Patents Assigned to Merck Sharp
  • Publication number: 20150218097
    Abstract: The invention provides compounds of Formula (I) for inhibiting gh cosidases, prodrugs of the compounds, and pharmaceutical compositions comprising the compounds or prodrugs of the compounds. The invention also provides method of treating diseases and disorders related to deficiency or over-expression of O-gh coprotein 2-acetamido-2-deoxy-?-D-glucopyranosidase (O-GlcNAcase), accumulation or deficiency of 2-acetamido-2-deoxy-?-D-glucopyranoside (O-GlcNAc).
    Type: Application
    Filed: August 29, 2013
    Publication date: August 6, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • Patent number: 9096559
    Abstract: The present invention relates to a novel class of 4-carboxybenzylamino derivatives. The 4-carboxybenzylamino compounds can be used to treat cancer. The 4-carboxybenzylamino compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: January 28, 2013
    Date of Patent: August 4, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul Harrington, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, Matthew G. Stanton, Paul Tempest, Kevin J. Wilson, David J. Witter
  • Patent number: 9096598
    Abstract: The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: August 4, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John W. Butcher, David Witter, Christopher Dinsmore, June Kim, John Hendrix, Raksha Archarya, Sean P. Ahearn, Joon Jung, Alexey Rivkin, Philip Jones
  • Patent number: 9096582
    Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing compounds of Formula (I) and use of the compounds in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: August 4, 2015
    Assignee: MERCK SHARP & DOHME CORP
    Inventors: William Greenlee, Dmitri Pissarnitski, Zhiqiang Zhao, Zhaoning Zhu
  • Patent number: 9095583
    Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
    Type: Grant
    Filed: February 10, 2012
    Date of Patent: August 4, 2015
    Assignees: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.
    Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
  • Publication number: 20150209424
    Abstract: The invention provides an inactivated varicella zoster virus (VZV), and compositions and vaccines comprising said inactivated VZV, wherein the infectivity of the VZV is undetectable and wherein the inactivated VZV induces an immune response against VZV when administered to a patient. In embodiments of the compositions described herein, the VZV is inactivated with gamma radiation. The invention also provides a method of preparing an inactivated VZV vaccine, the method comprising gamma irradiating a sample comprising a VZV using from about 5 kGy to about 50 kGy of gamma radiation. Also provided by the invention herein is a method of treatment of or immunization against HZ or other disease associated with the reactivation of VZV, the method comprising administering to a subject a vaccine or pharmaceutical composition comprising a therapeutically effective amount of an inactivated VZV and a pharmaceutically acceptable carrier, wherein the VZV is inactivated by gamma irradiation.
    Type: Application
    Filed: April 3, 2015
    Publication date: July 30, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: David L. Krah, Jill DeHaven, Jennifer A. Kriss, Colleen M. Barr, Mary Yagodich
  • Patent number: 9090661
    Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
    Type: Grant
    Filed: August 29, 2014
    Date of Patent: July 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, John A. McCauley, Steven W. Ludmerer, Kun Liu, Joseph P. Vacca, Hao Wu, Bin Hu, Richard Soll, Fei Sun, Xinghai Wang, Man Yan, Chengren Zhang, Mingwei Zheng, Bin Zhong, Jian Zhu
  • Patent number: 9089522
    Abstract: The present invention provides, in part, methods and compositions for treating lipid disorders comprising administering a polypeptide that inhibits PCSK9. A novel method for identifying polypeptides that interact with PCSK9 is also provided.
    Type: Grant
    Filed: May 21, 2009
    Date of Patent: July 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qing Zhang, Nicholas J. Murgolo, Joseph A. Hedrick
  • Patent number: 9085568
    Abstract: The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible 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 above mentioned 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: July 21, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hong Shen, Jason M. Cox, Hong Dong Chu
  • Publication number: 20150197772
    Abstract: The present invention relates to the construction and utilization of a new mammalian expression vector that contains a unique multiple cloning site (MCS), designated pUHAB. The pUHAB vector comprises a high copy replication origin (ColE1), a drug resistance gene (TK-Hygromycin), and a human cytomegalovirus promoter operably associated with a unique intron (hCMV/intron). Further, pUHAB comprises a selectable marker conferring resistance to kanamycin in bacterial cells, and a phage f1(+) region. pUHAB can be used to transiently or stably express cloned genes when transfected into mammalian cells. The invention also encompasses kits and host cells and cell lines comprising pUHAB, and methods of producing a recombinant protein using pUHAB.
    Type: Application
    Filed: January 28, 2015
    Publication date: July 16, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Deba P. Saha
  • Publication number: 20150197531
    Abstract: The present invention relates to Sulfonamide Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, W, X, R1, R2, R3, R4 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Sulfonamide Derivative, and methods of using the Sulfonamide Derivatives for improving the pharmacokinetics of a drug.
