Patents Assigned to Merck
  • Fused pyrrolidino-cyclopropane derivatives as selective 11-beta-hydroxysteroid dehydrogenase type 1 inhibitors
    Publication number: 20110172265
    Abstract: The present invention relates to fused pyrrolidino-cyclopropane derivatives according to formulae (I) to (IV) as selective inhibitors of the enzyme 11-beta-hydroxysteroid dehydrogenase type 1 (11-?-HSD-1) and the use of such compounds for the treatment and/or prevention of metabolic syndrome, diabetes, insulin resistance, obesity, lipid disorders, glaucoma, osteoporosis, cognitive disorders, anxiety, depression, immune disorders, hypertension and other diseases and conditions.
    Type: Application
    Filed: August 5, 2009
    Publication date: July 14, 2011
    Applicant: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Eric Valeur, Franck Lepifre, Didier Roche, Denis Carniato, Serge Christmann-Franck, Febien Schmidlin
  • 3H-IMIDAZO[4,5-B]PYRIDIN-5-OL DERIVATIVES USEFUL IN THE TREATMENT OF GPR81 RECEPTOR DISORDERS
    Publication number: 20110172209
    Abstract: The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
    Type: Application
    Filed: September 10, 2009
    Publication date: July 14, 2011
    Applicants: ARENA PHARMACEUTICALS, INC., MERCK & CO., INC.
    Inventors: P. Douglas Boatman, Benjamin R. Johnson, Jae-Kyu Jung, Michelle Kasem, Thomas O. Schrader, Philip J. Skinner, Steven Colletti
  • ANTIFUNGAL AGENTS
    Publication number: 20110172225
    Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their, pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.
    Type: Application
    Filed: September 25, 2008
    Publication date: July 14, 2011
    Applicants: Merck Sharp & Dohme Corp., Scynexis, Inc.
    Inventors: James M. Balkovec, Phieng Siliphaivanh, Frances A. Bouffard, Roland A. Bouffard, Michael R. Peel, Weiming Fan, Ahmed Mamai, Sarah Dimick Gray
  • Substituted imidazole 4-carboxamides as cholecystokinin-1 receptor modulators
    Patent number: 7977339
    Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.
    Type: Grant
    Filed: August 3, 2010
    Date of Patent: July 12, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
  • Optimized expression of HPV 58 L1 in yeast
    Patent number: 7976848
    Abstract: Synthetic DNA molecules encoding the HPV58 L1 protein are provided. Specifically, the present invention provides polynucleotides encoding HPV58 L1 protein, wherein said polynucleotides are codon-optimized for high level expression in a yeast cell. The synthetic molecules may be used to produce HPV58 virus-like particles (VLPs), and to produce vaccines and pharmaceutical compositions comprising the HPV58 VLPs. The vaccines of the present invention provide effective immunoprophylaxis against papillomavirus infection through neutralizing antibody and cell-mediated immunity and are also useful for treatment of existing HPV infections.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: July 12, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Janine T. Bryan, Michelle K. Brownlow, Loren D. Schultz, Xin-Min Wang, Kathrin U. Jansen
  • Adenine derivatives
    Patent number: 7977343
    Abstract: Novel adenine derivatives of the formula (I), in which R1, R2, R3, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: July 12, 2011
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Hans-Peter Buchstaller, Hans-Michael Eggenweiler, Bertram Cezanne, Michael Wolf
  • Recombinant carboxypeptidase B
    Patent number: 7977081
    Abstract: A nucleic acid coding for pro-carboxypeptidase B (Pro-CPB), comprising three segments A, B and C, wherein at least one of the segments has one of the sequences according to SEQ ID No. 1, 2 or 3.
    Type: Grant
    Filed: September 26, 2005
    Date of Patent: July 12, 2011
    Assignee: Merck Biosciences AG
    Inventors: Joop Van Den Heuvel, Joerg Bartuch, Arno Cordes
  • 7-AZAINDOLE DERIVATIVES
    Publication number: 20110166175
    Abstract: Novel 7-azaindole derivatives of the formula (I), in which U, L, R, Y, X1, X2 and X3 have the meanings indicated in Claim 1), are kinase inhibitors and can be used for the treatment of diseases and conditions such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systemic and pulmonary hypertonia, cardiovascular diseases and kidney diseases, generally in any type of fibroses, inflammatory processes, tumours and tumour diseases.
    Type: Application
    Filed: July 10, 2009
    Publication date: July 7, 2011
    Applicant: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventor: Markus Klein
  • Isolated organ perfusion combination therapy of cancer
    Publication number: 20110165150
    Abstract: The invention relates to a combination therapy for the treatment of tumors and tumor metastases comprising administration of integrin ligands, preferably integrin antagonists, together with co-therapeutic agents or therapy forms that have synergistic efficacy when administered together with said ligands, such as chemotherapeutic agents and/or radiation therapy, in isolated organ perfusion. The therapy results in a synergistic potential increase of the inhibition effect of each individual therapeutic on tumor cell proliferation, yielding more effective treatment than found by administering an individual component alone.
    Type: Application
    Filed: January 18, 2006
    Publication date: July 7, 2011
    Applicant: Merck Patent GmbH
    Inventors: Simon Goodman, Matthias Grell, Timo L.M. Ten Hagen, Alexander M.M. Eggermont
  • Method for substituting indenofluorenes
    Patent number: 7973203
    Abstract: The invention relates to a process for the preparation of trans-indenofluorene compounds of the formula (Ia) or cis-indenofluorene compounds of the formula (Ib) in a reaction with at least one compound of the formula (IIa) or (IIb) respectively with at least one compound of the R-Hal in the presence of at least one organic base and at least one organic, polar, aprotic solvent.
