Patents by Inventor Charles A. Lesburg

Charles A. Lesburg has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20240287022
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof wherein A, E, U, X, Y, Z, R1, R2 and n are as defined herein. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases. Also provided herein are pharmaceutical compositions comprising the compounds of the invention, or their pharmaceutically acceptable salts, and a pharmaceutically acceptable carrier and methods of treatment with the compounds of the invention.
    Type: Application
    Filed: June 23, 2022
    Publication date: August 29, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: BRANDON D. CASH, GEORGE MADALIN GIAMBASU, ANDREW M. HAIDLE, BRETT A. HOPKINS, MATTHEW A. LARSEN, CHARLES A. LESBURG, PING LIU, RYAN QUIROZ, SULAGNA SANYAL, CATHERINE M. WHITE, XIN YAN, XIAO MEI ZHENG
  • Publication number: 20240246937
    Abstract: The invention discloses a synthesizing method of benzimidazole derivant and intermediate, which is characterized by the following: proceeding arylation among aryl halide and primary amine; adopting L-pro as additive, cuprous iodide as catalyst; proceeding molecular arylation coupling reaction for aryl iodide or aryl bromide and primary amine; adopting iodo phenylamine compound and bromophenylamine compound as starting material; synthesizing the material through several-step transformation.
    Type: Application
    Filed: April 28, 2022
    Publication date: July 25, 2024
    Applicants: MERCK SHARP & DOHME LLC, MSD R&D (CHINA) CO., LTD.
    Inventors: George Madalin GIAMBASU, Andrew M. HAIDLE, Brett A. HOPKINS, James P. JEWELL, Matthew A. LARSEN, Charles A. LESBURG, Ping LIU, Qinglin PU, Sulagna SANYAL, Phieng SILIPHAIVANH, Matthew TUDOR, Catherine M. WHITE, Xin YAN, Lianyun ZHAO, Xiao Mei ZHENG, William P. KAPLAN, Michaelyn Claire LUX, Derun LI, Rebecca JOHNSON
  • Publication number: 20240208986
    Abstract: Described herein are compounds of Formula I: (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as RIPK1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for RIPK1-related diseases.
    Type: Application
    Filed: April 21, 2022
    Publication date: June 27, 2024
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Joanna L. Chen, Erin F. DiMauro, Kevin D. Dykstra, Xavier Fradera, Peter H. Fuller, Charles A. Lesburg, Min Lu, Joey L. Methot, Matthew J. Mitcheltree, Jing Su
  • Publication number: 20230183214
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as IL4I1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for IL4I1-related diseases.
    Type: Application
    Filed: May 4, 2021
    Publication date: June 15, 2023
    Applicant: Merck Sharp & Dohme LLC
    Inventors: Brandon D. CASH, Wenlang FU, George Madalin GIAMBASU, Andrew M. HAIDLE, Brett A. HOPKINS, Matthew A. LARSEN, Charles A. LESBURG, Ping LIU, Meredeth A. MCGOWAN, Qinglin PU, Sulagna SANYAL, Phieng SILIPHAIVANH, Catherine M. WHITE, Xin YAN
  • Patent number: 11311528
    Abstract: The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: March 15, 2019
    Date of Patent: April 26, 2022
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Matthew L. Childers, James P. Jewell, Charles A. Lesburg, Tony Siu
  • Patent number: 11274111
    Abstract: Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: March 15, 2022
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Abdelghani Abe Achab, Jared N. Cumming, Christian Fischer, Symon Gathiaka, Charles A. Lesburg, Derun Li, Min Lu, Matthew J. Mitcheltree, Anandan Palani, Rachel L. Palte, David L. Sloman, Hongjun Zhang
  • Publication number: 20220056051
    Abstract: Described herein are compounds of Formula (I), or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
    Type: Application
    Filed: December 13, 2019
    Publication date: February 24, 2022
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Matthew L. Childers, Jared N. Cumming, Symon Gathiaka, Charles A. Lesburg, Derun Li, Min Lu, Matthew J. Mitcheltree, Anandan Palani, Rachel L. Palte, Hongjun Zhang
  • Publication number: 20210163505
    Abstract: Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula (I) act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
    Type: Application
    Filed: June 14, 2019
    Publication date: June 3, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Jared N. Cumming, Christian Fischer, Symon Gathiaka, Charles A. Lesburg, Derun Li, Min Lu, Matthew J. Mitcheltree, Anandan Palani, Rachel L. Palte, David L. Sloman, Hongjun Zhang
  • Patent number: 11010591
