公开(公告)号：WO2023086399A1

公开(公告)日：2023-05-19

申请号：PCT/US2022/049426

申请日：2022-11-09

Applicant: NURIX THERAPEUTICS, INC. ,  GILEAD SCIENCES, INC. ,  WANG, Lan ,  ZAK, Mark Edward

Inventor： BUELL, John ,  COHEN, Frederick ,  PEMBERTON, Ryan ,  SHUNATONA, Hunter P.

IPC: C07D519/00 ,  A61K31/513 ,  A61K31/4745 ,  A61P35/00 ,  A61P37/02

Abstract: The present disclosure provides bifunctional compounds as HPK1 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by HPK1.

公开(公告)号：WO2023023527A1

公开(公告)日：2023-02-23

申请号：PCT/US2022/075036

申请日：2022-08-16

Applicant: GILEAD SCIENCES, INC.

Inventor： CHUN, Byoung-Kwon ,  CLARKE, Michael O. ,  ENSAN, Deeba ,  KALLA, Rao V. ,  MACKMAN, Richard L. ,  MANDA, Jagadeesh N. ,  NADUTHAMBI, Devan ,  SIEGEL, Dustin S.

IPC: C07F9/6561 ,  A61K31/706 ,  A61P31/12 ,  A61K31/215 ,  A61K45/06

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

公开(公告)号：WO2022225914A1

公开(公告)日：2022-10-27

申请号：PCT/US2022/025329

申请日：2022-04-19

Applicant: GILEAD SCIENCES, INC.

Inventor： ARMSTRONG, Megan K. ,  BRIZGYS, Gediminas J. ,  CASSIDY, James S. ,  CHIN, Elbert ,  CHOU, Chienhung ,  HUNG, Chao-I ,  LIN, David W. ,  MITCHELL, Michael L. ,  ROBERTS, Ezra ,  SCHROEDER, Scott D. ,  TAYLOR, James G. ,  THOMAS-TRAN, Rhiannon ,  WRIGHT, Nathan E. ,  YANG, Zheng-Yu

IPC: C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5365 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10

Abstract: The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition in a human.

公开(公告)号：WO2022173722A1

公开(公告)日：2022-08-18

申请号：PCT/US2022/015582

申请日：2022-02-08

Applicant: GILEAD SCIENCES, INC.

Inventor： AMMANN, Stephen E. ,  CANALES, Eda Y. ,  CHANG, Weng K. ,  CODELLI, Julian A. ,  JIANG, Lan ,  KINFE, Henok H. ,  LAZERWITH, Scott E. ,  MITCHELL, Michael L. ,  SCHROEDER, Scott D. ,  SHORE, Daniel G.

IPC: C07D495/04 ,  A61K31/407 ,  A61P3/10 ,  A61P19/00 ,  A61P29/00

Abstract: The present disclosure relates generally to thioeno[3, 2-], pyrrole derivatives pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions provided herein may be used for the treatment or prevention of an autoimmune disease and/or inflammatory condition, including systemic lupus erythematosus and cutaneous lupus erythematosus.

公开(公告)号：WO2022140390A1

公开(公告)日：2022-06-30

申请号：PCT/US2021/064618

申请日：2021-12-21

Applicant: GILEAD SCIENCES, INC.

Inventor： BYUN, Daniel H. ,  CAI, Zhenhong R. ,  CANALES, Eda Y. ,  DEBIEN, Laurent P. ,  HANSEN, Timothy R. ,  HUANG, Richard ,  JANSA, Petr ,  LEE, Rick A. ,  LOYER-DREW, Jennifer A. ,  MCFADDEN, Ryan ,  MITCHELL, Michael L. ,  PYUN, Hyung-Jung ,  SAITO, Roland D. ,  SANGI, Michael S. ,  SCHRIER, Adam J. ,  SHATSKIKH, Marina E. ,  TAYLOR, James G. ,  VAN VELDHUIZEN, Joshua J. ,  XU, Lianhong

IPC: C07D401/14 ,  C07D471/04 ,  C07D519/00 ,  A61P35/02 ,  A61K31/437

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.

