Patents Assigned to Merck Sharp
  • ANTI-CD27 ANTIBODIES
    Publication number: 20180086841
    Abstract: The present invention relates to anti-CD27 antibodies, as well as use of these antibodies in the treatment of diseases such as cancer and infectious disease.
    Type: Application
    Filed: September 25, 2017
    Publication date: March 29, 2018
    Applicants: Merck Sharp & Dohme Corp., Merck Sharp & Dohme B.V.
    Inventors: Amy M. Beebe, Jason Ka Jen Cheung, Veronica Juan, Laurence Fayadat-Dilman, Svetlana Sadekova, Jerelyn Wong, Hans van Eenennaam, Andrea van Elsas, Lars Guelen, Thierry Olivier Fischmann, Winifred W. Prosise
  • CHROMANE, ISOCHROMANE AND DIHYDROISOBENZOFURAN DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20180085358
    Abstract: The present invention provides certain substituted chromane, isochromane, and dihydroisobenzofuran compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein ring A is a moiety selected from: and ring B, n, R1, R2, R2A, R3, and R3A are as defined herein. The compounds of the invention are useful as mGluR2 inhibitors, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a patient for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, mild cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: September 25, 2017
    Publication date: March 29, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Iyassu K. Sebhat, Ashok Arasappan, Scott B. Hoyt, Robert R. Wilkening, Duane DeMong
  • Stable formulations of testosterone undecanoate
    Patent number: 9925200
    Abstract: The present invention is directed to stable pharmaceutical formulations. More specifically, the present invention is directed to stable pharmaceutical formulations of testosterone undecanoate.
    Type: Grant
    Filed: June 15, 2015
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp & Dohme B.V.
    Inventor: Gerritdina G. Schoonus-Gerritsma
  • Pegylated interleukin-10
    Patent number: 9925245
    Abstract: Interleukin-10 (IL-10) conjugated via a linker to one or more polyethylene glycol (PEG) molecules at a single amino acid residue of the IL-10, and a method for preparing the same, are provided. The method produces a stable mono-pegylated IL-10, which retains IL-10 activity, where pegylation is selective for the N-terminus on one subunit of IL-10 with little or no formation of monomeric IL-10. The method also provides a substantially homogenous population of mono-PEG-IL-10.
    Type: Grant
    Filed: December 10, 2015
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Seoju Lee, David C. Wylie, Susan V. Cannon-Carlson
  • Allosteric modulators of nicotinic acetylcholine receptors
    Patent number: 9926285
    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: October 9, 2017
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brendan M. Crowley, Brian T. Campbell, Joseph L. Duffy, Andrew John Harvey, Ian M. Bell
  • Ceftolozane-tazobactam pharmaceutical compositions
    Patent number: 9925196
    Abstract: Pharmaceutical compositions are provided in unit dosage forms comprising ceftolozane and tazobactam in separate unit dosage form containers, ceftolozane prepared in the absence of tazobactam, tazobactam prepared in the absence of ceftolozane, and/or compositions where ceftolozane and tazobactam are first combined within a unit dosage form container.
    Type: Grant
    Filed: March 16, 2016
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph Terracciano, Nicole Miller Damour, Chun Jiang, Giovanni Fogliato, Giuseppe Alessandro Donadelli, Dario Resemini
  • Method for treating cancer
    Patent number: 9925192
    Abstract: A method for the treatment of cancer by administering a therapeutically effective amount of a cyclin-dependent kinase (CDK) inhibitor with a therapeutically effective amount of a B cell chronic lymphocytic leukemia/lymphoma 2 inhibitor (“B Cell CLL/Lymphoma 2”, or “BCL-2”). Administration of the CDK inhibitor and BCL-2 inhibitor can be simultaneous, successive or separate.
    Type: Grant
    Filed: February 23, 2015
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Peter Strack, Robert Booher
  • Inhibitors of IRAK4 activity
    Patent number: 9926330
    Abstract: The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: March 27, 2018
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Michael D. Altman, Jason D. Brubaker, Matthew L. Childers, Anthony Donofrio, Thierry Fischmann, Craig R. Gibeau, Solomon D. Kattar, Charles A. Lesburg, Jongwon Lim, John K. F. MacLean, Umar F. Mansoor, Alan B. Northrup, John M. Sanders, Graham F. Smith
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9926317
    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: July 9, 2015
    Date of Patent: March 27, 2018
    Assignee: Merck Sharp Dohme Corp.
    Inventors: Alexander Pasternak, Ian Davies, Fa-Xiang Ding, Jinglong Jiang, Shuzhi Dong, Xin Gu
  • IMMUNOHISTOCHEMICAL ASSAY FOR DETECTING EXPRESSION OF PROGRAMMED DEATH LIGAND 1 (PD-L1) IN TUMOR TISSUE
    Publication number: 20180080938
    Abstract: The present disclosure provides processes for describing and quantifying the expression of human programmed death ligand-1 (PD-L1) in tumor tissue sections as detected by immunohistochemical assay using an antibody that specifically binds to PD-L1. The results generated using these processes have a variety of experimental, diagnostic and prognostic applications.