    Type: Application
    Filed: June 25, 2013
    Publication date: July 16, 2015
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Craig A. Coburn, Milana Maletic, Richard Soll, Chunsing Li, Yunfu Luo, Zhiqi Qi
  • Publication number: 20150197490
    Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
    Type: Application
    Filed: March 26, 2015
    Publication date: July 16, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Yanfeng Zhang, Aaron S. Cote, Jeremy Scott, Yekaterina Vaynshteyn
  • Patent number: 9079930
    Abstract: The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: September 19, 2012
    Date of Patent: July 14, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Qun Dang, Changyou Zhou, Wuxin Zou, Yuxia Hua
  • Patent number: 9080177
    Abstract: This application provides, in part, pAVEC plasmids and methods of use of such plasmids for the production of polypeptides such as immunoglobulins as well as the generation of recombined versions of such plasmids which contain polynucleotides encoding such polypeptides.
    Type: Grant
    Filed: April 2, 2012
    Date of Patent: July 14, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventor: Deba P. Saha
  • Publication number: 20150190402
    Abstract: The present invention is directed to a pharmaceutical composition comprising the compound suvorexant, or a pharmaceutically acceptable salt thereof, a concentration-enhancing polymer, and optionally a pharmaceutically acceptable surfactant. The concentration-enhancing polymer is a polymer that forms an amorphous dispersion with suvorexant, that is insoluble or almost completely insoluble in water by (a) dissolving the suvorexant or (b) interacting with the suvorexant in such a way that the suvorexant does not form crystals or crystalline domains in the polymer. A concentration-enhancing polymer is water soluble or readily disperse in water, so that when the polymer is placed in water or an aqueous environment (e.g. fluids in the gastrointestinal (GI) tract or simulated GI fluids), the solubility and/or bioavailability of suvorexant is increased over the solubility or bioavailability in the absence of the polymer.
    Type: Application
    Filed: May 29, 2013
    Publication date: July 9, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Paul A. Harmon, Narayan Variankaval
  • Publication number: 20150191461
    Abstract: The present invention provides novel pyrazole derivatives of formula I which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.
    Type: Application
    Filed: June 18, 2013
    Publication date: July 9, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, Michael D. Altman, Eric T. Romeo, Dilrukshi Vitharana, Brandon Cash, Tony Siu, Matthew Christopher, Solomon D. Kattar, Andrew M. Haidle, Kaleen Konrad Childers, Matthew L. Maddess, Michael H. Reutershan, Yves Ducharme, David J. Guerin, Kerrie Spencer, Christian Beaulieu, Vouy Linh Truong, Daniel Guay, Alan B. Northrup, Brandon M. Taoka, Jongwon Lim, Christian Fischer, John W. Butcher, Ryan D. Otte, Binyuan Sun, John Michael Ellis
  • Patent number: 9073879
    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 18, 2011
    Date of Patent: July 7, 2015
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Philippe G. Nantermet, Zhi-Qiang Yang, Constantine Kreatsoulas, Abbas M. Walji, Hong Zhu
  • Patent number: 9073825
    Abstract: A first aspect of the present invention describes a compound selected from group consisting of: wherein R is either H, C(O)RA, or C(O)NHCH(X)COOH; provided that X is a C2-C6 alkyl, or a C3-C8 cycloalkyl and RA is a C1-6 alkyl or aryl; These compounds are used to make Compound A
    Type: Grant
    Filed: August 16, 2012
    Date of Patent: July 7, 2015
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Nobuyoshi Yasuda, Jeffrey T. Kuethe, Guy Humphrey, Gregory L. Beutner, Yong-Li Zhong, Edward Cleator, Carl Baxter
  • Patent number: 9073929
    Abstract: This invention relates to tricyclic triazole analogs of the formula I or their pharmaceutically acceptable salts, wherein the variable are defined herein. The inventive compounds selectively inhibit aldosterone synthetase. This invention also provides for pharmaceutical compositions comprising the compounds of Formula I or their salts as well as to methods for the treatment, amelioration or prevention of conditions that could be treated by inhibiting aldosterone synthetase.
    Type: Grant
    Filed: April 20, 2012
    Date of Patent: July 7, 2015
    Assignees: ElexoPharm GmbH, Merck Sharp & Dohme Corp.
    Inventors: Scott B. Hoyt, Whitney Lane Petrilli, Clare London, Yusheng Xiong, Jerry Andrew Taylor, Amjad Ali, Michael Man-Chu Lo, Timothy J. Henderson, Qingzhong Hu, Rolf Hartmann, Lina Yin, Ralf Heim, Emmanuel Bey, Rohit Saxena, Swapan Kumar Samanta, Bheemashankar A. Kulkarni
  • Patent number: 9073882
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Grant
    Filed: October 21, 2011
    Date of Patent: July 7, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Haifeng Tang, Alexander Pasternak, Lihu Yang, Shawn P. Walsh, Barbara Pio, Aurash Shahripour, Nardos Teumelsan