Patents Assigned to Merck Sharp
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Publication number: 20190022115Abstract: The present invention is directed to 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. The present invention also provides processes for the preparation of 4?-substituted nucleoside derivatives of Formula (I) and derivatives thereof.Type: ApplicationFiled: September 16, 2016Publication date: January 24, 2019Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme LimitedInventors: Vinay M. Girijavallabhan, Mark McLaughlin, Edward Cleator, Jongrock Kong, Andrew William Gibson, David R. Lieberman, Alejandro Dieguez Vazquez, Stephen Philip Keen, Michael J. Williams, Jeffrey C. Moore, Erika M. Milczek, Feng Peng, Kevin M. Belyk, Zhiguo Jake Song
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Publication number: 20190023791Abstract: The present invention provides methods of treating cancer in a human in need thereof comprising administering to the human: a therapeutically effective amount of a monoclonal antibody that binds to human OX40 comprising: (a) a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:1; (b) a heavy chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:2; (c) a heavy chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:3; (d) a light chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:7; (e) a light chain variable region CDR2 comprising the amino acid sequence of SEQ ID NO:8; and (f) a light chain variable region CDR3 comprising the amino acid sequence of SEQ ID NO:9; and a therapeutically effective amount of a monoclonal antibody that binds to human PD-1 comprising: (a) a heavy chain variable region CDR1 comprising the amino acid sequence of SEQ ID NO:54; (b) a heavy chain variable region CDR2 comprising the amino acidType: ApplicationFiled: August 3, 2016Publication date: January 24, 2019Applicants: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED, MERCK SHARP & DOHME CORP.Inventors: Axel HOOS, David KAUFMAN, Elaine PINHEIRO, Herbert STRUEMPER, Niranjan YANAMANDRA
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Patent number: 10183968Abstract: Methods for preparing lyophilized pellets of biological materials are described. The pellets have a substantially spherical shape and are prepared by freezing droplets of a liquid composition of a desired biological material on a flat, solid surface, in particular, a surface that does not have any cavities, followed by lyophilizing the frozen droplets. These methods are useful for preparing lyophilized pellets having a high concentration of a desired biological material, in particular a therapeutic protein or vaccine, and which have a faster reconstitution time than lyophilized powder cakes prepared in vials.Type: GrantFiled: October 26, 2012Date of Patent: January 22, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Colleen Barr, Akhilesh Bhambhani, Robert Evans, Lynne Isopi, David Krah, Jennifer Kriss, Jessica Sinacola
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Publication number: 20190016734Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, R3, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.Type: ApplicationFiled: February 6, 2017Publication date: January 17, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Wen-Lian Wu, Jared N. Cumming, Brandon M. Taoka, Xing Dai
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Publication number: 20190015442Abstract: Disclosed herein is a method for inhibiting expression of a gene of a subject comprising administering (1) a composition comprising R-(L)a-(G)b; wherein R is an oligonucleotide selected from the group consisting of DNA, RNA, siRNA, and microRNA; L is a linker and each occurance of L is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; each of a and b is independently 0, 1, 2, 3 or 4; and (2) a composition comprising (P)c-(L)d-(G)e; wherein P is a peptide and each occurance of P is independently selected from Table 2; L is a linker and each occurance of L is independently selected from Table 3; G is a targeting ligand and each occurance of G is independently selected from Table 4; d is 0, 1, 2, 3, 4, 5 or 6; and each of c and e is independently 1, 2, 3, 4, 5 or 6. Compositions in (1) and (2) can be co-administered or sequentially administered.Type: ApplicationFiled: May 8, 2018Publication date: January 17, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Steven L. Colletti, Thomas J. Tucker, David M. Tellers, Boyoung Kim, Rob Burke, Kathleen B. Calati, Matthew G. Stanton, Rubina G. Parmar, Jeffrey G. Aaronson, Weimin Wang
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Publication number: 20190016729Abstract: 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: ApplicationFiled: September 17, 2018Publication date: January 17, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: John Y.L. Chung, Kevin Campos, Edwards 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
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Publication number: 20190010224Abstract: The present invention provides formulations of anti-IL-10 hum12G8, and their use in treating various disorders.Type: ApplicationFiled: December 20, 2016Publication date: January 10, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Chakravarthy Nachu Narasimhan, Ashwin Basarkar, Soumendu Bhattacharya, Wendy Benjamin, Mohammed Shameem
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Patent number: 10174037Abstract: The present invention is directed to dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.Type: GrantFiled: May 31, 2016Date of Patent: January 8, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yili Chen, Yimin Qian, Shimin Xu, Chunmei Hu
