Patents Assigned to Merck Sharp
  • Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
    Patent number: 9951079
    Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, X, Y, m, R1, R5, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: April 24, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark W. Embrey, Kerim Babaoglu, Abbas Walji, John S. Wai, Paul J. Coleman
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9951052
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention.
    Type: Grant
    Filed: October 27, 2014
    Date of Patent: April 24, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Haifeng Tang, Jessica Frie, Ronald Dale Ferguson, Zhiqiang Guo, Zhi-Cai Shi, Brian Cato, Qinghong Fu
  • Medication injector with near-empty alert
    Patent number: 9950126
    Abstract: A medication injector that has an alert indicator that alerts the user when the medication injector is approaching near the end of its medication supply is disclosed. The alert indicator gives the user an opportunity to make preparations to obtain additional medication for the injector if there is an insufficient amount of medication in the injector to enable the user to dispense the required dosage amount with the next injection. Initially, the alert indicator is not visible to the user, but becomes visible to the user when the injector is near empty.
    Type: Grant
    Filed: December 5, 2013
    Date of Patent: April 24, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter A. Basile, Jeffrey C. Givand, Steven Carl Persak
  • CEFTOLOZANE ANTIBIOTIC COMPOSITIONS
    Publication number: 20180104338
    Abstract: This disclosure provides pharmaceutical compositions comprising ceftolozane, pharmaceutical compositions comprising ceftolozane and tazobactam, methods of preparing those compositions, and related methods and uses of these compositions.
    Type: Application
    Filed: December 18, 2017
    Publication date: April 19, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph TERRACCIANO, Nicole Miller DAMOUR, Chun JIANG, Giovanni FOGLIATO, Giuseppe Alessandron DONADELLI, Dario RESEMINI
  • TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF
    Publication number: 20180105518
    Abstract: The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
    Type: Application
    Filed: April 4, 2016
    Publication date: April 19, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Yi Heng Chen, Ping Liu, Dongfang Meng, Jane Yang Wu, Chun Sing Li, Zhiqi Qi
  • CONTAINMENT AND TRANSFER DEVICE FOR HIGHLY ACTIVE OR SENSITIVE COMPOUNDS
    Publication number: 20180104149
    Abstract: A containment and transfer device for use with highly active or sensitive compounds, comprising a sleeve or a bag with one or more flexible walls, a first sanitary clamp, an endcap, a second sanitary clamp and a compression clamp. The sleeve or bag has a first end for connection to a container, and a second end for (a) connection to a storage or mixing vessel at the discharge location, or (b) connection to an endcap for transportation. The flexible walls surround and define an internal passageway in that permits compounds in the first end of the sleeve or bag to pass into the second end of the sleeve or bag. The compression clamp compresses the flexible walls of the sleeve or bag together to produce a barrier across the internal passageway, preventing the highly active or sensitive compound from flowing into the second end of the sleeve or bag during packing, transporting and discharging the device.
    Type: Application
    Filed: March 15, 2016
    Publication date: April 19, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: LEONARD A. NOWAK
  • Nargenicin compounds and uses thereof as antibacterial agents
    Patent number: 9944654
    Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: April 17, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Katherine Young, David B. Olsen, Sheo B. Singh, Jing Su, Robert R. Wilkening, James M. Apgar, Dongfang Meng, Dann Parker, Mihir Mandal, Lihu Yang, Ronald E. Painter, Qun Dang, Takao Suzuki
  • Factor XIa inhibitors
    Patent number: 9944643
    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: February 6, 2015
    Date of Patent: April 17, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Alan W. Hruza, Zahid Hussain, Charles Lesburg, Remond Moningka
  • Inhibitors of IRAK4 activity
    Patent number: 9943516
    Abstract: 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: Grant
    Filed: September 25, 2015
    Date of Patent: April 17, 2018
    Assignee: 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
  • FUSED TRICYCLIC HETEROCYCLIC COMPOUNDS AS HIV INTEGRASE INHIBITORS
    Publication number: 20180099967
    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: December 13, 2017
    Publication date: April 12, 2018
    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
  • Purine inhibitors of human phosphatidylinositol 3-kinase delta
    Patent number: 9938281
    Abstract: The instant invention provides compounds of formula I which are PI3K-delta inhibitors, and as such are useful for the treatment of PI3K-delta-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: April 10, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Michael D. Altman, Yongqi Deng, Solomon Kattar, Jason D. Katz, Joey L. Methot, Hua Zhou, Meredeth McGowan, Matthew P. Christopher, Yudith Garcia, Neville John Anthony, Francesc Xavier Fradera Llinas, Liping Yang, Changwei Mu, Xiaona Wang, Feng Shi, Baijun Ye, Sixing Zhang, Xiaoli Zhao, Rong Zhang, Kin Chiu Fong, Xiansheng Leng
  • Glycosidase inhibitors and uses thereof
    Patent number: 9938299
    Abstract: The invention provides compounds with enhanced permeability for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.
