Patents Assigned to Merck Sharp
  • Patent number: 8148349
    Abstract: The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I).
    Type: Grant
    Filed: December 14, 2007
    Date of Patent: April 3, 2012
    Assignees: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.P.A., Merck Sharp & Dohme Corp.
    Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
  • Patent number: 8148390
    Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c 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: Grant
    Filed: March 7, 2008
    Date of Patent: April 3, 2012
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Craig A. Stump, Ian M. Bell, Harold G. Selnick
  • Patent number: 8148535
    Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: April 3, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Scott Wolkenberg, M. Brad Nolt, Peter Manley, Nathan R. Kett, Mark T. Bilodeau
  • Publication number: 20120077964
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Application
    Filed: September 27, 2011
    Publication date: March 29, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Carl P. Sparrow, Ayesha Sitlani, Shilpa Pandit, Jon H. Condra, Holly A. Hammond
  • Publication number: 20120076799
    Abstract: Antagonists of human proprotein convertase subtilisin-kexin type 9 (“PCSK9”) are disclosed. The disclosed antagonists are effective in the inhibition of PCSK9 function and, accordingly, present desirable antagonists for the use in the treatment of conditions associated with PCSK9 activity. The present invention also discloses nucleic acid encoding said antagonists, vectors, host cells, and compositions comprising the antagonists. Methods of making PCSK9-specific antagonists as well as methods of using the antagonists for inhibiting or antagonizing PCSK9 function are also disclosed and form important additional aspects of the present disclosure.
    Type: Application
    Filed: September 23, 2011
    Publication date: March 29, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Carl P. Sparrow, Ayesha Sitlani, Shilpa Pandit, Jon H. Condra, Holly A. Hammond
  • Patent number: 8142794
    Abstract: The present invention features Ad6 vectors and a nucleic acid encoding a Met-NS3-NS4A-NS4B-NS5A-NS5B polypeptide containing an inactive NS5B RNA-dependent RNA polymerase region. The nucleic acid is particularly useful as a component of an adenovector or DNA plasmid vaccine providing a broad range of antigens for generating an HCV specific cell mediated immune (CMI) response against HCV.
    Type: Grant
    Filed: March 3, 2009
    Date of Patent: March 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Emilio A. Emini, David C. Kaslow, Andrew J. Bett, John W. Shiver, Alfredo Nicosia, Armin Lahm, Alessandra Luzzago, Riccardo Cortese, Stefano Colloca
  • Patent number: 8143405
    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 19, 2007
    Date of Patent: March 27, 2012
    Assignee: Merck, Sharp & Dohme Corp
    Inventor: Shaun R. Stauffer
  • Patent number: 8143289
    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: November 12, 2009
    Date of Patent: March 27, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ping Chen, Jason M. Cox, Ann E. Weber
  • Patent number: 8143266
    Abstract: Compounds of formula I: (wherein variables A1, A2, B, m, n, J, X, R4, G1, G2, G3 and Y are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the 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: Grant
    Filed: April 11, 2008
    Date of Patent: March 27, 2012
    Assignee: Merck, Sharp & Dohme Corp
    Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump
  • Patent number: 8138164
    Abstract: The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: March 20, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, Vincenzo Summa, Joseph P. Vacca
  • Patent number: 8138197
    Abstract: The invention relates to a compound of a general formula (I): wherein Ar1 represents a group formed from an aromatic ring selected from a group consisting of benzene, pyrazole, isoxazole, pyridine, indole, 1H-indazole, 1H-furo[2,3-c]pyrazole, 1H-thieno[2,3-c]pyrazole, benzimidazole, 1,2-benzisoxazole, imidazo[1,2-a]pyridine, imidazo[1,5-a]pyridine and 1H-pyrazolo[3,4-a]pyridine, having Ar2, and optionally having one or two or more substituents selected from R3; R1 and R2 each independently represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, an aralkyloxycarbonyl group, a carbamoyl-C1-C6 alkoxy group, a carboxy-C2-C6 alkenyl group, or a group of -Q1-N(Ra)-Q2-Rb; or a C1-C6 alkyl group optionally having a substituent; or an aryl or heterocyclic group optionally having a substituent; or a C1-C6 alkyl group or a C2-C6 alkenyl group having the aryl or heterocyclic group; T and U each independently represent a n
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: March 20, 2012
    Assignees: MSD K.K., Merck Sharp & Dohme Corp.
