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：US20180118734A1

公开(公告)日：2018-05-03

申请号：US15716431

申请日：2017-09-26

Applicant: Gilead Sciences, Inc.

Inventor： Zhenhong R. Cai ,  Hongyan Guo ,  Mingzhe Ji ,  Haolun Jin ,  Amy Lee ,  Ryan McFadden ,  Michael L. Mitchell ,  Manuel Munoz ,  Hyung-Jung Pyun ,  Lianhong Xu ,  Hong Yang

IPC: C07D417/14 ,  A61K45/06 ,  A61P31/18 ,  A61K31/454 ,  A61K31/428 ,  C07D498/04 ,  A61K31/5383 ,  C07D487/08 ,  A61K31/55 ,  C07D471/04 ,  A61K31/4545 ,  A61K31/496 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/5377 ,  C07D487/10 ,  C07D491/107 ,  C07D417/04 ,  C07D471/08 ,  A61K31/439 ,  A61K31/519 ,  A61K31/551

Abstract: Compounds disclosed herein including compounds of Formula I: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

公开(公告)号：US20140051656A1

公开(公告)日：2014-02-20

申请号：US13956195

申请日：2013-07-31

Applicant: Gilead Sciences, Inc.

Inventor： Hongyan Guo ,  Darryl Kato ,  Thorsten A. Kirschberg ,  Hongtao Liu ,  John O. Link ,  Michael L. Mitchell ,  Jay P. Parrish ,  Jianyu Sun ,  James Taylor ,  Elizabeth M. Bacon ,  Eda Canales ,  Aesop Cho ,  Choung U. Kim ,  Jeromy J. Cottell ,  Manoj C. Desai ,  Randall L. Halcomb ,  Michael Graupe ,  Evan S. Krygowski ,  Scott E. Lazerwith ,  Qi Liu ,  Richard L. Mackman ,  Hyung-Jung Pyun ,  Joseph H. Saugier ,  James D. Trenkle ,  Winston C. Tse ,  Randall W. Vivian ,  Scott D. Schroeder ,  William J. Watkins ,  Lianhong Xu

IPC: C07D403/14 ,  A61K45/06 ,  A61K31/4184

CPC classification number: C07D403/14 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/4184 ,  A61K31/427 ,  A61K31/435 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5415 ,  A61K31/55 ,  A61K45/06 ,  A61P31/12 ,  C07D207/16 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/04 ,  C07D491/113 ,  C07D495/04 ,  C07F5/025

Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.

公开(公告)号：US20130281434A1

公开(公告)日：2013-10-24

申请号：US13867016

申请日：2013-04-19

Applicant: GILEAD SCIENCES, INC.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: C07D491/06 ,  C07D277/82 ,  A61K31/428 ,  C07D417/10 ,  A61K31/5377 ,  C07D417/14 ,  A61K31/444 ,  A61K31/506 ,  A61K31/496 ,  A61K31/4741 ,  A61K31/4439

CPC classification number: C07D277/82 ,  A61K31/428 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D277/66 ,  C07D277/68 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06 ,  C07D498/04 ,  A61K2300/00

Abstract: Compounds of formula I′: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I′, processes for preparing compounds of formula I′, intermediates useful for preparing compounds of formula I′ and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.

Abstract translation: 提供式I'化合物或其盐。 包含式I'化合物的药物组合物，制备式I'化合物的方法，可用于制备式I'化合物的中间体和用于治疗HIV病毒增殖的治疗方法，治疗AIDS或延迟AIDS或ARC发作 还提供哺乳动物的症状。

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：US20210078959A1

公开(公告)日：2021-03-18

申请号：US16925096

申请日：2020-07-09

Applicant: Gilead Sciences, Inc.

Inventor： Zhenhong R. Cai ,  Aesop Cho ,  Ana Zurisadai Gonzalez Buenrostro ,  Xiaochun Han ,  Salman Y. Jabri ,  Ryan McFadden ,  Yingmei Qi ,  Johannes Voigt ,  Jie Xu ,  Lianhong Xu ,  Hong Yang

IPC: C07D247/00 ,  A61P31/18 ,  C07D401/10 ,  C07D403/14 ,  C07D233/88 ,  C07D487/04 ,  C07D417/10 ,  C07D471/04 ,  C07D417/14 ,  C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/10 ,  C07D413/10

Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.

公开(公告)号：US10774053B2

公开(公告)日：2020-09-15

申请号：US16158446

申请日：2018-10-12

Applicant: Gilead Sciences, Inc.

