Patents Assigned to Merck Sharp & Dohme
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9850245
    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 26, 2015
    Date of Patent: December 26, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Fa-Xiang Ding, Shuzhi Dong, Jinlong Jiang, Haifeng Tang, Xin Gu, Reynalda K. DeJesus, Jessica Frie, Qinghong Fu, Takao Suzuki, Zhifa Pu
  • DENGUE VIRUS VACCINE COMPOSITIONS AND METHODS OF USE THEREOF
    Publication number: 20170360917
    Abstract: The present invention relates to dengue virus vaccine compositions comprising a first and a second dengue vaccine, wherein the first dengue vaccine comprises at least one live, 5 attenuated dengue virus or live, attenuated chimeric dengue virus and the second dengue vaccine is a recombinant dengue subunit vaccine, a DNA vaccine, a conjugate vaccine, or an inactivated dengue vaccine; wherein the genome of the live attenuated dengue virus or the live attenuated chimeric dengue virus comprises a 30 nucleotide deletion of the TL2 stem-loop structure of the 3? untranslated region. The dengue virus vaccine compositions of the invention may further 10 comprise one or more adjuvants. In preferred embodiments of the invention, the first and the second dengue vaccine are tetravalent.
    Type: Application
    Filed: December 18, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Danilo R. Casimiro, Andrew Bett, Beth-Ann Griswold Coller, Govindarajan Dhanasekaran, Ramesh V. Chintala
  • PROCESS FOR THE PREPARATION OF TERT-BUTYL 4-((2S,5R)-6-(BENZYLOXY)-7-OXO-1,6-DIAZABICYCLO[3.2.1]OCTANE-2-CARBOXAMIDO)PIPERIDINE-1-CARBOXYLATE AND ANALOGS THEREOF
    Publication number: 20170362233
    Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include intermediates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 30, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zhijian Liu, Nobuyoshi Yasuda, Lu Yang, Artis Klapars, Kevin R. Campos, Mikhail Reibarkh
  • C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170362248
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, 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: Application
    Filed: November 20, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xing Dai, Jared N. Cumming, Hong Liu, Jack D. Scott
  • (S)-N-(3-(6-ISOPROPOXYPYRIDIN-3-YL)-1H-INDAZOL-5-YL)-1-(2-(4-(4-(1-METHYL-1H-1,2,4-TRIAZOL-3-YL)PHENYL)-3,6-DIHYDROPYRIDIN-1(2H)-YL)-2-OXOETHYL)-3-(METHYLTHIO)PYRROLIDINE-3-CARBOXAMIDE COMPOSITIONS FOR PHARMACEUTICAL PREPARATIONS
    Publication number: 20170362202
    Abstract: A composition comprising (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
    Type: Application
    Filed: December 14, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, Jason Wan, Scott T. Trzaska
  • NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
    Publication number: 20170360800
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N?; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to uses of the tricyclic compounds described herein 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: Application
    Filed: December 1, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew Lloyd Childers, Francesc Xavier Fradera Llinas, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Dann L. Parker, Jr., Nunzio Sciammetta, Patrick Pengcheng Shao, David L. Sloman, Wanying Sun, Feroze Ujjainwalla
  • PYRAZOLYL CARBOXYLIC ACID AND PYRAZOLYL UREA DERIVATIVE COMPOUNDS
    Publication number: 20170362183
    Abstract: Pyrazolyl carboxylic acid and pyrazolyl urea derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds.
    Type: Application
    Filed: December 18, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Yisheng Yang, Youchu Wang
  • NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
    Publication number: 20170362220
    Abstract: The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)? or —N?; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the tricyclic compounds described herein 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: Application
    Filed: December 1, 2015
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christian Fischer, Stephane L. Bogen, Matthew L. Childers, Francesc Xavier Fradera Llinas, Michael J. Ellis, Sara Esposite, Dawn M. Hoffman, Chunhui Huang, Solomon D. Kattar, Alexander J. Kim, John W. Lampe, Michelle R. Machacek, Daniel R. McMasters, Dann L. Parker, Jr., Michael H. Reutershan, Nunzio Sciammetta, Patrick Pengcheng Shao, David L. Sloman, Wanying Sun, Feroze Ujjainwalla, Zhicai Wu, Yang Yu, Craig R. Gibeau
  • GLYCAN-BASED ANTIBODY-DRUG CONJUGATES
    Publication number: 20170362338
    Abstract: Genetically engineered antibodies containing non-native N-glycosylated sites, preparation of the antibodies in yeast and fungi, site-specific conjugation of drugs to these antibodies, and methods of treatment utilizing these antibodies are described herein.
