Patents Assigned to Merck Sharp
  • NARGENICIN COMPOUNDS AND USES THEREOF AS ANTIBACTERIAL AGENTS
    Publication number: 20170305924
    Abstract: The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an antimycobacterially effective amount of nargenicin or a nargenicin-related compound and/or their pharmaceutically acceptable salts.
    Type: Application
    Filed: October 21, 2015
    Publication date: October 26, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Katherine Young, David B. Olsen, Sheo B. Singh, Jing Su, Robert R. Wilkening, James M. Apgar, Dongfang Meng, Dann Parker, Mihir Mandal, Lihu Yang, Ronald E. Painter, Qun Dang, Takao Suzuki
  • TETRAHYDRONAPHTHYRIDINE DERIVATIVES AS mGluR2-NEGATIVE ALLOSTERIC MODULATORS, COMPOSITIONS, AND THEIR USE
    Publication number: 20170305902
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and may be useful in methods of treating a person in need thereof for diseases or disorders in which the mGluR2-NAM receptor plays a causative role, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders.
    Type: Application
    Filed: August 24, 2015
    Publication date: October 26, 2017
    Applicants: Merck Sharp & Dohme Corp., Merck Canada Inc.
    Inventors: Ashok Arasappan, Christopher James Bungard, Jessica L. Frie, Yongxin Han, Scott B. Hoyt, Peter J. Manley, Robert S. Meissner, James J. Perkins, Iyassu K. Sebhat, Robert R. Wilkening, Kenneth J. Leavitt
  • METHYL DIAZEPANE OREXIN RECEPTOR ANTAGONISTS
    Publication number: 20170305916
    Abstract: The present invention is directed to methyl diazepane 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: November 20, 2015
    Publication date: October 26, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: SCOTT D. KUDUK, THOMAS S. REGER, JASON W. SKUDLAREK
  • Fused tricyclic compounds and methods of use thereof for the treatment of viral diseases
    Patent number: 9796705
    Abstract: The present invention relates to novel Fused Tricyclic Compounds, compositions comprising at least one Fused Tricyclic Compound, and methods of using Fused Tricyclic Compounds for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: October 24, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Pharmaceutical formulation containing thienotriazolodiazepine compounds
    Patent number: 9795612
    Abstract: A method of treating lymphoblastic leukemia, acute myeloid leukemia, BCR-ABL positive acute lymphoblastic leukemia or CD34 positive acute myeloid leukemia comprising the step of administering to a patient a pharmaceutically acceptable amount of a composition comprising a thienotriazolodiazepine compound according to Formula (1) as a solid dispersion wherein X is a halogen, R1 is C1-C4 alkyl, R2 is C1-C4 alkyl, a is an integer of 1-4, R3 is C1-C4 alkyl, C1-C4 hydroxyalkyl, C1-C4 alkoxy, phenyl optionally having substituent(s), or heteroaryl optionally having substituent(s), a pharmaceutically acceptable salt thereof or a hydrate thereof; and a pharmaceutically acceptable polymer. In one embodiment, the pharmaceutically acceptable polymer is HPMCAS.
    Type: Grant
    Filed: August 1, 2014
    Date of Patent: October 24, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Hervé Dombret
  • Assay for determining endogenous levels of analyte in vivo
    Patent number: 9797910
    Abstract: The present invention relates to an assay for determining endogenous levels of analyte in vivo. In particular, the present invention is directed to an assay for determining endogenous levels of stromal cell-derived factor (SDF-1) isoforms in vivo.
    Type: Grant
    Filed: June 13, 2014
    Date of Patent: October 24, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weixun Wang, Bernard Karsten Choi, Lucinda H. Cohen
  • Imidazo-pyrazine derivatives useful as soluble guanylate cyclase activators
    Patent number: 9796733
    Abstract: A compound of Formula II 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 II, 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 preparations which comprise compounds of Formula II or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: October 24, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Brian T. Campbell, Guizhen Dong, Joie Garfunkle, Alexander Kim, Olga Ornoski, Dann L. Parker, Jr., Subharekha Raghavan, Libo Xu, Zhiquang Yang
  • Alpha-7 nicotinic acetylcholine receptor modulators and uses thereof-I
    Patent number: 9790173
    Abstract: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases.
    Type: Grant
    Filed: February 17, 2017
    Date of Patent: October 17, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Andrew Harvey, Thomas Avery, Dharam Paul, Justin Ripper, Belinda Huff, Rajinder Singh, Laurent Schaeffer, Christophe Joseph, Christophe Morice, Bruno Giethlen
  • 4-imidazopyridazin-1-yl-benzamides and 4-imidazotriazin-1-yl-benzamides as BtK inhibitors
    Patent number: 9790226
    Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to Formula (I) in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders.
