Search Patents
  • Substituted-aminohydroxypropoxy-thiadiazoles, .beta.-blocking compositions and use
    Patent number: 4562184
    Abstract: Novel substituted-aminohydroxypropoxy-thiadiazoles and pharmaceutically acceptable salts thereof exhibit .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: April 2, 1984
    Date of Patent: December 31, 1985
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Cyclic Derivatives as Inhibitors of Stearoyl-Coenzyme a Delta-9 Desaturase
    Publication number: 20100004287
    Abstract: Cyclic amine derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
    Type: Application
    Filed: May 22, 2007
    Publication date: January 7, 2010
    Applicant: Merck Frosst Canada Ltd.
    Inventors: Yves Leblanc, Marc Gagnon
  • Heterocycle-substituted amides, carbamates and ureas as agents for the treatment of atherosclerosis
    Patent number: 5358946
    Abstract: This invention relates to imidazoles, namely, heterocycle-substituted amides, carbamates and ureas as inhibitors of acyl-CoA: cholesterol acyltransferase (ACAT), pharmaceutical compositions containing them, and their use as antihypercholesterolemic and/or antiatherosclerotic agents for the treatment of atherosclerosis.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: October 25, 1994
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Richard G. Wilde
  • Compounds containing basic and acidic termini useful as fibrinogen receptor antagonists
    Patent number: 5691329
    Abstract: This invention relates to novel compounds containing basic and acidic termini, 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: August 8, 1996
    Date of Patent: November 25, 1997
    Assignee: The DuPont Merck Pharmaceutical Company
    Inventors: William Frank DeGrado, Chu-Biao Xue
  • NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS
    Publication number: 20130143859
    Abstract: Compounds of structural formulas I-1 and I-2 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: June 3, 2011
    Publication date: June 6, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Wensheng Liu, Iyassu K. Sebhat, Dong-Ming Shen, Zhi-Cai Shi
  • Triazole derivative as an HSP 90 inhibitor
    Patent number: 8816070
    Abstract: 5-[4-(2-Methylphenyl)-3-hydroxy-4H-1,2,4-triazol-5-yl]-2,4-dihydroxy-N-methyl-N-butylbenzamide is an HSP90 inhibitor and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: August 26, 2014
    Assignee: Merck Patent GmbH
    Inventors: Hans Michael Eggenweiler, Michael Wolf, Hans Peter Buchstaller, Christian Sirrenberg
  • SUBSTITUTED IMIDAZOLE 4-CARBOXAMIDES AS CHOLECYSTOKININ-1 RECEPTOR MODULATORS
    Publication number: 20100311649
    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: Application
    Filed: August 3, 2010
    Publication date: December 9, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
  • Substituted pyrazoles, compositions containing such compounds and methods of use
    Patent number: 7989475
    Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
    Type: Grant
    Filed: March 19, 2009
    Date of Patent: August 2, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
  • Crystalline pharmaceutically acceptable salts of an oxazolidinone derivative
    Patent number: 6329393
    Abstract: A crystalline pharmaceutically acceptable benzenesulfonate salt of Compound A of formula: and solvates thereof are disclosed. Compound A and its benzenesulfonate salts are alpha 1a adrenergic receptor antagonists useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts are also disclosed.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Joseph S. Amato, Zhen Li, James A. McCauley
  • Five-membered heteroaromatic compounds as dopamine receptor subtype ligands
    Patent number: 5939436
    Abstract: A class of heteroaromatic compounds incorporating a substituted five-membered heteroaromatic nucleus which contains at least two nitrogen atoms are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia and depression.
    Type: Grant
    Filed: June 25, 1997
    Date of Patent: August 17, 1999
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Paul David Leeson, Kevin William Moore
  • Substituted piperidinyl compounds useful as GPR119 agonists
    Patent number: 9018200
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Oxadiazole Derivatives
    Publication number: 20100240658
    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: Application
    Filed: October 1, 2008
    Publication date: September 23, 2010
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnes Bombrun, Mathilde Muzerelle, Jerome Dorbais, Delphine Marin, Jerome Gonzalez, Patrick Gerber
  • Piperidine derivatives as melanocortin-4 receptor agonists
    Patent number: 7419990
    Abstract: Certain novel 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 16, 2004
    Date of Patent: September 2, 2008
    Assignee: Merck & Co., Inc.
    Inventors: Heather Sings, Feroze Ujjainwalla
  • Use of sigma receptor antagonists for treatment of amphetamine abuse
    Patent number: 5162341
    Abstract: The invention relates to a method of treating drug abuse or addiction involving amphetamine or amphetamine-related drugs with pharmacological effects similar to amphetamine in a mammal which comprises administering to the mammal an effective amount, to reduce the pharmacological effects of the amphetamine or amphetamine-related drug, of certain piperidine sigma receptor antagonists.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: November 10, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Leonard Cook
  • Cyclic compounds useful in the treatment of dyslipidaemia, atherosclerosis and diabetes, pharamaceutical compositions and preparation process
    Patent number: 6528538
    Abstract: The present invention relates to cyclic compounds which are of the class of compounds of formula I wherein X and Y represent an oxygen atom and to processes for preparing such compounds. The compounds are useful in the treatment of dyslipidemia, atherosclerosis, and diabetes.
    Type: Grant
    Filed: January 16, 2001
    Date of Patent: March 4, 2003
    Assignee: Merck Patentgesellschaft
    Inventors: Jean-Jacques Zeiller, Jean-Jacques Berthelon, Eric Raspé, Daniel Guerrier
  • Thiazole derivatives and use thereof
    Patent number: 7879888
    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: May 24, 2006
    Date of Patent: February 1, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6001835
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: December 14, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Christopher J. Dinsmore, Theresa M. Williams
  • Sulfonamide fibrinogen receptor antagonists
    Patent number: 6040317
    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: December 28, 1998
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Wasyl Halczenko, Melissa S. Egbertson, George D. Hartman, William L. Laswell
  • Arylthiazolidinedione derivatives
    Publication number: 20020037911
    Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.
    Type: Application
    Filed: November 21, 2001
    Publication date: March 28, 2002
    Applicant: Merck & Co., Inc.
    Inventors: Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
  • Sulfonamide fibrinogen receptor antagonists
    Patent number: 5814643
    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: May 22, 1997
    Date of Patent: September 29, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, William L. Laswell