Abstract: The present invention relates to compounds of general Formula (I) or a pharmaceutically acceptable salt thereof. The compounds can be used in the treatment of immune, autoimmune, inflammatory diseases, cardiovascular diseases, infectious diseases, bone resorption disorders, neurodegenerative diseases or proliferative diseases.
Type:
Grant
Filed:
December 13, 2010
Date of Patent:
July 8, 2014
Assignee:
Merck Sharp & Dohme B.V.
Inventors:
Tjeerd Andries Barf, Arthur Oubrie, Carsten Schultz-Fademrecht, Eduard Willem Zwart, Niels Hoogenboom, Sander Martijn De Wilde, Allard Kaptein
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.
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:
Application
Filed:
March 11, 2011
Publication date:
June 30, 2011
Applicant:
Merck & Co., Inc.
Inventors:
Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
Abstract: The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 1. The compounds are useful, for example, in the treatment of autoimmune disorders, such as multiple sclerosis.
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
Abstract: N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Type:
Grant
Filed:
January 30, 2003
Date of Patent:
July 19, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Michael R. Wood, Neville J. Anthony, Mark G. Bock, Dong-Mei Feng, Scott D. Kuduk, Dai-Shi Su, Jenny Miu-chun Wai
Abstract: A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
Type:
Grant
Filed:
November 22, 1993
Date of Patent:
September 19, 1995
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Raymond Baker, Victor G. Matassa, Leslie J. Street
Abstract: The invention relates to compounds of formula (I): wherein X, W, Q, R, R1 and R2 have the meanings given in claim 15. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
Abstract: This invention relates to a method for treating and preventing hypertension by administering a therapeutically effective amount of an agent capable of reducing uric acid levels in a patient in need of such treatment. Additionally, the scope of the invention includes a method of treating coronary heart disease by administering a therapeutically effective amount of an agent capable of reducing uric acid levels in a patient in need of such treatment.
Type:
Grant
Filed:
June 28, 2001
Date of Patent:
September 21, 2010
Assignees:
Merck Sharp & Dohme Corp., University of Washington
Inventors:
Salah Kivlighn, Richard Johnson, Marilda Mazzali
Abstract: Novel hetarylaminonaphthyridine derivatives of formula (I) wherein X, R1, R2, R3, R4, W1, W2, 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:
January 10, 2011
Publication date:
December 13, 2012
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Alfred Jonczyk, Dieter Dorsch, Frank Zenke, Christiane Amendt
Abstract: The invention relates to 5-(7-methoxy-3,3-dimethyl-2,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2,4-dienoic acid and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said compound.
Type:
Application
Filed:
July 1, 2013
Publication date:
January 16, 2014
Applicant:
Merck Patent GmbH
Inventors:
Soheila ANZALI, Francis Contard, Jean Jacques Zeiller
Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 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 12, 2010
Publication date:
September 6, 2012
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Alfred Jonczyk, Christiane Amendt, Frank Zenke
Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
July 26, 2002
Date of Patent:
October 25, 2005
Assignee:
Merck & Co., Inc.
Inventors:
Mark T. Bilodeau, Peter J. Manley, Adrienne Balitza, George D. Hartman, Leonard Rodman
Abstract: Compounds of the formula (I) and their physiologically acceptable salts and solvates are useful as integrin-inhibiting substances. They are especially useful in the prophylaxis and treatment of cardiovascular disorders, of thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, osteoporosis, in pathological conditions that are caused or propagated by angiogenesis and in tumor therapy.
Type:
Grant
Filed:
October 15, 2001
Date of Patent:
February 18, 2003
Assignee:
Merck Patent GmbH
Inventors:
Wolfgang Stähle, Rudolf Gottschlich, Simon Goodman
Abstract: Substituted 1H-Pyridinyl-2-ones are useful as GABAA-Alpha 2/3 ligands.
Type:
Grant
Filed:
February 11, 2000
Date of Patent:
March 13, 2001
Assignee:
Merck & 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
Abstract: The invention relates to 5-(7-methoxy-3,3-dimethyl-2,3-dihydro-1-benzoxepin-5-yl)-3-methyl-penta-2,4-dienoic acid and its use in compositions, especially topical, cosmetic and/or personal care compositions, and compositions containing said compound.
Type:
Application
Filed:
July 27, 2009
Publication date:
June 16, 2011
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Soheila Anzali, Francis Contard, Jean Jacques Zeiller
Abstract: New tetralin derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 and Z have the meanings indicated herein and salts thereof, exhibit an effect on the cardiovascular system.
Type:
Grant
Filed:
November 7, 1989
Date of Patent:
July 21, 1992
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Manfred Baumgarth, Rolf Gericke, Rolf Bergmann, Jacques De Peyer, Ingeborg Lues
Abstract: A fluorene compound, 4,4'-[9H-fluoren-9-ylidenebis(methylene)]bispyrimidine, or a pharmaceutically acceptable salt thereof is useful in treating various neurological disorders in mammals. This compound has efficacy over a broad dosage range as measured by hypoxia induced cognition impairment and has a wide safety margin as measured by the ratio of cognition to the onset of overt symptoms.
Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R7 and Y have the meanings indicated in Claim 1, are inhibitors of PDK1 and cell proliferation/cell vitality and can be employed for the treatment of tumours and for the treatment of inflammatory diseases.
Type:
Application
Filed:
June 17, 2010
Publication date:
May 10, 2012
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Michel Calderini, Margarita Wucherer-Plietker, Ulrich Graedler, Christina Esdar
Abstract: Compounds described by the chemical structural formula
or a pharmaceutically acceptable salt thereof, are useful in the treatment of pain, migraine, depression, anxiety, schizophrenia, Parkinson's disease, stroke, and in the treatment of neuropathies including postherpetic neuralgia, central pain from spinal cord injury, and phantom limb pain.
Type:
Grant
Filed:
June 25, 2001
Date of Patent:
August 27, 2002
Assignee:
Merck & Co., Inc.
Inventors:
David A. Claremon, John A. McCauley, Nigel J. Liverton, Cory R. Theberge