Search Patents
  • Sulfonamide fibrinogen receptor antagonists
    Patent number: 5880136
    Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: August 6, 1998
    Date of Patent: March 9, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, William L. Laswell
  • Isoxazoline compounds useful as fibrinogen receptor antagonists
    Patent number: 5446056
    Abstract: This invention relates to novel isoxazolines which are useful as antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of thromboembolic disorders.
    Type: Grant
    Filed: September 12, 1994
    Date of Patent: August 29, 1995
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: John Wityak, Thais M. Sielecki-Dzurdz
  • Treatment of psychosis using 1-cycloalkylpiperidines
    Patent number: 5296479
    Abstract: There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
    Type: Grant
    Filed: February 6, 1992
    Date of Patent: March 22, 1994
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Gary A. Cain, Paul J. Gilligan, Sang W. Tam
  • 3,3-disubstituted piperidine derivatives and their use as therapeutic agents
    Patent number: 5807865
    Abstract: The present invention relates to compounds of the formula (I) ##STR1## wherein X, Z, R, R.sup.1, R.sup.2, Ar, n and m are as defined herein which are of use in the treatment or prevention of neuropathy, asthma, osteoarthritis, rheumatoid arthritis or migraine.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: September 15, 1998
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Timothy Harrison, Christopher John Swain
  • Dihydroxypropylamine containing retroviral protease inhibitors
    Patent number: 5491149
    Abstract: This invention relates to substituted dihydroxypropylamines, a process to prepare intermediates useful for the synthesis of these compounds, compositions comprising such compounds, and a method of treating retroviral infection.
    Type: Grant
    Filed: August 26, 1994
    Date of Patent: February 13, 1996
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Prabhakar K. Jadhav
  • Pyrazolidine-1,2-dicarboxyldiphenylamide derivatives as coagulation factor Xa inhibitors for the treatment of thromboses
    Patent number: 7557102
    Abstract: Novel compounds of the formula (I), in which R, R1, R2 and R3 have the meanings indicated in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumors.
    Type: Grant
    Filed: March 9, 2004
    Date of Patent: July 7, 2009
    Assignee: Merck Patent GmbH
    Inventors: Werner Mederski, Christos Tsaklakidis, Dieter Dorsch, Bertram Cezanne, Johannes Gleitz
  • Tetrahydropyran derivatives as neurokinin receptor antagonists
    Patent number: 6906085
    Abstract: The present invention relates compounds of the formula (I): wherein R1, R2, R3, R4, R5, R6, R7 and R8 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: January 16, 2002
    Date of Patent: June 14, 2005
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Piotr Antoni Raubo, Christopher John Swain
  • Method for treating attention deficit disorder
    Patent number: 6121261
    Abstract: A tachykinin receptor antagonist is useful for treating or preventing attention deficit disorder, optionally associated with hyperactivity, in a patient.
    Type: Grant
    Filed: November 19, 1998
    Date of Patent: September 19, 2000
    Assignee: Merck & Co., Inc.
    Inventors: David L. Glatt, Mark S. Kramer, Nadia Rupniak
  • Fluorinated 2,4-diaryl-2,5-dihydropyrrole inhibitors of the mitotic kinesin KSP
    Patent number: 7465746
    Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: August 11, 2004
    Date of Patent: December 16, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Paul J. Coleman, Christopher D. Cox, Robert M. Garbaccio, George D. Hartman
  • Oxadiazole derivatives
    Patent number: 8202865
    Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: June 19, 2012
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnes Bombrun, Mathilde Muzerelle, Jermone Dorbais, Delphine Marin, Jerome Gonzalez, Patrick Gerber
  • Aminohydroxypropoxy substituted aryl compounds
    Patent number: 4616017
    Abstract: Novel tertiary aminohydroxypropoxy substituted aryl compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.
