Search Patents
  • Patent number: 7528139
    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
  • Patent number: 7790723
    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.
    Type: Grant
    Filed: April 28, 2003
    Date of Patent: September 7, 2010
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Patent number: 8426413
    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
  • 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
  • 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
  • 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
  • Patent number: 7875644
    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
  • Patent number: 6228867
    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
  • Patent number: 8440672
    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
  • Patent number: 6376493
    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
  • Patent number: 4181733
    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
  • Publication number: 20100280030
    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
  • Patent number: 7141572
    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
  • Publication number: 20110160183
    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
  • Patent number: 5451588
    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
  • Patent number: 6093717
    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
  • 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
  • Patent number: 4134983
    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.
    Type: Grant
    Filed: December 17, 1975
    Date of Patent: January 16, 1979
    Assignee: Merck & Co., Inc.
    Inventor: John J. Baldwin
  • Publication number: 20100331338
    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
  • Patent number: 4198513
    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.
    Type: Grant
    Filed: April 7, 1978
    Date of Patent: April 15, 1980
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Frederick C. Novello