Patents Assigned to Merck Sharp
  • Publication number: 20120016011
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of CTGF gene expression and/or activity, and/or modulate a CTGF gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against CTGF gene expression.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 19, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Victoria Pickering, Jyoti Shah, Walter Strapps
  • Publication number: 20120016010
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of Bach1 gene expression and/or activity, and/or modulate a Bach1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against Bach1 gene expression.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 19, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Victoria Pickering, Jyoti K. Shah, Walter Strapps
  • Publication number: 20120010272
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of ASK1 gene expression and/or activity, and/or modulate a ASK1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against ASK1 gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 12, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • Publication number: 20120010193
    Abstract: Compounds of Formula (I) (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: March 8, 2010
    Publication date: January 12, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20120009580
    Abstract: In one aspect, the present invention provides methods for amplifying a microRNA molecule to produce DNA molecules. The methods each include the steps of: (a) using primer extension to make a DNA molecule that is complementary to a target microRNA molecule; and (b) using a universal forward primer and a reverse primer to amplify the DNA molecule to produce amplified DNA molecules. In some embodiments of the method, at least one of the forward primer and the reverse primer comprise at least one locked nucleic acid molecule.
    Type: Application
    Filed: September 22, 2011
    Publication date: January 12, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Christopher K. Raymond
  • Patent number: 8093389
    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 indole, 1H-indazole, 2H-indazole, 1H-thieno[2,3-c]pyrazole, 1H-pyrazolo[3,4-b]pyridine, benzo[b]furan, benzimidazole, benzoxazole, 1,2-benzisoxazole and imidazo[1,2-a]pyridine; R1 and R2 each represent a hydrogen atom, a halogen atom, a cyano group, a C2-C6 alkenyl group, a C1-C6 alkoxy group, a halo-C1-C6 alkoxy group, a cyclo-C3-C6 alkyloxy group, a C2-C7 alkanoyl group, a halo-C2-C7 alkanoyl group, a C2-C7 alkoxycarbonyl group, a halo-C2-C7 alkoxycarbonyl group, a cyclo-C3-C6 alkyloxycarbonyl 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; an optionally-substituted C1-C6 alkyl, aryl or heterocyclic group; or a C1-C6 alkyl or C2-C6 alkenyl group having the aryl or heterocyclic group; R3 and R4 each represent a hydrogen atom, a halogen atom, a nitro group, a cyclo-C3-C
    Type: Grant
    Filed: January 8, 2008
    Date of Patent: January 10, 2012
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Tomoharu Iino, Hideki Jona, Jun Shibata, Tadashi Shimamura, Takeru Yamakawa, Lihu Yang
  • Patent number: 8093295
    Abstract: The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.
    Type: Grant
    Filed: May 16, 2006
    Date of Patent: January 10, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeannie Chow Wong, Benjamin Max Cohen, Aaron S. Cote, Erik A. Dienemann, Kimberly Gallagher, Craig Ikeda, Justin Moser, Pavol Rajniak, Robert A. Reed, Brian Sell, Cindy Starbuck, Hsien-Hsin Tung, Qingxi Wang, Vincent R. Capodanno
  • Publication number: 20120004281
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of NGF? gene expression and/or activity, and/or modulate a NGF? gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against NGF? gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 5, 2012
    Applicant: Merck Sharp & Dohme Corp
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • Publication number: 20120004280
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of FC?R1? gene expression and/or or activity, and/or modulate a FC?R1? gene expression pathway. Specifically, the invention relates to doublestranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against FC?R1? gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 5, 2012
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vasant Jadhav, Victoria Pickering, Walter Strapps
  • Publication number: 20120004282
    Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of ICAM-1 gene expression and/or activity, and/or modulate a ICAM-1 gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against ICAM-1 gene expression.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 5, 2012
    Applicant: Merck Sharp & Dohme Corp,
    Inventors: Victoria Pickering, Jyoti K. Shah, Walter Strapps
  • Patent number: 8080544
    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: Grant
    Filed: February 4, 2009
    Date of Patent: December 20, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
  • Patent number: 8080654
    Abstract: The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections.