Inventor： Zhenhong R. Cai ,  Aesop Cho ,  Ana Zurisadai Gonzalez Buenrostro ,  Xiaochun Han ,  Salman Y. Jabri ,  Ryan McFadden ,  Yingmei Qi ,  Johannes Voigt ,  Hong Yang ,  Jie Xu ,  Lianhong Xu

IPC: A61K31/497 ,  A61K31/4439 ,  A61K31/433 ,  A61K31/4196 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  C07D247/00 ,  A61P31/18 ,  C07D401/10 ,  C07D403/14 ,  C07D233/88 ,  C07D487/04 ,  C07D417/10 ,  C07D471/04 ,  C07D417/14 ,  C07D491/107 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/10 ,  C07D413/10 ,  A61K45/06

Abstract: The invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of Formula I, processes for preparing compounds of Formula I, therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS symptoms in a mammal using compounds of Formula I.

公开(公告)号：US09284323B2

公开(公告)日：2016-03-15

申请号：US14370466

申请日：2013-01-03

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Hongyan Guo ,  Paul Hrvatin ,  Eric Lansdon ,  John O. Link ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Randall W. Vivian ,  Lianhong Xu ,  Hong Yang

IPC: C07D491/06 ,  A61K45/06 ,  C07C59/64 ,  C07D213/55 ,  C07D231/56 ,  C07D491/04 ,  C07D277/34 ,  A61K31/192 ,  A61K31/426 ,  A61K31/436 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/506 ,  A61K31/5377 ,  C07D277/30

CPC classification number: C07D491/06 ,  A61K31/192 ,  A61K31/426 ,  A61K31/436 ,  A61K31/4402 ,  A61K31/4406 ,  A61K31/4409 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07C59/64 ,  C07D213/55 ,  C07D231/56 ,  C07D277/30 ,  C07D277/34 ,  C07D491/04

Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

Abstract translation: 本发明提供其化合物及其盐，如本文。 本发明还提供了包含本文公开的化合物的药物组合物，用于制备本文公开的化合物的方法，用于制备本文公开的化合物的中间体和治疗HIV感染的治疗方法，治疗HIV病毒的增殖，治疗AIDS或延迟 使用本文公开的化合物在哺乳动物中的AIDS或ARC症状。

公开(公告)号：US08987250B2

公开(公告)日：2015-03-24

申请号：US13866997

申请日：2013-04-19

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Gediminas Brizgys ,  Jake Cha ,  Xiaowu Chen ,  Hongyan Guo ,  Randall L. Halcomb ,  Xiaochun Han ,  Richard Huang ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu ,  Hong Yang

IPC: A01N43/00 ,  A61K31/00 ,  C07D417/14 ,  C07D417/10 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/506 ,  A61K31/496 ,  A61K31/428 ,  C07D471/04 ,  A61K31/437 ,  A61K31/513 ,  A61K31/497 ,  A61K31/5377 ,  A61K31/454 ,  C07D498/04 ,  A61K31/5383 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/501 ,  C07D487/04 ,  A61K31/4985 ,  A61K31/553 ,  A61K31/551 ,  A61K45/06 ,  A61K31/4741 ,  C07D277/82 ,  C07D491/06 ,  C07D417/04 ,  C07D277/66

CPC classification number: C07D277/82 ,  A61K31/428 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4741 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/551 ,  A61K31/553 ,  A61K45/06 ,  C07D277/66 ,  C07D277/68 ,  C07D417/04 ,  C07D417/10 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/06 ,  C07D498/04 ,  A61K2300/00

Abstract: Compounds disclosed herein including compounds of formula I′: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.

Abstract translation: 提供本文公开的化合物，包括式I'化合物及其盐。 还提供了包含本文公开的化合物的药物组合物，用于制备本文公开的化合物的方法，用于制备本文公开的化合物的中间体和使用本文公开的化合物治疗HIV感染的治疗方法。

公开(公告)号：US20150045374A1

公开(公告)日：2015-02-12

申请号：US14370464

申请日：2013-01-03

Applicant: Gilead Sciences, Inc.

Inventor： Kerim Babaoglu ,  Kyla L. Bjornson ,  Paul Hrvatin ,  Eric Lansdon ,  John O. Link ,  Hongtao Liu ,  Ryan McFadden ,  Michael L. Mitchell ,  Yingmei Qi ,  Paul A. Roethle ,  Lianhong Xu

IPC: C07D215/227 ,  A61K31/4704 ,  A61K31/506 ,  C07D519/00 ,  A61K31/4745 ,  A61K45/06 ,  C07D491/06 ,  A61K31/4741 ,  A61K31/497

CPC classification number: C07D215/227 ,  A61K31/4704 ,  A61K31/4741 ,  A61K31/4745 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  C07D491/06 ,  C07D519/00

Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.

Abstract translation: 本发明提供其化合物及其盐，如本文。 本发明还提供了包含本文公开的化合物的药物组合物，用于制备本文公开的化合物的方法，用于制备本文公开的化合物的中间体和治疗HIV感染的治疗方法，治疗HIV病毒的增殖，治疗AIDS或延迟 使用本文公开的化合物在哺乳动物中的AIDS或ARC症状。