Patents Assigned to Merck Sharp & Dohme
  • ERK inhibitors
    Patent number: 9884048
    Abstract: The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and an effective amount of at least one other pharmaceutically active ingredient (such as, for example, a chemotherapeutic agent), and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: February 6, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Phieng Siliphaivanh, Joey Methot, Kathryn Ann Lipford, Danielle Molinari, David L. Sloman, David Witter, Hua Zhou, Christopher Boyce, Xianhai Huang, Jongwon Lim, David Guerin, Ganesh Babu Karunakaran, Raman Kumar Bakshi, Ziping Liu, Jianmin Fu, Zhilong Wan, Wei Liu
  • Glucose-responsive insulin conjugates
    Patent number: 9884125
    Abstract: Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: February 6, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Songnian Lin, Christopher R. Moyes
  • Factor IXa Inhibitors
    Publication number: 20180030036
    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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
    Type: Application
    Filed: December 7, 2015
    Publication date: February 1, 2018
    Applicants: MERCK SHARP & DOHME CORP., MOCHIDA PHARMACEUTICAL CO., LTD
    Inventors: Ting Zhang, Yi-Heng Chen, Liangqin Guo, Alan Hruza, Tianying Jian, Bing Li, Dongfang Meng, Dann L. Parker, Edward C. Sherer, Harold B. Wood, Isao Sakurada
  • SUBSTITUTED QUINOLIZINE DERIVATIVES USEFUL AS HIV INTEGRASE INHIBITORS
    Publication number: 20180028509
    Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: October 5, 2017
    Publication date: February 1, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Tao Yu, Yonglian Zhang, Sherman Tim Waddell, Andrew Stamford, John S. Wai, Paul J. Coleman, John M. Sanders, Ronald Ferguson, Thomas H. Graham, Hong Li
  • ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS
    Publication number: 20180030007
    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
    Type: Application
    Filed: October 9, 2017
    Publication date: February 1, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Thomas J. Greshock, Deodial G. Guiadeen, Andrew John Harvey, Belinda C. Huff, Kenneth J. Leavitt, Vanessa L. Rada, John M. Sanders, William D. Shipe, Linda M. Suen, Ian M. Bell
  • Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
    Patent number: 9877957
    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, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Grant
    Filed: August 31, 2015
    Date of Patent: January 30, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason Imbriglio, Clare London, Zhijian Lu, James Tata, Yusheng Xiong, Ming You, Hyewon Youm
  • Factor IXa Inhibitors
    Publication number: 20180022747
    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 unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
    Type: Application
    Filed: February 12, 2016
    Publication date: January 25, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Dongfang Meng, Hong Li, Meng Yang, Manuel de Lera Ruiz, Sunita V. Dewnani, Tianying Jian, Dann L. Parker, Jr., Ting Zhang, Louis-Charles Campeau, Harold B. Wood, Jiayi Xu, Richard Berger, Jane Yang Wu, Robert K. Orr, Shawn P. Walsh, Bart Harper
  • Ceftolozane antibiotic compositions
    Patent number: 9872906
    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: September 16, 2015
    Date of Patent: January 23, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph Terracciano, Nicole Miller Damour, Chun Jiang, Giovanni Fogliato, Giuseppe Alessandro Donadelli, Dario Resemini
  • Dual chamber mixing syringes and methods of using same
    Patent number: 9872962
    Abstract: Provided are mixing syringes having two chambers defined by a pair of pistons located one above the other inside the syringe. Mixing of components separately stored in each of the two chambers occurs when a reversible valve occluding a bore in the distal piston near the discharge end is unseated by removing the retention sleeve and pressing the knob, and the proximal piston nearer the top of the syringe is moved axially toward the distal piston. Further movement of the proximal piston causes it to abut the distal piston resulting in the two pistons acting as one to dispel the now mixed components through the discharge end. Methods are provided for using the syringes for storage and mixing components; discharging the components from the syringe such as by administering the components to a patient in need thereof through a needle when the components are a medicament product.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: January 23, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Christopher J. Granelli
  • Methods and intermediates for preparing macrolactams
    Patent number: 9873707
    Abstract: The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: January 23, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Feng Xu, Richard Desmond, Guy R. Humphrey, Hongming Li, Ji Qi, Rebecca T. Ruck, Zhiguo Jake Song, Tao Wang, Yong-Li Zhong, Jeonghan Park, Laura Marie Artino, Richard John Varsolona
  • PREPARATION AND USE OF 7A-HETEROCYCLE SUBSTITUTED- 6,6-DIFLUORO BICYCLIC HIMBACINE DERIVATIVES AS PAR-1 RECEPTOR ANTAGONISTS
    Publication number: 20180015106
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.