    Type: Grant
    Filed: February 9, 2016
    Date of Patent: October 17, 2017
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Tjeerd A. Barf, Christiaan Gerardus Johannes Maria Jans, Adrianus Petrus Antonius de Man, Arthur A. Oubrie, Hans C. Raaijmakers, Johannes Bernardus Maria Rewinkel, Jan Gerard Sterrenburg, Jacobus C. H. M. Wijkmans
  • ANTI-LAG3 ANTIBODIES AND ANTIGEN-BINDING FRAGMENTS
    Publication number: 20170290914
    Abstract: The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAG3 as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the antibodies and fragments (e.g., including anti-PD1 antibodies) are included in the invention. Methods for treating or preventing cancer or infection using such compositions are also provided. In addition, methods for recombinant expression of the antibodies and fragments are part of the present invention.
    Type: Application
    Filed: August 17, 2015
    Publication date: October 12, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Linda Liang, Laurence Fayadat-Dilman, Rene De Waal Malefyt, Gopalan Raghunathan
  • Method of obtaining thermostable dried vaccine formulations
    Patent number: 9782470
    Abstract: This present invention relates to compositions and methods for stabilizing a dried vaccine formulations. In particular, the invention provides a method for producing a vaccine composition comprising the steps of providing an aqueous composition comprising a buffer, the vaccine components and between 17.5% w/w and 60% w/w of a non-polymeric sugar, freezing the composition, and applying microwave radiation under a pressure lower than atmospheric pressure in order to sublimate the composition and obtain a dried vaccine formulation. The invention also provides a product obtainable by this method.
    Type: Grant
    Filed: October 13, 2014
    Date of Patent: October 10, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Akhilesh Bhambhani, Robert K. Evans, Jessica Sinacola, Morrisa Jones
  • Factor Xla inhibitors
    Patent number: 9783530
    Abstract: The present invention provides a compound of Formula I (The chemical formula should be inserted here.) 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: Grant
    Filed: May 22, 2015
    Date of Patent: October 10, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Weiguo Liu, Scott D. Edmondson, Zhuyan Guo, Eric Mertz, Anthony K. Ogawa, Sung-Sau So, Wanying Sun, Linda L. Brockunier, Amjad Ali, Rongze Kuang, Heping Wu
  • Thiazole-substituted aminoheteroaryls as spleen tyrosine kinase inhibitors
    Patent number: 9783531
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R3, R5, R6, A, Cy and the subscripts r, s, and t 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 15, 2014
    Date of Patent: October 10, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, Eric T. Romeo, Alan B. Northrup, Michael D. Altman
  • Soluble guanylate cyclase activators
    Patent number: 9783552
    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 preparations which comprise compounds of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: October 10, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Xiaoqing Han, Alan Whitehead, Subharekha Raghavan, Timothy A. Cernak, Spencer Dreher, Jonathan Groeper, Jian Guo, Yong Zhang
  • Carbamate benzoxazine propionic acids and acid derivatives for modulation of RORgamma activity and the treatment of disease
    Patent number: 9783511
    Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, Ra1, Ra2, Rb1, Rb2, Rc, Rd, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.
    Type: Grant
    Filed: December 19, 2014
    Date of Patent: October 10, 2017
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Chad A. VanHuis, John MacLean, Brian M. Andresen, Kenneth J. Barr, Corey Bienstock, Matthew Daniels, Kun Liu, Yuan Liu, Catherine White, Nunzio Sciammetta, Vladimir Simov
  • Inhibitors of the renal outer medullary potassium channel
    Patent number: 9777002
    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: Grant
    Filed: November 22, 2013
    Date of Patent: October 3, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn P. Walsh, Brian Cato, Jessica L. Frie, Dooseop Kim, Alexander Pasternak, Zhi-Cai Shi
  • 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors
    Patent number: 9775839
    Abstract: The invention provides certain pyrazine-2-carboxamide compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein A, B, and X 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: March 9, 2015
    Date of Patent: October 3, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael D. Altman, Brandon Cash, John Michael Ellis, Matthew L. Maddess, Alan B. Northrup, Ryan D. Otte, Binyuan Sun
  • 4?-substituted nucleoside reverse transcriptase inhibitors
    Patent number: 9777035
    Abstract: The present invention is directed to 4?-substituted nucleoside derivatives of Formula I and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: October 3, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Vinay M. Girijavallabhan, David B. Olsen, Zhibo Zhang, Jianmin Fu, Bing-Yu Tang
  • SYNTHESIS OF CEPHALOSPORIN COMPOUNDS
    Publication number: 20170275300
    Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof.
    Type: Application
    Filed: August 14, 2015
    Publication date: September 28, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: David Waller, Gregory Gazda, Zachary Minden, Lisa Barton, Clifton Leigh
  • TETRAHYDROISOQUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2
    Publication number: 20170273966
    Abstract: The present invention relates to a compound represented by formula I:and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
    Type: Application
    Filed: August 31, 2015
    Publication date: September 28, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jason Imbriglio, Clare London, Zhijian Lu, James Tata, Yusheng Xiong, Ming You, Hyewon Youm