Search Patents
  • Glucokinase Activators
    Publication number: 20100331338
    Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.
    Type: Application
    Filed: February 2, 2009
    Publication date: December 30, 2010
    Applicant: Merck Patent GMBH
    Inventors: Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
  • Substituted hexahydroarylquinolizines
    Patent number: 4831035
    Abstract: Certain substituted hexahydroarylquinolizines and pharmaceutically acceptable salts thereof are peripherally selective .alpha..sub.2 -adrenoceptor antagonists. The compounds are adapted to be employed for the treatment of certain pathological disorders such as hypertension, diabetes, disorders involving platelet aggregation and the like without side effects attributable to effect on the central nervous system.
    Type: Grant
    Filed: July 27, 1987
    Date of Patent: May 16, 1989
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Joel R. Huff, Susan J. deSolms, Joseph P. Vacca, Jonathan M. Wiggins, Steven D. Young
  • Inhibitors of Akt activity
    Patent number: 7579355
    Abstract: The present invention is directed to compounds which contain a substituted pyridine moeity which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: April 20, 2004
    Date of Patent: August 25, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Mark E. Duggan, John C. Hartnett, Craig W. Lindsley, Zhicai Wu, Zhijian Zhao
  • Blockade of neuronal m-channels as a therapeutic approach to the treatment of neurological disease
    Patent number: 5750528
    Abstract: Compounds which block neuronal M-channels are useful for treating conditions involving neurotransmitter deficiencies, traumatic brain injury, or the depressive phase of bipolar disorder. Compounds can be evaluated for utility in treating these conditions by determining whether they are capable of blocking neuronal M-channels.
    Type: Grant
    Filed: February 1, 1995
    Date of Patent: May 12, 1998
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: Barry Stephen Brown, Simon Piers Aiken, Robert Zaczek, Paul Richard Hartig, Christopher Allan Teleha, Wendell Wilkie Wilkerson, Richard Alan Earl
  • Factor XIa inhibitors
    Patent number: 10123995
    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: January 15, 2016
    Date of Patent: November 13, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Eric Mertz, Weiguo Liu, Scott D. Edmondson, Amjad Ali, Ying-Duo Gao, Santhosh F. Neelamkavil, Sung-Sau So, Remond Moningka, Wanying Sun, Alan Hruza, Linda L. Brockunier
  • Isonicotinamide orexin receptor antagonists
    Patent number: 8592457
    Abstract: The present invention is directed to isonicotinamide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved.
    Type: Grant
    Filed: October 26, 2009
    Date of Patent: November 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey M. Bergman, Paul J. Coleman, Mamio Christa Mattern, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker
  • 16-substituted-6-aza-androsten-4-ene-3-ones as 5-.alpha.-reductase inhibitors
    Patent number: 5741795
    Abstract: Compounds of the formula I ##STR1## are inhibitors of 5.alpha.-reductase, and are useful for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, prostatic carcinoma, prostatitis and benign prostatic hyperplasia.
    Type: Grant
    Filed: October 17, 1996
    Date of Patent: April 21, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Susan D. Aster, Donald W. Graham, Derek J. Von Langen
  • Fibrinogen receptor antagonists
    Patent number: 5852045
    Abstract: Fibrinogen receptor antagonists having the structure, for example, of ##STR1## for example ##STR2##
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: December 22, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Ben C. Askew, George D. Hartman, Mark E. Duggan, Steven D. Young, John H. Hutchinson, John S. Wai, Melissa S. Egbertson, Laura M. Vassallo, Laura A. Libby, Amy E. Krause, Wasyl Halczenko, Nathan C. Ihle
  • Substituted 1H-pyridinyl-2-ones as GABAA alpha 2/3 ligands
    Patent number: 6352994
    Abstract: Compounds according to Formula (I) or a salt thereof are selective ligands for GABAA receptors useful for treatment of disorders of the central nervous system:
    Type: Grant
    Filed: January 4, 2001
    Date of Patent: March 5, 2002
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Ian James Collins, Stephen Robert Fletcher, Timothy Harrison, Paul David Leeson, Christopher Richard Moyes, Alan John Nadin, Michael Rowley, Timothy Jason Sparey, Martin Richard Teall
  • N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
    Patent number: 7053089
    Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: May 30, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Christopher F. Claiborne, John W. Butcher, David A. Claremon, Brian E. Libby, Nigel J. Liverton, Peter M. Munson, Kevin T. Nguyen, Brian Phillips, Wayne Thompson, John A. McCauley
  • Therapeutic compounds for treating dyslipidemic conditions
    Patent number: 7125865
    Abstract: The present invention relates to novel LXR ligands of Formula I and the pharmaceutically acceptable salts, esters and tautomers thereof, which are useful in the treatment of dyslipidemic conditions, particularly depressed levels of HDL cholesterol.
