Patents Assigned to Merck Sharp
  • AMINOTETRAHYDROPYRANS AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OR PREVENTION OF DIABETES
    Publication number: 20130157940
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans 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: Application
    Filed: February 7, 2013
    Publication date: June 20, 2013
    Applicant: Merck Sharp & Dohme Corp
    Inventor: Merck Sharp & Dohme Corp
  • 6-substituted sulfonyl azabicyclo[3.2.1]octanes useful to inhibit 11?-hydroxysteroid dehydrogenase type-I
    Patent number: 8466149
    Abstract: In its many embodiments, the present invention relates to a novel class of 6-substituted sulfonyl-1,3,3-trialkyl-6-azabicyclo[3.2.1]octane compounds useful to inhibit 11?-hydroxysteroid dehydrogenase type-I, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the expression of 11?-hydroxysteroid dehydrogenase type-I using such compounds or pharmaceutical compositions.
    Type: Grant
    Filed: August 12, 2008
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Craig D. Boyle, Samuel Chackalamannil, Unmesh Shah, Claire M. Lankin
  • 2,5-disubstituted morpholine orexin receptor antagonists
    Patent number: 8466281
    Abstract: The present invention is directed to 2,5-disubstituted morpholine amide 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: October 15, 2009
    Date of Patent: June 18, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Paul J. Coleman, Christopher D. Cox, Broc Flores, John D. Schreier
  • NOVEL PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
    Publication number: 20130150362
    Abstract: The present invention relates to certain pyrazolo[1,5-a]pyrimidine compounds of Formula (I) as inhibitors of mammalian Target Of Rapamycin (mTOR) kinase, which is also known as FRAP, RAFT, RAPT or SEP. The compounds may be used in the treatment of cancer and other disorders where mTOR is deregulated. The present invention further provides pharmaceutical compositions comprising the pyrazolo[1,5-a]pyrimidine compounds.
    Type: Application
    Filed: August 22, 2011
    Publication date: June 13, 2013
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Lianyun Zhao, Duan Liu, Shuyi Tang, Amit K. Mandal, Umar Faruk Mansoor, Lalanthi Dilrukshi Vitharana, Panduranga Adulla P. Reddy, M. Arshad Siddiqui
  • Pyrazolo[1,5-a]pyrimidine derivatives
    Patent number: 8461162
    Abstract: Compounds of the following formula (I) are inhibitors of microtubule affinity regulating kinase, and hence find use in the treatment of neurodegenerative diseases associated with hyperphosphorylation of tau.
    Type: Grant
    Filed: July 16, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew G. Stanton, Njamkou Noucti, David L. Sloman, Jongwon Lim, Benito Munoz
  • HCV NS3 protease inhibitors
    Patent number: 8461107
    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: April 16, 2009
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Nigel J. Liverton, John A. McCauley, John W. Butcher, Kevin F. Gilbert, Charles J. McIntyre, Michael T. Rudd
  • Pyridyl derivatives as histone deacetylase inhibitors
    Patent number: 8461189
    Abstract: The present invention relates to a novel class of pyridyl and pyrimidinyl derivatives. The pyridyl and pyrimidinyl compounds can be used to treat cancer. The pyridyl and pyrimidinyl 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: June 24, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard W. Heidebrecht, Jr., Thomas A. Miller, Matthew G. Stanton, David J. Witter
  • P2X3 receptor antagonists for treatment of pain
    Patent number: 8461185
    Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.
    Type: Grant
    Filed: October 29, 2008
    Date of Patent: June 11, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Christopher S. Burgey, Diem N. Nguyen, Daniel V. Paone, Craig M. Potteiger, Joseph P. Vacca
  • NOVEL PROLYLCARBOXYPEPTIDASE INHIBITORS
    Publication number: 20130143859
    Abstract: Compounds of structural formulas I-1 and I-2 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: June 3, 2011
    Publication date: June 6, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Thomas H. Graham, Wensheng Liu, Iyassu K. Sebhat, Dong-Ming Shen, Zhi-Cai Shi
  • Method for selecting SIRNAs from a plurality of SIRNAs for gene silencing
    Patent number: 8457902
    Abstract: The present invention provides a method for identifying siRNA target motifs in a transcript using a position-specific score matrix approach. The invention also provides a method for identifying off-target genes of an siRNA using a position-specific score matrix approach. The invention further provides a method for designing siRNAs with higher silencing efficacy and specificity. The invention also provides a library of siRNAs comprising siRNAs with high silencing efficacy and specificity.
