Patents Assigned to Merck Sharp
  • ANTIVIRAL BENZYL-AMINE PHOSPHODIAMIDE COMPOUNDS
    Publication number: 20190321380
    Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Application
    Filed: December 19, 2017
    Publication date: October 24, 2019
    Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Manuel de Lera Ruiz, Timothy J. Hartingh, Izzat Raheem, John Schreier, Jean-Laurent Paparin
  • FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS
    Publication number: 20190322666
    Abstract: The present invention relates to Fused Tricyclic Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocyclic Compound, and methods of using the Fused Tricyclic Heterocyclic Compounds for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: June 27, 2019
    Publication date: October 24, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Tao Yu, Sherman T. Waddell, Thomas H. Graham, Yonglian Zhang, John A. McCauley, Andrew W. Stamford, Jiaqiang Cai, Zhiqi Qi
  • Antiviral oxime phosphoramide compounds
    Patent number: 10450335
    Abstract: Compounds of Formula I: I and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: October 22, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wenlang Fu, Zhiqiang Guo, Ning Qi, Izzat T. Raheem, Petr Vachal, Ming Wang, John D. Schreier
  • Antiviral prodrugs of tenofovir
    Patent number: 10449208
    Abstract: Compounds of Formula I: and pharmaceutically acceptable salts and co-crystals thereof are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: October 22, 2019
    Assignees: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC.
    Inventors: Daniel Da Costa, Cyril B. Dousson, David Dukhan, Jean-Laurent Paparin, Houcine Rahali, Izzat Raheem
  • Dengue virus vaccine compositions and methods of use thereof
    Patent number: 10449243
    Abstract: The present invention relates to dengue virus vaccine compositions comprising a first and a second dengue vaccine, wherein the first dengue vaccine comprises at least one live, 5 attenuated dengue virus or live, attenuated chimeric dengue virus and the second dengue vaccine is a recombinant dengue subunit vaccine, a DNA vaccine, a conjugate vaccine, or an inactivated dengue vaccine; wherein the genome of the live attenuated dengue virus or the live attenuated chimeric dengue virus comprises a 30 nucleotide deletion of the TL2 stem-loop structure of the 3? untranslated region. The dengue virus vaccine compositions of the invention may further 10 comprise one or more adjuvants. In preferred embodiments of the invention, the first and the second dengue vaccine are tetravalent.
    Type: Grant
    Filed: December 18, 2015
    Date of Patent: October 22, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Danilo R. Casimiro, Andrew Bett, Beth-Ann Griswold Coller, Govindarajan Dhanasekaran, Ramesh V. Chintala
  • 6,6-FUSED HETEROARYL PIPERIDINE ETHER ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
    Publication number: 20190315762
    Abstract: The present invention is directed to 6,6-fused heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Application
    Filed: December 18, 2017
    Publication date: October 17, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xiaolei GAO, Sandra L. KNOWLES, Chunsing LI, Michael Man-Chu LO, Robert D. MAZZOLA, Jr., Ling TONG
  • INFLUENZA HEMAGGLUTININ PROTEIN VACCINES
    Publication number: 20190314486
    Abstract: The disclosure relates to influenza virus hemagglutinin protein and DNA vaccines, as well as methods of using the vaccines and compositions comprising the vaccines.
    Type: Application
    Filed: October 18, 2017
    Publication date: October 17, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jessica Anne Flynn, Lan Zhang, Kerim Babaoglu, Arthur Fridman, David Nickle
  • HETEROARYL PIPERIDINE ETHER ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
    Publication number: 20190315708
    Abstract: The present invention is directed to heteroarylpiperidine ether compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
    Type: Application
    Filed: December 18, 2017
    Publication date: October 17, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jianming BAO, Ronald FERGUSON, Xiaolei GAO, Scott HARRISON, Sandra L. KNOWLES, Michael Man-Chu LO, Robert D. Mazzola, Jr., Jeffrey W. Shubert
  • TETRACYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS
    Publication number: 20190315769
    Abstract: The present invention relates to Tetracyclic Heterocycle Compounds of Formula 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: Application
    Filed: June 20, 2019
    Publication date: October 17, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Thomas H. Graham, Tao Yu, Yonglian Zhang, John A. McCauley
  • Tricyclic compounds as inhibitors of mutant IDH enzymes
    Patent number: 10442819
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: October 15, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, J. Michael Ellis, Sara Esposite, Qingmei Hong, Chunhui Huang, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Ryan D. Otte, Dann L. Parker, Jr., Michael Reutershan, Nunzio Sciammetta, Pengcheng P. Shao, David L. Sloman, Feroze Ujjainwalla, Catherine White, Zhicai Wu, Yang Yu, Kake Zhao, Craig Gibeau, Tesfaye Biftu, Purakkattle Biju, Lei Chen, Joshua Close, Peter H. Fuller, Xianhai Huang, Min K. Park, Valdimir Simov, David J. Witter, Hongjun Zhang
  • N1-phenylpropane-1,2-diamine compounds with selective activity in voltage-gated sodium channels
    Patent number: 10442778
    Abstract: Disclosed are compounds of Formula A-1, or a salt thereof: Formula A-1, where J, K, Q and R1 are as defined herein, which compounds have properties for inhibiting sodium ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-1 or their salts, and methods of treating pain (e.g. chronic pain), or cough or itch disorders using the same.
