公开(公告)号：US20220227787A1

公开(公告)日：2022-07-21

申请号：US17558130

申请日：2021-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Eda Y. Canales ,  Laurent P. Debien ,  Petr Jansa ,  Rick A. Lee ,  Jennifer A. Loyer-Drew ,  Stephane Perreault ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Jennifer A. Treiberg ,  Joshua J. Van Veldhuizen ,  Lianhong Xu

IPC: C07D519/00

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.

公开(公告)号：US11976083B2

公开(公告)日：2024-05-07

申请号：US17242617

申请日：2021-04-28

Applicant: Gilead Sciences, Inc.

Inventor： Eda Y. Canales ,  Weng K. Chang ,  Laurent P. Debien ,  Petr Jansa ,  Jennifer A. Loyer-Drew ,  Luisruben P. Martinez ,  Stephane Perreault ,  Gary B Phillips ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Jennifer A. Treiberg ,  Joshua J. Van Veldhuizen

IPC: C07D471/18 ,  A61K31/4184 ,  A61K31/4188 ,  A61K31/437 ,  A61K45/06 ,  A61P3/10 ,  A61P7/02 ,  A61P19/02 ,  A61P35/00 ,  C07D471/12 ,  C07D471/14 ,  C07D487/08 ,  C07D491/22 ,  C07D498/18 ,  C07D498/22 ,  C07D513/18 ,  C07D519/00

CPC classification number: C07D519/00 ,  A61K45/06 ,  C07D471/14

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment 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：US20240376110A1

公开(公告)日：2024-11-14

申请号：US18663952

申请日：2024-05-14

Applicant: Gilead Sciences, Inc.

Inventor： Megan K. Armstrong ,  Elbert Chin ,  Chienhung Chou ,  Laurent P. Debien ,  Yifan Deng ,  Joshua D. Farr ,  Pancham Lal Gupta ,  Chao-I Hung ,  Benjamin J. June ,  Prasenjit K. Mukherjee ,  Shaina V. Nguyen ,  Gregory T. Notte ,  Daniel Roa ,  Adam J. Schrier ,  Katie A. Spence ,  Zheng-Yu Yang

IPC: C07D487/04 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/55 ,  A61K45/06 ,  A61P35/00 ,  C07D487/14 ,  C07D519/00

Abstract: The present disclosure relates generally to compounds that inhibit PRMT5. 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 inhibiting PRMT5. The disclosure further relates to the use of the compounds for the treatment of a disease or condition associated with chromosome 9p21 deletion, MTAP null, or any other MTAP deficiency. The disclosure further relates to the use of the compounds for the treatment of cancers.

公开(公告)号：US20240254118A1

公开(公告)日：2024-08-01

申请号：US18391258

申请日：2023-12-20

Applicant: Gilead Sciences, Inc.

Inventor： Megan K. Armstrong ,  Elbert Chin ,  Chienhung Chou ,  Laurent P. Debien ,  Joshua D. Farr ,  Pancham Lal Gupta ,  Chao-I Hung ,  Michael L. Mitchell ,  Prasenjit K. Mukherjee ,  Shaina V. Nguyen ,  Gregory T. Notte ,  Daniel Roa ,  Adam J. Schrier ,  Zheng-Yu Yang

IPC: C07D471/04 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  A61K31/4748 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  C07D401/12 ,  C07D491/048 ,  C07D513/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/473 ,  A61K31/4741 ,  A61K31/4743 ,  A61K31/4745 ,  A61K31/4748 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  C07D401/12 ,  C07D491/048 ,  C07D513/04 ,  C07D519/00

Abstract: The present disclosure relates generally to compounds that inhibit PRMT5. 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 inhibiting PRMT5. The disclosure further relates to the use of the compounds for the treatment of a disease or condition associated with chromosome 9p21 deletion or MTAP null. The disclosure further relates to the use of the compounds for the treatment of cancers.

公开(公告)号：US11878965B2

公开(公告)日：2024-01-23

申请号：US17557860

申请日：2021-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Zhenhong R. Cai ,  Eda Y. Canales ,  Laurent P. Debien ,  Timothy R. Hansen ,  Richard Huang ,  Petr Jansa ,  Rick A. Lee ,  Jennifer A. Loyer-Drew ,  Ryan McFadden ,  Michael L. Mitchell ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Joshua J. Van Veldhuizen ,  Lianhong Xu

IPC: C07D401/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00

CPC classification number: C07D401/04 ,  A61K31/437 ,  A61K31/454 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355 ,  A61K31/5383 ,  A61K45/06 ,  C07D401/14 ,  C07D519/00

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment 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：US20230090053A1

公开(公告)日：2023-03-23

申请号：US17557860

申请日：2021-12-21

Applicant: Gilead Sciences, Inc.

Inventor： Daniel H. Byun ,  Zhenhong R. Cai ,  Eda Y. Canales ,  Laurent P. Debien ,  Timothy R. Hansen ,  Richard Huang ,  Petr Jansa ,  Rick A. Lee ,  Jennifer A. Loyer-Drew ,  Ryan McFadden ,  Michael L. Mitchell ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Joshua J. Van Veldhuizen ,  Lianhong Xu

IPC: C07D401/04 ,  A61K45/06 ,  A61K31/437 ,  C07D519/00 ,  A61K31/5383 ,  C07D401/14 ,  A61K31/454 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5355

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment 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：US20230002412A1

公开(公告)日：2023-01-05

申请号：US17242617

申请日：2021-04-28

Applicant: Gilead Sciences, Inc.

Inventor： Eda Y. Canales ,  Weng K. Chang ,  Laurent P. Debien ,  Petr Jansa ,  Jennifer A. Loyer-Drew ,  Luisruben P. Martinez ,  Stephane Perreault ,  Gary B. Phillips ,  Hyung-Jung Pyun ,  Roland D. Saito ,  Michael S. Sangi ,  Adam J. Schrier ,  Marina E. Shatskikh ,  James G. Taylor ,  Jennifer A. Treiberg ,  Joshua J. Van Veldhuizen

IPC: C07D519/00 ,  C07D471/14 ,  A61K45/06

Abstract: The present disclosure relates to novel compounds for use in therapeutic treatment 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.