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.
Type:
Grant
Filed:
April 28, 2021
Date of Patent:
May 7, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
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
Abstract: The present disclosure provides a composition comprising Compound 1, or a pharmaceutically acceptable salt thereof, cyclodextrin, and, optionally, pH adjusting agents.
Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Type:
Grant
Filed:
June 21, 2022
Date of Patent:
May 7, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Julian A. Codelli, Michael Graupe, Juan A. Guerrero, Stephen D. Holmbo, Tetsuya Kobayashi, Yasamin Moazami, Leena B. Patel, Heath A. Weaver, Jie Xu, Suet C. Yeung, QingMing Zhu
Abstract: Provided herein are methods of treating or preventing a viral infection in a subject comprising administering a compound of Formula I, Formula Ia, or Formula Ib, or a pharmaceutically acceptable salt thereof, wherein the subject is not being treated with chloroquine, or an analog or salt thereof.
Abstract: The present disclosure provides bifunctional compounds of Formula (I), and pharmaceutically acceptable salts, isotopic forms, isolated stereoisomers, or mixtures of stereoisomers thereof, as IRAK4 degraders via ubiquitin proteasome pathway, and method for treating diseases modulated by IRAK4.
Type:
Grant
Filed:
August 18, 2022
Date of Patent:
May 7, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Wylie Palmer, Jeffrey Wu, John Lee, Kerem Ozboya, Tim Kane
Abstract: Compounds and methods of using said compounds, alone or in combination with additional agents, and pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.
Type:
Grant
Filed:
April 20, 2023
Date of Patent:
April 23, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Scott E. Lazerwith, Jonathan William Medley, Philip A. Morganelli, Thomas P. Stratton, Peiyuan Wang
Abstract: The present disclosure provides methods and compositions for treating, stabilizing or lessening the severity or progression of a non-alcoholic fatty liver disease.
Abstract: The present disclosure relates to compounds of Formula (Ia) and (Ib): or a pharmaceutically acceptable salt thereof, which are useful in the treatment of an HIV infection in heavily treatment-experienced patients with multidrug resistant HIV infection.
Type:
Grant
Filed:
July 15, 2019
Date of Patent:
April 2, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Laura Elizabeth Bauer, Anna Chiu, Eric M. Gorman, Andrew Stephen Mulato, Martin Sunkwang Rhee, Charles William Rowe, Scott P. Sellers, Dimitrios Stefanidis, Winston C. Tse, Stephen R. Yant, Dana J. Levine
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.
Type:
Grant
Filed:
June 23, 2021
Date of Patent:
March 26, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
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
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).
Type:
Grant
Filed:
December 6, 2022
Date of Patent:
March 26, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Brian P. Bestvater, Joshua A. Kaplan, Barton W. Phillips, Kin S. Yang, Anna Zagorska
Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Type:
Grant
Filed:
June 21, 2022
Date of Patent:
March 19, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Michael Graupe, Juan A. Guerrero, Stephen D. Holmbo, Jesse M. Jacobsen, Tetsuya Kobayashi, Leena B. Patel, Heath A. Weaver, Jie Xu, Suet C. Yeung
Abstract: The present disclosure generally relates to methods of treating or preventing cancer by administering an MCL-1 inhibitor and an antibody-drug conjugate, and optionally one or more additional anti-cancer agents. In particular, the MCL-1 inhibitor can be a compound of formula (I), (II) or (III), or compound A. The antibody-drug conjugate can comprises an anti-Trop-2 antibody and an anti-cancer agent (e.g., SN-38). The combination therapy for treating cancer can have synergistic effect.
Type:
Grant
Filed:
June 9, 2022
Date of Patent:
March 19, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Thomas F. Kenney, Clinton K. Matson, Chandrasekar Venkataramani
Abstract: The present disclosure provides diacylglycerol kinase modulating compounds, and pharmaceutical compositions thereof, for treating cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection. The compounds can be used alone or in combination with other agents.
Type:
Grant
Filed:
June 21, 2022
Date of Patent:
March 12, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Julian A. Codelli, Michael Graupe, Juan A. Guerrero, Jesse M. Jacobsen, Tetsuya Kobayashi, Jonathan William Medley, Yasamin Moazami, Leena B. Patel, Jie Xu, Suet C. Yeung
Abstract: The present disclosure relates generally to certain 6-azabenzimidazole compounds, pharmaceutical compositions comprising said compounds, and methods of making and using said compounds and pharmaceutical compositions. The compounds and compositions disclosed herein may be used for the treatment or prevention of diseases, disorders, or infections modifiable by hematopoietic progenitor kinase 1 (HPK1) inhibitors, such as HBV, HIV, cancer, and/or a hyper-proliferative disease.
Type:
Grant
Filed:
May 27, 2021
Date of Patent:
March 12, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Gayatri Balan, Mark J. Bartlett, Jayaraman Chandrasekhar, Julian A. Codelli, John H. Conway, Jennifer L. Cosman, Rao V. Kalla, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Joshua J. Van Veldhuizen, Suet C. Yeung, Jeff Zablocki
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.
Type:
Grant
Filed:
August 26, 2021
Date of Patent:
March 12, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Elaine Bunyan, Byoung-Kwon Chun, Kassibla E. Dempah, Hon C. Hui, Rao V. Kalla, Richard L. Mackman
Abstract: Provided herein is A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein the various substituents are described herein.
Type:
Grant
Filed:
October 27, 2022
Date of Patent:
March 5, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Gregory F. Chin, Michael O. Clarke, Jennifer L Cosman, Deeba Ensan, Bindu Goyal, Stephen Ho, Richard L Mackman, Michael R. Mish, Dustin S. Siegel, Kyle C. Tamshen, Hai Yang
Abstract: The present disclosure relates generally to methods of using modulators of COT (cancer Osaka thyroid) for treating, stabilizing, or lessening the severity or progression of liver disease, in particular, Nonalcoholic fatty liver disease (NAFLD) or nonalcoholic steatohepatitis (NASH).
Type:
Application
Filed:
September 25, 2023
Publication date:
February 29, 2024
Applicant:
Gilead Sciences, Inc.
Inventors:
David G. Breckenridge, Grant R. Budas, Ruchi Gupta, James G. Taylor, Matthew R. Warr, Nathan E. Wright
Inventors:
Benjamin Luke Kozub, Brian Nilstoft, Kevin Nguyen, James Paul Oberhauser, Roman Shumylo, Joseph Anthony Cordova, Jinhui Yun, William Harold Lizor, Jr., Adam Hilborn, Jesse Arnold Fourt, Léo Boris Marzolf, Pratap Uday Ganapathy, Brooke Genelle Thyng, Caricia Catalani, Soizic Porhel, Jose Angel Meza, Steven M. Scally, Mary Cassandra Lodwick
Inventors:
Benjamin Luke Kozub, Brian Nilstoft, Kevin Nguyen, James Paul Oberhauser, Roman Shumylo, Joseph Anthony Cordova, Jinhui Yun, William Harold Lizor, Jr., Adam Hilborn, Jesse Arnold Fourt, Léo Boris Marzolf, Pratap Uday Ganapathy, Brooke Genelle Thyng, Caricia Catalani, Soizic Porhel, Jose Angel Meza, Steven M. Scally, Mary Cassandra Lodwick