Abstract: A novel crystalline anhydrous toluenesulfonic acid salt form of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety is stable and non-hygroscopic. The crystalline salt form is useful for making pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.
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, 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, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
Type:
Grant
Filed:
April 8, 2003
Date of Patent:
February 23, 2010
Assignee:
Merck & Co., Inc.
Inventors:
Laurie A. Castonguay, William K. Hagmann, Linus S. Lin, Shrenik K. Shah
Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: The present invention provides methods for identifying a modulator of glucocorticoid receptor activity. In one embodiment, the methods include the steps of (a) contacting neuron-like cells, in vitro, with a chemical agent; (b) measuring the expression of a member, or group of members, of a group of genes (as defined herein) in the neuron-like cells contacted with the chemical agent; and (c) determining whether the chemical agent significantly alters the expression of the member, or group of members, of the group of genes, thereby determining whether the chemical agent is likely to be a modulator of glucocorticoid receptor activity. In another embodiment, an in vivo method for identifying a modulator of glucocorticoid receptor activity is provided.
Type:
Application
Filed:
October 14, 2009
Publication date:
February 18, 2010
Applicants:
ROSETTA INPHARMATICS LLC, MERCK & CO., INC.
Inventors:
David J. Stone, Janet E. Clark, Edward C. Hayes, III
Abstract: The present invention is directed to a process for preparing certain hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The compounds are useful in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.
Type:
Application
Filed:
July 7, 2006
Publication date:
February 11, 2010
Applicant:
MERCK & CO., INC.
Inventors:
Jeffrey T. Kuethe, Jingjun Yin, Mark A. Huffman, Michel Journet
Abstract: The present invention encompasses compounds of Formula I: as well as the pharmaceutically acceptable salts thereof. The compounds are S1P1/Edg1 receptor agonists and thus have immunosuppressive, anti-inflammatory and hemostatic activities by modulating leukocyte trafficking, sequestering lymphocytes in secondary lymphoid tissues, and enhancing vascular integrity. The invention is also directed to pharmaceutical compositions containing such compounds and methods of treatment or prevention.
Abstract: The present invention is directed to 2-substituted proline bis-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:
Application
Filed:
July 13, 2007
Publication date:
February 4, 2010
Applicant:
MERCK & CO., INC.
Inventors:
Christopher D. Cox, David B. Whitman, Michael J. Breslin
Abstract: Compounds having the structures 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: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
Type:
Grant
Filed:
July 1, 2005
Date of Patent:
January 26, 2010
Assignee:
Merck & Co., Inc.
Inventors:
Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
Abstract: A method for identifying a quantitative trait loci for a complex trait that is exhibited by a plurality of organisms in a population. The population is divided into a plurality of sub-populations using a classification scheme. Depending on what is known about the population, either a supervised or unsupervised classification is used. The classification scheme is derived from a plurality of cellular constituent measurements obtained from each organism in the population. For each sub-population in the plurality of sub-populations, a quantitative genetic analysis is performed on the sub-population in order to identify one or more quantitative trait loci for the complex trait.
Abstract: Pyrazole amides 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:
July 1, 2005
Date of Patent:
January 19, 2010
Assignee:
Merck & Co., Inc.
Inventors:
Teresa Beeson, Linda Brockunier, Emma R. Parmee, Subharekha Raghavan
Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention is also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyridine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
Abstract: Bicyclic compounds containing a phenyl or pyridyl ring fused to a cycloalkyl or heterocyclic ring, to which is attached a 5-membered heterocyclic ring, including pharmaceutically acceptable salts and prodrugs thereof, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly 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:
January 30, 2006
Publication date:
December 17, 2009
Applicant:
MERCK & CO., INC.
Inventors:
Min Ge, Lihu Yang, Changyou Zhou, Songnian Lin, Haifeng Tang, Eric Dean Cline, Sunita Malkani
Abstract: The present invention provides ribonucleoside 2?,3?-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2?,3?-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection.
Type:
Grant
Filed:
August 4, 2006
Date of Patent:
December 15, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Gabor Butora, Kenneth Alan Koeplinger, Malcolm MacCoss, Daniel R. McMasters, David B. Olsen, Lihu Yang
Abstract: The present invention relates to fluorinated aminoalkyl-4-oxo-3,4-dihydropyrido[3,4-d]pyrimidine derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Abstract: Compounds of Formula I: (where variables R1, R2, R3, R7, G, J, Q, T, W, X and Y 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, and 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:
January 13, 2006
Date of Patent:
December 15, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Christopher S. Burgey, Theresa M. Williams, Zhengwu J. Deng, Craig A. Stump
Abstract: The present invention relates to tricyclic pyrazoles according to Formula (I) that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
Type:
Grant
Filed:
June 27, 2005
Date of Patent:
December 15, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Jeffrey M. Bergman, Paul J. Coleman, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, Chunze Li, Lou Anne Neilson, Christy M. Olson, Edward S. Tasber
Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions.
Type:
Application
Filed:
April 3, 2009
Publication date:
December 10, 2009
Applicant:
Merck & Co., Inc.
Inventors:
James McSwiggen, David Morrissey, Roberto Guerciolini, Chandra Vargeese, Vasant Jadhav
Abstract: The present invention relates to pharmaceutical compositions comprising a combination of a particular dipeptidyl peptidase-IV (DPP-IV) inhibitor and a particular cannabinoid CB?1#191 receptor antagonist/inverse agonist, kits containing such combinations and methods of using such compositions for the treatment of diabetes, diabetes associated with obesity, diabetes-related disorders, obesity, and obesity-related disorders.
Type:
Application
Filed:
April 28, 2006
Publication date:
December 10, 2009
Applicant:
MERCK & CO., INC.
Inventors:
John M. Amatruda, Tung M. Fong, David E. Moller, Nancy A. Thornberry
Abstract: The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).
Type:
Grant
Filed:
July 1, 2005
Date of Patent:
December 8, 2009
Assignee:
Merck & Co., Inc.
Inventors:
Kevin R. Campos, Artis Klapars, J. Christopher McWilliams, C. Scott Shultz, Debra J. Wallace, Alex M. Chen, Lisa F. Frey, Andrey V. Peresypkin, Yaling Wang, Robert M. Wenslow, Cheng-Yi Chen