Patents Assigned to Merck Sharp
  • C2,C6 OXACYCLIC-FUSED THIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20150344500
    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, ring A, RA, m, -L1-, and RL 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: December 16, 2013
    Publication date: December 3, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Jared N. Cumming, David Earl Kaelin, Jr., Jack D. Scott, Wen-Lian Wu, Duane A. Burnett
  • Methods and compositions for regulating cell cycle progression
    Patent number: 9200275
    Abstract: In one aspect, a method is provided of inhibiting proliferation of a mammalian cell comprising introducing into said cell an effective amount of at least one at least one small interfering RNA agent (iRNA), wherein said iRNA comprises a nucleotide sequence of at least 15 nucleotides, wherein the nucleotide sequence comprises a seed region consisting of nucleotide positions 1 to 12, wherein position 1 represents the 5? end of the iRNA nucleotide sequence and wherein said seed region comprises a nucleotide sequence of at least six contiguous nucleotides that is complementary to six contiguous nucleotides within positions 1 to 12 of a nucleotide sequence, wherein position 1 represents the 5?end of the nucleotide sequence, wherein the nucleotide sequence is selected from the group consisting of SEQ ID NO: 1, SEQ ID NO:2, SEQ ID NO:3, SEQ ID NO:4, SEQ ID NO:5, SEQ ID NO:6, SEQ ID NO:7 and SEQ ID NO:8.
    Type: Grant
    Filed: June 14, 2007
    Date of Patent: December 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter S. Linsley, Janell Schelter, Julja Burchard, Lee Lim, Miho Kibukawa
  • Recombinant subunit dengue virus vaccine
    Patent number: 9198964
    Abstract: The present invention provides dengue virus vaccines and immunogenic compositions for administration to human subjects. The vaccine compositions of the present invention comprise recombinantly produced monomeric and/or dimeric forms of truncated dengue virus envelope glycoprotein that, when formulated together with an adjuvant and a pharmaceutically acceptable carrier, induce balanced tetravalent immune responses. In preferred embodiments of the compositions described herein, the DEN4 protein component is a dimeric form of DEN4. The compositions are designed to be acceptable for use in the general population, including immunosuppressed, immunocompromised, and immunosenescent individuals. Also provided herein are methods of inducing a protective immune response in a human patient population by administering the compositions described herein to the patients.
    Type: Grant
    Filed: October 27, 2011
    Date of Patent: December 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Beth-Ann Griswold Coller, Vidya B. Pai, D. Elliot Parks, Michele Yelmene, Andrew J. Bett, Timothy Martyak
  • Antibacterial agents
    Patent number: 9200026
    Abstract: Described herein are novel macrolides, the preparation of novel macrolides, the use of novel macrolides for preventing, treating, or ameliorating various conditions, and the use of novel macrolides as antibacterial agents.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: December 1, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Chang-Hsing Liang, Jonathan Duffield, Alex Romero, Yu-Hung Chiu, Steve Sucheck, Kenneth Marby, Youe-Kong Shue, Yoshitaka Ichikawa, Chan-Kou Hwang, David Rabuka, Sulan Yao
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9199949
    Abstract: The invention provides compounds 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: June 27, 2012
    Date of Patent: December 1, 2015
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Tong-Shuang Li, Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Quinoline amide M1 receptor positive allosteric modulators
    Patent number: 9199939
    Abstract: The present invention is directed to quinoline amide compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: December 13, 2010
    Date of Patent: December 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Kelly-Ann S. Schlegel, Zhi-Qiang Yang
  • Triazolyl PDE10 inhibitors
    Patent number: 9200001
    Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating 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: October 3, 2012
    Date of Patent: December 1, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
  • HETEROCYCLE-SUBSTITUTED TETRACYCLIC COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
    Publication number: 20150335648
    Abstract: The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2 R3, R4 and R are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetracyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: December 31, 2013
    Publication date: November 26, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Wensheng Yu, Ling Tong, Joseph A. Kozlowski, Oleg Selyutin, Lei Chen, Jae-Hun Kim, Deyou Sha, Razia Rizvi, Bandarpalle Shankar, Bin Hu, Bin Zhong, Dahai Wang, Jinglai Hao, Wei Wei, Tao Ji, Shuai Zan
  • NOVEL ANTIBACTERIAL AGENTS FOR THE TREATMENT OF GRAM POSITIVE INFECTIONS
    Publication number: 20150337013
    Abstract: The present invention relates to novel lipopeptide compounds, pharmaceutical compositions of these compounds and methods of using these compounds as antibacterial compounds. The compounds of the invention are particularly useful against a variety of bacteria, including resistant strains. The compounds are useful as antibacterial agents against Clostridium difficile.
    Type: Application
    Filed: August 4, 2015
    Publication date: November 26, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Chester A. Metcalf, III, Jing Li, Andre Lee Pearson
  • NOVEL 2-PYRIDINECARBOXAMIDE DERIVATIVES, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT
    Publication number: 20150336946
    Abstract: Novel pyridine-2-carboxamide derivatives of formula I and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included. The present invention relates to novel pyridine-2-carboxamide derivatives and salts thereof which are effective as glucokinase activating agents. Moreover, it relates to compositions containing such compounds, and methods of treatment.