    Type: Application
    Filed: September 26, 2017
    Publication date: January 18, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zhiqiang Yang, Guizhen Dong, Milana Maletic
  • Factor XIa inhibitors
    Patent number: 9868727
    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: July 23, 2015
    Date of Patent: January 16, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D. Edmondson, Zhuyan Guo, Sung-Sau So, Anthony K. Ogawa, Rongze Kuang, Heping Wu, Amjad Ali, Ying-Duo Gao, Yu Jiang, Chunsing Li, Tingting Yu
  • Diazine-fused amidines as BACE inhibitors, compositions, and their use
    Patent number: 9868738
    Abstract: In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, 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: Grant
    Filed: September 14, 2015
    Date of Patent: January 16, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shuwen He, Jared N. Cumming, Andrew W. Stamford
  • Azabenzimidazole tetrahydrofuran derivatives
    Patent number: 9868733
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: August 19, 2013
    Date of Patent: January 16, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James M. Apgar, Tesfaye Biftu, Ping Chen, Danqing Feng, Jacqueline D. Hicks, Ahmet Kekec, Kenneth J. Leavitt, Bing Li, Iyassu Sebhat, Xiaoxia Qian, Lan Wei, Robert R. Wilkening, Zhicai Wu, Ashok Arasappan
  • Hexahydro-1H-4,7-methanoisoindole-1,3-dione compounds
    Patent number: 9867821
    Abstract: The present invention is directed to therapeutic agents which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction.
    Type: Grant
    Filed: March 4, 2013
    Date of Patent: January 16, 2018
    Assignees: SUMITOMO DAINIPPON PHARMA CO., LTD., MERCK SHARP & DOHME CORP.
    Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter
  • CMV neutralizing antigen binding proteins
    Patent number: 9868777
    Abstract: The present invention is directed to antigen binding proteins including, but not limited to, monoclonal antibodies and antigen binding fragments thereof, that specifically bind to and preferably neutralize human cytomegalovirus (CMV). Also encompassed by the invention are antigen binding proteins that have been humanized. The antigen binding proteins of the invention are useful as a therapeutic agent for treating and/or preventing CMV infections in a patient in need thereof.
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: January 16, 2018
    Assignees: Merck Sharp & Dohme Corp., Board of Regents of the University of Texas System
    Inventors: Tong-Ming Fu, Dai Wang, Zhiqiang An
  • IMIDAZOPYRAZINE ANALOGS WITH 3-TERTIARY CARBON SUBSTITUTIONS AS BTK INHIBITORS
    Publication number: 20180009828
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
    Type: Application
    Filed: December 17, 2015
    Publication date: January 11, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: JIAN LIU, JOSEPH A. KOZLOWSKI, XIAOLEI GAO, DEODIAL GUY GUIADEEN, SHILAN LIU, DAHAI WANG
  • TRKA kinase inhibitors, compositions and methods thereof
    Patent number: 9862716
    Abstract: The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-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: Grant
    Filed: March 23, 2015
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Yi-Heng Chen, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Swati P. Mercer, Keith P. Moore, Ping Liu, Harold B. Wood, Chun Sing Li, Qinghua Mao, Douglas C. Beshore
  • Process for preparing chiral dipeptidyl peptidase-IV inhibitors
    Patent number: 9862725
    Abstract: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:
    Type: Grant
    Filed: July 16, 2015
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Feng Peng, Yonggang Chen, Amude Mahmoud Kassim, Cheng-yi Chen, Mathew Maust, Mark McLaughlin, Michael J. Zacuto, Qinghao Chen, Lushi Tan, Zhiguo Jake Song, Yang Cao, Feng Xu
  • Substituted quinolizine derivatives useful as HIV integrase inhibitors
    Patent number: 9861620
    Abstract: The present invention relates to Substituted Quinolizine Derivatives of Formula (I): and pharmaceutically acceptable salts or prodrug thereof, wherein X, Y, R1, R2, R3, R4, R5, R9 and R10 are as defined herein. The present invention also relates to compositions comprising at least one Substituted Quinolizine Derivative, and methods of using the Substituted Quinolizine Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: September 26, 2014
    Date of Patent: January 9, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Yonglian Zhang, Sherman Tim Waddell, Andrew Stamford, John S. Wai, Paul J. Coleman, John M. Sanders, Ronald Ferguson, Thomas H. Graham, Hong Li