Patents Assigned to Merck Sharp
  • Heterocyclic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes
    Patent number: 8653059
    Abstract: The present invention is directed to substituted six-membered heterocyclic 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 obesity and diabetes, 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 18, 2008
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tesfaye Biftu, Danqing Feng, Ann E. Weber, Jason M. Cox, Xiaoxia Qian, Jinyou Xu
  • Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists
    Patent number: 8653260
    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: June 20, 2012
    Date of Patent: February 18, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Richard Berger, Lehua Chang, Scott D. Edmondson, Stephen D. Goble, Sookhee Nicole Ha, Nam Fung Kar, Ihor E. Kopka, Bing Li, Gregori J. Morriello, Chris R. Moyes, Ding-Ming Shen, Liping Wang, Cheng Zhu
  • ANTIDIABETIC TRICYCLIC COMPOUNDS
    Publication number: 20140045746
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Application
    Filed: July 31, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: William K. Hagmann, Ravi P. Nargund, Timothy A. Blizzard, Hubert Josien, Purakkattle Biju, Christopher W. Plummer, Qun Dang, Bing Li, Linus S. Lin, Mingxiang Cui, Bin Hu, Jinglai Hao, Zhengxia Chen
  • SUBSTITUTED 1,3-BENZOTHIAZOL-2(3H)-ONES AND [1,3]THIAZOLO[5,4-B]PYRIDIN-2(1H)-ONES AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2
    Publication number: 20140045829
    Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological 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: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • Insulin-Like Growth Factor-1 Receptor Inhibitors
    Publication number: 20140045832
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: April 19, 2012
    Publication date: February 13, 2014
    Applicants: PIRAMAL ENTERPRISES LIMITED, MERCK SHARP & DOHME CORP.
    Inventors: Sarala Balachandran, Christopher J. Dinsmore, Abhijit Roychowdhury, Rajiv Sharma, Ram Asrey Vishwakarma
  • Diazeniumdiolate cyclopentyl derivatives
    Patent number: 8648058
    Abstract: A compound of formula I, wherein R1-R7 are defined herein, or stereoisomers therof, or pharmaceutically acceptable salts thereof, or pharmaceutically acceptable salts of stereoisomers thereof, and methods of using these compounds for treating hypertension.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: February 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Amjad Ali, Michael Man-Chu Lo, Edward Metzger, Lin Yan
  • RNA interference mediated inhibition of gene expression using chemically modified short interfering nucleic acid (siNA)
    Patent number: 8648185
    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 15, 2012
    Date of Patent: February 11, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James McSwigen, Leonid Beigelman
  • RORgammaT INHIBITORS
    Publication number: 20140038942
    Abstract: The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.
    Type: Application
    Filed: February 10, 2012
    Publication date: February 6, 2014
    Applicants: Merck Sharp & Dohme B.V., Merck Sharp & Dohme Corp.
    Inventors: Willem Frederik Johan Karstens, Mario Van Der Stelt, Jos Cals, Rita Corte Real Goncalves Azevedo, Kenneth Jay Barr, Hongjun Zhang, Richard Thomas Beresis, Dongshan Zhang, Xiaobang Duan
  • MODULATION OF PILR RECEPTORS TO TREAT MICROBIAL INFECTIONS
    Publication number: 20140037627
    Abstract: The present invention provides methods of using agonists and antagonists of PILR? and PILR?, respectively, to treat S. aureus infection, in particular, S. aureus infections of the lungs. Also provided are use agonists and antagonists of PILR? and PILR?, respectively, to prevent such infections.
    Type: Application
    Filed: August 8, 2013
    Publication date: February 6, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Antara Banerjee, Paul G. Heyworth
  • BRIDGED AND FUSED ANTIDIABETIC COMPOUNDS
    Publication number: 20140038970
    Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
    Type: Application
    Filed: October 2, 2013
    Publication date: February 6, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: HUBERT B. JOSIEN, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
  • Morpholinone compounds as factor IXa inhibitors
    Patent number: 8642582
    Abstract: The present invention provides a compound of Formula (I) as described herein, or a pharmaceutically acceptable salt or a solvate thereof. The present invention also provides pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing a thromboses, embolisms, hypercoagulability or fibrotic changes.
    Type: Grant
    Filed: December 3, 2009
    Date of Patent: February 4, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Hidemitsu Nishida, Fumihiko Saitoh, Tomokazu Hirabayashi, Samuel Chackalamannil, Tin-Yau Chan, Mariappan V. Chelliah, Martin C. Clasby, Michael Dwyer, William J. Greenlee, Yan Xia
  • METHODS OF CLASSIFYING HUMAN SUBJECTS WITH REGARD TO CANCER PROGNOSIS
    Publication number: 20140031251
    Abstract: In one aspect, methods, markers, and expression signatures are disclosed for assessing the degree to which a cell sample has epithelial cell-like properties or mesenchymal cell-like properties. In another aspect, methods are provided for predicting cancer patient prognosis based on whether the cancer is classified as having a high or low EMT Signature Score.
