Patents Assigned to Merck, Sharp & Dohms, Corp.
  • SUBSTITUTED 6-MEMBERED ARYL OR HETEROARYL ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20210077511
    Abstract: 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: March 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: BRENDAN M. CROWLEY, IAN M. BELL, ANDREW JOHN HARVEY, BRIAN T. CAMPBELL, THOMAS J. GRESHOCK, VANESSA L. RADA
  • Azabicyclo[4.1.0]heptane allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 10945771
    Abstract: The present invention is directed to azabicyclo[4.1.0]heptane 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: June 4, 2018
    Date of Patent: March 16, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dane James Clausen, James I. Fells, Joseph A. Kozlowski, Ping Liu, Robert D. Mazzola, Jr.
  • Oxazolidinone compounds and methods of use thereof as antibacterial agents
    Patent number: 10947205
    Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: March 16, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mihir B. Mandal, David B. Olsen, Jing Su, Lihu Yang, Katherine Young, Takao Suzuki, Lanying You
  • Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
    Patent number: 10947222
    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: Grant
    Filed: November 13, 2017
    Date of Patent: March 16, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dong-Ming Shen, Thomas H. Graham, Jinlong Jiang, Fa-Xiang Ding, Clare Tudge
  • PRMT5 inhibitors
    Patent number: 10947234
    Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: March 16, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, David J. Witter, Michael Hale Reutershan, Michael D. Altman, Paul Anthony Stupple
  • SPIROPIPERIDINE ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20210070745
    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 (I).
    Type: Application
    Filed: April 29, 2019
    Publication date: March 11, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Harry R. Chobanian, James I. Fells, Deodial G. Guiadeen, Thomas J. Greshock, Kenneth J. Leavitt, Vanessa L. Rada, Ian M. Bell
  • Intermediates in the synthesis of cephalosporin compounds
    Patent number: 10941161
    Abstract: Described herein are crystalline forms of a compound of formula (III?), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: March 9, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
  • OXAZOLIDINONE COMPOUNDS AND METHODS OF USE THEREOF AS ANTIBACTERIAL AGENTS
    Publication number: 20210061777
    Abstract: The present invention relates to oxazolidinone compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, E, and R1 are as defined herein. The present invention also relates to compositions which comprise at least one oxazolidinone compound of the invention. The invention also provides methods for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis comprising administering a therapeutically effective amount of an oxazolidinone of the invention and/or a pharmaceutically acceptable salt thereof, or a composition comprising such compound and/or salt.
    Type: Application
    Filed: November 10, 2020
    Publication date: March 4, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mihir B. Mandal, David B. Olsen, Jing Su, Lihu Yang, Katherine Young, Takao Suzuki, Lanying You
  • Substituted pyrazolo[3,4-d]pyrimidines as PDE9 inhibitors
    Patent number: 10934294
    Abstract: The present invention is directed to pyrazolopyrimidine compounds of the general structural formula I: which may be useful as therapeutic agents for the treatment of disorders associated with phosphodiesterase 9 (PDE9). The present invention also relates to the use of such compounds for treating cardiovascular and cerebrovascular diseases, such as hypertension, chronic kidney disease and heart failure, and neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: June 6, 2018
    Date of Patent: March 2, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ashok Arasappan, Jason M. Cox, John S. Debenham, Zhuyan Guo, Jiafang He, Zahid Hussain, Zhong Lai, Derun Li, Dongfang Meng, Subharekha Raghavan, Sriram Tyagarajan
  • 3-(1H-pyrazol-4-yl)pyridine allosteric modulators of the M4 muscarinic acetylcholine receptor
    Patent number: 10933056
    Abstract: 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 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: November 5, 2019
    Date of Patent: March 2, 2021
    Assignees: Merck Sharp & Dohme Corp., MSD R&D (China) Co. Ltd.
    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
  • IMIDAZO[1,2-C]QUINAZOLIN-5-AMINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
    Publication number: 20210053973
    Abstract: Disclosed are compounds having the structure of Formula I, or a pharmaceutically acceptable salt of any thereof: wherein: “Z” and R1 are defined herein, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Application
    Filed: December 10, 2018
    Publication date: February 25, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad ALI, Yeon-Hee LIM, Gioconda V. GALLO-ETIENNE, Joseph Michael KELLY, Michael BERLIN, Pauline TING, Jayaram R. TAGAT, Dong XIAO, Rongze KUANG, Heping WU, Hongwu WANG
  • OXO-TETRAHYDRO-ISOQUINOLINE CARBOXYLIC ACIDS AS STING INHIBITORS
    Publication number: 20210052573
    Abstract: The instant invention provides compounds of formula I which are STING inhibitors, and as such are useful for the treatment of STING-mediated diseases such as inflammation, asthma, COPD and cancer.