    Type: Grant
    Filed: May 20, 2011
    Date of Patent: December 20, 2011
    Assignees: Insituto di Ricerche di Biologia Molecolare P. Angeletti SpA, Merck Sharp & Dohme Corp.
    Inventors: Steven Harper, Vincenzo Summa, Nigel J. Liverton, John A. McCauley
  • Patent number: 8080543
    Abstract: The present invention relates to pyridine substituted ethanol compounds and derivatives thereof having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
    Type: Grant
    Filed: January 29, 2007
    Date of Patent: December 20, 2011
    Assignee: Merck Sharp & Dohme
    Inventors: B. Wesley Trotter, Kausik K. Nanda, Nathan R. Kett
  • Patent number: 8076455
    Abstract: The present inventors conducted a similarity search of the amino acid sequence of known G protein-coupled receptor proteins in GenBank, and obtained a novel human GPCR gene “BG37”, cDNA containing the ORF of the gene was cloned and its nucleotide sequence was determined. Moreover, novel GPCR “BG37” genes from mouse and rat were isolated. Use of the novel GPCR of the present invention enables screening of ligands, compounds inhibiting the binding to a ligand, and candidate compounds of pharmaceuticals which can regulate signal transduction from the “BG37” receptor.
    Type: Grant
    Filed: March 3, 2010
    Date of Patent: December 13, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Takaharu Maruyama, Takao Nakamura, Hiraku Itadani, Ken-ichi Tanaka
  • Patent number: 8076472
    Abstract: The present invention relates to compounds, compositions, and methods useful for modulating the expression of genes associated with respiratory and pulmonary disease, such as cholinergic muscarinic receptor genes, using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of cholinergic muscarinic receptor genes, or other genes involved in pathways of cholinergic muscarinic receptor gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of M3 muscarinic acetylcholine receptor or cholinergic receptor muscarinic 3 (CHRM3).
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: December 13, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James McSwiggen, Leonid Beigelman
  • Publication number: 20110301048
    Abstract: The present invention relates to genetic markers whose expression is correlated with breast cancer. Specifically, the invention provides sets of markers whose expression patterns can be used to differentiate clinical conditions associated with breast cancer, such as the presence or absence of the estrogen receptor ESR1, and BRCA1 and sporadic tumors, and to provide information on the likelihood of tumor distant metastases within five years of initial diagnosis. The invention relates to methods of using these markers to distinguish these conditions. The invention also relates to kits containing ready-to-use microarrays and computer software for data analysis using the statistical methods disclosed herein.
    Type: Application
    Filed: November 23, 2010
    Publication date: December 8, 2011
    Applicants: MERCK SHARP & DOHME CORP., THE NETHERLANDS CANCER INSTITUTE
    Inventors: HongYue Dai, Yudong He, Peter S. Linsley, Mao Mao, Christopher J. Roberts, Laura Johanna Van't Veer, Marc J. Van de Vijver, Rene Bernards, A.A. M. Hart
  • Patent number: 8071770
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 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: November 14, 2006
    Date of Patent: December 6, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Michael R. Wood, C. Blair Zartman
  • Patent number: 8071771
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 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: November 14, 2006
    Date of Patent: December 6, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump, Cory R. Theberge, C. Blair Zartman
  • Patent number: 8071568
    Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates 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 aryl phosphoramidates of the present invention.
    Type: Grant
    Filed: December 28, 2007
    Date of Patent: December 6, 2011
    Assignees: Merck Sharp & Dohme Corp., Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.
    Inventors: Frank Narjes, Cristina Gardelli, Monica Donghi, Barbara Attenni, Philippe L. Durette
  • Patent number: 8071306
    Abstract: In one aspect, the present invention provides methods for amplifying a microRNA molecule to produce DNA molecules. The methods each include the steps of: (a) using primer extension to make a DNA molecule that is complementary to a target microRNA molecule; and (b) using a universal forward primer and a reverse primer to amplify the DNA molecule to produce amplified DNA molecules. In some embodiments of the method, at least one of the forward primer and the reverse primer comprise at least one locked nucleic acid molecule.
    Type: Grant
    Filed: July 18, 2007
    Date of Patent: December 6, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Christopher K. Raymond