Search Patents
  • AMINOPYRIDINE DERIVATIVES FOR TREATING TUMORS AND INFLAMMATORY DISEASES
    Publication number: 20120115861
    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
  • HETEROARYLAMINOQUINOLINES AS TGF-BETA RECEPTOR KINASE INHIBITORS
    Publication number: 20120225875
    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
  • Pyridazinones as inhibitors of cyclooxygenase-2
    Patent number: 6004960
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: March 13, 1998
    Date of Patent: December 21, 1999
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien
  • Antagonists of gonadotropin releasing hormone
    Patent number: 5780437
    Abstract: There are disclosed compounds of formula (I) ##STR1## 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: December 5, 1996
    Date of Patent: July 14, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Narindar N. Girotra, Peter Lin, Matthew J. Wyvratt
  • NOVEL ARYLAMINO N-HETERARYL COMPOUNDS AS MEK INHIBITORS
    Publication number: 20100256149
    Abstract: The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: June 14, 2010
    Publication date: October 7, 2010
    Applicant: MERCK SERONO S.A.
    Inventors: Andreas Goutopoulos, Benny C. Askew, JR., Nhut Kiet Diep, Srinivasa Karra, Matthias Schwarz, Henry Yu
  • Aryl oximes
    Patent number: 7135471
    Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined 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: May 16, 2003
    Date of Patent: November 14, 2006
    Assignee: Merck Patent GmbH
    Inventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
  • Substituted pyrazolopyrimidines as angiotensin II antagonists
    Patent number: 5250521
    Abstract: Novel substituted pyrazolopyrimidines of formula (I) which are useful as angiotensin II antagonists, are disclosed.
    Type: Grant
    Filed: November 25, 1991
    Date of Patent: October 5, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Prasun K. Chakravarty, Malcolm MacCoss, Arthur A. Patchett, Thomas F. Walsh
  • Pyridazine derivatives as ligands for GABA receptors
    Patent number: 7381725
    Abstract: A class of pyridazine derivatives, substituted in the 4-position by an optionally substituted heteroaromatic ring, being selective ligands for GABAA receptors, in particular having high affinity for the ?2 and/or ?3 and/or ?5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: June 3, 2008
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Stephen Robert Fletcher, Angus Murray MacLeod, Monique Bodil Van Niel, Kevin Wilson
  • Inhibitors of janus kinases
    Patent number: 8431569
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: December 9, 2008
    Date of Patent: April 30, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jonathan R. Young, Jongwon Lim, Michelle R. Machacek, Brandon Mitsuo Taoka, Ryan D. Otte
  • Phenylsulphonylipiperazinyl derivatives as 5-HT receptor ligands
    Patent number: 6852718
    Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted piperazine ring are selective antagonists of the human 5-HT2A receptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of adverse conditions of the central nervous system, including schizophrenia and other psychotic disorders.
    Type: Grant
    Filed: March 30, 2001
    Date of Patent: February 8, 2005
    Assignee: Merck Sharp & Dohme Ltd
    Inventors: Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher
  • Diaryl Substituted Alkanes
    Publication number: 20120149674
    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: Application
    Filed: February 23, 2012
    Publication date: June 14, 2012
    Applicant: Merck Sharpe & Dohme Corp.
    Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
  • Imidazopyridines
    Patent number: 5389642
    Abstract: Novel imidazopyridine derivatives of the formula I ##STR1## in which R is ##STR2## and R.sup.1 to R.sup.4, X and Y are as defined herein, and their salts have antagonistic properties towards angiotensin(II) and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and increased intraocular pressure and also disorders of the central nervous system.
    Type: Grant
    Filed: December 16, 1993
    Date of Patent: February 14, 1995
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Dieter Dorsch, Werner Mederski, Mathias Osswald, Pierre Schelling, Norbert Beier, Ingeborg Lues, Klaus-Otto Minck
  • 1,5-diphenylpyrazoles II as HSP90 inhibitors
    Patent number: 7906657
    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: April 20, 2007
    Date of Patent: March 15, 2011
    Assignee: Merck Patent Gesellschaft MIT Beschraenkter Haftung
    Inventors: Hans-Michael Eggenweiler, Michael Wolf, Hans-Peter Buchstaller, Christian Sirrenberg
  • Crystalline (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl) piperazin-1-yl]methanone phosphate
    Patent number: 8188087
    Abstract: The present invention relates to novel crystalline forms of (3-cyano-1H-indol-7-yl)-[4-(4-fluorophenethyl)piperazin-1-yl]methanone phosphate and to pharmaceutical compositions containing said forms.
    Type: Grant
    Filed: April 24, 2007
    Date of Patent: May 29, 2012
    Assignee: Merck Patent GmbH
    Inventors: Susan Marie Reutzel-Eden, Gregory Alan Stephenson
  • Inhibitors of Janus kinases
    Patent number: 8278335
    Abstract: The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3, TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer.
    Type: Grant
    Filed: April 9, 2009
    Date of Patent: October 2, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michelle R. Machacek, Andrew Haidle, Anna A. Zabierek, Kaleen M. Konrad, Michael D. Altman
  • 2-amino-1,4-dihydropyridine derivatives with calcium agonist and alpha.sub.1 -antagonist activity
    Patent number: 5166148
    Abstract: There are provided novel 1,4-dihydropyridine compounds possessing both calcium agonist and alpha.sub.1 -antagonist activity useful for treating congestive heart failure, pharmaceutical compositions containing them and methods of using these compounds to treat congestive heart failure in a mammal.
    Type: Grant
    Filed: July 9, 1990
    Date of Patent: November 24, 1992
    Assignee: The Du Pont Merck Pharmaceutical Company
    Inventors: Paul E. Aldrich, Richard A. Earl, Philip Ma
  • Inhibitors of Akt activity
    Patent number: 8003643
    Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: August 23, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
  • N-substituted nonaryl-heterocyclic NMDA/NR2B antagonists
    Patent number: 7053089
    Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.
    Type: Grant
    Filed: February 20, 2002
    Date of Patent: May 30, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Christopher F. Claiborne, John W. Butcher, David A. Claremon, Brian E. Libby, Nigel J. Liverton, Peter M. Munson, Kevin T. Nguyen, Brian Phillips, Wayne Thompson, John A. McCauley
  • 1,2,4-Triazoles and a method for their preparation
    Patent number: 4256887
    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-hyperuricomic agents. Compositions useful in the treatment of gout and hyperuricomia containing a substituted triazole as the active ingredient are also provided.
    Type: Grant
    Filed: September 13, 1979
    Date of Patent: March 17, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Frederick C. Novello, John J. Baldwin
  • Process for the preparation of ring compounds
    Patent number: 7183447
    Abstract: In a process for the preparation of ring compounds via a combinatorial synthesis, the reaction procedure is based on a Suzuki coupling, subsequent halo-demetallation and finally a further Suzuki coupling. The Suzuki couplings are each carried out with a boronic acid or a boronic acid ester. The reaction procedure uses provides novel ring compounds and uses novel synthesis units used for this purpose. The novel ring compounds are suitable for use as constituents in liquid-crystalline mixtures.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: February 27, 2007
    Assignee: Merck Patent GmbH
    Inventors: Detlef Pauluth, Peer Kirsch, Peter Baeuerle, Oliver Deeg