    Type: Application
    Filed: April 21, 2017
    Publication date: December 21, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Robert Davidson, Bing Gong
  • Liquid formulations for an anti-TNF ? antibody
    Patent number: 9844594
    Abstract: The invention provides stable liquid formulations for a recombinant biopharmaceutical protein comprising a fully human anti-TNF monoclonal antibody.
    Type: Grant
    Filed: December 13, 2013
    Date of Patent: December 19, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Valentyn Antochshuk, Amardeep Bhalla, Azher M. Hussain
  • Pyrazolopyridyl compounds as aldosterone synthase inhibitors
    Patent number: 9844553
    Abstract: This invention relates to pyrazolopyridyl compounds of the structural formula: or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthase.
    Type: Grant
    Filed: April 27, 2016
    Date of Patent: December 19, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: D. Jonathan Bennett, Jaiqiang Cai, Emma Carswell, Andrew Cooke, Scott B. Hoyt, Clare London, John MacLean, Min K. Park, Paul Ratcliffe, Yusheng Xiong, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
  • INSULIN RECEPTOR PARTIAL AGONISTS
    Publication number: 20170355743
    Abstract: Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.
    Type: Application
    Filed: November 19, 2015
    Publication date: December 14, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Lin Yan, Pei Huo, Dmitri Pissarnitski, Danqing Feng, Ravi Nargund, Yuping Zhu, Ahmet Kekec, Christina B. Madsen-Duggan, Zhi-Cai Shi, Zhicai Wu, Yingjun Mu
  • ANTI-GITR ANTIBODIES
    Publication number: 20170355772
    Abstract: Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.
    Type: Application
    Filed: June 16, 2017
    Publication date: December 14, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Xiao Min Schebye, Grigori P. Ermakov, Douglas J. Hodges, Leonard G. Presta
  • ETHYLDIAMINE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170355692
    Abstract: The present invention is directed to ethyldiamne 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: Application
    Filed: December 14, 2015
    Publication date: December 14, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • FORMULATION INHIBITING EFFECTS OF LOW ACID ENVIRONMENT
    Publication number: 20170354658
    Abstract: The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.
    Type: Application
    Filed: December 1, 2015
    Publication date: December 14, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Lei Zhu, Yvonne Cegielnik, Qun Lu
  • ANTI-COAGULATION FACTOR XI ANTIBODIES
    Publication number: 20170355780
    Abstract: Antibodies that bind the apple 3 domain of human coagulation Factor XI and inhibit activation of FXI by coagulation factor XIIa as well as activation of FIX by FXIa are described.
    Type: Application
    Filed: June 12, 2017
    Publication date: December 14, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Zhu Chen, Kenneth Ellsworth, James Milligan, Elizabeth Oldham, Dietmar Seiffert, Vaishnavi Ganti, Mohammad Tabrizifard
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9839629
    Abstract: Novel spirocyclic compounds of formula I: and pharmaceutically acceptable salts thereof are disclosed as 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. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuzhi Dong, Alexander Pasternak, Xin Gu, Qinghong Fu, Jinlong Jiang, Fa-Xiang Ding, Haifeng Tang, Reynalda K. DeJesus, Takao Suzuki
  • Beta-tetrazolyl-propionic acids as metallo-beta-lactamase inhibitors
    Patent number: 9839642
    Abstract: The present invention relates to compounds of formula I that are metallo-?-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with ?-lactam antibiotics for overcoming resistance.
    Type: Grant
    Filed: May 4, 2015
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Shu-Wei Yang, Mihir Mandal, Jing Su, Guoqing Li, Weidong Pan, Haiqun Tang, Reynalda DeJesus, Jianping Pan, William Hagmann, Fa-Xiang Ding, Li Xiao, Alexander Pasternak, Yuhua Huang, Shuzhi Dong, Dexi Yang
  • Allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 9840481
    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: Grant
    Filed: March 20, 2017
    Date of Patent: December 12, 2017
    Assignee: 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
  • Piperazine derivatives as HIV protease inhibitors
    Patent number: 9840478
    Abstract: The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, 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.
    Type: Grant
    Filed: July 29, 2014
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter D. Williams, John A. McCauley, David Jonathan Bennett, Christopher J. Bungard, Lehua Chang, Michael P. Dwyer, M. Katharine Holloway, Kartik M. Keertikar, H. Marie Loughran, Jessie J. Manikowski, Gregori J. Morriello, Dong-Ming Shen, Edward C. Sherer, Jurgen Schultz, Sherman T. Waddell, Catherine M. Wiscount, Nicolas Zorn, Xin-Jie Chu, Satyanarayana Tummanapalli, Vijayasaradhi Sivalenka, Bin Hu, Tao Ji, Bin Zhong