Search Patents
  • 1,5-diphenylpyrazoles
    Patent number: 7932401
    Abstract: Novel 1,5 diphenylpyrazole derivatives of the formula (I), in which R1-R6 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 14, 2005
    Date of Patent: April 26, 2011
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Oxadiazole diaryl compounds
    Patent number: 8889668
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: December 12, 2012
    Date of Patent: November 18, 2014
    Assignee: Merck Serono SA
    Inventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
  • Fibrinogen receptor antagonists
    Patent number: 5358956
    Abstract: Novel fibrinogen receptor antagonists of the formula: ##STR1## are provided in which the claimed compounds exhibit fibrinogen receptor antagonist activity, inhibit platelet aggregation and are therefore useful in modulating thrombus formation.
    Type: Grant
    Filed: October 14, 1992
    Date of Patent: October 25, 1994
    Assignee: Merck & Co., Inc.
    Inventors: George D. Hartman, Wasyl Halczenko
  • Thiazole Derivatives and Use Thereof
    Publication number: 20110086843
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: November 23, 2010
    Publication date: April 14, 2011
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Use of sigma receptor antagonists for treatment of cocaine abuse
    Patent number: 5180729
    Abstract: The invention relates to a method of treating cocaine abuse or addiction in a mammal which comprises administering to the mammal an effective amount of a sigma receptor antagonist lacking or having relatively weak dopamine receptor-blocking activity, to reduce the pharmacological effects of the cocaine.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: January 19, 1993
    Assignee: Du Pont Merck Pharmaceutical Company
    Inventor: Leonard Cook
  • Substituted thiophene-2-sulfonamide antiglaucoma agents
    Patent number: 4721794
    Abstract: Thiophene-2-sulfonamides with a 5-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: January 26, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Shepard, Samuel L. Graham
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5965578
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: March 25, 1997
    Date of Patent: October 12, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Samuel L. Graham, Theresa M. Williams, John S. Wai
  • Prolylcarboxypeptidase inhibitors
    Patent number: 8569299
    Abstract: Compounds of structural formulas I-1 and I-2 are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: October 29, 2013
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Thomas H. Graham, Wensheng Liu, Iyassu K. Sebhat, Dong-Ming Shen, Zhi-Cai Shi
  • (Amidomethyl)nitrogen heterocyclic analgesics
    Patent number: 5254569
    Abstract: This invention relates to (amidomethyl)nitrogen heterocyclic and pyrrolidine compounds, pharmaceutical compositions containing them, methods of using such compounds and processes for making such compounds.
    Type: Grant
    Filed: January 14, 1991
    Date of Patent: October 19, 1993
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Robert S. Cheeseman, Hollis S. Kezar, III, Richard M. Scribner
  • Oxadiazole diaryl compounds
    Patent number: 8404676
    Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.
    Type: Grant
    Filed: October 1, 2008
    Date of Patent: March 26, 2013
    Assignee: Merck Serono SA
    Inventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
  • Tertiary aminohydroxypropoxy substituted thiadiazoles, pharmaceutical compositions and use
    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
  • Heterarylpiperidine modulators of chemokine receptor activity
    Patent number: 7491737
    Abstract: The present invention is directed to compounds of the formula (I): (wherein R1, R2, R3, R4, R5, R6, R10 and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
    Type: Grant
    Filed: October 24, 2003
    Date of Patent: February 17, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Stephen D. Goble, Alexander Pasternak, Lihu Yang
  • SUBSTITUTED PIPERIDINYL COMPOUNDS USEFUL AS GPR119 AGONISTS
    Publication number: 20140296202
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Application
    Filed: October 18, 2012
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5891889
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: April 1, 1997
    Date of Patent: April 6, 1999
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Robert P. Gomez, John S. Wai, Mark W. Embrey, Thorsten E. Fisher
  • Thiazole Derivatives and Use Thereof
    Publication number: 20110071113
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: November 23, 2010
    Publication date: March 24, 2011
    Applicant: MERCK SERONO SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jérôme Dorbais, Thomas Rueckle
  • Carbonyl compounds
    Patent number: 7906516
    Abstract: Novel compounds of the formula (I), in which D, E, G, W, X, Y, T, R1 and R2 are as defined in Patent Claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic diseases and for the treatment of tumours.
    Type: Grant
    Filed: March 8, 2004
    Date of Patent: March 15, 2011
    Assignee: Merck Patent GmbH
    Inventors: Christos Tsaklakidis, Dieter Dorsch, Werner Mederski, Bertram Cezanne, Johannes Gleitz
  • Pyrrolidine derived ?3 adrenergic receptor agonists
    Patent number: 8933102
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).
    Type: Grant
    Filed: October 24, 2011
    Date of Patent: January 13, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
  • THIAZOLE DERIVATIVES AND USE THEREOF
    Publication number: 20140228365
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Application
    Filed: February 7, 2014
    Publication date: August 14, 2014
    Applicant: Merck Serono S.A.
    Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
  • Thiazole derivatives and use thereof
    Patent number: 8399497
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: November 23, 2010
    Date of Patent: March 19, 2013
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Inhibitors of farnesyl-protein transferase
    Patent number: 5817678
    Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: November 15, 1996
    Date of Patent: October 6, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Byeong M. Kim, Anthony W. Shaw, Samuel L. Graham, S. Jane deSolms, Terrence M. Ciccarone