Patents Represented by Attorney, Agent or Law Firm Melvin Winokur
  • Patent number: 6835548
    Abstract: The invention includes mouse serotonin 5-HT2c receptor isoforms having amino acid replacements at one or more positions of the natural mouse serotonin 5-HT2c receptor polypeptide sequence, specifically at one or more of positions 157, 159 and 161. The polypeptides are useful for identifying ligands which bind with the serotonin 5-HT2c receptor and modulators of the serotonin 5-HT2c, and for identifying drugs with affinity for 5-HT2 receptors which are used to treat schizophrenia, Parkinsonism, and anxiety disorders.
    Type: Grant
    Filed: December 17, 2002
    Date of Patent: December 28, 2004
    Assignee: Merck & Company, Inc.
    Inventors: Tong M. Fong, Jie Liu, Leonardus H.T. Van Der Ploeg
  • Patent number: 6828322
    Abstract: A class of substituted 1,2,4-triazolo[4,3-b]pyridazine derivatives, possessing a fluoro-substituted phenyl ring at the 3-position and a heteroaryl-methoxy moiety at the 6-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: June 17, 2003
    Date of Patent: December 7, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: William Robert Carling, Jose Luis Castro Pineiro, Ian James Collins, Alexander Richard Guiblin, Timothy Harrison, Andrew Madin, Kevin William Moore, Michael Geoffrey Russell, Gayle Scott, Leslie Joseph Street
  • Patent number: 6818658
    Abstract: Certain novel 4-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
    Type: Grant
    Filed: February 3, 2003
    Date of Patent: November 16, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Feroze Ujjainwalla, Lin Chu, Mark T. Goulet, Bonnie Louridas, Matthew J. Wyvratt, Daniel Warner
  • Patent number: 6814895
    Abstract: The present invention is concerned with a novel process for the preparation of 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-one (CAS 30071-93-3). This compound is useful as an intermediate in the synthesis of therapeutic agents.
    Type: Grant
    Filed: January 28, 2004
    Date of Patent: November 9, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Raymond Cvetovich, Tomoyuki Asai, Yoshiko Yodogawa
  • Patent number: 6794405
    Abstract: Alicyclic imidazole compounds; pharmaceutically active compositions containing such compounds; and the use of such compounds in formulations for the control or prevention of disease states in which histamine H3 receptors are involved, such as allergy, inflammation, hypotension, glaucoma, sleeping disorders, states of hyper- and hypo-motility of the gastro-intestinal tract, cardiovascular disease, hypo- and hyper-activity of the central nervous system, Alzheimer's, schizophrenia, obesity and migraines are disclosed.
    Type: Grant
    Filed: August 4, 2003
    Date of Patent: September 21, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Yajing Rong, Jack B. Jiang, Syed M. Ali
  • Patent number: 6777433
    Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes, obesity, and diabetes-related diseases.
    Type: Grant
    Filed: June 28, 2002
    Date of Patent: August 17, 2004
    Assignee: Merck Frosst Canada & Co.
    Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Robert Young
  • Patent number: 6777430
    Abstract: A class of phenylsulphonyl derivatives wherein the sulphonyl moiety is also attached to an N-arylalkyl-substituted azetidine, pyrrolidine or piperidine 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 depression.
    Type: Grant
    Filed: April 1, 2003
    Date of Patent: August 17, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Peter Blurton, Frank Burkamp, Susan Koon-Fung Cheng, Stephen Robert Fletcher, Angus Murray MacLeod, Daniel Spinks, Monique Bodil Van Niel
  • Patent number: 6777395
    Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
    Type: Grant
    Filed: January 18, 2002
    Date of Patent: August 17, 2004
    Assignees: Merck & Co., Inc., Isis Pharmaceuticals, Inc.
    Inventors: Balkrishen Bhat, Neelima Bhat, Anne B. Eldrup, Thazha P. Prakash, Marija Prhavc, Quanlai Song, Phillip Dan Cook, Steven S. Carroll, Malcolm Maccoss, David B. Olsen
  • Patent number: 6777580
    Abstract: The present invention is concerned with novel processes for the preparation of (R)-1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-ol. This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: August 17, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Paul Devine, Hansen Karl
  • Patent number: 6764842
    Abstract: The present invention relates to a novel enantioselective bioreduction using a yeast microorganism for the preparation of the chiral allylic alcohols of structural formula I (R is hydrogen or methyl) which are useful in the asymmetric synthesis of integrin &agr;v&bgr;3 receptor antagonists.
