Patents Assigned to Merck Sharp
  • ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF-I
    Publication number: 20170158628
    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: Application
    Filed: February 17, 2017
    Publication date: June 8, 2017
    Applicant: 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
  • TrKA Kinase Inhibitors, Compositions and Methods Thereof
    Publication number: 20170158698
    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: Application
    Filed: March 23, 2015
    Publication date: June 8, 2017
    Applicant: 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
  • Thiazole-substituted aminoheteroaryls as Spleen Tyrosine Kinase inhibitors
    Patent number: 9670196
    Abstract: The invention provides certain thiazole-substituted aminoheteroaryl compounds of the Formula (I) (I), or pharmaceutically acceptable salts thereof, wherein ring R1, R2, R3, R4, ring A, and the subscripts n1, n2, and 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: June 6, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas A. Miller, Alessia Petrocchi, Eric T. Romeo, Dilrukshi Vitharana, Solomon D. Kattar, Alan B. Northrup, Michael D. Altman, Neville J. Anthony
  • Glycosidase inhibitors and uses thereof
    Patent number: 9670195
    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: June 6, 2017
    Assignees: Alectos Therapeutics Inc., Merck Sharp & Dohme Corp.
    Inventors: Ernest J. McEachern, Jianyu Sun, David J. Vocadlo, Yuanxi Zhou, Harold G. Selnick
  • ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS AND USES THEREOF
    Publication number: 20170152221
    Abstract: Disclosed are compounds of Formula (IVA), or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof: Formula (IVA), wherein “RIa”, “RIb”, “RIc”, “RId”, “RIe”, are defined herein above, which compounds are believed suitable for use in positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7 nAChR) receptors, for example, those found in the cerebral cortex and the hippocampus. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Alzheimer's disease (AD), schizophrenia, and Parkinson's disease (PD), or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
    Type: Application
    Filed: June 11, 2015
    Publication date: June 1, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: KENNETH LEAVITT, BRENDAN CROWLEY, IAN M. BELL, ANDREW HARVEY, THOMAS AVERY, DHARAM PAUL, JUSTIN RIPPER, BELINDA HUFF, RAJINDER SINGH, LAURENT SCHAEFFER, CHRISTOPHE JOSEPH, CHRISTOPHE MORICE, BRUNO GIETHLEN, PATRICK BAZZINI, AURELIE FROMEYER
  • 3-aminocycloalkyl compounds as RORgammaT inhibitors and uses thereof
    Patent number: 9663522
    Abstract: The present invention relates to compounds according to Formula I and pharmaceutically acceptable salts or solvates thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or conditions.
    Type: Grant
    Filed: August 14, 2013
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kenneth J. Barr, John K. Maclean, Hongjun Zhang, Richard T. Beresis, Neville J. Anthony, Matthew Daniels, Blair T. Lapointe, Nunzio Sciammetta
  • Lipopeptide compositions and related methods
    Patent number: 9662397
    Abstract: The present disclosure provides novel powder daptomycin formulations which have improved chemical stability and faster reconstitution times when in the solid state. Some examples of the compositions comprise daptomycin and sucrose.
    Type: Grant
    Filed: August 12, 2015
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sandra O'Connor, Sophie Sun, Gaauri Naik
  • Fused bicyclic isoxazolines as inhibitors of cholesterol ester transfer protein
    Patent number: 9663534
    Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is (CH2) or O, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:
    Type: Grant
    Filed: December 12, 2014
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pengcheng Patrick Shao, Feng Ye, Petr Vachal
  • Pyrimidine PDE10 inhibitors
    Patent number: 9663513
    Abstract: The present invention is directed to pyrimidine 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: November 15, 2013
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Casey C. McComas, Thomas S. Reger
  • Process for making reverse transcriptase inhibitors
    Patent number: 9663490
    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: Grant
    Filed: December 4, 2013
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tetsuji Itoh, Ingyu Jeon, Ian Mangion, Gang Qian, Benjamin D. Sherry, Donald R. Gauthier, Yang Cao
  • Quinoline carboxamide and quinoline carbonitrile derivatives as mGluR2-negative allosteric modulators, compositions, and their use
    Patent number: 9663506
    Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, 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: Grant
    Filed: February 18, 2016
    Date of Patent: May 30, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
  • 2-Acylamidomethyl and sulfonylamidomethyl benzoxazine carbamates for inhibition of RORgamma activity and the treatment of disease
    Patent number: 9663502
    Abstract: The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, Ra, Rb, Rc, Rd, Rg, 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: May 30, 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, Neville J. Anthony, Matthew Daniels, Yuan Liu, Catherine White, Blair T. Lapointe, Nunzio Sciammetta, Vladimir Simov, Wesley B. Trotter, Kun Liu
  • Factor XIa inhibitors
    Patent number: 9663527
    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: Grant
    Filed: February 6, 2015
    Date of Patent: May 30, 2017
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Santhosh F. Neelamkavil, Scott D. Edmondson, Zhuyan Guo, Alan W. Hruza, Zahid Hussain, Charles A. Lesburg, Remond Moningka, Anthony K. Ogawa, Rudrajit Mal
  • PROCESS FOR PREPARING BETA 3 AGONISTS AND INTERMEDIATES
    Publication number: 20170145014
    Abstract: The application is directed to efficient and economical processes as described in more detail below for the preparation of the beta 3 agonists of the formula of 1-7 and intermediate compounds that can be used for making these agonists. The present disclosure relates to a process for making beta-3 agonists and intermediates using ketoreductase (KRED) biocatalyst enzymes and methods of using the biocatalysts.
