Patents Assigned to Merck Sharp
  • 6,7-dihydro-5H-pyrrolo[3,4-B]pyridin-5-one allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 10329289
    Abstract: The present invention is directed to 6,7-dihydro-5H-pyrrolo[3,4-b]pyridine-5-one 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: Grant
    Filed: December 21, 2016
    Date of Patent: June 25, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jianming Bao, Xiaolei Gao, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Debra L. Ondeyka, Andrew W. Stamford, Fengqi Zhang
  • Pyrrolotriazine inhibitors of IRAK4 activity
    Patent number: 10329295
    Abstract: The present invention relates to pyrrolotriazine 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: March 7, 2016
    Date of Patent: June 25, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Michael D. Altman, Jason D. Brubaker, Craig R. Gibeau
  • CHROMANE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND USES THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20190185486
    Abstract: The present invention relates to novel Chromane-Substituted Tetracyclic Compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2 R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising a Chromane-Substituted Tetracyclic Compound, and methods of using the Chromane-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: August 14, 2017
    Publication date: June 20, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Wensheng Yu, Joseph A. Kozlowski, Ling Tong, Craig A. Cobum, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang
  • ANTIVIRAL PRODRUGS OF TENOFOVIR
    Publication number: 20190183912
    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: Application
    Filed: August 22, 2017
    Publication date: June 20, 2019
    Applicants: Merck Sharp & Dohme Corp., IDENIX PHARMACEUTICALS LLC
    Inventors: Daniel Da Costa, Cyril B. Dousson, David Dukhan, Jean-Laurent Paparin, Houcine Rahali, Izzat Raheem
  • DEUTERATED NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20190185508
    Abstract: The present invention is directed to deuterated 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, 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 and/or ARC.
    Type: Application
    Filed: December 6, 2018
    Publication date: June 20, 2019
    Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Francois-Rene Alexandre, Izzat Raheem
  • 3-ARYL- HETEROARYL SUBSTITUTED 5-TRIFLUOROMETHYL OXADIAZOLES AS HISTONEDEACETYLASE 6 (HDAC6) INHIBITORS
    Publication number: 20190185462
    Abstract: The present invention is directed to substituted 5-trifluoromethyl oxadiazole compounds of generic formula (I) or a pharmaceutically acceptable salt thereof. In particular, the invention is directed to a class of aryl and heteroaryl substituted 5-trifluoromethyl oxadiazole compounds of formula I which may be useful as HDAC6 inhibitors for treating cellular proliferative diseases, including cancer, neurodegenerative diseases, such as schizophrenia and stroke, as well as other diseases.
    Type: Application
    Filed: June 19, 2017
    Publication date: June 20, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abbas Walji, Richard Berger, Craig A. Stump, Kelly Ann S. Schlegel, James J. Mulhearn, Thomas J. Greshock, Deping Wang, Mark E. Fraley, Kristen G. Jones
  • PD1 and/or LAG3 binders
    Patent number: 10323090
    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: Grant
    Filed: November 17, 2016
    Date of Patent: June 18, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Edward Bowman, Maribel Beaumont, Marie-Ange Buyse, Carlo Boutton, Bruno Dombrecht, David Vlerick, Robert A. Kastelein
  • Antibody neutralizing human respiratory syncytial virus
    Patent number: 10323079
    Abstract: The present invention relates to monoclonal antibodies which have high anti-RSV neutralizing titers. The invention further provides for isolated nucleic acids encoding the antibodies of the invention and host cells transformed therewith. The invention yet further provides for diagnostic, prophylactic and therapeutic methods employing the antibodies and nucleic acids of the invention, particularly as a passive immunotherapy agent in infants and the elderly.
    Type: Grant
    Filed: March 22, 2018
    Date of Patent: June 18, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kalpit A. Vora, Kara S. Cox, Aimin Tang, Zhifeng Chen, Daniel DiStefano, Lan Zhang, Hua-Poo Su
  • CARBOCYCLIC NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20190177326
    Abstract: The present invention is directed carbocyclic nucleoside reverse transcriptase inhibitors compounds of Formula I and their use in the inhibition of HIV reverse transcriptase, 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 and/or ARC.
    Type: Application
    Filed: December 6, 2018
    Publication date: June 13, 2019
    Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLC
    Inventors: Francois-Rene Alexandre, Rachid Rahali, Izzat Raheem, Christophe Parsy
  • INSULIN RECEPTOR PARTIAL AGONISTS
    Publication number: 20190177393
    Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
    Type: Application
    Filed: May 23, 2017
    Publication date: June 13, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Lin Yan, Pei Huo, Dmitri Pissarnitski, Danqing Feng, Ravi Nargund, Christina Madsen-Duggan, Yuping Zhu, Ahmet Kekec, Zhicai Wu
  • INSULIN-INCRETIN CONJUGATES
    Publication number: 20190175744
    Abstract: Insulin-incretin conjugates comprising a peptide having agonist activity at the glucagon-like 1 (GLP-1) receptor, the glucagon (GCG) receptor, and/or the gastric inhibitory protein (GIP) receptor conjugated to an insulin molecule having agonist activity at the insulin receptor and use of the conjugates for treatment of metabolic diseases, for example, Type 2 diabetes, are described.