    Abstract: A protein crystallization trial is automatically analyzed by capturing images of the protein drops in the trial. A machine-learned model, such as a neural network, is applied to classify the images. The model generates a predicted classification from among a set of possible classifications which includes one or more crystal type classifications and one or more non-crystal type classifications. Users may be notified automatically of newly identified crystals (e.g., drops that are classified as a crystal type). The notification may include a link to a user interface that includes results of the trial.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: May 18, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Soheil Ghafurian, Ilknur Icke, Charles A. Lesburg, Belma Dogdas
  • Publication number: 20210052573
    Abstract: The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Application
    Filed: March 15, 2019
    Publication date: February 25, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Matthew L. Childers, James P. Jewell, Charles A. Lesburg, Tony Siu
  • Publication number: 20210040127
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
    Type: Application
    Filed: March 8, 2019
    Publication date: February 11, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Matthew L. Childers, Jared N. Cumming, Christian A. Fischer, Symon Gathiaka, Hakan Gunaydin, Charles A. Lesburg, Derun Li, Min Lu, Anandan Palani, Rachel L. Palte, Qinglin Pu, David L. Sloman, Sung-Sau So, Chunrui Sun, Hongjun Zhang
  • Publication number: 20200250397
    Abstract: A protein crystallization trial is automatically analyzed by capturing images of the protein drops in the trial. A machine-learned model, such as a neural network, is applied to classify the images. The model generates a predicted classification from among a set of possible classifications which includes one or more crystal type classifications and one or more non-crystal type classifications. Users may be notified automatically of newly identified crystals (e.g., drops that are classified as a crystal type). The notification may include a link to a user interface that includes results of the trial.
    Type: Application
    Filed: February 1, 2019
    Publication date: August 6, 2020
    Inventors: Soheil Ghafurian, Ilknur Icke, Charles A. Lesburg, Belma Dogdas
  • Patent number: 9969749
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: May 15, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian M. Andresen, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. MacLean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Luis Torres
  • Patent number: 9944643
    Abstract: The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: April 17, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Alan W. Hruza, Zahid Hussain, Charles Lesburg, Remond Moningka
  • Patent number: 9943516
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: April 17, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brian M. Andresen, Jason D. Brubaker, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Charles A. Lesburg, Jongwon Lim, John K. F. Maclean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Graham F. Smith, Luis Torres
  • Patent number: 9932350
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: April 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. Maclean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Graham F. Smith
  • Patent number: 9926330
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: March 27, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Michael D. Altman, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. MacLean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Graham F. Smith
  • Publication number: 20170275297
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: September 25, 2015
    Publication date: September 28, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Michael D. ALTMAN, Brian M. ANDRESEN, Jason D. BRUBAKER, Matthew L. CHILDERS, Anthony DONOFRIO, Thierry FISCHMANN, Craig R. GIBEAU, Solomon D. KATTAR, Charles A. LESBURG, Jongwon LIM, John K.F. MACLEAN, Umar F. MANSOOR, Alan B. NORTHRUP, John SANDERS, Graham F. SMITH, Luis TORRES
  • Publication number: 20170247388
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: September 25, 2015
    Publication date: August 31, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: MICHAEL D. ALTMAN, JASON D. BRUBAKER, MATTHEW L. CHILDERS, ANTHONY DONOFRIO, THIERRY FISCHMANN, CRAIG R. GIBEAU, SOLOMON D. KATTAR, CHARLES A. LESBURG, JONGWON LIM, JOHN K.F. MACLEAN, UMAR F. MANSOOR, ALAN B. NORTHRUP, JOHN M. SANDERS, GRAHAM F. SMITH
  • Publication number: 20170217981
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibutors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Application
    Filed: September 25, 2015
    Publication date: August 3, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: MICHAEL D. ALTMAN, JASON D. BRUBAKER, MATTHEW L. CHILDERS, ANTHONY DONOFRIO, THIERRY FISCHMANN, CRAIG R. GIBEAU, SOLOMON D. KATTAR, CHARLES A. LESBURG, JONGWON LIM, JOHN K.F. MACLEAN, UMAR F. MANSOOR, ALAN B. NORTHRUP, JOHN M. SANDERS, GRAHAM F. SMITH