    Type: Grant
    Filed: June 4, 1984
    Date of Patent: October 7, 1986
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Substituted imidazole 4-carboxamides as cholecystokinin-1 receptor modulators
    Patent number: 7858629
    Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
    Type: Grant
    Filed: April 10, 2007
    Date of Patent: December 28, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
  • Thiazolylimidazole derivatives and their use as inhibitors of microsomal triglyceride transfer protein
    Patent number: 7767819
    Abstract: The present invention relates to thiazolylimidazole derivatives of the general formula (I) in which: G represents a bond or a divalent radical chosen from the groups g1, g2 and g3; and R1, R2, R3, R4, R5, R6, Y and Z are as defined in the description. Application of the compounds of the formula (I) to the treatment of hypertriglyceridaemia, hypercholesterolaemia and dyslipidaemia.
    Type: Grant
    Filed: January 17, 2005
    Date of Patent: August 3, 2010
    Assignee: Merck Patent GmbH
    Inventors: Philippe Guedat, Olivier Chevreuil, Thierry Convard
  • Aliphatic hydroxy substituted piperidyl diaryl pyrrole derivatives as antiprotozoal agents
    Patent number: 6528531
    Abstract: Trisubstituted pyrroles are antiprotozoal agents useful in the treatment and prevention of protozoal diseases in human and animals, including the control of coccidiosis in poultry.
    Type: Grant
    Filed: November 10, 2000
    Date of Patent: March 4, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Tesfaye Bitfu, Danqing D. Feng, Gui-Bai Liang, Mitree M. Ponpipom, Xiaoxia Qian, Michael H. Fisher, Matthew J. Wyvratt, Robert L. Bugianesi
  • THIAZOLYL PIPERIDINE DERIVATIVES
    Publication number: 20110105505
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R9, R10, R11, Q and W have the meanings indicated in Claim 1, and precursors thereof are inhibitors of sphingosine kinase and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: May 28, 2009
    Publication date: May 5, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRÄNKTER HAFTUNG
    Inventors: Frank Stieber, Timo Heinrich, Dirk Wienke
  • Acylated piperidine derivatives as melanocortin 4-receptor agonists
    Patent number: 7618987
    Abstract: Certain novel N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: November 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Raman K. Bakshi, James P. Dellureficio, Ravi P. Nargund
  • Adhesion receptor antagonists
    Patent number: 5532255
    Abstract: Compounds of the formula ##STR1## in which R.sup.1, X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumors.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: July 2, 1996
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Peter Raddatz, Joachim Gante, Horst Juraczyk, Hanns Wurziger, Helmut Prucher, Sabine Bernotat-Danielowski, Guido Melzer
  • Antihypercholesterolemic compounds
    Patent number: 4916162
    Abstract: Novel 3-hydroxy-3-methylglutary-coenzyme A (HMG-CoA) reductase inhibitors which are useful as antihypercholesterolemic agents and are represented by the following general structural formulae (I) and (II): ##STR1## and pharmaceutically acceptable salts of the compounds (II) in which Z is hydrogen are disclosed.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: April 10, 1990
    Assignee: Merck & Co., Inc.
    Inventors: William F. Hoffman, Clarence S. Rooney, Ta Jyh Lee
  • Thiazole derivatives and use thereof
    Patent number: 8802861
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: January 11, 2005
    Date of Patent: August 12, 2014
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Piperidine and azetidine derivatives as GlyT1 inhibitors
    Patent number: 7655644
    Abstract: The present invention provides compounds of formula (I), wherein both p's are one or two, R1 is generally heteroaryl or cycloalkyl, R2 is C3-6cycloalkyl or phenyl and R3 is heteroaryl, and pharmaceutically acceptable salts thereof, as GlyT1 inhibitors for treating schizophrenia, pharmaceutical compositions comprising the same and methods for their preparation.
    Type: Grant
    Filed: December 21, 2005
    Date of Patent: February 2, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Stephen Robert Fletcher, Andrew Jennings, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street, Joanne Thomson