    Type: Grant
    Filed: November 18, 2006
    Date of Patent: July 5, 2011
    Assignee: Merck Patent GmbH
    Inventor: Arne Buesing
  • Macrocyclic quinoxaline compounds as HCV NS3 protease inhibitors
    Patent number: 7973040
    Abstract: The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections.
    Type: Grant
    Filed: July 17, 2009
    Date of Patent: July 5, 2011
    Assignees: Merck Sharp & Dohme Corp., Istituto di Ricerche di Biologia Molecolare P. Angeletti SpA
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley
  • Liquid-crystalline medium
    Patent number: 7972664
    Abstract: Disclosed are a liquid-crystalline medium, which contains a compound of formula I and the use thereof for electro-optical purposes, in particular for TN, TFT, IPS or OCB displays.
    Type: Grant
    Filed: May 12, 2010
    Date of Patent: July 5, 2011
    Assignee: Merck Patent Gesellschaft MIT Beschrankter Haftung
    Inventors: Michael Wittek, Elvira Montenegro, Konstantin Schneider, Brigitte Schuler
  • Sulfonyl amino cyclic derivatives and use thereof
    Patent number: 7973039
    Abstract: The present invention is related to derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Grant
    Filed: December 19, 2005
    Date of Patent: July 5, 2011
    Assignee: Merck Serono SA
    Inventors: Dominique Swinnen, Agnes Bombrun, Patrick Gerber, Catherine Jorand-Lebrun
  • Fluticasone propionate nasal pharmaceutical formulations and methods of using same
    Patent number: 7972626
    Abstract: Nasal pharmaceutical formulations comprising a drug substance having a specific particle size distribution profile are disclosed herein. Such profile provides increased bioavailability, increased efficacy or prolonged therapeutic effect of the drug substance when administered intranasally. The formulations of the present invention may comprise one or more corticosteroids having a specific particle size distribution profile. In a preferred embodiment, the corticosteroid is fluticasone or a pharmaceutically acceptable derivative thereof for the treatment of one or more symptoms of rhinitis. Preferably, the drug substance is fluticasone propionate. The formulations herein may be provided as an aqueous suspension suitable for inhalation via the intranasal route.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: July 5, 2011
    Assignee: Merck Patent GmbH
    Inventor: Imtiaz Chaudry
  • Cathepsin cysteine protease inhibitors
    Patent number: 7973037
    Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.
    Type: Grant
    Filed: April 8, 2008
    Date of Patent: July 5, 2011
    Assignees: Axys Pharmaceuticals, Inc., Merck Canada Inc.
    Inventors: Christopher I. Bayly, Cameron Black, Serge Leger, Chun Sing Li, Dan McKay, Christophe Mellon, Jacques Yves Gauthier, Vouy-Linh Truong, Cheuk Lau, Michel Therien, Michael J. Green, Bernard L. Hirschbein, James William Janc, James T. Palmer, Chitra Baskaran
  • Beclomethasone dipropionate monohydrate nasal pharmaceutical formulations and methods of using the same
    Patent number: 7972627
    Abstract: Nasal pharmaceutical formulations comprising a drug substance having a specific particle size distribution profile are disclosed herein. Such profile provides increased bioavailability, increased efficacy or prolonged therapeutic effect of the drug substance when administered intranasally. The formulations of the present invention may comprise one or more corticosteroids having a specific particle size distribution profile. In a preferred embodiment, the corticosteroid is beclomethasone or a pharmaceutically acceptable derivative thereof for the treatment of one or more symptoms of rhinitis. Preferably, the drug substance is beclomethasone dipropionate. The formulations herein may be provided as an aqueous suspension suitable for inhalation via the intranasal route.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: July 5, 2011
    Assignee: Merck Patent GmbH
    Inventor: Imtiaz Chaudry
  • Reducing the immunogenicity of fusion proteins
    Patent number: 7973150
    Abstract: Disclosed are compositions and methods for producing fusion proteins with reduced immunogenicity. Fusion proteins of the invention include a junction region having an amino acid change that reduces the ability of a junctional epitope to bind to MHC Class II, thereby reducing its interaction with a T-cell receptor. Methods of the invention involve analyzing, changing, or modifying one or more amino acids in the junction region of a fusion protein in order to identify a T-cell epitope and reduce its ability to interact with a T cell receptor. Compositions and methods of the invention are useful in therapy.
    Type: Grant
    Filed: September 1, 2009
    Date of Patent: July 5, 2011
    Assignee: Merck Patent GmbH
    Inventors: Stephen D. Gillies, Jeffrey Way, Anita A. Hamilton
  • Potassium channel inhibitors
    Patent number: 7973059
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: July 5, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott Wolkenberg, Mark T. Bilodeau, M. Brad Nolt
  • EDGE DELETION OF THIN-LAYER SOLAR MODULES BY ETCHING
    Publication number: 20110159636
    Abstract: The present invention relates to a fast and inexpensive method which can be carried out locally for the wet-chemical edge deletion of “solar modules” by applying etching pastes which are suitable for this purpose and, when the reaction is complete, removing the paste residues or cleaning the substrate surface in a suitable manner. An etching paste newly developed for the purpose is employed in the method.
    Type: Application
    Filed: August 5, 2009
    Publication date: June 30, 2011
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Oliver Doll, Ingo Koehler
  • INHIBITORS OF AKT ACTIVITY
    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