    Type: Application
    Filed: December 12, 2013
    Publication date: November 26, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Songnian Lin, Emma R. Parmee, Jiayi Xu
  • NOVEL GLUCOKINASE ACTIVATOR COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF TREATMENT
    Publication number: 20150336991
    Abstract: Novel pyridine-2-carboxamide derivatives of formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are effective as glucokinase activating agents. Pharmaceutical compositions and methods of treatment are also included.
    Type: Application
    Filed: December 12, 2013
    Publication date: November 26, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Songnian Lin, Rui Zhang, Brian Campbell, Sunita V. Dewnani, Jiayi Xu, Libo Xu, Emma R. Parmee, Roman Kats-Kagan
  • Mineralocorticoid receptor antagonists
    Patent number: 9193717
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: November 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hong Shen, Christine Yang, Jason M. Cox, Kun Liu
  • Oxazole derivatives useful as modulators of FAAH
    Patent number: 9193697
    Abstract: The present invention is directed to certain Oxazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: November 24, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: ZhiQiang Yang, Philippe G. Nantermet, Constantine Kreatsoulas, Keith P. Moore, Evan Foster Shalen
  • Triazolopyridyl compounds as aldosterone synthase inhibitors
    Patent number: 9193724
    Abstract: This invention relates to triazolopyridyl 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: September 17, 2012
    Date of Patent: November 24, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: D. Jonathan Bennett, Jaiqiang Cai, Emma Carswell, Andrew Cooke, Scott B. Hoyt, Clare London, John MacLean, Paul Ratcliffe, Jerry Andrew Taylor, Yusheng Xiong, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
  • SUBSTITUTED PYRROLOPYRIMIDINES AS HDM2 INHIBITORS
    Publication number: 20150329548
    Abstract: The present invention provides substituted pyrrolopyrimidines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Application
    Filed: December 18, 2013
    Publication date: November 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Christopher Dinsmore, Francesc Xavier Fradera Llinas, Amit Ashokro Kudale, Michelle Machacek, Michael Hale Reutershan, Christopher Francis Thompason, B. Wesley Trotter, Liping Yang, Michael D. Altman, Stephane L. Bogen, Ronald J. Doll, Matthew E. Voss
  • Factor IXa Inhibitors
    Publication number: 20150329562
    Abstract: The present invention provides a compound of Formula (I) wherein R1, R2, R3 and R4 are independently H or C1-6 alkyl, provided that when R1, R2, and R3 are H, R4 is C1-6 alkyl, and when R1, R2, and R4 are H, R3 is C1-6 alkyl, and when R1, R3, and R4 are H, R2 is C1-6 alkyl, and when R2, R3, and R4 are H, R is C1-6 alkyl; 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.
    Type: Application
    Filed: December 16, 2013
    Publication date: November 19, 2015
    Applicants: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Cameron James Smith, John Qiang Tan, Ting Zhang, James Balkovec, William John Greenlee, Liangqin Guo, Yi-Heng Chen, Yili Chen, Samuel Chackalamannil, Tomokazu Hirabayashi, Mika Sekioka
  • Inhibitors of the Renal Outer Medullary Potassium Channel
    Publication number: 20150329557
    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 conditions associated with excessive salt and water retention.
    Type: Application
    Filed: December 13, 2013
    Publication date: November 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda Keh DeJesus, Jessica L. Frie, Barbara Pio, Haifeng Tang, Shawn P. Walsh
  • AMINO-PYRIMIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS
    Publication number: 20150329531
    Abstract: The invention provides certain amino-pyrimidine-containing compounds. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
    Type: Application
    Filed: December 9, 2013
    Publication date: November 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Michelle R. Machacek
  • PROCESS FOR MAKING REVERSE TRANSCRIPTASE INHIBITORS
    Publication number: 20150329521
    Abstract: The present invention is directed to a novel process for synthesizing 3-(substituted phenoxy)-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl])-pyridin-2(1H)-one derivatives. The compounds synthesized by the processes of the invention are HIV reverse transcriptase inhibitors useful for inhibiting reverse transcriptase, HIV replication and the treatment of human immunodeficiency virus infection in humans.
    Type: Application
    Filed: December 4, 2013
    Publication date: November 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tetsuji Itoh, Ingyu Jeon, Ian Mangion, Gang QIAN, Benjamin D. Sherry, Donald R. Gauthier, Yang CAO
  • PROCESS FOR PURIFYING INSULIN AND ANALOGUES THEREOF
    Publication number: 20150329612
    Abstract: A process is described for purifying insulin and insulin analogues that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed under low to moderate pressure at an elevated temperature.
    Type: Application
    Filed: December 12, 2013
    Publication date: November 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michael P. COLEMAN, Allison D. ORTIGOSA, Mark C. SLEEVI, Kartoa CHOW