Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLs, and tauphosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ? 1-42.
Type:
Application
Filed:
October 21, 2005
Publication date:
July 24, 2008
Applicants:
Merck & Co., Inc., Northwestern University
Inventors:
Paul Acton, Zhigiang An, Andrew J. Bett, Robert Breese, Elizabeth Chen Dodson, Gene Kinney, William L. Klein, Mary P. Lambert, Xiaoping Liang, Paul Shughrue, William R. Strohl, Kirsten Viola, Lei Chang
Abstract: Compounds of structural formula as herein defined are disclosed as useful in a method for modulating the androgen receptor in a tissue selective manner in a patient in need of such modulation, as well as in a method of activating the function of the androgen receptor in a patient, and in particular the method wherein the function of the androgen receptor is blocked in the prostate of a male patient or in the uterus of a female patient and activated in bone and/or muscle tissue.
Type:
Grant
Filed:
September 27, 2002
Date of Patent:
July 22, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Jiabing Wang, Mark E. Duggan, David B. Whitman
Abstract: The present invention is directed to compounds which contain a five-membered heterocyclic ring fused to a substituted pyrazine 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.
Type:
Grant
Filed:
October 24, 2003
Date of Patent:
July 15, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, Craig W. Lindsley, Zhijian Zhao
Abstract: The present invention provides methods for the use of visible and/or near-infrared spectroscopic methodology to monitor and control processes for the generation of particles, including processes that provide for a reduction in particle size and processes that result in an increase in particle size. One embodiment of the present invention employs visible and/or near-infrared diffuse reflectance spectroscopy to monitor particle size. The present invention is particularly useful for monitoring particle size of optically dense samples and is further useful for monitoring the endpoint of particle generation processes. In contrast to methods known in the art, the present invention is especially useful for on-line monitoring of particle size.
Type:
Grant
Filed:
August 23, 2002
Date of Patent:
July 15, 2008
Assignee:
Merck & Co. Inc.
Inventors:
Steven M. Arrivo, William E. Bowen, Robert A. Reed, John P. Higgins
Abstract: 8-Hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds are inhibitors of HIV integrase and inhibitors of HIV replication. More particularly, the compounds are of Formula (I): wherein R1, R2, R3, R4, R5 and R6 are defined herein. The compounds are useful in the prevention and treatment of infection by ITV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing, treating or delaying the onset of AIDS and methods of preventing or treating infection by HIV are described.
Abstract: The present invention is directed to compounds comprising a 2,3-diphenylquinoxaline moiety which inhibit the activity of Akt, a serine/threonine protein kinase.
Abstract: Substituted aryl and heteroaryl derivatives are disclosed. The compounds are useful for treating type 2 diabetes and related conditions. Pharmaceutical compositions and methods of treatment are also included.
Type:
Application
Filed:
March 17, 2006
Publication date:
July 3, 2008
Applicant:
MERCK & CO., INC.
Inventors:
John E. Stelmach, Keith G. Rosauer, Emma R. Parmee, James R. Tata
Abstract: Pyrrole compounds of Formula (I): and pharmaceutically acceptable salts thereof (where A, B, R11, R12, R13, W, X, Y and Z are as defined herein), which are substituted directly, or by a bridge, with i) a heteroaryl moiety containing N adjacent to the point of connection of the heteroaryl and ii) another heteroaryl or aryl ring, with at least one of the rings being further substituted with another ring, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, panic, and bipolar disorder, as well as in the treatment of pain, Parkinson's disease, cognitive dysfunction, epilepsy, circadian rhythm disorders, drug addiction, drug abuse, drug withdrawal, obesity and other diseases
Type:
Grant
Filed:
March 31, 2004
Date of Patent:
July 1, 2008
Assignee:
Merck & Co. Inc.
Inventors:
Nicholas D. P. Cosford, Dehua Huang, Jeffrey R. Roppe, Nicholas D. Smith, Lida R. Tehrani
Abstract: N-aryl arylsulfonamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
Type:
Grant
Filed:
June 30, 2004
Date of Patent:
July 1, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, John Jin Lim, Dai-shi Su, Michael R. Wood
Abstract: The present invention is directed to compounds of the formula (1) Wherein A, B, D, X, Y, n, R1, R3, R4, R5, R15, R16, R17, R18 and the dashed line are as defined herein which are useful as modulators of chemokine receptor activity.
Type:
Grant
Filed:
March 12, 2004
Date of Patent:
July 1, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Stephen D. Goble, Alexander Pasternak, Sander G. Mills, Changyou Zhou, Lihu Yang
Abstract: Indoles having aryloxyalkanoic acid substituents or arylalkanoic acid substituents are agonists or partial agonists of PPAR gamma and are useful in the treatment and control of hyperglycemia that is symptomatic of type II diabetes, as well as dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.
Type:
Grant
Filed:
August 28, 2003
Date of Patent:
July 1, 2008
Assignee:
Merck & Co., Inc.
Inventors:
John J. Acton, III, Peter T. Meinke, Harold B. Wood, Regina M. Black
Abstract: The present invention relates to oxadiazoles 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:
Application
Filed:
August 15, 2005
Publication date:
June 26, 2008
Applicant:
MERCK & CO., INC.
Inventors:
Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio
Abstract: The present invention is directed to compounds of structural formula (I) 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.
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, including alcohol and nicotine addiction, 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:
October 27, 2004
Date of Patent:
June 24, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Shrenik K. Shah, Quang T. Truong, Hongbo Qi, William K. Hagmann
Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.
Type:
Grant
Filed:
October 24, 2003
Date of Patent:
June 24, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
Abstract: The present invention is directed to compounds of Formula I: 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.
Type:
Grant
Filed:
February 9, 2005
Date of Patent:
June 24, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Theresa M. Williams, Christopher S. Burgey, Thomas J. Tucker, Craig A. Stump, Ian M. Bell
Abstract: The present invention is directed to 3-amino-4-phenylbutanoic acid derivatives 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:
Grant
Filed:
January 27, 2004
Date of Patent:
June 17, 2008
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Charles G. Caldwell, Joseph L. Duffy, Robert J. Mathvink, Liping Wang, Ann E. Weber
Abstract: Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein Z, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Type:
Application
Filed:
March 4, 2005
Publication date:
June 12, 2008
Applicant:
MERCK & CO., INC.
Inventors:
Matthew M. Morrissette, Peter D. Williams, John S. Wai, Thorsten E. Fisher, Terry A. Lyle
Abstract: A method of safely and specifically treating the combined metabolic disturbances of insulin resistance and visceral adiposity in male subject with visceral adiposity, metabolic syndrome (also known as the ‘insulin resistance syndrome’, and ‘syndrome X’), type II diabetes, or insulin resistance by administering a 5-alpha reductase inhibiting compound of structural formula I, II, III, or IV is disclosed. The method is also concerned with the use of the 5alpha reductase inhibiting compound together with antidiabetic agents, lipid lowering agents, antihypertensive agents, antiobesity agents, testosterone, testosterone precursors, testosterone prodrugs, testosterone analogs, and other androgen receptor agonists for treating visceral adiposity, metabolic syndrome, type II diabetes and insulin resistance in men.