    Type: Grant
    Filed: March 27, 2002
    Date of Patent: July 20, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Michael G. Sturr, Russell Fieldon Boyd, Kodzo Gbewonyo, Joseph Nti-Gyabaah, David J. Pollard, James Christopher McWilliams, Kathleen A. Telari
  • Patent number: 6756511
    Abstract: Gamma-secretase inhibitors, useful in the treatment or prevention of Alzheimer's disease, are disclosed. The preferred compounds have, as the central portion of the molecule, the structure (a) and are di-astereoisomers of known protease inhibitors.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: June 29, 2004
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Jose Luis Castro Pineiro, Timothy Harrison, Peter Alan Hunt, Alan John Nadin
  • Patent number: 6753410
    Abstract: The present invention is directed to compounds and pharmaceutical compositions comprising the compounds which are inhibitors of the enzyme gamma secretase and which are useful in the treatment or prevention of diseases in which the beta-amyloid peptide is involved, such as Alzheimer's disease.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: June 22, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Alan John Nadin, Joseph George Neduvelil, Mohinder K. Sardana, Jules A. Shafer, Stephen J. Gardell, Ming-Tain Lai, Yueming Li, Bruce D. Dorsey, Dennis C. Dean
  • Patent number: 6730681
    Abstract: A class of substituted or 6,7-ring fused [1, 2, 3]triazolo[1,5-&agr;]-pyrimidine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and an amino moiety at the 5-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Mark Stuart Chambers, Ian James Collins, Simon Charles Goodacre, David James Hallett, Philip Jones, Linda Elizabeth Keown, Robert James Maxey, Leslie Joseph Street
  • Patent number: 6730676
    Abstract: A class of pyrazino[2,3-d]pyridazine derivatives, possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 5-position, a substituted alkoxy moiety at the 3-position, and a range of substituents at the 2-position, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 and/or &agr;5 subunit thereof, and 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: June 18, 2002
    Date of Patent: May 4, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Wesley Peter Blackaby, Richard Thomas Lewis, Leslie Joseph Street
  • Patent number: 6730690
    Abstract: Compounds having Formula I, including pharmaceutically acceptable salts, hydrates and solvates thereof: are selective inhibitors of the 11&bgr;-HSD1 enzyme. The compounds are useful for the treatment of diabetes, such as noninsulin-dependent diabetes (NIDDM), hyperglycemia, obesity, insulin resistance, dylsipidemia, hyperlipidemia, hypertension, Syndrome X, and other symptoms associated with NIDDM.
    Type: Grant
    Filed: June 9, 2003
    Date of Patent: May 4, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Steven H. Olson, James M. Balkovec, Yuping Zhu
  • Patent number: 6727249
    Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen, C1-4alkyl optionally substituted by a hydroxy, methoxy or benzyloxy group, or CO2(C1-2alkyl); Z is —CR9R10CH2— or —CH2CR9R10—; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.
    Type: Grant
    Filed: April 1, 2002
    Date of Patent: April 27, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Neil Roy Curtis, Ian Thomas Huscroft, Janusz Jozef Kulagowski, Piotr Antoni Raubo
  • Patent number: 6727244
    Abstract: This invention is concerned with mammalian metabolites of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist that is useful in the prevention and treatment of certain disorders, including emesis and psychiatric disorders such as depression and anxiety.
    Type: Grant
    Filed: April 24, 2003
    Date of Patent: April 27, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Su-er Wu Huskey, Shuet-Hing Lee Chiu
  • Patent number: 6723735
    Abstract: The present invention is directed to 3-phenylimidazol[4,5-b]pyridine derivatives, that are selective ligands for GABAA receptors. These compounds are useful in the treatment and prevention of disorders of the central nervous system, including anxiety and convulsions.
    Type: Grant
    Filed: February 25, 2002
    Date of Patent: April 20, 2004
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: David James Hallett, Michael Rowley
  • Patent number: 6713508
    Abstract: A class of benzopyrancarboxylic acid derivatives comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.
    Type: Grant
    Filed: October 29, 2001
    Date of Patent: March 30, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Soumya P. Sahoo, Hiroo Koyama, Daniel J. Miller, Julia K. Boueres, Ranjit C. Desai
  • Patent number: 6699871
    Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
    Type: Grant
    Filed: July 5, 2002
    Date of Patent: March 2, 2004
    Assignee: Merck & Co., Inc.
    Inventors: Scott D. Edmondson, Michael H. Fisher, Dooseop Kim, Malcolm Maccoss, Emma R. Parmee, Ann E. Weber, Jinyou Xu