Patents Assigned to Merck Sharp & Dohme
  • PROCESS FOR PHOSPHONIC ACID
    Publication number: 20100324287
    Abstract: The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.
    Type: Application
    Filed: August 25, 2010
    Publication date: December 23, 2010
    Applicant: Merck Sharp & Dohme
    Inventors: James Michael McNamara, Louis Matty, Jonathan D. Rosen
  • Quinolizidinone M1 Receptor Positive Allosteric Modulators
    Publication number: 20100324024
    Abstract: The present invention is directed to compounds of formula (I) (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: Application
    Filed: February 3, 2009
    Publication date: December 23, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Ronald K. Chang, Christina Ng Di Marco
  • Tricyclic heteroaromatic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 7855206
    Abstract: The present invention is directed to novel substituted tricyclic heteroaromatic compounds 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 9, 2007
    Date of Patent: December 21, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jason M. Cox, Hong Dong
  • Morpholine carboxamide prokineticin receptor antagonists
    Patent number: 7855201
    Abstract: The present invention is directed to morpholine carboxamide compounds which are antagonists of prokineticin receptors, in particular antagonists of prokineticin 2 receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which prokineticin 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 prokineticin receptors are involved.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: December 21, 2010
    Assignee: Merck Sharp & Dohme. Corp.
    Inventors: Wayne J. Thompson, Jeffrey Y. Melamed
  • Peptide conjugate compositions and methods for the prevention and treatment of alzheimer's disease
    Patent number: 7850973
    Abstract: The invention provides compositions and methods for the treatment of diseases associated with amyloid deposits of A? in the brain of a patient, such as Alzheimer's disease. Such methods entail administering an immunogenic fragment of A?, lacking a T-cell epitope, capable of inducing a beneficial immune response in the form of antibodies to A?. In another aspect, the immunogenic fragment of A? is capable of elevating plasma A? levels. The immunogenic fragments comprise linear or multivalent peptides of A?. Pharmaceutical compositions comprise the immunogenic fragment chemically linked to a carrier molecule which may be administered with an adjuvant.
    Type: Grant
    Filed: May 1, 2006
    Date of Patent: December 14, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Victor M. Garsky, Joseph G. Joyce, Paul M. Keller, Gene Kinney, Xiaoping Liang, John W. Shiver
  • Spirolactam aryl CGRP receptor antagonists
    Patent number: 7851464
    Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, E1, E2, E3, E4, E5, G1, G2, J and K 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 14, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Harold G. Selnick, Michael R. Wood, Cory R. Theberge, Craig A. Stump, Steven N. Gallicchio, C. Blair Zartman
  • Cyclohexanesulfonyl derivatives as GLYT1 inhibitors to treat schizophrenia
    Patent number: 7851638
    Abstract: The present invention provides compounds of formula I: wherein R1 is an alkyl, phenyl, heterocyclyl, cycloalkyl, alkoxy, ester, amino or amide group; R2 is a phenyl, heterocyclyl, alkyl, cycloalkyl or cycloalkylalkyl group; R3 is an alkyl, cycloalkyl, cycloalkylalkyl, amino or heterocyclyl group; R4 and R5 are hydrogen or alkyl or form a cycloalkyl ring; A is O or N; and m is zero or one; as inhibitors of GlyT1 and thus as useful for treating or preventing diseases such as schizophrenia; with the provision of pharmaceutical compositions, first and second medical uses and methods of treatment.
    Type: Grant
    Filed: October 1, 2009
    Date of Patent: December 14, 2010
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Wesley Peter Blackaby, Jose Luis Castro Pineiro, Richard Thomas Lewis, Elizabeth Mary Naylor, Leslie Joseph Street
  • SUBSTITUTED IMIDAZOLE 4-CARBOXAMIDES AS CHOLECYSTOKININ-1 RECEPTOR MODULATORS
    Publication number: 20100311649
    Abstract: Certain novel substituted imidazole 4-carboxamides are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R , such as obesity, and diabetes.
    Type: Application
    Filed: August 3, 2010
    Publication date: December 9, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Scott Edmondson, Alexa Hansen, Cheng Zhu
  • 1,3,5-substituted phenyl derivative compounds useful as beta-secretase inhibitors for the treatment of Alzheimer's disease
    Patent number: 7847100
    Abstract: The present invention is directed to 1,3,5-phenyl substituted derivative compounds 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: April 15, 2005
    Date of Patent: December 7, 2010
    Assignee: Merck, Sharp & Dohme, Inc.
