Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
Type:
Grant
Filed:
May 11, 2021
Date of Patent:
February 20, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Elizabeth M. Bacon, Gayatri Balan, Chien-Hung Chou, Christopher T. Clark, Jeromy J. Cottell, Musong Kim, Thorsten A. Kirschberg, John O. Link, Gary Phillips, Scott D. Schroeder, Neil H. Squires, Kirk L. Stevens, James G. Taylor, William J. Watkins, Nathan E. Wright, Sheila M. Zipfel
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 relates generally to certain tricyclic compounds, pharmaceutical compositions comprising said compounds, and methods of making said compounds and pharmaceutical compositions. The compounds of the disclosure are useful in treating or preventing human immunodeficiency virus (HIV) infection.
Type:
Grant
Filed:
February 3, 2023
Date of Patent:
February 13, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Hang Chu, Ana Z. Gonzalez Buenrostro, Hongyan Guo, Xiaochun Han, Anna E. Hurtley, Lan Jiang, Jiayao Li, David W. Lin, Michael L. Mitchell, Devan Naduthambi, Gregg M. Schwarzwalder, Suzanne M. Szewczyk, Matthew J. Von Bargen, Qiaoyin Wu, Hong Yang, Jennifer R. Zhang
Abstract: The present disclosure relates generally to compounds that bind to and act as degraders of an IKAROS Family Zinc Finger (IKZF) protein, such as IKZF2 (Helios) and/or IKZF4 (Eos). 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 and degradation of an IKZF protein, such as IKZF2 and/or IKZF4, including cancer.
Type:
Grant
Filed:
April 7, 2023
Date of Patent:
February 13, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Gayatri Balan, Peter A. Blomgren, Chen Chen, Julian A. Codelli, Zhimin Du, Musong Kim, Dorothée Saddier Axe, Gregg M. Schwarzwalder, Rhiannon Thomas-Tran, Michael T. Tudesco, Chandrasekar Venkataramani, William J. Watkins, Brian M. Weist, Suet C. Yeung, Helen Yu
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:
November 9, 2021
Date of Patent:
February 13, 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, Zachary A. Kasun, Musong Kim, Seung H. Lee, Jennifer R. Lo, Jennifer A. Loyer-Drew, Scott A. Mitchell, Thao D. Perry, Gary B. Phillips, Patrick J. Salvo, Sundaramoorthi Swaminathan, Joshua J. Van Veldhuizen, Suet C Yeung, Jeff Zablocki
Abstract: Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein L, R1, R5, W, X, Y1, Y2, and Z are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
November 22, 2021
Date of Patent:
January 30, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
Manoj C. Desai, Mingzhe Ji, Haolun Jin, Hyung-Jung Pyun, Teresa Alejandra Trejo Martin
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:
December 21, 2021
Date of Patent:
January 23, 2024
Assignee:
Gilead Sciences, Inc.
Inventors:
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
Abstract: 1?-Cyano nucleoside analogs of Formula I and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.
Type:
Grant
Filed:
March 6, 2023
Date of Patent:
December 26, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Daniel H. Byun, Yifan Deng, Jennifer L. Cosman Ellis, Rao V. Kalla, Richard L. Mackman, Dustin S. Siegel, Xianhuang Zeng
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.
Type:
Grant
Filed:
November 18, 2021
Date of Patent:
December 26, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Gediminas J. Brizgys, James S. Cassidy, Chienhung Chou, Jeromy J. Cottell, Chao-I Hung, Kavoos Kolahdouzan, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang
Abstract: The present disclosure relates to pharmaceutically acceptable salts, cocrystals, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yOpyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2- ((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment of a Retroviridae viral infection including an infection caused by the HIV virus.
