Patents Assigned to Merck Sharp
  • CGRP RECEPTOR ANTAGONISTS
    Publication number: 20100298303
    Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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 CGRP is involved.
    Type: Application
    Filed: July 7, 2010
    Publication date: November 25, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daniel Vincent Paone, Anthony W. Shaw
  • PRODRUGS OF CGRP RECEPTOR ANTAGONISTS
    Publication number: 20100298269
    Abstract: Disclosed are prodrug compounds of formula (I) (wherein variables R1 and R2 are as described herein) which are analogues of an antagonist of CGRP receptors and which are useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.
    Type: Application
    Filed: February 4, 2009
    Publication date: November 25, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
  • 3,5-SUBSTITUTED-1,3-OXAZOLIDIN-2-ONE DERIVATIVES
    Publication number: 20100292241
    Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: January 14, 2009
    Publication date: November 18, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
  • Process for the preparation of bicyclo[3.1.0]hexanols
    Patent number: 7834222
    Abstract: A process for the preparation of a the formula (I): which process comprises the intramolecular cyclopropanation of an epoxide of me formula (II); in the presence of 0.05 to 0.75 equivalents of a secondary amine base and at least one equivalent of an alkyl lithium base, wherein R R1, R2 and R3 are each hydrogen or C1-4 alkyl or R1 and R2 are linked to form- a C3-7 cycloaUcyl or C3-7 cycloalkenyl ring.
    Type: Grant
    Filed: August 1, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Matthew Bio, Karel Marie Joseph Brands, Edward Cleator
  • Radiolabeled glycine transporter inhibitors
    Patent number: 7834031
    Abstract: The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: H. Donald Burns, Terence G. Hamill, Craig W. Lindsley
  • Angiotensin II receptor antagonists
    Patent number: 7834042
    Abstract: A compound having the structure (Formula I), wherein Y is —Y1—Y2—Y3—Y4—Y5—; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali
  • Fused-aromatic compounds having anti-diabetic activity
    Patent number: 7834036
    Abstract: Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dyslipidermia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
  • Benzothiophene derivatives
    Patent number: 7834034
    Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dawn M. Mampreian, Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Spirocyclic compounds
    Patent number: 7834026
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott C. Berk, Joshua Close, Christopher Hamblett, Richard W. Heidebrecht, Solomon D. Kattar, Laura T. Kliman, Dawn M. Mampreian, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Paul Tempest, Anna A. Zabierek
  • HCV protease substrates
    Patent number: 7834145
    Abstract: The present invention features HCV NS3 protease substrates containing a europium label and a quenching group. The europium label and quenching group are located on different sides of an ester HCV NS3 protease cleavage site. The substrate can be used in a time-resolved fluorescence (TRF) assay to measure HCV protease activity.
    Type: Grant
    Filed: March 17, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shi-Shan Mao, S. Dale Lewis
  • Aminoalkylphenols, methods of using and making the same
    Patent number: 7834062
    Abstract: The present invention relates to Mannich base antimalarial aminoalkylphenol compounds and their use against protozoa of the genus Plasmodium, particularly emerging strains of drug-resistant Plasmodia. This invention further relates to compositions containing such compounds and a process for making the compounds. This and other aspects of the invention are realized upon review of the entire specification.
    Type: Grant
    Filed: August 13, 2009
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Conrad P. Dorn, Mary Ann Powles, Thomas F. Walsh, Matthew J. Wyvratt
  • Benzylether and benzylamino beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 7829597
    Abstract: The present invention is directed to compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: September 29, 2004
    Date of Patent: November 9, 2010
    Assignee: Merck, Sharp & Dohme, Inc.
    Inventors: Philippe G. Nantermet, Hemaka Anthony Rajapakse, Harold G. Selnick
  • Process for the preparation of CGRP antagonist
    Patent number: 7829699
    Abstract: An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1?-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.
    Type: Grant
    Filed: April 6, 2007
    Date of Patent: November 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin Belyk, Nelo Rivera
  • Quinoline potassium channel inhibitors
    Patent number: 7825131
    Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: September 17, 2004
    Date of Patent: November 2, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman
  • Heteroaryl piperidine glycine transporter inhibitors
    Patent number: 7825135
    Abstract: The present invention is directed to pyridyl, pyridazinyl, pyrimidinyl and pyrazinyl piperidine compounds that inhibit the glycine transporter GlyT1 and which are useful in the treatment of neurological and psychiatric disorders associated with glycinergic or glutamatergic neurotransmission dysfunction and diseases in which the glycine transporter GlyT1 is involved.
    Type: Grant
    Filed: March 23, 2005
    Date of Patent: November 2, 2010
    Assignees: Merck Sharp & Dohme Limited, Merck Sharp & Dohme Corp.
    Inventors: Wesley Blackaby, Mark E. Duggan, David Hallett, George D. Hartman, Andrew S. Jennings, William H. Leister, Richard T. Lewis, Craig W. Lindsley, Elizabeth Naylor, Leslie J. Street, Yi Wang, David D. Wisnoski, Scott E. Wolkenberg, Zhijian Zhao
  • Aminomethyl beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 7820674
    Abstract: The present invention is directed to aminomethyl compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: October 26, 2010
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer
  • Tyrosine Kinase Inhibitors
    Publication number: 20100267707
    Abstract: The present invention relates to 4-indol-3-yl-N-phenylpyrimidin-2-amine derivatives, that are useful for treating cellular proliferative diseases, for treating disorders associated with MET activity, and for inhibiting the receptor tyrosine kinase MET. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: June 18, 2007
    Publication date: October 21, 2010
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Ekaterina S. Kozina, Tony Siu
  • 1-hydroxycycloalkanecarboxamide derivatives
    Patent number: 7816380
    Abstract: ?-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C1-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
    Type: Grant
    Filed: May 30, 2006
    Date of Patent: October 19, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Michael R. Wood
  • Cyclic ketal beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 7816378
    Abstract: The present invention is directed to cyclic ketal compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Grant
    Filed: July 28, 2006
    Date of Patent: October 19, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Philippe G. Nantermet, Joseph P. Vacca
  • Substituted amides
    Patent number: 7816534
    Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
    Type: Grant
    Filed: April 16, 2009
    Date of Patent: October 19, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: William K. Hagmann, Linus S. Lin, Shrenik K. Shah, Ravindra N. Guthikonda, Hongbo Qi, Linda L. Chang, Ping Liu, Helen M. Armstrong, James P. Jewell, Thomas J. Lanza, Jr.