Patents Assigned to Merck & Co., Inc.
  • 3-fluoro-piperidines as NMDA/NR2B antagonists
    Patent number: 7592360
    Abstract: Compounds represented by Formula (I) or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for treating conditions such as, for example, Parkinson's disease, Alzheimer's disease, migraine, epilepsy and pain.
    Type: Grant
    Filed: May 28, 2004
    Date of Patent: September 22, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Nigel J. Liverton, Christopher F. Claiborne, David A. Claremon, John A. McCauley
  • Fused Aminopiperidines as Dipeptidyl Peptidase-4 Inhibitors for the Treatment or Prevention of Diabetes
    Publication number: 20090233936
    Abstract: The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 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-4 enzyme is involved.
    Type: Application
    Filed: December 8, 2006
    Publication date: September 17, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Jason M. Cox, Scott D. Edmondson, Anthony Mastracchio
  • Biaryl substituted pyrazoles as sodium channel blockers
    Patent number: 7589116
    Abstract: Biaryl substituted pyrazole compounds are sodium channel blockers useful for the treatment of pain and other conditions. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treatment of conditions, including acute pain, chronic pain, visceral pain, inflammatory pain, and neuropathic pain, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more therapeutically active compounds.
    Type: Grant
    Filed: March 30, 2004
    Date of Patent: September 15, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Prasun K. Chakravarty, Michael H. Fisher, Jeffrey M. Fisher, legal representative, William H. Parsons, Sriram Tyagarajan, Bishan Zhou
  • Inhibitors of Akt activity
    Patent number: 7589068
    Abstract: The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: February 10, 2006
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Nicholas D. P. Cosford, Mark E. Layton, Jun Liang, Craig W. Lindsley, Philip E. Sanderson, Zhijian Zhao
  • Aminoalkylphenols, methods of using and making the same
    Patent number: 7589127
    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: June 20, 2003
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Mary Ann Powles, Thomas F. Walsh, Matthew J. Wyvratt
  • Tetrahydropyran heterocyclic cyclopentyl heteroaryl modulators of chemokine receptor activity
    Patent number: 7589085
    Abstract: The present invention is further directed to compounds of the formulas: (I) (II) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24 and R25 are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.
    Type: Grant
    Filed: August 6, 2004
    Date of Patent: September 15, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Gabor Butora, Lihu Yang, Stephen D. Goble
  • Cyclopropyl group substituted oxazolidinone antibiotics and derivatives thereof
    Patent number: 7582659
    Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: January 22, 2007
    Date of Patent: September 1, 2009
    Assignees: Merck & Co., Inc., Kyorin Pharmaceutical Co., Ltd.
    Inventor: Yasumichi Fukuda
  • Process for making N-sulfonated-amino acid derivatives
    Patent number: 7579487
    Abstract: This invention relates to a process for preparing optically active ?-amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.
    Type: Grant
    Filed: May 6, 2005
    Date of Patent: August 25, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Spencer D. Dreher, Norihiro Ikemoto, C. Scott Shultz, J. Michael Williams
  • Inhibitors of Akt activity
    Patent number: 7579355
    Abstract: The present invention is directed to compounds which contain a substituted pyridine moeity 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: April 20, 2004
    Date of Patent: August 25, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Mark T. Bilodeau, Mark E. Duggan, John C. Hartnett, Craig W. Lindsley, Zhicai Wu, Zhijian Zhao
  • Ophthalmic compositions for treating ocular hypertension
    Patent number: 7576122
    Abstract: This invention relates to potent potassium channel blocker compounds of Formula I or a formulation thereof for the treatment of glaucoma and other conditions which leads to elevated intraoccular pressure in the eye of a patient. This invention also relates to the use of such compounds to provide a neuroprotective effect to the eye of mammalian species, particularly humans.