    Type: Application
    Filed: March 13, 2017
    Publication date: June 13, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Anandan Palani, Chunhui Huang, Zhiqiang Yang, Lin Yan, Songnian Lin, Pei Huo, Qiaolin Deng, Elisabetta Bianchi, Federica Orvieto
  • HETEROCYCLE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20190175602
    Abstract: The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2 R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetra-cyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: August 14, 2017
    Publication date: June 13, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Wensheng Yu, LING Tong, Joseph A. Koziowski, Craig: A Coburn, De-yi J. Yang, Deyou Sha, Jae-Hun. Kim, Michael Dwyer, Kartik M. Keertikar, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang
  • Taste-Masked Formulations of Raltegravir
    Publication number: 20190167591
    Abstract: Disclosed are taste-masked pharmaceutical formulations of raltegravir comprising coated API granules mixed with a screened powder excipient blend in either tablet or sachet form. The core and coated granules are produced using a Wurster process for enhanced control of particle size. Also disclosed are methods of treating HIV, e.g., in pediatric populations.
    Type: Application
    Filed: December 14, 2018
    Publication date: June 6, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Karen Cassidy Thompson, Kimberly Nicole Kaighn, Indra Neil Mukherjee, Catherine Elizabeth Diimmler, Hedy Teppler Weiser, Christopher Mancinelli
  • 7-aminocephem derivative compounds
    Patent number: 10308666
    Abstract: This disclosure provides methods of making certain 7-aminocephem derivatives useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Grant
    Filed: March 14, 2018
    Date of Patent: June 4, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas
  • Piperidine oxadiazole and thiadiazole orexin receptor antagonists
    Patent number: 10308645
    Abstract: The present invention is directed to piperidine oxadiazole and thiadiazole orexin compounds which are antagonists of orexin receptors. 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 orexin 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 prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: September 27, 2015
    Date of Patent: June 4, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel Liverton, Scott D. Kuduk, Yunfu Luo, Na Meng, Tingting Yu
  • Process for making M1 receptor positive allosteric modulators
    Patent number: 10308633
    Abstract: This invention provides novel processes for the preparation of compounds such as 3-[(1S,2S)-2-hydroxycyclohexyl]-6-[(6-methylpyridin-3-yl)methyl]benzo[h]-quinazolin-4(3H)-one, salts and derivatives thereof. The compounds synthesized by the processes of the invention are useful for treating Alzheimer's disease and other diseases (e.g., cognitive impairment, schizophrenia, pain disorders, and sleep disorders) mediated by the muscarinic M1 receptor.
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: June 4, 2019
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme Limited
    Inventors: Qinghao Chen, Shane W. Krska, Lushi Tan, Peter E. Maligres, Jeremy Scott, Carl Baxter, Gavin William Stewart, Andrew Gibb
  • SUBSTITUTED TETRAHYDROISOQUINOLINE COMPOUNDS USEFUL AS GPR120 AGONISTS
    Publication number: 20190161448
    Abstract: The present invention relates to a compound represented by formula (I) and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, NASH, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: May 19, 2017
    Publication date: May 30, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Gregory L. Adams, Jason M. Cox, John S. Debenham, Scott Edmondson, Eric J. Gilbert, Yan Guo, Yu Jiang, Hubert Josien, Hyunjin M. Kim, Ping Lan, Shouwu Miao, Christopher W. Plummer, Murali Rajagopalan, Unmesh Shah, Zhongxiang Sun, Quang T. Truong, Feroze Ujjainwalla, Francisco Velazquez, Srikanth Venkatraman, Takao Suzuki, Nengxue Wang
  • Crystal forms of a CCR5 antagonist
    Patent number: 10301281
    Abstract: The present disclosure relates to forms of a CCR5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3S)-4-((1R)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone.
    Type: Grant
    Filed: November 11, 2015
    Date of Patent: May 28, 2019
    Assignees: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: Alfred Y. Lee, William De Wildt
  • Process for refolding recombinant chymotrypsin
    Patent number: 10301611
    Abstract: A process for refolding recombinant chymotrypsin produced from prokaryote host cells is described. In particular, the present invention provides a process for refolding recombinant chymotrypsin produced from E. coli is described.
    Type: Grant
    Filed: November 13, 2015
    Date of Patent: May 28, 2019
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Mark C. Sleevi, Jack Lile, Bryn Grimison
  • ANTIBODIES SPECIFIC FOR IMMUNOGLOBULIN-LIKE TRANSCRIPT 3 (ILT3) AND USES THEREOF
    Publication number: 20190153093
    Abstract: Humanized, non-promiscuous monoclonal antibodies specific for immunoglobulin-like transcript 3 (ILT3), also known as Leukocyte immunoglobulin-like receptor subfamily B member 4 (LILRB4), are described.
    Type: Application
    Filed: November 15, 2018
    Publication date: May 23, 2019
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: MICHAEL A. MEEHL, PHILIP E. BRANDISH, LAURENCE FAYADAT-DILMAN, VERONICA JUAN, CARL MIECZKOWSKI, LATIKA SINGH