Search Patents
  • Substituted 8-arylquinoline phosphodiesterase-4 inhibitors
    Patent number: 6410563
    Abstract: Novel substituted 8-arylquinolines, wherein the aryl group at the 8-position contains a substituent substituted-alkenyl group, are PDE4 inhibitors.
    Type: Grant
    Filed: December 20, 2000
    Date of Patent: June 25, 2002
    Assignee: Merck Frosst Canada & Co.
    Inventors: Denis Deschenes, Daniel Dube, Michel Gallant, Yves Girard, Patrick Lacombe, Dwight MacDonald, Anthony Mastracchio, Helene Perrier
  • AMINOPYRIMIDINE DERIVATIVES FOR USE AS MODULATORS OF KINASE ACTIVITY
    Publication number: 20150126484
    Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: May 7, 2015
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Lizbeth Celeste Deselm, Yufang Xiao, Hui Qiu, Constantin Neagu, Igor Mochalkin, Theresa L. Johnson
  • Isoquinoline potassium channel inhibitors
    Patent number: 7763614
    Abstract: The present invention relates to compounds of structural formula I: I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: September 22, 2004
    Date of Patent: July 27, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Isaacs, Christopher J. Dinsmore, B. Wesley Trotter, Nigel Liverton, Douglas C. Beshore, Nathan R. Kett, Charles J. McIntyre, Kausik K. Nanda, David A. Claremon
  • Aminomethyloxooxazlidinyl arylbenzene derivatives useful as antibacterial agents
    Patent number: 5130316
    Abstract: Novel aminomethyloxooxazolidinyl arylbenzene derivatives, wherein the aryl includes the phenyl, substituted phenyl, pyridyl, and substituted pyridyl groups, such as (l)-N-{3-[4-(4 '-pyridyl)phenyl]-2-oxooxazolidin-5-ylmethyl}acetamide, possess useful antibacterial activity.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: July 14, 1992
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventors: Randall K. Carlson, Chung-Ho Park, Walter A. Gregory
  • BENZOTHIAZOLONE DERIVATIVES
    Publication number: 20110269756
    Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
    Type: Application
    Filed: December 8, 2009
    Publication date: November 3, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
  • Class III antiarrhythmic agents
    Patent number: 5032604
    Abstract: Compounds of structural formula: ##STR1## wherein R' is hydrogen or an aromatic ring system, and Q is a substituted nitrogen or a nitrogen containing heterocycle, and E is --S-- or --O--, are Class III antiarrhythmic agents.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: July 16, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David A. Claremon, Jason M. Elliott, Gerald S. Ponticello, David C. Remy, Harold G. Selnick
  • 4-Heteroaryl- 1,4-dihydropyridine compounds with calcium agonist and alpha.sub.1 -antagonist activity
    Patent number: 5580871
    Abstract: There are provided novel 1,4-dihydropyridine compounds, compositions containing them and methods of using them to treat congestive heart failure.
    Type: Grant
    Filed: March 9, 1995
    Date of Patent: December 3, 1996
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventor: Richard A. Earl
  • Tertiary aminohydroxypropoxy substituted thiadiazoles, pharmaceutical compositions and use
    Patent number: 4539318
    Abstract: Novel tertiary aminohydroxypropoxy substituted thiadiazole 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: September 3, 1985
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Gerald S. Ponticello
  • Biheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5880140
    Abstract: The present invention is directed to compounds of the formula A which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras: ##STR1## 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: April 1, 1997
    Date of Patent: March 9, 1999
    Assignee: Merck & Co., Inc.
    Inventor: Neville J. Anthony
  • Substituted pyrazines, pyrimidines and pyridazines for use in the treatment of glaucoma
    Patent number: 5219849
    Abstract: A class of pyrazine, pyrimidine and pyridazine derivatives, substituted by a non-aromatic azabicyclic ring system and optionally by up to two further substituents, is of use in the preparation of medicaments, especially formulations adapted for topical administration to the eye, suitable for the treatment of glaucoma and/or for reducing intraocular pressure.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: June 15, 1993
    Assignee: Merck Sharp & Dohme
    Inventors: Victor Lotti, Graham A. Showell
  • Quinoline inhibitor of the macrophage stimulating 1 receptor MSTR1
    Patent number: 9481668
    Abstract: The compound N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)-3-fluorophenyl)-5-ethyl-1 -(pyrimidin-5-yl)-1H-pyrazole-4-carboxamide and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, is an inhibitor of RON and can be employed, for the treatment of cancer.