    Type: Grant
    Filed: May 4, 2011
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Aimee L. Jackson, Steven R. Bartz, Julja Burchard, Peter S. Linsley, Ge Wei, Guy L. Cavet
  • Imidazole derivatives useful as inhibitors of FAAH
    Patent number: 8455528
    Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.
    Type: Grant
    Filed: June 4, 2009
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
  • Soluble epoxide hydrolase inhibitors, compositions containing such compounds and methods of treatment
    Patent number: 8455520
    Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: July 11, 2008
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
  • Soluble guanylate cyclase activators
    Patent number: 8455638
    Abstract: A compound having the structure useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, angina pectoris, thromboses, restenoses, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver in a human or animal patient.
    Type: Grant
    Filed: September 2, 2008
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amy R. Bittner, Ronald M. Kim, John W. Mirc, Emma R. Parmee, Christopher Joseph Sinz, Qiang Tan
  • Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 8455533
    Abstract: The present invention is directed to novel substituted aminotetrahydropyrans 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: August 23, 2010
    Date of Patent: June 4, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Ping Chen, Danqing Feng, Xiaoxia Qian
  • Therapeutic compounds
    Patent number: 8455477
    Abstract: The present invention relates to pyrazolopyridines and imidazopyridines which are inhibitors of the kinase PDK1 and are thus useful for the treatment of myeloproliferative disorders or cancer. The compounds are also useful as inhibitors of other kinases such as FGFR3, NTRK3, RP-S6K and WEE1. Furthermore, the present compounds also selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: June 4, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Jason Katz, James Jewell, Joon Jung, Solomon Kattar, Yongquan Hou, Rachel MacCoss, Satoru Ito
  • Compounds for the treatment of inflammatory diseases
    Patent number: 8450355
    Abstract: This invention relates to compounds of the Formula (I)-(IX):, as defined herein, or a pharmaceutically acceptable salt, solvate or ester thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? combinations thereof.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: May 28, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Michael K. C. Wong, Wensheng Yu, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Joseph A. Kozlowski, Seong Heon Kim, Guowei Zhou, De-Yi Yang, Razia K. Rizvi, Lei Chen, Aneta Maria Kosinzki, Kristin E. Rosner, Luke Fire, Judson E. Richard, Dansu Li
  • Formulations of suberoylanilide hydroxamic acid and methods for producing same
    Patent number: 8450372
    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: January 13, 2010
    Date of Patent: May 28, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Jeannie Chow Wong, Aaron S. Cote, Erik A. Dienemann, Kimberly Gallagher, Craig Ikeda, Justin Moser, Pavol Rajniak, Robert A. Reed, Cindy Starbuck, Hsien-Hsin Tung, Qingxi Wang, Benjamin Max Cohen, Vincent R. Capodanno, Brian Sell, Thomas A. Miller
  • Thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidinone compounds as BACE-1 inhibitors, compositions, and their use
    Patent number: 8450331
    Abstract: In its many embodiments, the present invention provides certain thiophenyl-substituted 2-imino-3-methyl pyrrolo pyrimidone compounds, including compounds (or tautomers or a pharmaceutically acceptable salts thereof) having the structural Formula (III): wherein R2, R3, R4, R5, R6, R7, R8, and R9 are each selected independently and as defined herein. Pharmaceutical compositions comprising one or more such compounds, and methods for their preparation and use in treating pathologies associated with amyloid beta (A?) protein, including Alzheimer's Disease, are also disclosed.
    Type: Grant
    Filed: April 21, 2009
    Date of Patent: May 28, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhaoning Zhu, Andrew Stamford, Mihirbaran Mandal, Xiaoxiang Liu
  • SPIROCYCLIC COMPOUNDS
    Publication number: 20130131041
    Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can 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: Application
    Filed: December 19, 2012
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventor: Merck Sharp & Dohme Corp.
  • SPIROXAZOLIDINONE COMPOUNDS
    Publication number: 20130131042
    Abstract: Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
    Type: Application
    Filed: August 12, 2011
    Publication date: May 23, 2013
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Joseph L. Duffy, Jianming Bao, Debra L. Ondeyka, Sriram Tyagarajan, Patrick Shao, Feng Ye, Revathi Katipally, Aaron Zwicker, Edward C. Sherer, Michael A. Plotkin, Remond Moningka, Zahid Hussain, Harold B. Wood, Feroze Ujjainwalla, F. Anthony Romero, Paul E. Finke, Yi Zang, Weiguo Liu