Abstract: Compounds of the formula (I), in which R6, R7, R8, R9 and X have the meanings indicated in claim 1, are inhibitors of tyrosine kinases, in particular TIE-2, and Raf kinases and can be employed, inter alia, for the treatment of tumours.
Type:
Grant
Filed:
March 17, 2005
Date of Patent:
May 5, 2009
Assignee:
Merck Patent Gesellschaft Mit Beschrankter Haftung
Inventors:
Guenter Hoelzemann, Helene Crassier, Alfred Jonczyk, Wolfgang Staehle, Wilfried Rautenberg
Abstract: Thiazole derivatives of the formula I in which R1, R2, R3, V, W, X and B are as defined in claim 1, 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.
Abstract: The instant invention provides compounds of Formula II which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula II are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Grant
Filed:
February 23, 2012
Date of Patent:
April 23, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
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
Abstract: Novel tertiary aminohydroxypropoxy substituted thiadiazole compounds exhibit .alpha..sub.1 -adrenoceptor and serotonin antagonism and are also useful as antihypertensive agents.
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.
Abstract: Compounds of the formula (I), in which R1, R2, R3a, R3b, R3c and R3d 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:
Grant
Filed:
July 18, 2006
Date of Patent:
January 25, 2011
Assignee:
Merck Patent GmbH
Inventors:
Dieter Dorsch, Oliver Schadt, Andree Blaukat
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Type:
Grant
Filed:
March 25, 1999
Date of Patent:
May 8, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
Abstract: The instant invention provides compounds of Formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of Formula (I) are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Grant
Filed:
August 29, 2007
Date of Patent:
May 14, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Anthony Ogawa, Feroze Ujjainwalla, Ellen K. Vande Bunte, Lin Chu, Debra Ondeyka, Ihor Kopka, Bing Li, Hyun Ok, Minal J. Patel, Jinyou Xu, Rosemary Sisco
Abstract: A group of compounds of, the preparation of, and the methods of use of benzoylpyridazine derivatives and the physiologically acceptable salts and solvates thereof, which have valuable pharmacological properties while well tolerated. They selectively inhibit phosphodiesterase IV with an intracellular increase in the CAMP level, and have an inhibitory effect on the formation of tumor necrosis factor.
Type:
Grant
Filed:
May 3, 2001
Date of Patent:
April 23, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Rochus Jonas, Michael Wolf, Franz-Werner Kluxen
Abstract: Disclosed are carboxyl derivatives, i.e., esters, anhydrides and amides, of the antibiotic thienamycin, which has the following structure: ##STR1## Such derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such derivatives, pharmaceutical compositions comprising such derivatives, and methods of treatment comprising administering such derivatives and compositions when an antibiotic effect is indicated.
Type:
Grant
Filed:
December 16, 1977
Date of Patent:
January 1, 1980
Assignee:
Merck & Co., Inc.
Inventors:
Burton G. Christensen, Raymond A. Firestone
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:
May 8, 2008
Publication date:
November 4, 2010
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Inventors:
Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
Abstract: Hydrazono-malonitrile derivatives of the formula (I) in which R1, R2, R3, R3? and R4 have the meanings given in Claim 1 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:
October 10, 2002
Date of Patent:
November 28, 2006
Assignee:
Merck Patent Gesellschaft
Inventors:
Hans-Michael Eggenweiler, Michael Wolf, Norbert Beier, Pierre Schelling, Thomas Ehring
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: 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: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: ##STR1## wherein Y.sup.1 and Y.sup.2 are independently selected from the group consisting ofhydrogen,C.sub.1-4 alkyl,C.sub.1-4 alkoxy,C.sub.
Type:
Grant
Filed:
May 26, 1999
Date of Patent:
July 25, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Philip E. Sanderson, Adel M. Naylor-Olsen
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
Abstract: Novel 3-amino-2-OR-propoxyaryl 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.
Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.
Type:
Application
Filed:
February 2, 2009
Publication date:
December 30, 2010
Applicant:
Merck Patent GMBH
Inventors:
Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
Abstract: Triazoles substituted at the 3 and 5 positions having an optional substituent in the 1 position are provided. Methods of preparing the novel substituted triazoles are described. The substituted triazoles are useful as anti-gout and anti-hyperuricemic agents. Compositions useful in the treatment of gout and hyperuricemia containing a substituted triazole as the active ingredient are also provided.