Patents Assigned to Merck Sharp & Dohme
  • 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
  • Publication number: 20150182503
    Abstract: The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiomers of the compounds, to processes for preparing compounds of the Formula I, to their potential use for the therapy and prophylaxis of the above-mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.
    Type: Application
    Filed: July 15, 2013
    Publication date: July 2, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Timothy A. Cernak, Kevin D. Dykstra, Dong-Ming Shen, Kun Liu, Andrew Stamford, John Qiang Tan
  • Patent number: 9067941
    Abstract: The present invention is directed to fused heterocyclic azaindane carboxamide derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: December 16, 2011
    Date of Patent: June 30, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Anthony Ginnetti, Ashley Nomland, Daniel V. Paone
  • Patent number: 9062059
    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: August 20, 2012
    Date of Patent: June 23, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, Vadim Y. Dudkin, Jeffrey Kern, Mark E. Layton, Izzat T. Raheem
  • Patent number: 9061041
    Abstract: The present invention relates to 2?-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Substituted Nucleoside Derivative, and methods of using the 2?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: June 23, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Vishal Verma, Frank Bennett, Angela Kerekes, Ashok Arasappan, Dmitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Patent number: 9062007
    Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.
    Type: Grant
    Filed: January 6, 2014
    Date of Patent: June 23, 2015
    Assignees: Merck Sharp & Dohme Corp., Pharmacopeia Drug Discovery, Inc.
    Inventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voight, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey H. Lowrie, Kurt W. Saionz, Suresh D. Babu
  • Patent number: 9062070
    Abstract: The present invention provides compounds of Formula Ia 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: August 16, 2012
    Date of Patent: June 23, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Timothy Blizzard, Harry Chobanian, Reynalda de Jesus, Fa-Xiang Ding, Shuzhi Dong, Candido Gude, Dooseop Kim, Haifeng Tang, Shawn Walsh, Barbara Pio, Jinlong Jiang
  • Patent number: 9062071
    Abstract: The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: June 23, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yao Ma, Manami Shizuka, Timothy J. Guzi, Yuan Liu, Yuan Tian, Brian R. Lahue, Craig R. Gibeau, Gerald W. Shipps, Jr., Yaolin Wang, Stephane L. Bogen, Latha G. Nair, Weidong Pan, Mark A. McCoy, Matthew E. Voss, Margarita Kirova-Snover, W. Bent Clayton
  • Patent number: 9056859
    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 (Kir 1.1). 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 24, 2011
    Date of Patent: June 16, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Reynalda K. deJesus, Yuping Zhu, Lihu Yang, Shawn Walsh, Haifeng Tang, Dooseop Kim, Barbara Pio, Aurash Shahripour, Kevin Belyk
  • Publication number: 20150158935
    Abstract: The present invention relates to methods of inducing an immune response to Staphylococcus comprising administering a composition comprising an SA2493-related polypeptide from Staphylococcus aureus as well as derivatives or fragments there-of. The present invention also encompasses methods of treating and/or reducing the likelihood of a Staphylococcus infection by administering a composition comprising an SA2493-related polypeptide or an antibody that specifically binds to an SA2493 polypeptide, derivative or fragments thereof. Compositions administered in the methods of the invention can include one or more additional antigens including, but not limited to, IsdB. Compositions used to practice the methods of the invention are also encompassed.
    Type: Application
    Filed: July 9, 2013
    Publication date: June 11, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Tessie B. McNeely, Leslie Cope, Gregory D. Pancari, Amita Joshi
  • Patent number: 9051329
    Abstract: The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: June 9, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Wen-Lian Wu
  • Patent number: 9044463
    Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: June 2, 2015
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Cristian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
  • Publication number: 20150147337
    Abstract: Crystalline forms of antibodies to human IL-23, such as antibodies to human IL-23p19, are provided, as well as methods of producing such crystalline forms, and uses of such crystalline forms, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders. In various embodiments, the anti-hulL-23 antibody crystals, such as anti-hulL-23p19 antibody crystals of the present invention are obtainable by batch crystallization methods, vapor diffusion methods, liquid-liquid diffusion methods, and dialysis. In other aspects, the invention relates to suspensions of the crystalline anti-hulL-23 antibodies of the present invention, including those at higher concentrations and lower viscosities than would be possible with a corresponding non-crystalline solution at the same concentration of antibody. In other embodiments, the anti-huiL-23 antibody crystals of the present invention have increased stability, i.e.
    Type: Application
    Filed: June 25, 2013
    Publication date: May 28, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Paul Reichert, Winifred W. Prosise, Peter Orth, Chakravarthy Nachu Narasimhan, Ramesh S. Kashi
  • Publication number: 20150141428
    Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be 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 Trk-A, Trk-B and/or Trk-C.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 21, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
  • Patent number: 9029377
    Abstract: Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Anthony Ogawa, Feroze Ujjainwalla, Lin Chu, Bing Li, Lan Wei, Jinyou Xu, Hyun Ok, Aaron Lackner, Ihor Kopka
  • Patent number: 9029362
    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to ?-amyloid (“A?”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: March 21, 2014
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jack D. Scott, Andrew W. Stamford, Eric J. Gilbert, Jared N. Cumming
  • Patent number: 9029364
    Abstract: The present invention is directed to 2,5-disubstituted thiomorpholine amide compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 2,5-disubstituted thiomorpholine amide compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
    Type: Grant
    Filed: October 16, 2012
    Date of Patent: May 12, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Christina Di Marco
  • Patent number: 9023790
    Abstract: The present invention relates to aqueous solutions useful as pharmaceutical compositions of posaconazole for intravenous administration. These compositions include a solubilizing agent, such as a modified ?-cyclodextrin in an acidified solution, which can also include a chelating agent such as disodium edetate (EDTA). In clinical trials, a 200 mg posaconazole dose of the selected composition was found to achieve acceptable pharmacokinetic properties.
    Type: Grant
    Filed: June 24, 2011
    Date of Patent: May 5, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Susan K. Heimbecher, David Monteith, James D. Pipkin
  • Patent number: 9023865
    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 (1).
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: May 5, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jongwon Lim, Elizabeth Helen Kelley, Joey L. Methot, Hua Zhou, Alessia Petrocchi, Umar Faruk Mansoor, Christian Fischer, Brendan O'Boyle, David Joseph Guerin, Corey E. Bienstock, Christopher W. Boyce, Matthew H. Daniels, Danielle Falcone, Ronald D. Ferguson, Salem Fevrier, Xianhai Huang, Kathryn Ann Lipford, David L. Sloman, Kevin Wilson, Wei Zhou, David Witter, Milana M. Maletic, Phieng Siliphaivanh
  • Patent number: 9024032
    Abstract: The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 5, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, James C. Barrow, Michael S. Poslusney, Scott T. Harrison, B. Wesley Trotter, James Mulhearn, Kausik K. Nanda, Peter J. Manley, Zhijian Zhao, Jeffrey W. Schubert, Nathan Kett, Amy Zartman