Patents Assigned to Merck Sharp and Dohme
  • N-substituted oxindoline derivatives as calcium channel blockers
    Patent number: 8273749
    Abstract: A series of N-substituted oxindole derivatives represented by Formula I, or pharmaceutically acceptable 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, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, 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: September 30, 2008
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Scott B. Hoyt, Clare London
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8273737
    Abstract: The present invention is directed to compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (SINA)
    Patent number: 8273866
    Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified 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 capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
    Type: Grant
    Filed: November 24, 2003
    Date of Patent: September 25, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James McSwiggen, Leonid Beigelman
  • ANGIOTENSIN II RECEPTOR ANTAGONISTS
    Publication number: 20120238608
    Abstract: A compound having the structure wherein R is, for example, Y is selected from the group consisting of 1) R5, 2) —C(R1R2) (C(R3R4))0-1Y1R5, and 3) —C(R1R2)—O—Y1R5; R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is; Y1 is selected from the group consisting of C(O)—O— and P(O)(OR6)—O—; and R6 is hydrogen or CH3, or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Application
    Filed: May 30, 2012
    Publication date: September 20, 2012
    Applicant: Merck Sharp & Dohme
    Inventors: Amjad Ali, Michael Man-chu Lo, Iyassu K. Sebhat, Chris Franklin, Nicoletta Almirante, Silvia Stefanini, Stefano Biondi, Ennio Ongini
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
    Patent number: 8268986
    Abstract: The present invention concerns methods and reagents useful in modulating gene expression in a variety of applications, including use in therapeutic, diagnostic, target validation, and genomic discovery applications. Specifically, the invention relates to synthetic chemically modified 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 capable of mediating RNA interference (RNAi) against target nucleic acid sequences. The small nucleic acid molecules are useful in the treatment of any disease or condition that responds to modulation of gene expression or activity in a cell, tissue, or organism.
    Type: Grant
    Filed: May 11, 2011
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonid Beigelman, James McSwiggen
  • Pharmaceutical composition comprising oxyntomodulin derivatives and a method for reducing body weight using the composition
    Patent number: 8268779
    Abstract: Modified oxyntomodulin derivatives. Such derivatives can be used for the treatment of metabolic diseases such as diabetes and obesity.
    Type: Grant
    Filed: March 21, 2011
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ranabir Sinha Roy, Elisabetta Bianchi, Antonello Pessi, Paolo Ingallinella, Donald J. Marsh, George J. Eiermann, Yingjun Mu, Yun-Ping Zhou
  • 5, 6-ring annulated indole derivatives and use thereof
    Patent number: 8268803
    Abstract: The present invention relates to 5,6-ring annulated indole derivatives of the formula (I), compositions comprising at least one 5,6-ring annulated indole derivatives, and methods of using the 5,6-ring annulated indole derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: December 17, 2007
    Date of Patent: September 18, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Frank Bennett, Srikanth Venkatraman, F. George Njoroge, Kevin X. Chen, Neng-Yang Shih, Stuart B. Rosenblum, Joseph A. Kozlowski
  • FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY
    Publication number: 20120232086
    Abstract: The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R1, R2, and R3, and rings C and D are as herein described. The present invention also provides compositions comprising at least one Fused Tricyclic Compound, and use of such compounds in the treatment of central nervous system diseases or disorders such as Parkinson's disease.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 13, 2012
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Joel M. Harris, Bernard R. Neustadt, Andrew W. Stampford
  • METHOD FOR PRODUCING PROTEINS IN PICHIA PASTORIS THAT LACK DETECTABLE CROSS BINDING ACTIVITY TO ANTIBODIES AGAINST HOST CELL ANTIGENS
    Publication number: 20120232007
    Abstract: Methods for producing proteins and glycoproteins in Pichia pastoris that lack detectable cross binding activity to antibodies made against host cell antigens are described. In particular, methods are described wherein recombinant Pichia pastoris strains that do not display a ?-mannosyltransferase 2 activity with respect to an N-glycan or O-glycan and do not display at least one activity selected from a ?-mannosyltransferase 1, 3, and 4 activity to produce recombinant proteins and glycoproteins. These recombinant Pichia pastoris strains can produce proteins and glycoproteins that lack detectable ?-mannosidase resistant ?-mannose residues thereon and thus, lack cross binding activity to antibodies against host cell antigens. Further described are methods for producing bi-sialylated human erythropoietin in Pichia pastoris that lack detectable cross binding activity to antibodies against host cell antigens.
