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  • Substituted pyridazines having cytokine inhibitory activity
    Patent number: 6602872
    Abstract: There are disclosed compounds of formula (I) and pharmaceutically acceptable salts thereof which exhibit utility for the treatment of cytokine mediated diseases such as arthritis.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: August 5, 2003
    Assignee: Merck & Co., Inc.
    Inventors: Charles J. McIntyre, Nigel J. Liverton, David A. Claremon
  • Chroman derivatives
    Patent number: 6040308
    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: October 28, 1994
    Date of Patent: March 21, 2000
    Assignee: Merck Gesellschaft mit beschrankter Haftung
    Inventors: Gunther Hausler, Rolf Gericke, Hanns Wurziger, Manfred Baumgarth, Inge Lues, Jacques De Peyer, Rolf Bergmann
  • Amino-phenyl-thiadiazoledioxides as gastric secretion inhibitors
    Patent number: 4567191
    Abstract: Novel amino-phenyl-thiadiazoledioxides and related compounds and processes for preparing such compounds are disclosed. The compounds are useful for suppressing gastric acid secretions in mammals.
    Type: Grant
    Filed: June 7, 1983
    Date of Patent: January 28, 1986
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Adolph Pietruszkiewicz, William A. Bolhofer, William C. Lumma, Jr.
  • Pyridazinone derivatives
    Patent number: 8921357
    Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R4? 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 tumors.
    Type: Grant
    Filed: March 5, 2013
    Date of Patent: December 30, 2014
    Assignee: Merck Patent GmbH
    Inventors: Dieter Dorsch, Frank Stieber, Oliver Schadt, Andree Blaukat
  • Pyrmidine derivatives
    Patent number: 5763448
    Abstract: A class of substituted pyrimidine derivatives are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment of disorders of the dopamine system, in particular schizophrenia ##STR1##
    Type: Grant
    Filed: March 18, 1996
    Date of Patent: June 9, 1998
    Assignee: Merck, Sharp & Dohme Limited
    Inventors: William Robert Carling, Ian James Collins, Michael Rowley, Paul David Leeson
  • PYRIDINE-AND PYRAZINE DERIVATIVES
    Publication number: 20140142097
    Abstract: Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases
    Type: Application
    Filed: April 11, 2012
    Publication date: May 22, 2014
    Applicant: Merck Patent GmbH
    Inventors: Guenter Hoelzemann, Hans-Michael Eggenweiler, Srinivasa R. Karra
  • 4-heteroaryl-and 4-aryl-1,4-dihydropyridine, derivatives with calcium agonist and alpha.sub.1 -antagonist activity
    Patent number: 5166147
    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: July 9, 1990
    Date of Patent: November 24, 1992
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventor: Richard A. Earl
  • Hetaryl-[1,8]naphthyridine derivatives
    Publication number: 20140038960
    Abstract: Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: October 4, 2013
    Publication date: February 6, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Alfred Jonczyk, Dieter Dorsch, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
  • Benzimidazole compounds
    Patent number: 5401738
    Abstract: Benzimidazole compounds of the formula I ##STR1## and salts thereof, exhibit antagonistic properties toward angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and an increased intraocular pressure, as well as disturbances of the central nervous system.
    Type: Grant
    Filed: June 11, 1993
    Date of Patent: March 28, 1995
    Assignee: Merck Patent Gesellschaft mit beschrankter
    Inventors: Werner Mederski, Dieter Dorsch, Norbert Beier, Pierre Schelling, Ingeborg Lues, Klaus-Otto Minck, Mathias Osswald
  • Pyridazine derivatives
    Patent number: 7563790
    Abstract: Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumors, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: July 21, 2009
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • 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
  • BENZONITRILE DERIVATIVES AS KINASE INHIBITORS
    Publication number: 20140228340
    Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.
    Type: Application
    Filed: August 13, 2012
    Publication date: August 14, 2014
    Applicant: MERCK PATENT GMBH
    Inventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler
  • Novel pyrrolidone derivatives for use as MetAP-2 inhibitors
    Publication number: 20110263561
    Abstract: Compounds of the formula (I), in which R, X, Y, Z, R3 and R4 have the meanings indicated in claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.
    Type: Application
    Filed: May 13, 2009
    Publication date: October 27, 2011
    Applicant: Merck Patent GmbH
    Inventors: Timo Heinrich, Mireille Krier, Thorsten Knoechel, Alfred Jonczyk, Frank Zenke, Holger Enderle
  • Pyridazine derivatives
    Patent number: 7129241
    Abstract: Pyridazine derivatives of the formula (I) act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDS
    Type: Grant
    Filed: May 12, 2003
    Date of Patent: October 31, 2006
    Assignee: Merck Patent Gesellschaft
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • 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
  • 3-Amino-2-hydroxypropoxyaryl imidazole derivatives
    Patent number: 4440774
    Abstract: Novel substituted imidazoles of the formula ##STR1## and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: April 20, 1981
    Date of Patent: April 3, 1984
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • 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
  • 2-(heterocyclylbenzyl)pyridazinone derivatives
    Patent number: 8435981
    Abstract: Compounds of the formula (I) in which R1, R2, R3, R4 and R5 have the meanings indicated in claim 1 are inhibitors of tyrosine kinases, in particular of met kinase and can be employed inter alia for the treatment of tumors.
    Type: Grant
    Filed: July 12, 2007
    Date of Patent: May 7, 2013
    Assignee: Merck Patent Gesellschaft mit Beschränkter Haftung
    Inventors: Dieter Dorsch, Oliver Schadt, Andree Blaukat, Frank Stieber
  • 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
  • .beta.-Adrenergic 2-[4-(3-amino-2-hydroxypropoxy)phenyl]imidazoles
    Patent number: 4567276
    Abstract: Novel substituted imidazoles and methods for their preparation are disclosed. These imidazoles, and their salts, exhibit pharmacological activity which includes antihypertensive activity and .beta.-adrenergic blocking activity.
    Type: Grant
    Filed: June 13, 1983
    Date of Patent: January 28, 1986
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin