Abstract: The present invention is directed to imidazolidinone 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:
November 10, 2006
Date of Patent:
August 23, 2011
Assignee:
Merck. Sharp & Dohme Corp.
Inventors:
James C. Barrow, Kenneth E. Rittle, Phung Le Bondiskey
Abstract: Described herein are solid, stable pharmaceutical formulations of cannabinoid receptor inverse agonists, such as taranabant, and processes of making such formulations. Additionally, described herein are solid stable pharmaceutical formulations of cannabiniod inverse agonists, such as taranabant, and an additional therapeutic agent, as well as processes for making such pharmaceutical formulations.
Type:
Grant
Filed:
April 17, 2009
Date of Patent:
August 23, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Craig McKelvey, Sarah Geers, Justin Moser, Bhagwant Rege, Dina Zhang, Sutthilug Sotthivirat
Abstract: The present invention is directed to pyridyl carboxamide 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:
August 7, 2008
Date of Patent:
August 23, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Swati P. Mercer, Thomas S. Reger, Anthony J. Roecker, Justin T. Steen
Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c 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:
Grant
Filed:
September 9, 2005
Date of Patent:
August 23, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Cory R. Theberge, Craig A. Stump, Xufang Zhang, Steven N. Gallicchio, C. Blair Zartman
Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and 2) —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5; Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—NR3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.
Type:
Application
Filed:
April 25, 2011
Publication date:
August 18, 2011
Applicant:
MERCK SHARP & DOHME CORP.
Inventors:
Amjad ALI, Michael Man-Chu LO, Christopher FRANKLIN, Brent R. WHITEHEAD
Abstract: The present invention relates generally to a method for increasing the yield of plasmid DNA production. The method includes the steps of selecting a highly productive clonal subtype of a strain of E. coli, including but not limited to the DH5 strain, harboring a DNA plasmid and cultivating said clonal subtype with fed-batch fermentation in a chemically-defined medium. The plasmid DNA production process described herein can generate record quantities of plasmid DNA when said highly productive clonal subtypes are cultivated on an industrial scale. The disclosed method can be used for the production of pharmaceutical grade DNA for use in polynucleotide vaccination and gene therapy treatment regimens.
Type:
Grant
Filed:
January 31, 2005
Date of Patent:
August 16, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michel Chartrain, Laura Kizer Bentley, Barbara Ann Krulewicz, Kristin M. Listner, Wen-jun Sun, Chanyong Brian Lee
Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, Huntington's disease movement disorders, and schizophrenia.
Type:
Grant
Filed:
January 16, 2008
Date of Patent:
August 16, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
John S. Debenham, Jeffrey J. Hale, Pei Huo, Christina B. Madsen-Duggan, Thomas F. Walsh, Lin Yan
Abstract: The present invention is directed to substituted diazepan 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:
Application
Filed:
April 19, 2011
Publication date:
August 11, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Jeffrey M. Bergman, Michael J. Breslin, Paul J. Coleman, Christopher D. Cox, Swati P. Mercer, Anthony J. Roecker
Abstract: Compounds of Formula I: (where variables R1, A, B, W, X, Y and Z 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:
Grant
Filed:
March 14, 2006
Date of Patent:
August 9, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Daniel V. Paone, Diem N. Nguyen, Anthony W. Shaw, Christopher S. Burgey, Thomas J. Tucker, Samuel L. Graham
Abstract: Antibodies specific for Dkk-1, an inhibitor of the osteoanabolic Wnt/LRP5 signaling pathway, are described. The antibodies, which inhibit binding of Dkk-1 to LRP5, are useful in compositions for stimulating bone growth, in particular, compositions for treating bone disorders which result in a loss in bone, for example, osteoporosis.
Type:
Grant
Filed:
February 6, 2008
Date of Patent:
August 9, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Zhiqiang An, Fang Chen, John E. Fisher, Helmut Glantschnig, Donald B. Kimmel, Alfred A. Reszka, Fubao Wang
Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.
Type:
Application
Filed:
February 7, 2011
Publication date:
August 4, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Lin Chu, Ihor E. Kopka, Bing Li, Anthony K. Ogawa, Feroze Ujjainwalla
Abstract: The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) 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:
April 14, 2011
Publication date:
August 4, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Edmondson, Michael H. Fisher, Dooseop Kim, Malcolm Maccoss, Emma R. Parmee, Ann E. Weber, Jinyou Xu
Abstract: Glucagon receptor antagonist compounds are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
March 19, 2007
Date of Patent:
August 2, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ronald M. Kim, Emma R. Parmee, Qiang Tan, Ashley Rouse Lins, Jiang Chang, Cangming Yang
Abstract: The present invention relates to substituted pyrazoles, compositions containing such compounds and methods of treatment The compounds are glucagon receptor antagonists and thus are useful for treating, preventing or delaying the onset of type 2 diabetes mellitus.
Type:
Grant
Filed:
March 19, 2009
Date of Patent:
August 2, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Emma Parmee, Subharekha Raghavan, Teresa Beeson, Dong-Ming Shen
Abstract: The present invention is directed to compounds of Formula (I): where variables A1, A2, B, J, K, m, n, R4, R5a, R5b, R5c and X 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:
Grant
Filed:
September 6, 2005
Date of Patent:
August 2, 2011
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Ian M. Bell, Craig A. Stump, Cory R. Theberge
Abstract: Compounds of formula (I) modulate the activity of gamma secretase and hence find use in treatment or prevention of Alzheimer's disease and related conditions.
Type:
Grant
Filed:
April 2, 2007
Date of Patent:
July 26, 2011
Assignee:
Merck, Sharp & Dohme Limited
Inventors:
Andrew Madin, Mark Peter Ridgill, Janusz Josef Kulagowski
Abstract: This invention relates to compounds, compositions, and methods useful for modulating platelet derived growth factor (PDGF) and/or platelet derived growth factor receptor (PDGFr) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of platelet derived growth factor (PDGF) and/or platelet derived growth factor receptor (PDGFr) gene expression and/or activity by RNA interference (RNAi) using small nucleic acid molecules. In particular, the instant invention features 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 and methods used to modulate the expression of platelet derived growth factor (PDGF) and/or platelet derived growth factor receptor (PDGFr) genes, such as PDGF and/or PDGFr.
Abstract: Devices and methods for determining risk groups for patients according to their propensity to adhere to a medication prescription The “Adherence Estimator™” device of the present invention comprises an incremented scale of potential total scores, a prescription survey having questions directed to assessing a patient's beliefs in respect to no more than three domains, the three domains being commitment, concerns and cost, a response recording tool, a scoring matrix and an interpretation tool Embodiments of the invention, which may be implemented in electronic or non-electronic forms, automatically score and interpret responses to the prescription survey questions in order to determine and assign patients to a high risk group, a medium risk group or a low risk group Non-electronic devices of the invention may be constructed from a variety of materials, including without limitation, paper, paper-based products, plastic, wood or metal.
Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. The compounds have 3 cyclic groups connected by single bonds, as for example triphenyl, which are attached directly to the ring of formula I or attached at the position B.
Type:
Application
Filed:
March 28, 2011
Publication date:
July 21, 2011
Applicant:
Merck Sharp & Dohme Corp.
Inventors:
Amjad ALI, Zhijian Lu, Peter J. Sinclair, Yi-Heng Chen, Cameron J. Smith, Hong Li