公开(公告)号：WO2022108984A1

公开(公告)日：2022-05-27

申请号：PCT/US2021/059648

申请日：2021-11-17

Applicant: GILEAD SCIENCES, INC.

Inventor： DIXON, Darryl D. ,  ISCHAY, Michael A. ,  JOHNSON, Trevor C. ,  MERIT, Jeffrey E. ,  REGENS, Christopher S. ,  STANDLEY, Eric A. ,  STEINHUEBEL, Dietrich P.

IPC: C07C255/59 ,  C07C255/54 ,  C07C205/37 ,  C07C217/86 ,  C07D267/12 ,  C07D317/22

Abstract: The invention relates in particular to methods and intermediates for the synthesis of Compound 1 that inhibits MCL1 and is useful in the treatment of cancers.

公开(公告)号：WO2022103758A1

公开(公告)日：2022-05-19

申请号：PCT/US2021/058638

申请日：2021-11-09

Applicant: GILEAD SCIENCES, INC.

Inventor： MARTIN, Stephen R. ,  MOLDT, Brian ,  PARVANGADA, Aiyappa

IPC: C12Q1/70 ,  A61K39/42 ,  A61P31/18 ,  G01N33/569

Abstract: Provided are methods for identifying patient populations infected with HIV that can be targeted by antibodies that bind to HIV gp120 CD4 binding site (CD4bs) region.

公开(公告)号：WO2022047065A2

公开(公告)日：2022-03-03

申请号：PCT/US2021/047800

申请日：2021-08-26

Applicant: GILEAD SCIENCES, INC.

Inventor： CHUN, Byoung-Kwon ,  HUI, Hon C. ,  KALLA, Rao V. ,  MACKMAN, Richard L.

IPC: C07D487/04 ,  A61P31/14 ,  A61P31/12 ,  C07B2200/13 ,  C07H7/06

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

公开(公告)号：WO2021247217A1

公开(公告)日：2021-12-09

申请号：PCT/US2021/032293

申请日：2021-05-13

Applicant: GILEAD SCIENCES, INC.

Inventor： BESTVATER, Brian P. ,  DU, Zhimin ,  FARAND, Julie ,  KAPLAN, Joshua A. ,  TANG, Doris T. ,  VENKATARAMANI, Chandrasekar ,  WANG, Peiyuan ,  YANG, Kin S. ,  ZAGORSKA, Anna

IPC: A61P9/00 ,  A61P11/00 ,  A61P13/12 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  C07D249/06 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D471/04 ,  A61K31/506 ,  A61K31/4439

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：WO2021222353A1

公开(公告)日：2021-11-04

申请号：PCT/US2021/029557

申请日：2021-04-28

Applicant: GILEAD SCIENCES, INC.

Inventor： CANALES, Eda Y. ,  CHANG, Weng K. ,  DEBIEN, Laurent P. ,  JANSA, Petr ,  LOYER-DREW, Jennifer A. ,  MARTINEZ, Luisruben P. ,  PERREAULT, Stephane ,  PHILLIPS, Gary B. ,  PYUN, Hyung-Jung ,  SAITO, Roland D. ,  SANGI, Michael S. ,  SCHRIER, Adam J. ,  SHATSKIKH, Marina E. ,  TAYLOR, James G. ,  TREIBERG, Jennifer A. ,  VAN VELDHUIZEN, Joshua J.

IPC: C07D471/18 ,  C07D471/22 ,  C07D487/08 ,  C07D491/22 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18 ,  A61P3/10 ,  A61P7/02 ,  A61P19/02 ,  A61P35/00

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatement of a disease associated with peptidylarginine deiminases (PADs), such as peptidylarginine deiminase type 4 (PAD4). The present disclosure also relates to processes and intermediates for the preparation of such compounds, methods of using such compounds and pharmaceutical compositions comprising the compounds described herein.