Patents Assigned to Merck Sharp
  • Factor XIIa Inhibitors
    Publication number: 20190352294
    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 XIIa inhibitors.
    Type: Application
    Filed: November 13, 2017
    Publication date: November 21, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ashwin U. Rao, Brian Alexander McKittrick, Matthew Lombardo, Jacqueline D. Hicks, Amy Bittner McCracken, Hong Dong Chu, Sung-Sau So, Peter Orth, Zhicai Wu, Ping Lan, John S. Debenham, Brent R. Whitehead, Jerry A. Taylor, Zhongxiang Sun, Revathi Reddy Katipally, Jonathan E. Gable, Markus K. Dahlgren, Sathesh P. Bhat
  • Tetracyclic heterocycle compounds useful as HIV integrase inhibitors
    Patent number: 10479801
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein A, X, R1, R2, R3 and R7 are as defined herein. The present invention also relates to compositions comprising at least one Tetracyclic Heterocycle Compound, and methods of using the Tetracyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: November 30, 2017
    Date of Patent: November 19, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
  • Pegylated interleukin-10
    Patent number: 10471126
    Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: November 12, 2019
    Assignee: Merck Sharp & Dohme Ltd
    Inventors: Seoju Lee, David C. Wylie, Susan V. Cannon-Carlson
  • Aminopyrazine compounds with A2A antagonist properties
    Patent number: 10472347
    Abstract: Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein “R1”, “RA-1”, “R2”, “R3”, and “Het” are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: November 12, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rongze Kuang, Pauline Ting, Amjad Ali, Heping Wu, Michael Berlin, Andrew Stamford, Hongwu Wang, Gang Zhou, David Kim, Qiaolin Deng, Yeon-Hee Lim, Younong Yu
  • Methods of preparing hydroxylamine derivatives useful in the preparation of anti-infective agents
    Patent number: 10472345
    Abstract: The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: November 12, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Aaron M. Dumas, Jeremy P. Scott, Michael Shevlin, Zhijian Liu, John Y. L. Chung, Feng Xu, Dongfang Meng
  • Factor XIa inhibitors
    Patent number: 10472344
    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: November 29, 2016
    Date of Patent: November 12, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony K. Ogawa, Linda Brockunier, James Tata, Dann L. Parker, Jr., Ming Wang
  • HETEROCYCLIC COMPOUNDS AS HIV PROTEASE INHIBITORS
    Publication number: 20190337902
    Abstract: The present invention is directed to compounds of Formula (I), pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.
    Type: Application
    Filed: December 1, 2017
    Publication date: November 7, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tanweer Khan, Elizabeth Smith, Peter Williams, Catherine Wiscount, Brian McKittrick, John McCauley
  • ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20190337910
    Abstract: The present disclosure relates to compounds of formula (I) that are useful as modulators of ?7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation.
    Type: Application
    Filed: March 20, 2017
    Publication date: November 7, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: BRENDAN M. CROWLEY, BRIAN T. CAMPBELL, JOSEPH L. DUFFY, THOMAS J. GRESHOCK, DEODIAL G. GUIADEEN, ANDREW JOHN HARVEY, BELINDA C. HUFF, KENNETH J. LEAVITT, VANESSA L. RADA, JOHN M. SANDERS, WILLIAM D. SHIPE, LINDA M. SUEN, IAN M. BELL
  • BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
    Publication number: 20190337917
    Abstract: Compounds of general formula (Ia), compounds of general formula (Ia?), compounds of general formula (Ib), compounds of general formula (Ib?), compounds of general formula (I), compounds of general formula (I?), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
    Type: Application
    Filed: July 16, 2019
    Publication date: November 7, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Michael D. Altman, Brandon D. Cash, Wonsuk Chang, Jared N. Cumming, Andrew M. Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Rui Liang, Jongwon Lim, Min Lu, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Sriram Tyagarajan
  • BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
    Publication number: 20190337918
    Abstract: Compounds of general formula (Ia), compounds of general formula (Ia?), compounds of general formula (Ib), compounds of general formula (Ib?), compounds of general formula (I), compounds of general formula (I?), and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, R6, R8, R9, X1, X2, and X3 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds of the disclosure.
    Type: Application
    Filed: July 16, 2019
    Publication date: November 7, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Michael D. Altman, Brandon D. Cash, Wonsuk Chang, Jared N. Cumming, Andrew M. Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Rui Liang, Jongwon Lim, Min Lu, Ryan D. Otte, Tony Siu, Benjamin Wesley Trotter, Sriram Tyagarajan
  • PD1 AND/OR LAG3 BINDERS
    Publication number: 20190338025
    Abstract: The present invention provides molecules, such as ISVDs and Nanobodies, that bind to PD1 and LAG3 and, optionally to human serum albumin. These molecules have been engineered so as to reduce the incidence of binding by pre-existing antibodies in the bodies of a subject administered such a molecule. Methods for increasing immune response, treating cancer and/or treating an infectious disease with such molecules are provided.
