2019-04-09

申请号：US16020777

申请日：2018-06-27

Applicant: Gilead Sciences, Inc.

Inventor： Zhimin Du ,  Juan A. Guerrero ,  Joshua A. Kaplan ,  John E. Knox, Jr. ,  Jennifer R. Lo ,  Scott A. Mitchell ,  Devan Naduthambi ,  Barton W. Phillips ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  William J. Watkins ,  Zhongdong Zhao

IPC: C07D405/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/107 ,  C07D491/113 ,  C07D498/04 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/541

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

公开(公告)号：US20250026744A1

公开(公告)日：2025-01-23

申请号：US18747316

申请日：2024-06-18

Applicant: Gilead Sciences, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Morin Mae Frick ,  Elizabeth M. Horstman ,  Joshua A. Kaplan ,  Jeffrey E. Kropf ,  William J. Watkins

IPC: C07D413/14 ,  A61K31/397 ,  A61K31/4439 ,  A61K31/519 ,  A61K31/53 ,  A61P1/16

Abstract: The present disclosure relates generally to compounds that bind to FXR and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

公开(公告)号：US11225473B2

公开(公告)日：2022-01-18

申请号：US16741101

申请日：2020-01-13

Applicant: Gilead Sciences, Inc.

Inventor： Peter A. Blomgren ,  Kevin S. Currie ,  Morin Mae Frick ,  Elizabeth M. Horstman ,  Joshua A. Kaplan ,  Jeffrey E. Kropf ,  William J. Watkins

IPC: C07D413/14 ,  A61K31/4439 ,  A61P1/16 ,  A61K31/519 ,  A61K31/53 ,  A61K31/397

Abstract: The present disclosure relates generally to compounds that bind to FXR and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.

公开(公告)号：US10328053B2

公开(公告)日：2019-06-25

申请号：US15686499

申请日：2017-08-25

Applicant: Gilead Sciences, Inc.

Inventor： Jinfa Du ,  Joshua A. Kaplan ,  Thorsten A. Kirschberg ,  Tetsuya Kobayashi ,  Scott E. Lazerwith ,  Rick Andrew Lee ,  Jonathan William Medley ,  Michael L. Mitchell ,  Philip Anthony Morganelli ,  Hyung-Jung Pyun ,  Sophia L. Shevick ,  Neil H. Squires ,  William J. Watkins

IPC: A61K31/403 ,  A61P31/20 ,  A61K31/03 ,  A61K31/16 ,  C07D487/04 ,  C07D519/00 ,  A61K31/38 ,  A61K31/4192

Abstract: This application relates generally to certain substituted pyrrolizine compounds, and pharmaceutical compositions which inhibit HBV replication, and methods of making and using them.

公开(公告)号：US10316049B2

公开(公告)日：2019-06-11

申请号：US15380836

申请日：2016-12-15

Applicant: Gilead Sciences, Inc.

Inventor： Zhimin Du ,  David Dornan ,  Juan A. Guerrero ,  Joshua A. Kaplan ,  John E. Knox ,  Devan Naduthambi ,  Barton W. Phillips ,  Susanna Y. Stinson ,  Chandrasekar Venkataramani ,  Peiyuan Wang ,  William J. Watkins

IPC: A61K31/505 ,  A61K45/06 ,  C07D239/42 ,  C07D401/10 ,  C07D413/12 ,  C07F9/6558 ,  C07D405/12 ,  A61K31/4433 ,  A61K31/519 ,  A61K9/00 ,  C07D403/10 ,  A61K31/4439 ,  C07D401/12 ,  A61K31/4545 ,  C07D401/14 ,  A61K31/506 ,  C07D413/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/675

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