    Type: Application
    Filed: March 12, 2014
    Publication date: May 25, 2017
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Feng Xu, Zhuqing Liu, Richard Desmond, Jeonghan Park, Alexei Kalinin, Birgit Kosjek, Hallena Strotman, Hongmei Li, Johannah Moncecchi
  • Compositions and methods for treating cancer
    Patent number: 9655899
    Abstract: The instant invention relates to methods for the treatment of WEE1 kinase associated cancer by administering a WEE1 inhibitor, wherein the WEE1 inhibitor is WEE1-1 or a pharmaceutically acceptable salt thereof, or WEE1-2 or a pharmaceutically acceptable salt thereof. In another embodiment, the invention relates to a method for treating a WEE1 kinase associated cancer patient, comprising administering a WEE1 inhibitor, wherein the cancer cells of said patient to be treated are characterized by low expression levels of PKMYT1.
    Type: Grant
    Filed: November 22, 2013
    Date of Patent: May 23, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Stuart Denham Shumway
  • Tetrahydronaphthyridine and related bicyclic compounds for inhibition of ROR? activity and the treatment of disease
    Patent number: 9657033
    Abstract: The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.
    Type: Grant
    Filed: May 7, 2013
    Date of Patent: May 23, 2017
    Assignees: Lycera Corporation, Merck Sharp & Dohme Corp.
    Inventors: Thomas D. Aicher, Kenneth J. Barr, Blair T. Lapointe, Vladimir Simov, Karin A. Stein, William D. Thomas, Peter L. Toogood, Chad A. Van Huis, Catherine M. White
  • Cathepsin cysteine protease inhibitors
    Patent number: 9656990
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: February 6, 2015
    Date of Patent: May 23, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shawn Stachel, Daniel V. Paone, Jing Li, Anthony Ginnetti, Jianmin Fu, Shimin Xu
  • REGIOSELECTIVE N-2 ARYLATION OF INDAZOLES
    Publication number: 20170137403
    Abstract: A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.
    Type: Application
    Filed: January 30, 2017
    Publication date: May 18, 2017
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Cheol K. Chung, Mark E. Scott, Paul Gerard Bulger, Kevin Michael Belyk, John Limanto, Guy R. Humphrey
  • Liquid formulations for TNFR:Fc fusion proteins
    Patent number: 9649383
    Abstract: The invention provides stable liquid formulations for a recombinant biopharmaceutical protein comprising a soluble form of the human p75 TNF receptor fused to an Fe domain of a human immunoglobulin protein (TNFR:Fc). Typically, biopharmaceutical proteins such as monoclonal antibodies (mAbs) and immunoglobulin fusion proteins (e.g., immunoadhesion proteins) are produced by recombinant DNA technology in mammalian cell expression systems. In order to guarantee the reproducible clinical performance of a biopharmaceutical product, manufacturers have to deliver a product of consistent and reproducible quality.
    Type: Grant
    Filed: November 15, 2013
    Date of Patent: May 16, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ramesh S. Kashi, Shona P. Patel, Sarita Mittal, Ashwin Basarkar, Shuai Shi
  • Indole derivatives useful as anti-diabetic agents
    Patent number: 9650375
    Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.
    Type: Grant
    Filed: March 10, 2014
    Date of Patent: May 16, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John J. Acton, III, Rajan Anand, Ashok Arasappan, Qun Dang, Iyassu Sebhat, Zhifa Pu, Takao Suzuki