Patents Assigned to Merck Sharp & Dohme
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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.
  • 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
  • 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
  • Covalently stabilized chimeric coiled-coil HIV gp41 N-peptides with improved antiviral activity
    Patent number: 7811577
    Abstract: Methods of covalently-stabilizing alpha-helical, chimeric peptides constrained within a homotrimeric or heterotrimeric coiled-coil structure are disclosed. The coiled-coil structures made by the methods disclosed within this specification mimic all or a portion of the internal, trimeric coiled-coil motif contained within the fusogenic conformation of an enveloped virus membrane-fusion protein, particularly the internal coiled-coil domain of the HIV gp41 ectodomain. The HIV-derived, chimeric peptides disclosed comprise a non-HIV, soluble, trimeric form of a coiled-coil fused in helical phase to all or a portion of the N-helix of HIV gp41 and are covalently-stabilized in a homotrimeric or heterotrimeric coiled-coil structure through the formation of disulfide or chemoselective bonds between said peptides.
    Type: Grant
    Filed: May 27, 2005
    Date of Patent: October 12, 2010
    Assignees: Merck Sharp & Dohme Corp., Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Elisabetta Bianchi, Antonello Pessi, Romas Geleziunas, David Bramhill
  • Substitued [1,2,4]triazolo[1,5-a]pyrazines as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7812027
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme 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: May 11, 2007
    Date of Patent: October 12, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Ann E. Weber
  • HIV reverse transcriptase inhibitors
    Patent number: 7807684
    Abstract: Compounds having the structure: are HIV reverse transcriptase inhibitors, wherein A, X, Y, Z, R1 and R2 are defined herein. The compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: July 17, 2006
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Sandeep A. Saggar, John T. Sisko, Thomas J. Tucker, Robert M. Tynebor, Dai-Shi Su, Neville J. Anthony
  • Method to confer cell culture replication activity to different Hepatitis C virus isolates
    Patent number: 7807455
    Abstract: The present invention features methods for producing HCV replicons using HCV encoding sequences from different isolates. The featured methods are based on the discovered importance of NS3 amino acid position 470 in conferring cell culture replication activity to different HCV isolates.
    Type: Grant
    Filed: February 9, 2004
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jay Grobler, Osvaldo Flores, Eric J. Markel
  • Process for {3-[2()-[(1)-1-[3,5-bis(trifluoromethyl) phenyl]ethoxy]-3()-(4-fluorophenyl)morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid
    Patent number: 7807829
    Abstract: The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(tri-fluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: October 5, 2010
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.
    Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
  • Antibiotic compound
    Patent number: 7807445
    Abstract: Fermentation of a nutrient medium with a eubacterium Streptomyces sp. yields a novel antibacterial compound of structural formula (I).
    Type: Grant
    Filed: May 20, 2005
    Date of Patent: October 5, 2010
    Assignees: Merck Sharp and Dohme de Espana, S.A., Merck Sharp & Dohme Corp.
    Inventors: Angela Basilio, Olga Genilloud, Hiranthi Jayasuriya, Ignacio Gonzalez, Sheo B. Singh, Oscar Salazar, Jun Wang
  • Compositions and methods for exon profiling
    Patent number: 7807447
    Abstract: The present invention provides methods for analyzing exon expression profiles of a cell or type of cell. In the invention, the expression levels of a plurality of individual exons or multiexons for each of a plurality of genes in the genome of an organism are measured and analyzed to determine the biological state, such as the exon expression state or transcriptional state, of the cell or type of cell. The methods of the invention are useful for determination of alternative RNA splicing in a plurality of genes. The invention also provides nucleic acid probe arrays for determining in parallel the expression levels of a plurality of exons or multiexons for each of a plurality of genes in the genome of an organism. The invention further provides methods for determining the effects of perturbations, such as perturbations by drugs, on exon expression and alternative RNA splicing pathways.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Daniel D. Shoemaker, Stewart Scherer, Stephen H. Friend
  • Antidiabetic oxazolidinediones and thiazolidinediones
    Patent number: 7807692
    Abstract: Phenoxyphenyl and phenoxybenzyl oxazolidine-2,4-diones and thiazolidine-2,4-diones are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Grant
    Filed: June 30, 2006
    Date of Patent: October 5, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James F. Dropinski, Peter T. Meinke, Guo Q. Shi, Yong Zhang
  • CETP INHIBITORS
    Publication number: 20100249024
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula 1, A1 and A2 are each an aromatic ring, a 5-6-membered heterocyclic ring, an aromatic ring fused to a heterocyclic ring, a phenyl ring fused to a heterocyclic ring, or a cycloalkyl ring.
    Type: Application
    Filed: June 14, 2010
    Publication date: September 30, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Joann Bohn, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi
  • Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
    Patent number: 7803951
    Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
    Type: Grant
    Filed: March 24, 2006
    Date of Patent: September 28, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Rui Liang, Emma R. Parmee