Abstract: Compounds having the following Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use and preparation are disclosed:
Type:
Grant
Filed:
July 3, 2019
Date of Patent:
August 24, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Britton Kenneth Corkey, Jennifer Leigh Cosman, Elfatih Elzein, Xiaofen Li
Abstract: Compounds for use in treating or preventing human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following formula (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2, L, W1, W2, X, Y, and Z are as defined herein. Methods associated with the preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
March 20, 2020
Date of Patent:
August 10, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Hang Chu, Ana Z. Gonzalez Buenrostro, Hongyan Guo, Xiaochun Han, Lan Jiang, Jiayao Li, Michael L. Mitchell, Hyung-Jung Pyun, Scott D. Schroeder, Gregg M. Schwarzwalder, Nathan D. Shapiro, Devleena M. Shivakumar, Qiaoyin Wu, Hong Yang, Jennifer R. Zhang
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.
Type:
Grant
Filed:
March 2, 2020
Date of Patent:
August 3, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Elizabeth M. Bacon, Elbert Chin, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, John O. Link, Nathan Shapiro, Teresa Alejandra Trejo Martin, Zheng-Yu Yang
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:
October 30, 2019
Date of Patent:
July 27, 2021
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: The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.
Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.
Type:
Grant
Filed:
December 17, 2019
Date of Patent:
July 20, 2021
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: The invention provides compounds having Formula (I): or a pharmaceutically acceptable salt thereof, as well as pharmaceutical compositions comprising the same, processes for their preparation, and methods of treating and preventing HIV infection by their administration.
Type:
Grant
Filed:
July 29, 2019
Date of Patent:
July 6, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Elbert Chin, Darryl Kato, John O. Link, Nathan Shapiro, Zheng-Yu Yang
Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.
Type:
Grant
Filed:
August 9, 2019
Date of Patent:
July 6, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel
Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.
Type:
Grant
Filed:
August 13, 2019
Date of Patent:
June 29, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Stephen Ammann, Elizabeth M. Bacon, Gediminas Brizgys, Elbert Chin, Chienhung Chou, Jeromy J. Cottell, Marilyn Ndukwe, Marina Shatskikh, James G. Taylor, Nathan E. Wright, Zheng-Yu Yang, Sheila M. Zipfel
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:
Application
Filed:
November 25, 2020
Publication date:
June 24, 2021
Applicant:
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
Abstract: Compounds having the following Formula I and/or Formula II and methods of their use and preparation are disclosed:
Type:
Grant
Filed:
August 20, 2018
Date of Patent:
June 22, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Mark J. Bartlett, Britton Kenneth Corkey, Jennifer Leigh Cosman, Kristyna M. Elbel, Elfatih Elzein, Rao V. Kalla, Dmitry Koltun, Xiaofen Li, Eric Q. Parkhill, Thao Perry
Abstract: The invention provides compounds of formula (I): or a salt thereof as described herein. The invention also provides 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 a Retroviridae viral infection including an infection caused by the HIV virus.
Type:
Grant
Filed:
May 22, 2019
Date of Patent:
June 15, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Steven S. Bondy, Carina E. Cannizzaro, Chien-Hung Chou, Randall L. Halcomb, Yunfeng E. Hu, John O. Link, Qi Liu, Scott D. Schroeder, Winston C. Tse, Jennifer R. Zhang
Abstract: The present application provides the compounds of formula (J), or pharmaceutically acceptable salts, isomers, tautomer, or a mixture thereof, wherein n, W, A?, B?, R1, R2, and R3 are described herein. The compounds are inhibitors to the activities of phosphatidylinositol 3-kinase (PI3K) and are useful for treating conditions mediated by one or more PI3K isoforms. The present application further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts, isomers, tautomer, or mixture thereof, and methods of using these compounds and compositions for treating conditions mediated by one or more PI3K isoforms.
Type:
Grant
Filed:
June 10, 2015
Date of Patent:
June 1, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Shaopei Cai, Zhimin Du, Musong Kim, Jennifer A. Loyer-Drew, Devan Naduthambi, Leena Patel, Barton W. Phillips, Gary Phillips, Kirk L. Stevens, Jennifer Anne Treiberg, Joshua Van Veldhuizen, William J. Watkins, Suet Chung Yeung
Abstract: Provided are methods for treating Arenaviridae and Coronaviridae virus infections by administering nucleosides and prodrugs thereof, of Formula I: wherein the 1? position of the nucleoside sugar is substituted. The compounds, compositions, and methods provided are particularly useful for the treatment of Lassa virus and Junin virus infections.
Type:
Grant
Filed:
April 30, 2020
Date of Patent:
May 18, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Michael O' Neil Hanrahan Clarke, Joy Yang Feng, Robert Jordan, Richard L. Mackman, Adrian S. Ray, Dustin Siegel
Abstract: Provided are processes and intermediates for the syntheses of nucleosides of pyrrolo[1,2-f][1,2,4]triazinyl and imidazo[1,2-f][1,2,4]triazinyl heterocycles of Formula I.
Type:
Grant
Filed:
June 18, 2018
Date of Patent:
April 27, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Thomas Butler, Aesop Cho, Benjamin R. Graetz, Choung U. Kim, Samuel E. Metobo, Oliver L. Saunders, Andrew W. Waltman, Jie Xu, Lijun Zhang
Abstract: The present disclosure generally relates to compounds and pharmaceutical compositions that may be used in methods of treating cancer.
Type:
Grant
Filed:
April 23, 2020
Date of Patent:
April 27, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Hang Chu, Juan A. Guerrero, Anna E. Hurtley, Tae H. Hwang, Lan Jiang, Darryl Kato, Tetsuya Kobayashi, John E. Knox, Scott E. Lazerwith, Xiaofen Li, David W. Lin, Jonathan W. Medley, Michael L. Mitchell, Devan Naduthambi, Zachary Newby, Neil H. Squires, Vickie H. Tsui, Chandrasekar Venkataramani, William J. Watkins, Hong Yang
Abstract: The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. 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 said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
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: Methods of making compounds of Formula I are disclosed:
Type:
Grant
Filed:
November 18, 2019
Date of Patent:
April 13, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Anna Chiu, John Enquist, Jr., Nolan Griggs, Christopher Hale, Norihiro Ikemoto, Katie Ann Keaton, Matt Kraft, Scott E. Lazerwith, Michel Leeman, Zhihui Peng, Kate Schrier, Jonathan Trinidad, Jochem Van Herpt, Andrew W. Waltman
Abstract: The present invention relates to compounds of Formula (I): wherein X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
Type:
Grant
Filed:
August 1, 2019
Date of Patent:
August 31, 2021
Assignee:
Gilead Sciences, Inc.
Inventors:
Britton Corkey, Michael Graupe, Keith Koch, Lawrence S. Melvin, Jr., Gregory Notte