    Type: Application
    Filed: September 22, 2017
    Publication date: March 22, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Marisa Dolled-Filhart, Kenneth Emancipator, Frank Lynch, Robert H. Pierce, Dianna Wu
  • PROCESS OF MAKING AND USING PHARMACEUTICAL FORMULATIONS OF ANTINEOPLASTIC AGENTS
    Publication number: 20180078546
    Abstract: In its several embodiments, this invention discloses a pharmaceutical formulation comprising at least one antineoplastic agent or a pharmaceutically acceptable salt thereof, and at least one dissolution enhancing agent sufficient to substantially dissolve said at least one antineoplastic agent in at least one aqueous diluent, wherein said dissolution enhancing agent is urea, L-histidine, L-threonine, L-asparagine, L-serine, L-glutamine or mixtures thereof; a lyophilized powder comprising said pharmaceutical formulation, and articles of manufacture thereof.
    Type: Application
    Filed: November 29, 2017
    Publication date: March 22, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Sydney O. Ugwu, Vinay Radhakrishnan, Peter M. Ihnat, Leonore C. Witchey-Lakshmanan
  • FACTOR XIa INHIBITORS
    Publication number: 20180079743
    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, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
    Type: Application
    Filed: April 11, 2016
    Publication date: March 22, 2018
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Eric Mertz, Scott D. Edmondson, Sung-Sau So, Wanying Sun, Weiguo Liu, Santhosh F. Neelamkavil, Ying-Duo Gao, Alan Hruza, Yi Zang, Amjad Ali, Rudrajit Mal, Jiafang He, Rongze Kuang, Heping Wu, Anthony K. Ogawa, Andrew F. Nolting
  • BTK INHIBITORS
    Publication number: 20180079752
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
    Type: Application
    Filed: May 31, 2016
    Publication date: March 22, 2018
    Applicants: MERCK SHARP & DOHME CORP., MERCK SHARP & DOHME B.V.
    Inventors: ADRIANUS PETRUS ANTONIUS DE MAN, RONALD KIM, JIAN LIU, JOSEPH A. KOZLOWSKI, SOBHANA BABU BOGA, THIERRY FISCHMANN, DEODIAL Guy GUIADEEN, ILSE HENDRICA MARIA POLS-DE ROOIJ, SHILAN LIU, HAO WU
  • Methyl oxazole orexin receptor antagonists
    Patent number: 9920038
    Abstract: The present invention is directed to methyloxazole 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: Grant
    Filed: November 30, 2015
    Date of Patent: March 20, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Nigel Liverton, Yunfu Luo
  • COMBINATION OF A PD-1 ANTAGONIST AND ERIBULIN FOR TREATING CANCER
    Publication number: 20180071247
    Abstract: The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and eribulin or a pharmaceutically acceptable salt thereof, and the use of the combination therapies for the treatment of cancer.
    Type: Application
    Filed: March 3, 2016
    Publication date: March 15, 2018
    Applicants: MERCK SHARP & DOHME CORP., Eisai R&D Management Co., Ltd.
    Inventors: Junji MATSUI, Gursel AKTAN, Vassiliki KARANTZA, RuiRong YUAN, Yasuhiro FUNAHASHI, Erhan BERRAK
  • PYRROLO[2,3-C]PYRIDINES AS IMAGING AGENTS FOR NEUROFIBRILARY TANGLES
    Publication number: 20180071412
    Abstract: The present invention is directed to pyrrolopyridine compounds of formula (I) or their pharmaceutically acceptable salts, which may be suitable for imaging tau aggregates, b-sheet aggregates, beta-amyloid aggregates or alpha-synuclein aggregates, and hence are useful in binding and imaging tau aggregates in Alzheimer's patients. More specifically, this invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study tau deposits in brain in vivo to allow diagnosis of Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology. The invention further relates to a method of measuring clinical efficacy of therapeutic agents for Alzheimer's disease and other neurodegenerative diseases characterized by tau pathology.
    Type: Application
    Filed: October 4, 2017
    Publication date: March 15, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Abbas M. Walji, Eric Hostetler, Thomas J. Greshock, Jing Li, Keith P. Moore, Idriss Bennacef, James Mulhearn, Harold Selnick, Yaode Wang, Kun Yang, Jianmin Fu
  • TrKA kinase inhibitors, compositions and methods thereof
    Patent number: 9914736
    Abstract: The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (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: March 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Helen Mitchell, Mark E. Fraley, Andrew J. Cooke, Craig A. Stump, Xu-Fang Zhang, Casey C. McComas, Kathy Schirripa, Melody McWherter, Ping Liu, Dann Parker, Chun Sing Li, Qinghua Mao
  • Factor IXa inhibitors
    Patent number: 9914727
    Abstract: The present invention provides compounds of Formula (I) and pharmaceutical compositions comprising compounds of Formula I, and methods for using compounds of Formula I for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: March 13, 2018
    Assignees: 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
  • CONJUGATE BASED SYSTEMS FOR CONTROLLED DRUG DELIVERY
    Publication number: 20180064824
    Abstract: Conjugates which comprise a drug and a ligand which includes a first saccharide; wherein the conjugate is characterized in that, when the conjugate is administered to a mammal, at least one pharmacokinetic or pharmacodynamic property of the conjugate is sensitive to serum concentration of a second saccharide. Exemplary conjugates and sustained release formulations are provided in addition to methods of use and preparation.
    Type: Application
    Filed: August 18, 2017
    Publication date: March 8, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Todd C. Zion, Thomas M. Lancaster
  • ANTIVIRAL BETA-AMINO ACID ESTER PHOSPHODIAMIDE COMPOUNDS
    Publication number: 20180065999
    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: Application
    Filed: September 25, 2017
    Publication date: March 8, 2018
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Petr Vachal, Izzat Raheem, Zhiqiang Guo, Timothy John Hartingh