Patents Assigned to Merck Sharp and Dohme
  • Publication number: 20130053352
    Abstract: A compound having the structure or a pharmaceutically acceptable salt thereof, wherein R1 is hydrogen, —OH, —O—C1-6 alkyl, ?O, or halogen; R2 is hydrogen, C(O)OR8, C6H5C(O)OR8, (CH2)1-2OH, CR9R10OH, C(O)O(CH2)0-2 aryl, C(O)NR9R10, C(O)SO2NR9R10, C6H5OR9, W—C(O)OR8, W—OR9, Y, or P(O)(OR9)(ORlO); R3 is hydrogen or —C1-6 alkyl; R4 is hydrogen, —OH or —C(O)OR9; R5 is hydrogen or deuterium; R6 and R7 are independently —C1-6 alkyl, fluoro-substituted —C1-6 alkyl, deutero-substituted —C1-6 alkyl or —(CH2)1-2R11, wherein any carbon atom of the fluoro-substituted —C1-6 alkyl is mono- or di-substituted with fluoro, and any carbon atom of the deutero-substituted —C1-6 alkyl is mono- or di-substituted with fluoro; R8, in each instance in which it occurs, is independently hydrogen, —C1-6 alkyl, or —(CH2)2N+(CH3)3; R9 and R10, in each instance in which they occur, are independently —C1-6 alkyl; R11 is —OH, —O—C1-6 alkyl, -0CD3, —OC(O)OC1-6 alkyl, —NH2, —C6H5, —N3, or W; W is an unsubslituted 5- or 6-raembered heteroaryl ri
    Type: Application
    Filed: February 10, 2011
    Publication date: February 28, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lin Yan
  • Patent number: 8383810
    Abstract: A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a ?-(substituted-amino)amide, a ?-(substituted-amino)acid ester, or a ?-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.
    Type: Grant
    Filed: December 12, 2011
    Date of Patent: February 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tiruvettipuram K. Thiruvengadam, John S. Chiu, Xiaoyong Fu, Timothy L. McAllister
  • Patent number: 8383113
    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: February 8, 2012
    Date of Patent: February 26, 2013
    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 Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kristen Viola
  • Patent number: 8383350
    Abstract: Provided are assays to measure the presence and quantity of an antibody of interest in a patient's bloodstream or other biological sample. ECL and ELISA methods, and kits for such assays, as well as anti-idiotypic antibodies provided to detect levels of the antibody in biological samples, which are from, for example, animal models and human patients.
    Type: Grant
    Filed: December 19, 2007
    Date of Patent: February 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Karen Kolz, Constance M. Cullen
  • Patent number: 8383818
    Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic derivatives as a2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the a2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 19, 2009
    Date of Patent: February 26, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Junying Zheng, Jianhua Chao, Kevin D. McCormick, Robert G. Aslanian, Mwangi W. Mutahi, Christopher W. Boyce, Walter S. Won
  • Patent number: 8383638
    Abstract: The present invention is directed to aminobenzoquinazolinone 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: December 13, 2010
    Date of Patent: February 26, 2013
    Assignee: Merck Sharp & Dohme
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Christina Ng DiMarco, Thomas J. Greshock
  • Publication number: 20130045914
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: Merck Sharp & Dohme Corp
    Inventor: Merck Sharp & Dohme Corp.
  • Patent number: 8377874
    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 23, 2007
    Date of Patent: February 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, Joseph P. Vacca, John A. McCauley, Michael T. Rudd
  • Patent number: 8377955
    Abstract: The present invention is directed to novel branched 3- and 6-substituted quinoline derivatives which are antagonists of CGRP receptors and 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: June 3, 2009
    Date of Patent: February 19, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Michael R. Wood, June J. Kim, Kathy Schirripa
  • Patent number: 8377911
    Abstract: A compound having the structure formula (I) or a pharmaceutically acceptable salt thereof, and methods of using the compounds for treating hypertension.
    Type: Grant
    Filed: September 20, 2010
    Date of Patent: February 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Lin Yan
  • Patent number: 8377928
    Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives of Formula (I): The invention also relates to compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Grant
    Filed: November 13, 2008
    Date of Patent: February 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski
  • Patent number: 8377954
    Abstract: The present invention is directed to bicyclic spiropiperidine 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: December 28, 2007
    Date of Patent: February 19, 2013
    Assignee: Merck, Sharp & Dohme, Corp
    Inventors: Shaun R. Stauffer, Samuel L. Graham
  • Patent number: 8377873
    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 treating or preventing HCV infections.
    Type: Grant
    Filed: October 19, 2007
    Date of Patent: February 19, 2013
    Assignees: Merck Sharp & Dohme Corp., Istituto di Ricerche di Biologia Molecolare P. Angeletti S.R.L.
    Inventors: Nigel J. Liverton, Vincenzo Summa, Joseph P. Vacca, Maria Emilia Di Francesco, Marco Pompei
  • Patent number: 8378088
    Abstract: In one aspect, the invention generally relates to compositions comprising miR-34 and siRNAs functionally and structurally related to miR-34 for the treatment of cancer.
    Type: Grant
    Filed: May 5, 2008
    Date of Patent: February 19, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michele A Cleary, Aimee L Jackson, Peter S Linsley, Julja Burchard, Lee P Lim, Jill F Magnus
  • Publication number: 20130040932
    Abstract: A series of substituted aryl sulfone 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: Application
    Filed: September 24, 2012
    Publication date: February 14, 2013
    Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.
    Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
  • Publication number: 20130040929
    Abstract: Compounds of structural formula I are inhibitors of prolylcarboxypeptidase (PrCP). The compounds of the present invention are useful for the prevention and treatment of conditions related to the enzymatic activity of PrCP such as abnormal metabolism, including obesity; diabetes; metabolic syndrome; obesity related disorders; and diabetes related disorders.
    Type: Application
    Filed: May 6, 2011
    Publication date: February 14, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Jeffrey J. Hale, Jinlong Jiang, Dong-Ming Shen, Zhi-Cai Shi, Min Shu, Zhicai Wu, Cangming Yang
  • Patent number: 8372402
    Abstract: Nucleic acids encoding mammalian, e.g., primate, receptors, purified receptor proteins and fragments thereof. Antibodies, both polyclonal and monoclonal, are also provided. Methods of using the compositions for both diagnostic and therapeutic utilities are described.
    Type: Grant
    Filed: January 13, 2012
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Madaline Chirica, Robert A. Kastelein, Kevin Moore, Christi L. Parham
  • Patent number: 8372859
    Abstract: Compounds of formula I: (wherein variables A, m, n, J, Re, Rf, R4, Ea, Eb, Ec, RPG 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; and 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 7, 2008
    Date of Patent: February 12, 2013
    Assignee: Merck, Sharp & Dohme Corp.
    Inventors: Michael R. Wood, June Kim, Melody McWherter, Harold G. Selnick, Kathy Schirripa
  • Patent number: 8372980
    Abstract: Fused-ring, heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein ?represents an optional double bond, and wherein An, En, Mn, Gn, Jn, R3, n7, R8, R9, R10, R11, R32, R33, X, Y, B and Het are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Mariappan V. Chelliah, Samuel Chackalamannil
  • Patent number: 8372863
    Abstract: The present invention relates to tetrahydro-1H-pyrrolo fused pyridone compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: February 11, 2009
    Date of Patent: February 12, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew J. Clements, Vincent J. Colandrea, John S. Debenham, Jeffrey J. Hale, Christina B. Madsen-Duggan, Thomas F. Walsh