    Type: Grant
    Filed: August 27, 2004
    Date of Patent: August 18, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Dong-Ming Shen, James B. Doherty
  • Inhibitors of Akt activity
    Patent number: 7576209
    Abstract: The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
    Type: Grant
    Filed: December 4, 2007
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Kelly, III, Mark E. Layton, Philip E. Sanderson
  • Asymmetric hydrogenation process
    Patent number: 7576118
    Abstract: The present invention provides an asymmetric hydrogenation process for the preparation of chiral cycloalkanoindole DP receptor antagonists in high enantiomeric excess.
    Type: Grant
    Filed: April 1, 2005
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: David M. Tellers, Guy R. Humphrey
  • Morpholinyl piperidine glycine transporter inhibitors
    Patent number: 7576083
    Abstract: The present invention is directed to morpholinyl 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: April 29, 2005
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Craig W. Lindsley, Scott E. Wolkenberg, Zhijian Zhao
  • Substituted amides
    Patent number: 7576239
    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: January 14, 2008
    Date of Patent: August 18, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Linus S. Lin, William K. Hagmann, Sanjeev Kumar, Wenji Yin, George Doss
  • Substituted pyrazoles, compositions containing such compounds and methods of use
    Patent number: 7572922
    Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
    Type: Grant
    Filed: January 23, 2004
    Date of Patent: August 11, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
  • Biaryl substituted triazoles as sodium channel blockers
    Patent number: 7572822
    Abstract: Biaryl substituted triazole compounds represented by Formula I, II or III, or pharmaceutically acceptable salts thereof, and a process for making such compounds and salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: August 11, 2009
    Assignee: Merck & Co. Inc.
    Inventors: Prasun K. Chakravarty, Louis L. Zuegner, III, legal representative, William H. Parsons, Brenda Palucki, Bishan Zhou, Min K. Park, Michael H. Fisher
  • Substituted imidazoles as cannabinoid receptor modulators
    Patent number: 7572785
    Abstract: The use of compounds of the present invention as antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor particularly in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB1) receptor. The invention is concerned with the use of these novel compounds to selectively antagonize the Cannabinoid-1 (CB1) receptor. As such, compounds of the present invention are useful as psychotropic 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, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, particularly to opiates, alcohol, and nicotine.
    Type: Grant
    Filed: November 3, 2005
    Date of Patent: August 11, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Paul E. Finke, Sander G. Mills, Christopher W. Plummer, Shrenik K. Shah, Quang T. Truong
  • Azetidine glycine transporter inhibitors
    Patent number: 7572792
    Abstract: The present invention is directed to azetidine 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: April 25, 2005
    Date of Patent: August 11, 2009
    Assignees: Merck & Co., Inc., Merck Sharp & Dohme Limited
    Inventors: Craig W Lindsley, David Hallett, Scott E. Wolkenberg
  • Method for Assessing Airborn Microorganisms
    Publication number: 20090197299
    Abstract: The present invention relates to an environmental sampling method for assessing airborne microorganisms. The method comprises retaining organisms suspended in air to a polymeric pad via gravitational settling or forced impact, dissolving the polymeric pad in a buffered salt solution, and determining the number and kind of microorganisms in the buffered salt solution. Neither the polymeric pad nor the buffered salt solution inhibits the growth of the microorganisms to be determined.
    Type: Application
    Filed: November 29, 2006
    Publication date: August 6, 2009
    Applicant: MERCK & CO., INC.
    Inventors: Diego Vargas, Luis A. Baez
  • HCV RNA-dependent RNA polymerase
    Patent number: 7569374
    Abstract: The present invention features NS5B polypeptides from different clinically important HCV genotypes. The polypeptides can be used individually, or as part of a panel of RNA-dependent RNA polymerases, to evaluate the effectiveness of a compound to inhibit NS5B activity.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: August 4, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Donald J. Graham, Amy L. Simcoe, Steven W. Ludmerer, Osvaldo A. Flores, Robert L. LaFemina