Patents Assigned to Merck Sharp
  • Engineered anti-TSLP antibody
    Patent number: 8512705
    Abstract: The invention relates to binding compounds that specifically bind to human TSLP, as well as uses thereof, e.g., in the treatment of inflammatory disorders.
    Type: Grant
    Filed: June 25, 2012
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Rene de Waal Malefyt
  • Engineered anti-IL-23p19 antibodies
    Patent number: 8513389
    Abstract: Engineered antibodies to human IL-23p19 are provided, as well as uses thereof, e.g. in treatment of inflammatory, autoimmune, and proliferative disorders.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: August 20, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Leonard G. Presta, Brian M. Beyer, Richard N. Ingram, Peter Orth, Yan-Hui Liu
  • 3-imidazo[4,5-b]pyridin-5-ol derivatives useful in the treatment of GPR81 receptor disorders
    Patent number: 8507473
    Abstract: The present invention is directed to certain 3H-imidazo[4,5-b]pyridin-5-ol derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the GPR81 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of GPR81 associated disorders, for example, dyslipidemia, atherosclerosis, atheromatous disease, hypertension, coronary heart disease, stroke, insulin resistance, impaired glucose tolerance, type 2 diabetes, syndrome X, obesity, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type 1 diabetes and acne.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: August 13, 2013
    Assignees: Arena Pharmaceuticals, Inc., Merck Sharp & Dohme Corp.
    Inventors: P. Douglas Boatman, Benjamin R. Johnson, Jae-Kyu Jung, Michelle Kasem, Thomas O. Schrader, Philip J. Skinner, Steven Colletti
  • Soluble guanylate cyclase activators
    Patent number: 8507512
    Abstract: This inventions relates to compounds having the structure Formula I and pharmaceutically acceptable salts thereof which are soluble guanylate cyclase activators. The compounds are useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, pulmonary hypertension, angina pectoris, thromboses, restenosis, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ronald M. Kim, Emma R. Parmee, Christopher Joseph Sinz, Olga A. Ziouzina
  • 3- and 6-quinolines with N-attached heterocyclic CGRP receptor antagonists
    Patent number: 8507477
    Abstract: Compounds of Formula (I): (where variables R1A, R1B, R2, R3, R4, A, and Z are as defined 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 these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP receptors are involved.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: August 13, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Michael R. Wood, Ian M. Bell, June J. Kim, Harold G. Selnick, Craig A. Stump
  • Heterocyclic derivatives
    Patent number: 8507521
    Abstract: The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp + Dohme B.V.
    Inventors: Julia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
  • Heterocyclic quinolizine derived M1 receptor positive allosteric modulators
    Patent number: 8507494
    Abstract: The present invention is directed to novel 3-oxo-2,3-dihydropyrazolo[4,3-c]quinolizine derived compounds of generic formula (I) or a pharmaceutically acceptable salt thereof, 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: April 25, 2011
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Douglas C. Beshore, Scott D. Kuduk
  • Process for producing bicycloaniline derivatives
    Patent number: 8507504
    Abstract: The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2?-methyl-2?,3?-dihydro-1?H-spiro[cyclopropane-1,4?-isoquinolin]-7?-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: August 13, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Shuntaro Furukawa, Taketo Ikeno, Shinji Kato, Masashi Kawasaki, Hisaki Kojima, Wataru Minagawa, Naotaka Sawada, Fuyuki Yamamoto, Sachin Lohani, Yaling Wang
  • MAMMALIAN GENES; RELATED REAGENTS
    Publication number: 20130203060
    Abstract: Nucleic acids encoding a new family of small cysteine rich soluble proteins, from a mammal, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.
    Type: Application
    Filed: April 1, 2013
    Publication date: August 8, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • Functionally selective alpha2C adrenoreceptor agonists
    Patent number: 8501747
    Abstract: In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C 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 ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Manuel de lera Ruiz, Kevin D. McCormick, Christopher W. Boyce, Robert G. Aslanian, Younong Yu, Pietro Mangiaracina, Junying Zheng, Michael Y. Berlin, Stephanie Louise Ciesla, Chia-Yu Huang, Bo Liang
  • 4-fluoro-piperidine T-type calcium channel antagonists
    Patent number: 8501773
    Abstract: The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric 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: June 28, 2006
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Craig W. Lindsley, William D. Shipe, Zhiqiang Yang, David Wisnoski
  • Methods to treat and/or prevent mucositis
    Patent number: 8501717
    Abstract: The present invention relates to methods useful for treating and/or preventing mucositis using an active vitamin D compound.
    Type: Grant
    Filed: February 8, 2008
    Date of Patent: August 6, 2013
    Assignee: Merck, Sharp & Dohme Corp.
    Inventor: Chen Zong
  • Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
    Patent number: 8501786
    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: Grant
    Filed: March 23, 2009
    Date of Patent: August 6, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Bart Harper, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
  • HIV protease inhibitors
    Patent number: 8497383
    Abstract: Compounds of Formula (I) are disclosed; wherein XA, k, A, B, R3A, R3B, R4 and R5 are defined herein. The compounds of Formula (I) are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: May 18, 2010
    Date of Patent: July 30, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Coburn, M. Katharine Holloway, Joseph P. Vacca
  • ANTAGONISTS OF PCSK9
    Publication number: 20130189278
    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: January 15, 2013
    Publication date: July 25, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • 2-aminoimidazole beta-secretase inhibitors for the treatment of alzheimer's disease
    Patent number: 8492387
    Abstract: The present invention is directed to 2-aminoimidazole 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: February 18, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck, Sharp & Dohme, Corp.
    Inventors: Ivory D. Hills, Craig A. Coburn, Samuel L. Graham, Keith P. Moore, Philippe G. Nantermet, Hemaka A. Rajapakse, Shawn J. Stachel, Hong Zhu
  • Alkoxy tetrahydro-pyridopyrimidine PDE10 inhibitors
    Patent number: 8492392
    Abstract: The present invention is directed to alkoxy tetrahydro-pyridopyrimidine compounds of formula I, which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: July 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Izzat T. Raheem, John D. Schreier
  • Spiroazaindoles
    Patent number: 8492398
    Abstract: The present invention relates to spiroazaindole compounds useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
    Type: Grant
    Filed: April 28, 2009
    Date of Patent: July 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joan M. Pierce (nee Fletcher), Jeffrey J. Hale, Shouwu Miao, Petr Vachal
  • IL-B30 antibodies
    Patent number: 8492528
    Abstract: Purified genes encoding interleukin-B30 from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding this molecule are provided. Methods of using said reagents and diagnostic kits are also provided.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: July 23, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: J. Fernando Bazan
  • ?-lactamase inhibitors
    Patent number: 8487093
    Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.
    Type: Grant
    Filed: January 15, 2009
    Date of Patent: July 16, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin