Patents Assigned to Merck Sharp
  • Soluble guanylate cyclase stimulators
    Patent number: 10428076
    Abstract: The invention provides compounds of the Formula (I) or a pharmaceutically acceptable salts thereof, wherein X, Y, Z, R1, R2, R4, Ra, and the subscripts m, p, and q 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 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 for preparing pharmaceuticals for this purpose.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: October 1, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Yi-Heng Chen, Guoqing Li, Joie Garfunkle, Hong-Dong Li, Shouwu Miao, Subharekha Raghavan, Cameron J. Smith, John Stelmach, Alan Whitehead, Rui Zhang, Yong Zhang, Jianmin Fu, Gang Ji, Falong Jiang
  • Method of microwave vacuum drying spherical-shaped pellets of biological materials
    Patent number: 10429129
    Abstract: Methods for preparing dried pellets of biological materials are described. The pellets can have a substantially spherical shape and are prepared by freezing droplets of a liquid composition of a desired biological material on a solid surface followed by microwave vacuum drying the frozen droplets. These methods are useful for preparing dried 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: Grant
    Filed: October 13, 2014
    Date of Patent: October 1, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Jessica Sinacola, Rebecca Lizzano
  • Process for purifying insulin and analogues thereof
    Patent number: 10421795
    Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed under low to moderate pressure at an elevated temperature.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: September 24, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael P. Coleman, Allison D. Ortigosa, Mark C. Sleevi, Kartoa Chow
  • Ceftolozane antibiotic compositions
    Patent number: 10420841
    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: Grant
    Filed: December 18, 2017
    Date of Patent: September 24, 2019
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Joseph Terracciano, Nicole Miller Damour, Chun Jiang, Giovanni Fogliato, Giuseppe Alessandron Donadelli, Dario Resemini
  • METHODS FOR USING TRIAZOLO-PYRAZINYL SOLUBLE GUANYLATE CYCLASE ACTIVATORS IN FIBROTIC DISORDERS
    Publication number: 20190282579
    Abstract: Provided are methods for treating or preventing a fibrotic disease selected from systemic sclerosis, cystic fibrosis, non-alcoholic steatohepatitis, Peyronie's disease, or interstitial lung disease; the method comprising administering a therapeutically effective amount of a compound of Formula (I) (wherein R1, R2, R3, R4, and R5 are as herein described) or a pharmaceutically acceptable salt thereof, to a patient in need of such therapy.
    Type: Application
    Filed: May 12, 2017
    Publication date: September 19, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Guizhen Dong, Subharekha Raghavan, Zhiqiang Yang
  • Compound useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolc disease
    Patent number: 10414774
    Abstract: Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jared N. Cumming, Kevin D. Dykstra, Alan Hruza, Derun Li, Hong Liu, Haiqun Tang, Brandon M. Taoka, Andreas Verras, Shawn P. Walsh, Wen-Lian Wu
  • Compounds useful for altering the levels of bile acids for the treatment of diabetes and cardiometabolic disease
    Patent number: 10414775
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.
    Type: Grant
    Filed: August 10, 2017
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John P. Caldwell, Mary Ann Caplen, Jared N. Cumming, Kevin D. Dykstra, Alan Hruza, Claire Lankin, Derun Li, Hong Liu, Amy McCracken, Brian McKittrick, Ashwin Rao, Jayaram Tagat, Haiqun Tang, Brandon M. Taoka, Andreas Verras, Shawn P. Walsh, Wen-Lian Wu, Tianyuan Zhang
  • Benzo[b]thiophene compounds as sting agonists
    Patent number: 10414747
    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: Grant
    Filed: October 2, 2017
    Date of Patent: September 17, 2019
    Assignee: 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
  • Intravaginal ring drug delivery system
    Patent number: 10413504
    Abstract: Described herein is an intra-vaginal drug delivery system comprising (i) a core comprising a first thermoplastic polymer and a first therapeutic agent, wherein the first therapeutic agent is dissolved in the first thermoplastic polymer, and (ii) a skin surrounding the core comprising a second thermoplastic polymer, wherein the first therapeutic agent is less permeable in the second thermoplastic polymer than the first thermoplastic polymer, and a second therapeutic agent in solid form, wherein the second therapeutic agent is loaded in a portion of the skin.
    Type: Grant
    Filed: December 4, 2014
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wouter de Graaff, Willy J. H. Verhoeven
  • Co-agonists of the glucagon and GLP-1 receptors
    Patent number: 10413593
    Abstract: Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor and the glucagon (GCG) receptor, and the use of such GLP-1 receptor/GCG receptor co-agonists for treatment of metabolic disorders such as diabetes, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and obesity.
