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).
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Publication number: 20240287022Abstract: 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: ApplicationFiled: June 23, 2022Publication date: August 29, 2024Applicant: Merck Sharp & Dohme LLCInventors: 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
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Publication number: 20240246937Abstract: 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: ApplicationFiled: April 28, 2022Publication date: July 25, 2024Applicants: 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
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Publication number: 20240208986Abstract: 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: ApplicationFiled: April 21, 2022Publication date: June 27, 2024Applicant: Merck Sharp & Dohme LLCInventors: 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
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Publication number: 20230183214Abstract: 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: ApplicationFiled: May 4, 2021Publication date: June 15, 2023Applicant: Merck Sharp & Dohme LLCInventors: 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
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Patent number: 11311528Abstract: 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: GrantFiled: March 15, 2019Date of Patent: April 26, 2022Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Matthew L. Childers, James P. Jewell, Charles A. Lesburg, Tony Siu
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Patent number: 11274111Abstract: 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: GrantFiled: June 14, 2019Date of Patent: March 15, 2022Assignee: 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
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Publication number: 20220056051Abstract: 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: ApplicationFiled: December 13, 2019Publication date: February 24, 2022Applicant: 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
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Publication number: 20210163505Abstract: 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: ApplicationFiled: June 14, 2019Publication date: June 3, 2021Applicant: 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
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Patent number: 11010591Abstract: 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: GrantFiled: February 1, 2019Date of Patent: May 18, 2021Assignee: Merck Sharp & Dohme Corp.Inventors: Soheil Ghafurian, Ilknur Icke, Charles A. Lesburg, Belma Dogdas
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Publication number: 20210052573Abstract: 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: ApplicationFiled: March 15, 2019Publication date: February 25, 2021Applicant: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Matthew L. Childers, James P. Jewell, Charles A. Lesburg, Tony Siu
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Publication number: 20210040127Abstract: 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: ApplicationFiled: March 8, 2019Publication date: February 11, 2021Applicant: 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
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Publication number: 20200250397Abstract: 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: ApplicationFiled: February 1, 2019Publication date: August 6, 2020Inventors: Soheil Ghafurian, Ilknur Icke, Charles A. Lesburg, Belma Dogdas
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Patent number: 9969749Abstract: 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: GrantFiled: September 25, 2015Date of Patent: May 15, 2018Assignee: 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
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Patent number: 9944643Abstract: 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: GrantFiled: February 6, 2015Date of Patent: April 17, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Alan W. Hruza, Zahid Hussain, Charles Lesburg, Remond Moningka
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Patent number: 9943516Abstract: 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: GrantFiled: September 25, 2015Date of Patent: April 17, 2018Assignee: 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
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Patent number: 9932350Abstract: 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: GrantFiled: September 25, 2015Date of Patent: April 3, 2018Assignee: 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
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Patent number: 9926330Abstract: 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: GrantFiled: September 25, 2015Date of Patent: March 27, 2018Assignee: 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
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Publication number: 20170275297Abstract: 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: ApplicationFiled: September 25, 2015Publication date: September 28, 2017Applicant: 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
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Publication number: 20170247388Abstract: 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: ApplicationFiled: September 25, 2015Publication date: August 31, 2017Applicant: 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
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Publication number: 20170217981Abstract: 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: ApplicationFiled: September 25, 2015Publication date: August 3, 2017Applicant: 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