Patents Assigned to Merck Sharp & Dohme
  • PROCESS FOR PRODUCING RECOMBINANT TRYPSIN
    Publication number: 20170335308
    Abstract: A process for producing recombinant trypsin from prokaryote host cells in high yield and high specific activity is described. In particular, a process for producing recombinant trypsin from E. coli is described.
    Type: Application
    Filed: November 13, 2015
    Publication date: November 23, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mark C. Sleevi, Jack Lile
  • Spirocyclic Heterocyclic Compounds Useful As HIV Integrase Inhibitors
    Publication number: 20170334924
    Abstract: The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle Compounds for treating or preventing HIV infection in a subject.
    Type: Application
    Filed: December 4, 2015
    Publication date: November 23, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Mark W. Embrey, Thomas H. Graham, Izzat T. Raheem, John D. Schreier, Sherman T. Waddell, John S. Wai, Lihong Hu, Xuanjia Peng
  • Antiviral beta-amino acid ester phosphodiamide compounds
    Patent number: 9822138
    Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: November 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Petr Vachal, Izzat Raheem, Zhiqiang Guo, Timothy John Hartingh
  • Process for making beta 3 agonists and intermediates
    Patent number: 9822121
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: November 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R. Scott Hoerrner, Stephen Keen, Dave Lieberman, Zhuqing Liu, Joseph Lynch, Kevin M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong
  • Method for preparing crystalline insulin
    Patent number: 9822158
    Abstract: A method for crystallizing insulin or insulin analogs under alkaline conditions and purifying the insulin or insulin analog crystals by filtering through a filter and drying the insulin or insulin analog crystals captured on the filter to produce crystalline insulin or insulin analog crystal compositions is described. In particular aspects, the method may be used to crystalize insulin glargine.
    Type: Grant
    Filed: December 1, 2014
    Date of Patent: November 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Allison D. Ortigosa, William Perry, Mark C. Sleevi, Luis Sierra
  • Pharmaceutical formulation comprising losartan potassium and chlorthalidone
    Patent number: 9820973
    Abstract: The invention is a pharmaceutical tablet formulation comprising between about 12.5 mg and 100 mg losartan potassium, between about 6.25 mg and about 50 mg chlorthalidone, and sodium bicarbonate in an amount between about 1.0% and about 10.0% by weight.
    Type: Grant
    Filed: November 24, 2014
    Date of Patent: November 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jan-Piet Wijgergangs, Jocominus Antonius Maria Zwinkels, Albert Falivene Aldea
  • Triazolo-pyrazinyl derivatives useful as soluble guanylate cyclase activators
    Patent number: 9822130
    Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of Formula I, or a pharmaceutically acceptable salt thereof, for their use in the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 19, 2015
    Date of Patent: November 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Raphaelle Berger, Guizhen Dong, Subharekha Raghavan, Zhiqiang Yang
  • Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
    Patent number: 9822107
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring B, and the subscript r are as defined herein. 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).
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: November 21, 2017
    Assignees: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Brian M. Andresen, Kenneth L. Arrington, Ryan D. Otte, John Michael Ellis, John W. Butcher, Alan B. Northrup, Joel S. Robichaud, Jacques Yves Gauthier, Jean-Francois Fournier
  • SURFACE DISPLAY OF WHOLE ANTIBODIES IN EUKARYOTES
    Publication number: 20170327817
    Abstract: Methods for display of recombinant whole immunoglobulins or immunoglobulin libraries on the surface of eukaryote host cells, including yeast and filamentous fungi, are described. The methods are useful for screening libraries of recombinant immunoglobulins in eukaryote host cells to identify immunoglobulins that are specific for an antigen of interest.
    Type: Application
    Filed: January 27, 2016
    Publication date: November 16, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
  • Selective glycosidase inhibitors and uses thereof
    Patent number: 9815861
    Abstract: The invention provides compounds with enhanced permeability 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: December 11, 2015
    Date of Patent: November 14, 2017
    Assignees: Alectos Therapeutics, Inc., Merck Sharp & Dohme Corp.