    Type: Grant
    Filed: May 7, 2014
    Date of Patent: November 1, 2016
    Assignee: Merck Patent GmbH
    Inventors: Oliver Schadt, Christina Esdar, Carsten Schultz-Fademrecht, Jan Eickhoff
  • Pyridyl piperidine orexin receptor antagonists
    Patent number: 8242121
    Abstract: The present invention is. directed to pyridyl piperidine compounds of formula (I) 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: May 22, 2008
    Date of Patent: August 14, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, John D. Schreier
  • Arylheteroaryl inhibitors of farnesyl-protein transferase
    Patent number: 5872136
    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 27, 1997
    Date of Patent: February 16, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Samuel L. Graham
  • Chroman derivatives
    Patent number: 5387587
    Abstract: Chroman derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 have the meanings defined herein, and their salts have an effect on the cardiovascular system.
    Type: Grant
    Filed: September 27, 1991
    Date of Patent: February 7, 1995
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Gunther Hausler, Rolf Gericke, Hanns Wurziger, Manfred Baumgarth, Inge Lues, Jacques De Peyer, Rolf Bergmann
  • Inhibitors of farnesyl-protein transferase
    Patent number: 6093737
    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: December 23, 1997
    Date of Patent: July 25, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, Lekhanh O. Tran, Steven D. Young
  • Novel Imidazole Amines as Modulators of Kinase Activity
    Publication number: 20140343029
    Abstract: The invention provides novel imidazole amine compounds according to Formula (I) and Formula (II) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
    Type: Application
    Filed: September 12, 2012
    Publication date: November 20, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Ruoxi Lan, Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Lizbeth Celeste Deselm, Hui Qiu, Constantin Neagu, Donald Bankston, Christopher Charles Victor Jones
  • 1-substituted azaoxindoles and pharmaceutical compositions
    Patent number: 5428035
    Abstract: Compounds of Formula I have been shown to enhance the release of the neurotransmitter acetylcholine, and thus may be useful as chemical intermediates and as pharmacological agents in the treatment of diseases of man, such as in Alzheimer's Disease and other conditions involving learning and cognition, where subnormal levels of this neurochemical are found.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: June 27, 1995
    Assignee: The Dupont Merck Pharmaceutical Company
    Inventor: Christopher A. Teleha
  • Use of ectoine or ectoine derivatives in cosmetic formulations
    Publication number: 20030157040
    Abstract: The invention relates to the use of one or more compounds selected from the compounds of formulas (Ia) and (Ib), their physiologically compatible salts and their stereoisomeric forms, where R1, R2, R3, R4 and n have the meanings given in claim no. 1, for the preparation of a cosmetic formulation. Said use is advantageous in protecting and stabilizing the nucleic acids of human skin cells.
    Type: Application
    Filed: January 31, 2003
    Publication date: August 21, 2003
    Applicant: Merck Patent GmbH
    Inventors: Joachim Bunger, Hans-Jurgen Driller
  • Fibrinogen receptor antagonists
    Patent number: 5397791
    Abstract: Fibrinogen receptor antagonists having the formula ##STR1## for example ##STR2##
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: March 14, 1995
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, John D. Prugh, Wasyl Halczenko, Melissa Egbertson, Nathan Ihle
  • Bipiperidinyl compounds, compositions, containing such compounds and methods of treatment
    Patent number: 8445499
    Abstract: Bipiperidinyl compounds of the formula: are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: May 21, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Harold B. Wood, Alan D. Adams, Stanley Freeman, Jason W. Szewczyk, Conrad Santini, Yong Huang