    Type: Application
    Filed: March 15, 2019
    Publication date: February 25, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Matthew L. Childers, James P. Jewell, Charles A. Lesburg, Tony Siu
  • Substituted sulfoximine compounds as indoleamine 2,3-dioxygenase (IDO) inhibitors
    Patent number: 10927086
    Abstract: Compounds of Formula I, or a pharmaceutically acceptable salt, solvate or hydrate thereof: (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
    Type: Grant
    Filed: February 19, 2018
    Date of Patent: February 23, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Dane Clausen, Liangqin Guo, Yongxin Han, Shuwen He, Joseph Kozlowski, Derun Li, Qinglin Pu, Wensheng Yu, Hongjun Zhang
  • Methods for using triazolo-pyrazinyl soluble guanylate cyclase activators in fibrotic disorders
    Patent number: 10925876
    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: Grant
    Filed: May 12, 2017
    Date of Patent: February 23, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Guizhen Dong, Subharekha Raghavan, Zhiqiang Yang
  • METHODS FOR TREATING CANCER WITH ANTI-PD-1 ANTIBODIES
    Publication number: 20210047408
    Abstract: The present invention relates to methods for treating cancer in a patient comprising administering a PD-1 antagonist, e.g., an anti-PD-1 antibody or antigen binding fragment thereof (e.g. pembrolizumab), in specific amounts to the patient about every six weeks. In some embodiments, the amount of anti-PD-1 antibody or antigen binding fragment thereof is about 400 mg. In certain embodiments, the PD-1 antagonist is pembrolizumab, or an antigen binding fragment thereof. Also provided are compositions and kits comprising a dosage of an anti-PD-1 antibody, or antigen-binding fragment thereof, and uses thereof for treating cancer.
    Type: Application
    Filed: February 8, 2019
    Publication date: February 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mallika Lala, Lokesh Jain, Mengyao Li
  • METHOD FOR PREPARING ANTIBODIES HAVING IMPROVED PROPERTIES
    Publication number: 20210047670
    Abstract: The present invention is directed to methods and compositions for the production of Fc-containing polypeptides having improved properties and comprising mutations at positions 243 and 264 of the Fc region.
    Type: Application
    Filed: October 20, 2020
    Publication date: February 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Terrance A. Stadheim, Dongxin Zha, Liming Liu
  • METHOD OF MICROWAVE VACUUM DRYING SPHERICAL-SHAPED PELLETS OF BIOLOGICAL MATERIALS
    Publication number: 20210048247
    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: Application
    Filed: October 27, 2020
    Publication date: February 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Jessica Sinacola, Rebecca Lizzano
  • METHODS FOR TREATING CANCER WITH ANTI PD-1 ANTIBODIES AND ANTI CTLA4 ANTIBODIES
    Publication number: 20210047409
    Abstract: The present invention relates to methods for treating cancer in a patient comprising administering an anti-PD-1 antibody or antigen binding fragment thereof in specific amounts to the patient about every six weeks, in combination with administering an anti-CTLA4 antibody to the patient about every six weeks. In certain embodiments, the PD-1 antagonist is pembrolizumab, or an antigen binding fragment thereof. Also provided are compositions comprising a dosage of an anti-PD-1 antibody, or antigen-binding fragment thereof, and a dosage of an anti-CTLA4 antibody or antigen-binding fragment thereof, and uses thereof for treating cancer.
    Type: Application
    Filed: February 8, 2019
    Publication date: February 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mallika Lala, Lokesh Jain, Mengyao Li, Rachel Allison Altura, Archie Ngai-chiu Tse
  • SCALABLE CHROMATOGRAPHY PROCESS FOR PURIFICATION OF HUMAN CYTOMEGALOVIRUS
    Publication number: 20210047626
    Abstract: The present invention relates to a scalable process for the purification of human cytomegalovirus particles from cell culture medium. In particular, the process involves a two step chromatography process starting with an anion exchange chromatography step followed by a polishing chromatography step selected from mixed mode chromatography or cation exchange chromatography.
    Type: Application
    Filed: April 18, 2019
    Publication date: February 18, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Adam Kristopeit, Janelle Konieizko, Wanli Ma, Katie Phillips, Andrew Swartz, Sheng-Ching Wang, Marc D. Wenger, Matthew Woodling, Tiago Matos
  • ARGINASE INHIBITORS AND METHODS OF USE
    Publication number: 20210040127
    Abstract: Described herein are compounds of Formula I or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as arginase inhibitors and can be useful in preventing, treating or acting as a remedial agent for arginase-related diseases.
    Type: Application
    Filed: March 8, 2019
    Publication date: February 11, 2021
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abdelghani Abe Achab, Matthew L. Childers, Jared N. Cumming, Christian A. Fischer, Symon Gathiaka, Hakan Gunaydin, Charles A. Lesburg, Derun Li, Min Lu, Anandan Palani, Rachel L. Palte, Qinglin Pu, David L. Sloman, Sung-Sau So, Chunrui Sun, Hongjun Zhang