    Type: Grant
    Filed: July 21, 2003
    Date of Patent: October 24, 2006
    Assignee: Merck & Co., Inc.
    Inventors: A. Brian Jones, Alan D. Adams, Ahren I. Green, Shaei Y. Huang, Bruno Tse, Clare E. Gutteridge, Yuan Cheng
  • NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS
    Publication number: 20130040929
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 6, 2011
    Publication date: February 14, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey J. Hale, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Zhicai Wu, Cangming Yang
  • Muscarine antagonists
    Patent number: 5756508
    Abstract: This invention is concerned with novel 1,3-dihydro-1-?1-(1-heteroarylpiperidin-4-yl)piperidin-4-yl!-2H-benzimidaz olones, derivatives thereof, their preparation, method of use and pharmaceutical compositions. These compounds are endowed with antimuscarinic activity and are useful in the treatment and/or prevention of myopia (commonly known as nearsightedness).
    Type: Grant
    Filed: October 28, 1996
    Date of Patent: May 26, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Wayne J. Thompson, Richard W. Ransom, Pierre Mallorga, Michael F. Sugrue
  • Diaryl Substituted Alkanes
    Publication number: 20120149674
    Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
    Type: Application
    Filed: February 23, 2012
    Publication date: June 14, 2012
    Applicant: Merck Sharpe & Dohme Corp.
    Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
  • 4-aminobenzoylguanidine derivatives
    Patent number: 5739142
    Abstract: 4-Aminobenzoylguanidines of the formula I ##STR1## in which A, R.sub.1, R.sub.2 and R.sub.3 have the meanings given, and the physiologically unobjectionable salts thereof exhibit antiarrhythmic properties and are active as inhibitors of the cellular Na.sup.+ /H.sup.+ antiporter.
    Type: Grant
    Filed: January 26, 1996
    Date of Patent: April 14, 1998
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Rolf Gericke, Manfred Haumgarth, Norbert Beier, Klaus-Otto Minck
  • (N-phthalimidoalkyl) piperidines useful as treatments for psychosis
    Patent number: 5356906
    Abstract: There is described novel (N-phthalimidoalkyl) piperidine compounds which exhibit selective sigma-receptor antagonism and therefore are useful in the treatment of physiological or drug induced psychosis and dyskinesia in a mammal. Also described are pharmaceutical compositions containing sigma selective compounds and methods of using these compositions for treating physiological or drug induced psychosis or dyskinesia in a mammal. Further provided are methods for preparing the compounds of this invention.
    Type: Grant
    Filed: April 30, 1992
    Date of Patent: October 18, 1994
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Engelbert Ciganek, Sang W. Tam, Ann S. Wright
  • Inhibitors of Akt activity
    Patent number: 8003643
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: August 23, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • Triazole derivatives as inhibitors of 11-?-hydroxysteroid dehydrogenase-1
    Patent number: 7504402
    Abstract: Triazole derivatives of structural formula I are selective inhibitors of the 11?-hydroxysteroid dehydrogenase-1. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dyslipidemia, hyperlipidemia, hypertension, Metabolic Syndrome, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: December 14, 2004
    Date of Patent: March 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Sherman T. Waddell, Gina M. Santorelli, Milana M. Maletic, Aaron H. Leeman, Xin Gu, Donald W. Graham, James M. Balkovec, Susan D. Aster
  • Inhibitors of Akt activity
    Patent number: 7576209
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
  • Unsaturated hydroxyalkylquinoline acids as leukotriene antagonists
    Patent number: 5856322
    Abstract: Compounds having the formula I: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating angina, cerebral spasm, glomerular nephritis, hepatitis, endotoxemia, uveitis, and allograft rejection.
    Type: Grant
    Filed: February 8, 1996
    Date of Patent: January 5, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Michel L. Belley, Serge Leger, Patrick Roy, Marc Labelle, Yi Bin Xiang, Daniel Guay