    Inventors: Tomoharu Iino, Hideki Jona, Hideki Kurihara, Masayuki Nakamura, Kenji Niiyama, Jun Shibata, Tadashi Shimamura, Hitomi Watanabe, Takeru Yamakawa, Lihu Yang
  • Patent number: 8138219
    Abstract: Novel compounds of the structural formula (I) are antagonists of the 5-HT6 receptor and are useful in the treatment, prevention and suppression of diseases mediated by the 5-HT6 receptor. The compounds of the present invention are useful in the treatment of obesity, diabetes, metabolic disorder, cognitive disorders, age related cognitive disorder, depression, mania, bipolar disorders, schizophrenia, anxiety, generalized anxiety disorder, panic disorder, and obsessive compulsive disorder, epilepsy, convulsions, migraine, substance withdrawal from substances including but not limited to opiates, nicotine, tobacco products, alcohol, benzodiazepines, sedatives, and the like, sleep disorders, attention deficit/hyperactivity disorder, and Alzheimer's disease.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: March 20, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Alexander Pasternak, Michael J. Szymonifka
  • Patent number: 8133885
    Abstract: The present invention relates to compounds having general Formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to pharmaceutical compositions comprising said compounds and the use of these derivatives to modulate glucocorticoid receptor activity.
    Type: Grant
    Filed: February 14, 2006
    Date of Patent: March 13, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ralf Plate, Guido Jenny Rudolf Zaman, Pedro Harold Han Hermkens, Christiaan Gerardus Johannes Maria Jans, Rogier Christian Buijsman, Adrianus Petrus Antonius De Man, Paolo Giovanni Martino Conti, Scott James Lusher, Willem Hendrik Abraham Dokter
  • Patent number: 8133891
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B1, B2, B3, B4, D1, D2, J, K, T, U, V, W, X, Y, Z, R4, R5a, R5b, R5c, m and n are 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: Grant
    Filed: March 5, 2010
    Date of Patent: March 13, 2012
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Craig A. Stump, Cory R. Theberge, Joseph P. Vacca, C. Blair Zartman, Xufang Zhang
  • Patent number: 8128930
    Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLs, and tau phosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ? 1-42.
    Type: Grant
    Filed: July 1, 2010
    Date of Patent: March 6, 2012
    Assignees: Northwestern University, Merck Sharp & Dohme Corp.
    Inventors: Paul Acton, Zhiqiang An, Andrew J. Bett, Robert Breese, Lei Chang, Elizabeth Chen Dodson, Gene Kinney, William L. Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kristen Viola
  • Patent number: 8129413
    Abstract: The present invention relates to a process for producing N-{(1S)-1-[2-(1-{[(3S,4R)-1-tert-butyl-4-(2,4-difluorophenyl)pyrrolidin-3-yl]carbonyl}piperidin-4-yl)-5-chlorophenyl]ethyl}acetamide, and novel crystalline salts, hydrates, solvates, and polymorphic forms thereof.
    Type: Grant
    Filed: June 23, 2006
    Date of Patent: March 6, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ralph Calabria, Yu Cheng, Russell R. Ferlita, Ashkan Kamali, Jerry A. Murry, David Mathre, Andrey V. Peresypkin, Karen Thompson, Jian Wang, Robert M. Wenslow
  • Publication number: 20120053181
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: April 28, 2010
    Publication date: March 1, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Peter Lin, Lehua Chang, Scott D. Edmondson
  • Patent number: 8124108
    Abstract: The present invention features polypeptides comprising an amino acid sequence structurally related to SEQ ID NO: 1 and uses of such polypeptides. SEQ ID NO: 1 is a truncated derivative of a full-length S. epidermidis polypeptide. The full-length naturally occurring polypeptide is referred to herein as full-length ORF1319e. A His-tagged derivative of SEQ ID NO: 1 was found to produce a protective immune response against S. epidermidis.
    Type: Grant
    Filed: January 18, 2008
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Annaliesa S. Anderson, Tessie McNeely, James C. Cook, III, William L. McClements, Donna L. Montgomery
  • Patent number: 8124628
    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: Grant
    Filed: April 6, 2007
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Lin Chu, Bing Li, Anthony K. Ogawa, Hyun O. Ok, Debra L. Ondeyka, Minal Patel, Rosemary Sisco, Feroze Ujjainwalla, Jinyou Xu
  • Patent number: 8124633
    Abstract: The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety.
    Type: Grant
    Filed: April 7, 2008
    Date of Patent: February 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Robert J. DeVita, Sander G. Mills, Jinlong Jiang, Andrew J. Kassick, Jianming Bao