Abstract: Disclosed are syntheses of a Cot (cancer Osaka thyroid) inhibitor, which has the following formula:
Type:
Grant
Filed:
March 31, 2021
Date of Patent:
December 19, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Kevin M. Allan, Lina Chan, Andrei Chtchemelinine, Jeffrey T. Deignan, Kassibla E. Dempah, Kelly J. Eberle, Danielle M. Elfgren, Timothy G. Elford, Kevin D. Haggerty, Jesse W. Li, Tianmin Niu, Andrew C. Stevens, Ana F. Voica, Kevin S. Williamson, Boran Xu, Guojun Yu
Abstract: Compounds and methods of using said compounds, singly or in combination with additional agents, and salts or pharmaceutical compositions of said compounds for the treatment of viral infections are disclosed.
Type:
Grant
Filed:
March 6, 2023
Date of Patent:
December 19, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Daniel H. Byun, Yifan Deng, Jennifer L. Cosman Ellis, Rao V. Kalla, Richard L. Mackman, Dustin S. Siegel, Xianhuang Zeng
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:
December 18, 2020
Date of Patent:
December 19, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Masaaki Sawa, Mai Arai, Ryoko Nakai, Hirokazu Matsumoto, Catherine Pugh, Eric Hu, Juan Guerrero, Jesse Jacobsen, Jonathan William Medley, Jie Xu, Latesh Lad, Leena Patel, Michael Graupe, Qingming Zhu, Stephen Holmbo, Tetsuya Kobayashi, Will Watkins, Yasamin Moazami, Suet C. Yeung, Julian A. Codelli, Heath A. Weaver
Abstract: The present disclosure relates to choline salts, and crystalline forms thereof, of a compound which is N—((S)-1-(3-(4-chloro-3-(methylsulfonamido)-1-(2,2,2-trifluoroethyl)-1H-indazol-7-yl)-6-(3-methyl-3-(methylsulfony)but-1-yn-1-yl)pyridin-2-yl)-2-(3,5-difluorophenyl)ethyl)-2-((3bS,4aR)-5,5-difluoro-3-(trifluoromethyl)- 3b,4,4a,5-tetrahydro-1H-cyclopropa[3,4]cyclopenta[1,2-c]pyrazol-1-yl)acetamide, which is useful in the treatment and prevention of a Retroviridae viral infection including an infection caused by the HIV virus.
Abstract: The present disclosure relates to a method of preventing and/or treating liver disease comprising administering an ACC inhibitor in combination with an FXR agonist to a patient in need thereof.
Type:
Grant
Filed:
February 27, 2020
Date of Patent:
December 5, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Jamie Geier Bates, David Gordon Clarkson Breckenridge, John T. Liles
Abstract: This application relates generally to toll like receptor modulator compounds and pharmaceutical compositions which, among other things, modulate toll-like receptors (e.g. TLR8), and methods of making and using them.
Type:
Grant
Filed:
August 11, 2021
Date of Patent:
November 28, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Gregory Chin, Richard L. Mackman, Michael R. Mish, Jeff Zablocki
Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by herpesviruses.
Type:
Application
Filed:
February 6, 2023
Publication date:
November 16, 2023
Applicants:
Novartis AG, Gilead Sciences, Inc.
Inventors:
Zef Konst, Yipin Lu, Robert Joseph Moreau, Naomi Samadara Rajapaksa, Galen Shearn-Nance, David Charles Tully, Michael Robert Turner, Joseph Michael Young, Qian Zhao, Britton K. Corkey, Samuel E. Metobo
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:
January 19, 2023
Date of Patent:
November 14, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Elaine Bunyan, Byoung-Kwon Chun, Kassibla E. Dempah, Hon C. Hui, Rao V. Kalla, Richard L. Mackman
Abstract: The present disclosure provides methods of preventing HIV in a subject, comprising administering to the subject a therapeutically effective amount of a compounds of Formula (Ia) or (Ib): or a pharmaceutically acceptable salt thereof, optionally in combination with one or more additional therapeutic agents. Methods of reducing the risk of acquiring HIV (e.g., HIV-1 and/or HIV-2) are also provided.
Type:
Grant
Filed:
November 25, 2020
Date of Patent:
November 7, 2023
Assignee:
Gilead Sciences, Inc.
Inventors:
Elena Bekerman, Wade S. Blair, Anna Chiu, Tomas Cihlar, Dana J. Levine, Winston C. Tse, Stephen R. Yant, Jim X. Zheng