    Inventors: James C. Barrow, Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Harold G. Selnick, Shaun R. Stauffer, Craig A. Coburn
  • Process for 5-[[2(r)-[1(r)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(s)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3h-1.,2,4-triazol-3-one
    Patent number: 7847095
    Abstract: The present invention is concerned with a novel process for the preparation of the compound 5-[[2(R)-[1(R)-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4 -tria-zol-3-one. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of psychiatric disorders, inflammatory diseases and emesis.
    Type: Grant
    Filed: April 17, 2003
    Date of Patent: December 7, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: David Hands, Mark Huffman, Mahmoud S. Kaba, Joseph F. Payack
  • CGRP RECEPTOR ANTAGONISTS
    Publication number: 20100298303
    Abstract: The present invention is directed to compounds of Formula I: and Formula II: (where variables R1, R2, R3, R4, A, B, G, J, Q, T, U, V, W, X and Y 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: Application
    Filed: July 7, 2010
    Publication date: November 25, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Daniel Vincent Paone, Anthony W. Shaw
  • PRODRUGS OF CGRP RECEPTOR ANTAGONISTS
    Publication number: 20100298269
    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: Application
    Filed: February 4, 2009
    Publication date: November 25, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Steven N. Gallicchio, Valentino J. Stella
  • 3,5-SUBSTITUTED-1,3-OXAZOLIDIN-2-ONE DERIVATIVES
    Publication number: 20100292241
    Abstract: The present invention is directed to 3,5-disubstituted-1,3-oxazolidin-2-one derivatives which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neuro-ological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate 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 metabotropic glutamate receptors are involved.
    Type: Application
    Filed: January 14, 2009
    Publication date: November 18, 2010
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Edward Brnardic, Mark Fraley, Mark Layton, Robert Garbaccio
  • Radiolabeled glycine transporter inhibitors
    Patent number: 7834031
    Abstract: The present invention is directed to radiolabeled glycine transporter inhibitors which are useful for the labeling and diagnostic imaging of glycine transporters in mammals.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: H. Donald Burns, Terence G. Hamill, Craig W. Lindsley
  • Benzothiophene derivatives
    Patent number: 7834034
    Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 14, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Dawn M. Mampreian, Thomas A. Miller, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
  • Process for the preparation of bicyclo[3.1.0]hexanols
    Patent number: 7834222
    Abstract: A process for the preparation of a the formula (I): which process comprises the intramolecular cyclopropanation of an epoxide of me formula (II); in the presence of 0.05 to 0.75 equivalents of a secondary amine base and at least one equivalent of an alkyl lithium base, wherein R R1, R2 and R3 are each hydrogen or C1-4 alkyl or R1 and R2 are linked to form- a C3-7 cycloaUcyl or C3-7 cycloalkenyl ring.
    Type: Grant
    Filed: August 1, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Matthew Bio, Karel Marie Joseph Brands, Edward Cleator
  • Angiotensin II receptor antagonists
    Patent number: 7834042
    Abstract: A compound having the structure (Formula I), wherein Y is —Y1—Y2—Y3—Y4—Y5—; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali
  • Fused-aromatic compounds having anti-diabetic activity
    Patent number: 7834036
    Abstract: Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dyslipidermia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
    Type: Grant
    Filed: March 3, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp
    Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
  • Spirocyclic compounds
    Patent number: 7834026
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds, represented by the following structural Formula: I Wherein A, B and D are independently selected from CR12, NR1a, C(O) and O; E is selected from a bond, CR12, NR1a, C(O) and O; wherein at least one of A, B, D or E is CR12; and provided that when A is O, then E is not O; G is CR12; R is selected from NH2 and OH; These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing termin differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: November 16, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott C. Berk, Joshua Close, Christopher Hamblett, Richard W. Heidebrecht, Solomon D. Kattar, Laura T. Kliman, Dawn M. Mampreian, Joey L. Methot, Thomas Miller, David L. Sloman, Matthew G. Stanton, Paul Tempest, Anna A. Zabierek
  • Conjugates and compositions for cellular delivery
    Patent number: 7833992
    Abstract: This invention features conjugates, degradable linkers, compositions, methods of synthesis, and applications thereof, including cholesterol derived conjugates of biologically active compounds, including antibodies, antivirals, chemotherapeutics, peptides, proteins, hormones, nucleosides, nucleotides, non-nucleosides, and nucleic acids including enzymatic nucleic acids, DNAzymes, allozymes, antisense, dsRNA, siNA, siRNA, triplex oligonucleotides, 2,5-A chimeras, decoys and aptamers.
    Type: Grant
    Filed: April 30, 2003
    Date of Patent: November 16, 2010
    Assignee: Merck Sharpe & Dohme
    Inventors: Chandra Vargeese, Peter Haeberli, Weimin Wang, Tongqian Chen