    Type: Grant
    Filed: October 22, 2015
    Date of Patent: September 17, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Elisabetta Bianchi, Paul E. Carrington, Qiaolin Deng, Ravi Nargund, Federica Orvieto, Anandan Palani, Antonello Pessi, Thomas Joseph Tucker, Chengwei Wu
  • PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS
    Publication number: 20190275024
    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: April 26, 2019
    Publication date: September 12, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Cheng Wang, C. Blair Zartman
  • INDOLE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2
    Publication number: 20190276443
    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, nonalcoholic steatohepatitis (NASH), cardiorenal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Application
    Filed: November 13, 2017
    Publication date: September 12, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Thomas H. Graham, Jinlong Jiang, Fa-Xiang Ding, Clare Tudge
  • Bicyclic aryl monobactam compounds and methods of use thereof for the treatment of bacterial infections
    Patent number: 10407421
    Abstract: The present invention relates to bicyclic aryl monobactam compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein A1, L, M, W, X, Y, Z, RX and Rz are as defined herein. The present invention also relates to compositions which comprise a bicyclic aryl monobactam compound of the invention or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The invention further relates to methods for treating a bacterial infection comprising administering to the patient a therapeutically effective amount of a compound of the invention, either alone or in combination with a therapeutically effective amount of one or more beta-lactamase inhibitor compounds.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: September 10, 2019
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Weiguo Liu, Fa-Xiang Ding, Wanying Sun, Reynalda Keh Dejesus, Haifeng Tang, Xianhai Huang, Jinlong Jiang, Yan Guo, Hongwu Wang
  • Biocatalytic transamination process
    Patent number: 10407702
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: employing dynamic kinetic resolution (DKR). The DKR process involves an enzymatic enantioselective amination reaction catalyzed by transaminases. The process can be used to manufacture key intermediates in the preparation of poly (ADP-ribose) polymerase (PARP) inhibitors which may be useful for the treatment of cancer.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: September 10, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Gerard Bulger, Birgit Kosjek, Nelo Rivera
  • Purifying insulin using cation exchange and reverse phase chromatography in the presence of an organic modifier and elevated temperature
    Patent number: 10407483
    Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed in the presence of a water miscible organic modifier and at an elevated temperature followed by reverse phase chromatography performed in the presence of a water miscible organic modifier and at an elevated temperature.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: September 10, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, Michael P. Coleman, Shibu T. George, Michael A. Rauscher, Mark C. Sleevi, Kartoa Chow
  • Manually-Actuated Injection Device for High-Viscosity Drugs
    Publication number: 20190269857
    Abstract: A manually actuated drug-injecting device is configured such that the grip strength of the entire hand (i.e., majority of fingers closing toward the palm or heel of the hand) is employed to discharge medication through a hypodermic needle and into a patient's body. The device is well suited for delivering medications with high viscosity and/or by patients (e.g., elderly patients) with reduced finger strength and dexterity. The device includes a grip member, a push member (which causes the medication to be injected), and a force-transfer mechanism that couples the grip member to the push member. Suitably, the device is configured to be held transverse to the palm of the medication-administering hand, with a discharge port located by the outer, blade edge of the administering hand, when the device is being gripped to administer medication.
    Type: Application
    Filed: November 20, 2017
    Publication date: September 5, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Peter A. BASILE, Henry J. MACK, Jr., Oliver SHA, Steven G. MIGGELS
  • TREATING CANCER WITH A COMBINATION OF A PD-1 ANTAGONIST AND AN IL-27 ANTAGONIST
    Publication number: 20190270802
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and an antagonist of IL-27, and the use of the combination therapies for the treatment of cancer. In certain embodiments, the PD-1 antagonist is an anti-human PD-1 antibody, or antigen binding fragment thereof. In further embodiments, the anti-PD-1 antibody is pembrolizumab. In certain embodiments the antagonist of IL-27 is an anti-IL-27 antibody, or antigen binding fragment thereof, an anti-p28 antibody, or antigen binding fragment thereof, or an anti-EBI-3 antibody, or antigen binding fragment thereof. Also provided are medicaments, compositions, and kits comprising a PD-1 antagonist and an IL-27 antagonist for use in treating cancer.
    Type: Application
    Filed: October 19, 2017
    Publication date: September 5, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Nataliya Tovbis Shifrin, Rene de Waal Malefyt
  • HYDROXY ISOXAZOLE COMPOUNDS USEFUL AS GPR120 AGONISTS
    Publication number: 20190269679
    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: December 11, 2017
    Publication date: September 5, 2019
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John S. Debenham, Jason M. Cox, Ping Lan, Zhongxiang Sun, Zhe Feng, Chunrui Sun, Michael W. Seganish, Zhong Lai, Cheng Zhu, Thomas Bara, Murali Rajagopalan, Qun Dang, Hyunjin M. Kim, Bin Hu, Jinglai Hao
  • Tricyclic compounds as inhibitors of mutant IDH enzymes
    Patent number: 10399972
    Abstract: The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds 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: October 25, 2016
    Date of Patent: September 3, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David J. Witter, Tesfaye Biftu, Purakkattle Biju, Stephane L. Bogen, Qingmei Hong, Chunhui Huang, Xianhai Huang, Bing Li, Min K. Park, David L. Sloman
  • Anti-GITR antibodies
    Patent number: 10400040
    Abstract: Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: September 3, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiao Min Schebye, Grigori P. Ermakov, Douglas J. Hodges, Leonard G. Presta