    Type: Grant
    Filed: December 20, 2013
    Date of Patent: April 10, 2018
    Assignees: ALECTOS THERAPEUTICS, INC., MERCK SHARP & DOHME CORP.
    Inventors: Harold G. Selnick, Kun Liu, Ernest J. McEachern, Ramesh Kaul, Zhongyong Wei, Yaode Wang, Jiang Chang
  • 6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists
    Patent number: 9938276
    Abstract: The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine 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 potential prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: December 14, 2015
    Date of Patent: April 10, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • Oral pharmaceutical formulation of omarigliptin
    Patent number: 9937153
    Abstract: The present invention is directed to stable, oral pharmaceutical formulations of dipeptidyl peptidase-4 inhibitors, such as omarigliptin. Such pharmaceutical formulations comprise omarigliptin; and neutral excipients, wherein the neutral excipient is present in the amount of at least 75% by weight of the pharmaceutical formulation and comprises at least one non-reducible sugar diluent or a mixture of non-reducible sugar diluents.
    Type: Grant
    Filed: August 25, 2014
    Date of Patent: April 10, 2018
    Assignees: Merck Sharp & Dohme LTD., Merck Sharp & Dohme Corp.
    Inventors: Vincent Brett Cooper, Kathryn Alanna Bradley, Samuel Robert Pygall, Rajan Gupta, Madison Paige Stanford, Lin Xie
  • COMBINATION OF A PD-1 ANTAGONIST AND A VEGF-R/FGFR/RET TYROSINE KINASE INHIBITOR FOR TREATING CANCER
    Publication number: 20180092901
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and a multi-RTK inhibitor, and the use of the combination therapies for the treatment of cancer. The multi-RTK inhibitor may be represented by Formula (I): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl, R2 is a hydrogen atom or C1-6 alkoxy, and R3 is a hydrogen atom or a halogen atom. A tumor therapeutic agent is disclosed that combines a compound or pharmaceutically acceptable salt thereof represented by Formula I and an anti-PD-1 antibody.
    Type: Application
    Filed: March 3, 2016
    Publication date: April 5, 2018
    Applicants: MERCK SHARP & DOHME CORP., Eisai R&D Management Co., Ltd.
    Inventors: Andrew Evan DENKER, Yu KATO, Kimiyo TABATA, Yusaku HORI
  • PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS
    Publication number: 20180092900
    Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Application
    Filed: December 4, 2017
    Publication date: April 5, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • BENZO[b]THIOPHENE COMPOUNDS AS STING AGONISTS
    Publication number: 20180093964
    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: October 2, 2017
    Publication date: April 5, 2018
    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
  • METHOD OF TREATING ACUTE MIGRAINE WITH CGRP-ACTIVE COMPOUND
    Publication number: 20180092899
    Abstract: A method of alleviating or mitigating at least one symptom of migraine attack by administering to a patient suffering from a migraine attack a therapeutically effective amount of the compound of Formula I: or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 29, 2017
    Publication date: April 5, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Chi-Chung Liu, David Michelson, Gene Marcantonio, Kyle Fliszer, Rebecca White, Mark Fraley, Leonardo Allain, Tiffani Voss, John Limanto
  • Antidiabetic tricyclic compounds
    Patent number: 9932311
    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: Grant
    Filed: September 30, 2014
    Date of Patent: April 3, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Purakkattle Biju, Steven L. Colletti, Mingxiang Cui, William K. Hagmann, Bin Hu, Hubert Josien, Nam Fung Kar, Anilkumar Nair, Ravi Nargund, Donald M. Sperbeck, Cheng Zhu
  • Inhibitors of IRAK4 activity
    Patent number: 9932350
    Abstract: 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: Grant
    Filed: September 25, 2015
    Date of Patent: April 3, 2018
    Assignee: 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