Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and 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:
Grant
Filed:
November 11, 2009
Date of Patent:
June 24, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
Abstract: The invention encompasses a novel class of cyclobutyl sulfone derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.
Type:
Grant
Filed:
April 17, 2009
Date of Patent:
June 24, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard W. Heidebrecht, Chaomin Li, Benito Munoz, Andrew Rosenau, Laura M. Surdi, Paul Tempest
Abstract: The present invention relates to novel heterocyclic compounds as Fatty Acid Binding Protein (FABP) 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.
Type:
Grant
Filed:
October 1, 2010
Date of Patent:
June 24, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Gerald W. Shipps, Jr., Clifford C. Cheng, Xioahua Huang, Abdelghani Achab, Peter Orth, Johannes H. Voigt
Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
Type:
Grant
Filed:
December 18, 2009
Date of Patent:
June 24, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John W. Clader, Dmitri A. Pissarnitski, Hubert B. Josien, Hongmei Li
Abstract: The present invention relates to 1-(4-ureidobenzoyl)piperazine derivatives having the general Formula I (We bring to your attention that formula I is not provided on this electronic version as it is provided in the abstract of the paper copy) Wherein R1 is (C1-8)alkyl, (C3-8)cycloalkyl or (C3-8)cycloalkyl(C1-3)alkyl, each of which may be substituted by hydroxy, cyano or halogen; R2 represents 1 or 2 optional halogens; R3 is (C1-6)alkyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl, each of which may be substituted by one or more halogens; A represents a heteroaryl ring system comprising 1-3 heteroatoms selected from N, O and S, which ring system is 5- or 6-membered when X is C, and 5-membered when X is N; n is 1 or 2; or a pharmaceutically acceptable salt thereof; to pharmaceutical compositions comprising the same, and to the use of a these 1-(4-ureidobenzoyl)piperazine derivatives for the manufacture of a medicament for treating or preventing atherosclerosis and related disorders associated with cholester
Inventors:
Andrew John Cooke, David Jonathan Bennett, Andrew Stanley Edwards, Andrew Laird Roughton, Irina Neagu, Jui-Hsiang Chan, Koc-Kan Ho, Nasrin Ansari, Michelle Lee Morris, Yajing Rong, Michael Ohlmeyer
Abstract: The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
Type:
Grant
Filed:
December 15, 2010
Date of Patent:
June 24, 2014
Assignees:
Merck Sharp & Dohme Corp., Merck Canada Inc.
Inventors:
Kaleen Konrad Childers, Andrew M. Haidle, Michelle R. Machacek, Alan B. Northrup
Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.
Type:
Application
Filed:
February 21, 2014
Publication date:
June 19, 2014
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
John Y. L. Chung, Yanfeng Zhang, Laura Artino, Aaron S. Cote, Donal Desmond, Jeremy Scott, Yekaterina Vaynshteyn
Abstract: The present invention is directed to certain oxazole 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:
Application
Filed:
December 6, 2013
Publication date:
June 19, 2014
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Harry Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo
Abstract: The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and 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 10, 2011
Date of Patent:
June 17, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Mark E. Fraley, Steven N. Gallicchio, Anthony Ginnetti, Helen J. Mitchell, Daniel V. Paone, Donnette D. Staas, Heather E. Stevenson, Cheng Wang, C. Blair Zartman
Abstract: Intelligent refrigerator system for storing pharmaceutical product containers, such as vials, ampules, syringes, bottles, medication tubes, blister packs and cartons, at the point of dispensing. Embodiments of the invention use product identification technology, such as radio-frequency identification (RFID) tags and readers, to uniquely identify containers as they are added to or removed from the cold storage compartment of the refrigerator, and automatically retrieve from a local or remote database a variety of details associated with the containers and their contents, such as manufacturing data, expiration dates, time out of refrigeration, inventory levels, safety information, usage statistics, known contraindications and warnings, etc. If the details indicate that there is a problem with a particular pharmaceutical (e.g.
Abstract: Beta-carboline derivatives of structural formula I are selective antagonists of the somatostatin subtype receptor 3 (SSTR3) and are useful for the treatment of Type 2 diabetes mellitus and of conditions that are often associated with this disease, including hyperglycemia, insulin resistance, obesity, lipid disorders, and hypertension. The compounds are also useful for the treatment of depression and anxiety.
Type:
Grant
Filed:
January 11, 2011
Date of Patent:
June 17, 2014
Assignee:
Merck Sharp & Dohme Corp
Inventors:
Liangqin Guo, William K. Hagmann, Shuwen He, Zhong Lai, Jian Liu, Ravi P. Nargund, Shrenik K. Shah, Quang T. Truong
Abstract: The present invention is directed to 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.
Abstract: The present invention provides compositions and methods for treating disorders of cholesterol and lipid metabolism by administration of an anti-PCSK9 antibody or a peptide inhibitor of PCSK9.
Type:
Application
Filed:
December 2, 2013
Publication date:
June 12, 2014
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Joseph A. Hedrick, Frederick James Monsma, Tatyana Churakova, Diane Hollenbaugh
Abstract: The novel protein SA1789 from Staphylococcus aureus is provided as well as nucleic acid and nucleic acid sequence homologues encoding this protein. Also provided is a composition, particularly a S. aureus vaccine, comprising SA1789 protein or a fragment or derivative thereof capable of generating an immune response that leads to the killing and clearance of S. aureus.
Type:
Grant
Filed:
July 8, 2011
Date of Patent:
June 10, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Tessie B. McNeely, Hongxia Fan, Mark Andrew Miller
Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.
Type:
Grant
Filed:
April 25, 2011
Date of Patent:
June 10, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Richard Berger, Scott D. Edmondson, Bart H. Harper
Abstract: Methods of using PCSK9 antagonists More specifically, methods for measuring circulating PCSK9 levels in a biological sample by means of an immunoassay The immunoassay used can be a solid phase immunoassay, such as a dissociation-enhanced lanthanide fluorescence immunoassay utilizing an E07 capture antibody or coating and a G08 or H23 detecting antibody.
Type:
Grant
Filed:
December 2, 2009
Date of Patent:
June 10, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Yan Ni, Ayesha Sitlani, Shilpa Pandit, Dale Lewis, Xun Shen, Sharon Lobo, Timothy McCabe, Jon Condra, Rose Cubbon
Abstract: In one aspect, the present invention provides methods of determining whether an agent is more like a partial agonist of a target molecule than a full agonist of the same target molecule. In another aspect, the present invention provides methods to select a candidate compound that may reduce blood plasma glucose concentration in a mammal. Populations of genes are provided that are useful in the practice of the present invention.
Type:
Grant
Filed:
August 12, 2011
Date of Patent:
June 3, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Yejun Tan, Hongyue Dai, Pek Yee Lum, John Ryan Thompson, Joel Peter Berger, Eric Stanley Muise, Richard F. Raubertas, Kenny Kin Chung Wong
Abstract: Compounds of Formula I are capable of modulating the body's production of cyclic guanosine monophosphate (“cGMP”) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the Formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the Formula I.
Type:
Grant
Filed:
November 16, 2009
Date of Patent:
June 3, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Linda L. Brockunier, Jian Guo, Emma R. Parmee, Subharekha Raghavan, Keith Rosauer, Darby Schmidt, John E. Stelmach
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:
Grant
Filed:
August 12, 2011
Date of Patent:
June 3, 2014
Assignee:
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