    Type: Application
    Filed: May 17, 2019
    Publication date: November 7, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Bowman, Maribal Beaumont, Marie-Ange Buyse, Carlo Boutton, Bruno Dombrecht, Robert A. Kastelein, David Vlerick
  • PROCESS OF MAKING AND USING PHARMACEUTICAL FORMULATIONS OF ANTINEOPLASTIC AGENTS
    Publication number: 20190336495
    Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
    Type: Application
    Filed: July 16, 2019
    Publication date: November 7, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sydney O. Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
  • ANTIDIABETIC SPIROCHROMAN COMPOUNDS
    Publication number: 20190337961
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Application
    Filed: December 15, 2017
    Publication date: November 7, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael Miller, Harry R. Chobanian, Shuwen He, Jinsong Hao, Barbara Pio, Yan Guo, Dong Xiao
  • Process for preparing beta-lactamase inhibitor hydroxylurea intermediates
    Patent number: 10464937
    Abstract: The present invention relates to processes for the preparation of N-protected (2S,5R)-6-hydroxy-7-oxo-N-piperidin-4-yl-1,6-diazabicyclo[3.2.1]octane-2-carboxamide intermediates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.
    Type: Grant
    Filed: September 14, 2017
    Date of Patent: November 5, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jianguo Yin, Zhijian Liu, Nobuyoshi Yasuda, Mark Weisel
  • INDAZOLE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2
    Publication number: 20190330239
    Abstract: The present invention relates to a compound represented by formula I?: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Application
    Filed: November 13, 2017
    Publication date: October 31, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Thomas H. Graham, Wensheng Liu, Clare Tudge, Andreas Verras, Jinlong Jiang
  • PD1 AND/OR LAG3 BINDERS
    Publication number: 20190330339
    Abstract: The present invention provides molecules, such as ISVDs and Nanobodies, that bind to PD1 and LAG3 and, optionally to human serum albumin. These molecules have been engineered so as to reduce the incidence of binding by pre-existing antibodies in the bodies of a subject administered such a molecule. Methods for increasing immune response, treating cancer and/or treating an infectious disease with such molecules are provided.
    Type: Application
    Filed: May 17, 2019
    Publication date: October 31, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Bowman, Maribel Beaumont, Marie-Ange Buyse, Carlo Boutton, Bruno Dombrecht, Robert A. Kastelein, David Vlerick
  • COMBINATIONS OF PD-1 ANTAGONISTS AND CYCLIC DINUCLEOTIDE STING AGONISTS FOR CANCER TREATMENT
    Publication number: 20190328762
    Abstract: Therapeutic combinations that comprise at least one antagonist of the Programmed Death 1 receptor (PD-1) and at least one cyclic dinucleotide compound that activates the Stimulator of Interferon Genes (STING) pathway are disclosed herein. Also disclosed is the use of such therapeutic combinations for the treatment of cancers.
    Type: Application
    Filed: December 15, 2017
    Publication date: October 31, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Saso Cemerski, Jared N Cumming, Johnny E Kopinja, Yanhong Ma, Samanthi A Perera, Benjamin Wesley Trotter, Archie Ngai-Chiu Tse
  • PD1 AND/OR LAG3 BINDERS
    Publication number: 20190330340
    Abstract: The present invention provides molecules, such as ISVDs and Nanobodies, that bind to PD1 and LAG3 and, optionally to human serum albumin. These molecules have been engineered so as to reduce the incidence of binding by pre-existing antibodies in the bodies of a subject administered such a molecule. Methods for increasing immune response, treating cancer and/or treating an infectious disease with such molecules are provided.
    Type: Application
    Filed: May 17, 2019
    Publication date: October 31, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Bowman, Maribel Beaumont, Marie-Ange Buyse, Carlo Boutton, Bruno Dombrecht, Robert A. Kastelein, David Vlerick
  • AMINOPYRAZOLES AS JANUS KINASE INHIBITORS
    Publication number: 20190330195
    Abstract: The instant invention provides compounds which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Application
    Filed: December 7, 2017
    Publication date: October 31, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Peter Fuller, Jason Brubaker, Hongbo Zeng, Joshua Close, Jonathan Young
  • Process for preparing substituted tetracyclic heterocycle compounds
    Patent number: 10457690
    Abstract: The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: October 29, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jingjun Yin, Tetsuji Itoh, Jianguo Yin, Bangping Xiang, Kevin R. Campos, Alexei Kalinin, Zhuqing Liu, Melodie Deniz Christensen, Kevin M. Belyk, Richard J. Varsolona, Andrew Brunskill