Patents Assigned to Merck Sharp & Dohme
  • 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
  • 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
  • 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
  • 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 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 4-PYRIDINONETRIAZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
    Publication number: 20150329539
    Abstract: The present invention relates to 4-Pyridinonetriazine Derivatives of Formula (I); and pharmaceutically acceptable salts thereof, wherein A, X, Y, R1, R2, R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one 4-Pyridinonetriazine Derivative, and methods of using the 4-Pyridinonetriazine Derivatives for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: December 12, 2013
    Publication date: November 19, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mark W. Embrey, Thomas H. Graham, Abbas Walji, Sherman T. Waddell, Tao Yu, Yonglian Zhang, Wensheng Liu, Paul J. Coleman, John Wai, Thomas Steele, Christina Di Marco
  • 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
  • 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
  • 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
  • Method for preparing antibodies having improved properties
    Patent number: 9187552
    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: Grant
    Filed: May 25, 2011
    Date of Patent: November 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Terrance A. Stadheim, Dongxing Zha, Liming Liu
  • Pyrrolidine derived ?3 adrenergic receptor agonists
    Patent number: 9186354
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor. (I).
    Type: Grant
    Filed: July 18, 2011
    Date of Patent: November 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Harvey R. Wendt, Scott D. Edmondson
  • Process for preparing chiral dipeptidyl peptidase-IV inhibitors
    Patent number: 9187488
    Abstract: A process for the preparation of pyrazolopyrolidines of structural formula I: and W is or P, wherein in P is an amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: November 17, 2015
    Assignees: Merck Sharp & Dohme Corp, Merck Sharp & Dohme Ltd.
    Inventors: Michael J. Zacuto, Robert F. Dunn, Aaron J. Moment, Jacob M. Janey, David Lieberman, Faye Sheen, Nadine Bremeyer, Jeremy Scott, Jeffrey T. Kuethe, Lushi Tan, Qinghao Chen