    Type: Grant
    Filed: March 17, 2017
    Date of Patent: October 15, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony J. Roecker, Mark E. Layton, Thomas J. Greshock, Joseph E. Pero, Michael J. Kelly, III, Ting Zhang
  • Forms of R)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate
    Patent number: 10442829
    Abstract: A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the crystalline form may be used in antibiotics.
    Type: Grant
    Filed: May 3, 2018
    Date of Patent: October 15, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katharina Reichenbacher, Robert J. Duguid, Jacqueline A. Ware, Douglas Phillipson
  • Composition and Methods for Treating Chronic Kidney Disease
    Publication number: 20190307735
    Abstract: This invention relates to the treatment of chronic kidney disease, including diabetic nephropathy, focal segmental glomerulosclerosis (FSGS), nephrotic syndrome, non-diabetic chronic kidney disease, renal fibrosis or acute kidney injury by the administration of an RGD mimetic integrin receptor antagonist, either as a single agent or in combination with other agents.
    Type: Application
    Filed: June 18, 2019
    Publication date: October 10, 2019
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Jason M. Cox, Lijun Ma, Xiaoyan Zhou, Robin E. Haimbach, Paul J. Coleman, Haihong Zhou, David E. Kelley, Selwyn Aubrey Stoch, Le T. Duong, Maarten Hoek
  • SUBSTITUTED BICYCLIC HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20190308945
    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: October 30, 2017
    Publication date: October 10, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: BRENDAN M. CROWLEY, IAN M. BELL, ANDREW JOHN HARVEY, WILLIAM D. SHIPE, KENNETH J. LEAVITT, JOHN M. SANDERS, DEODIAL GUY GUIADEEN, LINDA M. SUEN, THOMAS J. GRESHOCK, VANESSA L. RADA
  • FUSED PYRAZINE DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE STIMULATORS
    Publication number: 20190307753
    Abstract: The invention provides certain fused pyrazine compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, R1, R3, R4a, R5a, R5b, R6, and the subscript t are as described herein. The compounds or their pharmaceutically acceptable salts can modulate the body's production of cyclic guanosine monophosphate (“cGMP”), and are generally suitable for the therapy and prophylaxis of diseases or disorders which are associated with a disturbed cGMP balance. The invention also provides pharmaceutical compositions which comprise compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention also relates to methods for use of the compounds or their pharmaceutically acceptable salts in the therapy and prophylaxis of the abovementioned diseases and disorders and for preparing pharmaceutical s for this purpose.
    Type: Application
    Filed: May 11, 2017
    Publication date: October 10, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alan Whitehead, Olga Ornoski, Subharekha Raghavan, Raphaelle Berger, Joie Garfunkle, Zhiqiang Yang, Gang JI, Falong Jiang, Jianmin Fu
  • Process for making beta 3 agonists and intermediates
    Patent number: 10435410
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Grant
    Filed: September 17, 2018
    Date of Patent: October 8, 2019
    Assignee: MERCK SHARP & DOHME CORPORATION
    Inventors: John Y. L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R. Scott Hoerrner, Stephen Keen, Dave Lieberman, Zhuqing Liu, Joseph Lynch, Kevin M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong
  • Oxazole orexin receptor antagonists
    Patent number: 10435398
    Abstract: The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 27, 2015
    Date of Patent: October 8, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Yunfu Luo
  • Regioselective N-2 arylation of indazoles
    Patent number: 10435386
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: October 8, 2019
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
  • STING AGONIST COMPOUNDS
    Publication number: 20190300513
    Abstract: Compounds of general formula (I), of general formula (II), of general formula (III), of general formula (IV), of general formula (V), of general formula (VI), and their pharmaceutically acceptable salts, wherein all variables are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are compositions comprising such compounds, processes for the synthesis of such compounds, and to uses of such compounds, including administration of such compounds to induce immune response, to induce STING-dependent type I interferon production, and/or to treat a cell proliferation disorder, such as cancer.
    Type: Application
    Filed: April 1, 2019
    Publication date: October 3, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brandon D. Cash, Matthew Lloyd Childers, Jared N. Cumming, Duane E. DeMong, Andrew Marc Haidle, Timothy J. Henderson, James P. Jewell, Matthew A. Larsen, Jongwon Lim, Min Lu, Ryan D. Otte, Benjamin Wesley Trotter
  • ANTI-CD27 ANTIBODIES
    Publication number: 20190300618
    Abstract: The present invention relates to anti-CD27 antibodies, as well as use antibodies in the treatment of diseases such as cancer and infectious disease.
    Type: Application
    Filed: September 25, 2017
    Publication date: October 3, 2019
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.
    Inventors: Amy M. Beebe, Jason Ka Jen Cheung, Veronica Juan, Laurence Fayadat-Dilman, Svetlana Sadekova, Jerelyn Wong, Hans van Eenennaam, Andrea van Elsas, Lars Guelen, Thierry Olivier Fischmann, Winifred W. Prosise