    Inventors: Ramesh Kaul, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou, Yongbao Zhu
  • Pyrimidone carboxamide compounds as PDE2 inhibitors
    Patent number: 9815796
    Abstract: Disclosed are pyrimidine carboxamide compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2), pharmaceutical compositions and uses thereof.
    Type: Grant
    Filed: December 17, 2014
    Date of Patent: November 14, 2017
    Assignees: Merck Sharp & Dohme Corp., MSD R & D (China) Co. LTD.
    Inventors: Dong Ming Shen, Melissa Egbertson, Richard Berger, XiaoXia Qian, Yimin Qian, Bart Harper, Meng Yang, Zack Zhiqiang Guo, Vanessa L. Rada, Deping Wang, Timothy A. Cernak, Christopher Sinz, Ming Wang, Jonathan E. Wilson, Shimin Xu
  • TrkA kinase inhibitors, compositions and methods thereof
    Patent number: 9815846
    Abstract: The present invention is directed to six membered 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: November 14, 2017
    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, Kerim Babaoglu, Dongfang Meng, Jane Wu, Ping Liu, Harold B. Wood, Jianming Bao, Chun Sing Li, Qinghua Mao, Zhiqi Qi
  • NOVEL COMPOUNDS THAT ARE ERK INHIBITORS
    Publication number: 20170320882
    Abstract: Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).
    Type: Application
    Filed: July 21, 2017
    Publication date: November 9, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Xianhai Huang, Ronald D. Ferguson, Wei Zhou, Christopher W. Boyce, Phieng Siliphaivanh, David J. Witter, Milana M. Maletic, Joseph A. Kozlowski, Kevin J. Wilson
  • AMIDOETHYL AZOLE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170320856
    Abstract: The present invention is directed to amidoethyl azole 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 18, 2015
    Publication date: November 9, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Yunfu Luo
  • 6,5-BICYCLIC OCTAHYDROPYRROLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170320874
    Abstract: The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine 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: November 9, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Scott D. Kuduk, Nigel Liverton, Gang Zhou
  • Factor XIa inhibitors
    Patent number: 9809545
    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, hypercoaguability or fibrotic changes.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: November 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Scott Edmondson, Mark Erion, Santhosh Neelamkavil, Zhuyan Guo, Rudrajit Mal, Jiafang He, Weiguo Liu, Ellen K. Vande Bunte
  • Engineered anti-IL-23p19 antibodies
    Patent number: 9809648
    Abstract: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: November 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Brian M. Beyer, Richard N. Ingram, Peter Orth, Yan-Hui Liu
  • Factor IXa inhibitors
    Patent number: 9808445
    Abstract: In its many embodiments, the present invention provides a novel class of benzamide compounds represented by Formula (I) or pharmaceutically acceptable salts or solvates thereof, or pharmaceutical compositions comprising one or more said compounds or pharmaceutically acceptable salts or solvates thereof, and methods for using said compounds or pharmaceutically acceptable salts or solvates thereof for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: April 10, 2015
    Date of Patent: November 7, 2017
    Assignees: Merck Sharp & Dohme Corp., Mochida Pharmaceutical Co., Ltd.
    Inventors: Isao Sakurada, Tomokazu Hirabayashi, Yoshitaka Maeda, Hiroshi Nagasue, Takashi Mizuno, Jiayi Xu, Ting Zhang, Cameron Smith, Dann Parker
  • Preparation and use of 3-pyridyl substituted-6,6-difluoro bicyclic himbacine derivatives as par-1 receptor antagonists
    Patent number: 9808473
    Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is halo; —CN; alkyl; cycloalkyl; alkoxy; phenyl, which is optionally substituted one or twice independently by alkyl, halo, or —CN; or a thiophene ring, which is optionally substituted once or twice independently by alkyl. 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: Grant
    Filed: August 18, 2014
    Date of Patent: November 7, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James Francis Dropinski, Milana Maletic, Jae-Hun Kim, Deyou Sha
  • Glycosidase inhibitors and uses thereof
    Patent number: 9809537
    Abstract: The invention provides compounds for 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: August 29, 2013
    Date of Patent: November 7, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Yongbao Zhu, Harold G. Selnick