    Type: Application
    Filed: November 2, 2011
    Publication date: January 30, 2014
    Applicants: H. Lee Moffitt Cancer Center and Research Institute, Inc., Merck Sharp & Dohme Corp.
    Inventors: Timothy Yeatman, Andrey Loboda, Michael Nebozhyn, Hongyue Dai
  • PAVEC
    Publication number: 20140030760
    Abstract: This application provides, in part, pAVEC plasmids and methods of use of such plasmids for the production of polypeptides such as immunoglobulins as well as the generation of recombined versions of such plasmids which contain polynucleotides encoding such polypeptides.
    Type: Application
    Filed: April 2, 2012
    Publication date: January 30, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventor: Deba P. Saha
  • INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL
    Publication number: 20140031349
    Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and conditions associated with excessive salt and water retention.
    Type: Application
    Filed: July 25, 2013
    Publication date: January 30, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Fa-Xiang Ding, Shuzhi Dong, Jessica Frie, Xin Gu, Jinlong Jiang, Alexander Pasternak, Haifeng Tang, Zhicai Wu, Yang Yu, Takao Suzuki
  • METHODS OF PREDICTING CANCER CELL RESPONSE TO THERAPEUTIC AGENTS
    Publication number: 20140030255
    Abstract: In one aspect, methods, markers, and expression signatures are disclosed for assessing the degree to which a cell sample has epithelial cell-like properties or mesenchymal cell-like properties. In another aspect, methods are provided for predicting whether a subject with cancer will respond to treatment with an agent, based on whether the cancer is classified as having a high or low EMT Signature Score.
    Type: Application
    Filed: November 2, 2011
    Publication date: January 30, 2014
    Applicant: MERCK SHARP & DOHME CORP.
    Inventors: Andrey Loboda, Michael Nebozhyn, Hongyue Dai
  • Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
    Patent number: 8637507
    Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose. An illustrative compound of the invention is shown below: formula (I).
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Gang Zhou, Grant Wishart, Pauline C. Ting, Robert G. Aslanian, Nicolas Zorn, David Won-shik Kim
  • Engineered anti-TSLP antibody
    Patent number: 8637019
    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 and allergic inflammatory response.
    Type: Grant
    Filed: November 2, 2010
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventor: Leonard G. Presta
  • Heterocycle phenyl amide T-type calcium channel antagonists
    Patent number: 8637513
    Abstract: The present invention is directed to heterocycle phenyl 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: October 23, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: James C. Barrow, Paul J. Coleman, Thomas S. Reger, Kelly-Ann S. Schlegel, Youheng Shu, Zhi-Qiang Yang
  • Eukaryotic cell display systems
    Patent number: 8637435
    Abstract: The present invention provides expression vectors and helper display vectors which can be used in various combinations as vector sets for display of polypeptides on the outer surface of eukaryotic host cells. The expression vector of the invention can be used alone for soluble expression without having to change or reengineer the display vectors. The display systems of the invention are particularly useful for displaying a genetically diverse repertoire or library of polypeptides on the surface of yeast cells, and mammalian cells.
    Type: Grant
    Filed: November 14, 2008
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kevin Caili Wang, Peter Peizhi Luo, Pingyu Zhong, Jian Wang
  • 6-mercapto-cyclodextrin derivatives:reversal agents for drug-induced neuromuscular block
    Patent number: RE44733
    Abstract: Disclosed is a 6-mercapto-cyclodextrin derivative having general formula (I) wherein m is 0-7 and n is 1-8 and m+n=7 or 8; R is (C1-6)alkylene, optionally substituated with 1-3 OH groups, or (CH2)o-phenylene-(CH2)p—; o and p are independently 0-4; X is COOH, CONHR1, NHCOR2, SO2OH, PO(OH)2, O(CH2—CH2—O)q—H, OH or tetrazol-5-yl; R1 is H or (C1-3)alkyl; R2 is carboxyphenyl; q is 1-3; or pharmaceutically acceptable salts thereof. The 6-mercaptocyclodextrin derivative is highly suitable for use in the reversal of drug-induced neuromuscular block.
    Type: Grant
    Filed: March 28, 2012
    Date of Patent: January 28, 2014
    Assignee: Merck Sharp & Dohme B.V.
    Inventors: Mingiang Zhang, Ronald Palin, Jonathan Bennett