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Publication number: 20190000957Abstract: The present invention relates to thermally stable oral rotavirus vaccine formulations comprising one or more rotavirus reassortant or attenuated rotavirus strains, a pharmaceutically acceptable calcium salt, adipic acid, sucrose, and sodium phosphate, wherein each of the one or more rotavirus reassortant or attenuated rotavirus strain is stable for 7 days at 37° C., for 45 days at 25° C. and for 2 years or more at 2-8° C. The calcium containing formulations of the invention may further comprise one or more excipients which are present in an amount that is effective to optimize the calcium ions free in solution to stabilize the rotavirus particles. In embodiments of the invention, the formulation comprises a surfactant, such as polysorbate 80.Type: ApplicationFiled: December 13, 2016Publication date: January 3, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Robert K. Evans, Erica L. Strable, Lynne Isopi
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Publication number: 20190000824Abstract: The present invention is directed to pyrazol-4-yl-pyridine 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 5 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: ApplicationFiled: December 19, 2016Publication date: January 3, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: John J. Acton, III, Jianming Bao, Melissa Egbertson, Xiaolei Gao, Scott T. Harrison, Sandra L. Knowles, Chunsing Li, Michael Man-Chu Lo, Robert D. Mazzola, Jr., Zhaoyang Meng, Michael T. Rudd, Oleg B. Selyutin, David M. Tellers, Ling Tong, Jenny Miu-Chun Wai
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Publication number: 20190002480Abstract: The present invention relates to novel Silane-Containing Heterocyclic Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, A?, B, B?, R1 R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one Silane-Containing Heterocyclic Compound, and methods of using the Silane-Containing Heterocyclic Compounds for treating or preventing HCV infection in a patient.Type: ApplicationFiled: December 16, 2016Publication date: January 3, 2019Applicant: Merck Sharp & Dohme Corp.Inventors: Joseph A. Kozlowski, Wensheng Yu
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Patent number: 10167298Abstract: The present invention relates to novel Pseudopolymorphs of Compound A, compositions comprising at least one Pseudopolymorph of Compound A, and methods of using the Pseudopolymorphs of Compound A for preparing compositions useful for treating or preventing HCV infection in a patient, wherein Compound A has the structure.Type: GrantFiled: October 24, 2014Date of Patent: January 1, 2019Assignee: Merck Sharp & Dohme Corp.Inventors: Michael McNevin, Yong Liu, Ian Mangion, Alfred Lee, Joyce Stellabott, Benjamin D. Sherry, Gary Martin, Kung-I Feng, Scott Schultz, Ryan Cohen, Yanfeng Zhang
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Publication number: 20180370973Abstract: The present invention is directed to fused heteroaryl derivative 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 pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: December 18, 2015Publication date: December 27, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Nigel Liverton, Douglas C. Beshore, Na Meng, Yunfu Luo
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Publication number: 20180371083Abstract: The present invention relates to anti-TIGIT antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.Type: ApplicationFiled: August 9, 2016Publication date: December 27, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Sybil M.G. Williams, Wolfgang Seghezzi, Laurence Fayadat-Dilman, Linda Liang, Veronica Juan
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Publication number: 20180370947Abstract: 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: ApplicationFiled: November 29, 2016Publication date: December 27, 2018Applicant: MERCK SHARP & DOHME CORP.Inventors: Anthony K. Ogawa, Linda Brockunier, James Tata, Dann L. Parker, Jr., Ming Wang
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Publication number: 20180369375Abstract: The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAG3 as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the antibodies and fragments (e.g., including anti-PD1 antibodies) are included in the invention. Methods for treating or preventing cancer or infection using such compositions are also provided. In addition, methods for recombinant expression of the antibodies and fragments are part of the present invention.Type: ApplicationFiled: December 13, 2016Publication date: December 27, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Rene De Waal Malefyt, Laurence Fayadat-Dilman, Linda Liang
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Patent number: 10160762Abstract: The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.Type: GrantFiled: May 24, 2016Date of Patent: December 25, 2018Assignee: Merck Sharp & Dohme Corp.Inventors: Dong-Ming Shen, Michael P. Dwyer, Christopher J. Sinz, Deping Wang, Shawn J. Stachel, Daniel V. Paone, Ashley Forster, Richard Berger, Yili Chen, Yimin Qian, Shimin Xu, Chunmei Hu, William D. Shipe, Jianmin Fu, Zhigang Guo, Haitang Li, Yingjian Bo
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Publication number: 20180362562Abstract: 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: ApplicationFiled: December 5, 2016Publication date: December 20, 2018Applicants: Merck Sharp & Dohme Corp., Idenix Pharmaceuticals LLCInventors: Izzat Tiedje Raheem, Timothy J. Hartingh, John Schreier, Jean-Laurent Paparin
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Publication number: 20180362661Abstract: Antibodies that bind the apple 2 domain of human coagulation Factor XI and inhibit activation of FXI by coagulation factor XIIa are described.Type: ApplicationFiled: August 13, 2018Publication date: December 20, 2018Applicants: Merck Sharp & Dohme Corp,, Adimab, LLCInventors: Zhu Chen, Kenneth Ellsworth, James A. Milligan, Elizabeth Oldham, Dietmar Seiffert, Vaishnavi Ganti, Mohammad Tabritzifard, Bianka Prinz
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Publication number: 20180362530Abstract: The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.Type: ApplicationFiled: July 5, 2016Publication date: December 20, 2018Applicant: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Xianhai Huang, Yeon-Hee Lim, Rongze Kuang, Heping Wu, Rajan Anand, Younong Yu, Edward Metzger, Michael Man-Chu LO, Pauline C. Ting, Andrew W. Stamford, Paul Tempest