    Type: Application
    Filed: October 11, 2010
    Publication date: September 13, 2012
    Applicant: MERCK SHARP & DOHME CORP
    Inventors: Piotr Bobrowicz, Sujatha Gomathinayagam, Stephen Hamilton, Huijuan Li, Natarajan Sethuraman, Terrance A. Stadheim, Stefan Wildt
  • Antifungal composition with enhanced bioavailability
    Patent number: 8263600
    Abstract: A liquid suspension comprising an antifungally effective amount of the micronized compound represented by the chemical structural formula I: at least one thickening agent, a non-ionic surfactant, and a pharmaceutically acceptable liquid carrier is disclosed.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Stefan Sharpe, Joel Sequeira, David Harris, Shashank Mahashabde
  • Method for detecting autoprocessed, secreted PCSK9
    Patent number: 8263353
    Abstract: The present invention provides a method for detecting autoprocessed, secreted PCSK9, a protein involved in cholesterol homeostasis, and for effectively identifying compounds that inhibit autocleavage and secretion from cells. The disclosed method involves the insertion of an epitope tag into a PCSK9 expression construct immediately C-terminal to the pro domain ending at an amino acid residue corresponding to Q152 of human PCSK9. Upon autoprocessing, the epitope tag is exposed and capable of recognition by anti-epitope antibodies or other suitable identification system, allowing for the selective and exclusive identification and/or quantification of processed PCSK9. The present disclosure thus advances the goal of providing enabling technology to the art for the effective identification of therapeutics effective in combating coronary heart disease.
    Type: Grant
    Filed: March 21, 2008
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ayesha Sitlani, Timothy S. Fisher, Joseph C. Santoro
  • OXO bridged diazepan orexin receptor antagonists
    Patent number: 8263586
    Abstract: The present invention is directed to oxo bridged diazepan compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin 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 orexin receptors are involved.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher D. Cox, David B. Whitman
  • Pyridyl amide T-type calcium channel antagonists
    Patent number: 8263627
    Abstract: The present invention is directed to pyridyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels 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 T-type calcium channels are involved.
    Type: Grant
    Filed: January 18, 2011
    Date of Patent: September 11, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Thomas S. Reger, Zhi-Qiang Yang
  • NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS
    Publication number: 20120225886
    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: August 24, 2010
    Publication date: September 6, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gregori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Quinolizidinone M1 receptor positive allosteric modulators
    Patent number: 8258135
    Abstract: The present invention is directed to spiropiperidine compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: October 15, 2008
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald K. Chang, Scott D. Kuduk
  • Pharmaceutical composition of a tachykinin receptor antagonist
    Patent number: 8258132
    Abstract: The present invention is directed to novel pharmaceutical compositions of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine. The pharmaceutical compositions of this invention useful in the treatment or prevention of disorders such as psychiatric disorders including depression and anxiety, inflammatory diseases and emesis.
    Type: Grant
    Filed: December 9, 2002
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: H. William Bosch, Elaine Liversidge, Suhas D. Shelukar, Karen C. Thompson
  • Crystalline salt form of an antidiabetic compound
    Patent number: 8258161
    Abstract: A novel crystalline anhydrous toluenesulfonic acid salt form of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety is stable and non-hygroscopic. The crystalline salt form is useful for making pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.
    Type: Grant
    Filed: February 28, 2008
    Date of Patent: September 4, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Aquiles E. Leyes
  • Piperidine derivatives
    Patent number: 8252803
    Abstract: Compounds of formula I: I selectively inhibit production of Ab(1-42) and hence find use in treatment of Alzheimer's disease and other conditions associated with deposition of A(b) in the brain.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: August 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Alexey A. Rivkin
  • Angiotensin II receptor antagonists
    Patent number: 8252825
    Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, and Y is 1) —(CH2)3R5, 2) —C(O)(CH2)2R5, 3) —C(R1R2)OC(O)O(CH2)nR5, wherein n is 1 or 2, 4) —C(R1R2)OC(O)CH2CH2R5, 5) —C(R1R2)OC(O)OCH2CH2C(R3R4)R5, provided that when Y is —C(O)(CH2)2R5, then R is R1, R2, R3 and R4 are independently selected from the group consisting of hydrogen and C1-4 alkyl; R5 is —CH(ONO2)CH(ONO2)R6; R6 is selected from CH3, CH2CH3 and CH(CH3)2; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: August 28, 2012
    Assignees: NicOx, Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Nicoletta Almirante, Silvia Stefanini, Laura Storoni, Stefano Biondi, Ennio Ongini
  • Hexahydro-1H-4,7-methanoisoindole-1,3-dione compounds
    Patent number: 8252799
    Abstract: The present invention is directed to therapeutic agents of the formula (I) which are atypical antipsychotics and which are useful in the treatment of neurological and psychiatric disorders associated with dopamine D2 and serotonin 5-HT2A neurotransmission dysfunction. wherein; R1 is C1-6alkyl, which is unsubstituted or substituted with 1-6 fluoro, wherein R1 and the hydroxyl group on the ring are attached to the same carbon atom; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: August 28, 2012
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mark T. Bilodeau, Kausik K. Nanda, B. Wesley Trotter