Abstract: Disclosed are compounds of the formula: where variables Z, X, R15, R2, R3, and Rc are defined herein. Compounds disclosed herein are inhibitors of the beta-secretase enzyme and are therefore useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal.
Type:
Grant
Filed:
June 6, 2006
Date of Patent:
January 12, 2010
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth T. TenBrink
Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.
Abstract: Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists.
Type:
Grant
Filed:
May 5, 2006
Date of Patent:
December 22, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Francine S. Grant, Sarah Bartulis, Louis Brogley, Michael S. Dappen, Ramesh Kasar, Mohammed A. Khan, Martin Neitzel, Michael A. Pleiss, Eugene D. Thorsett, John Tucker, Michael Ye, Jon E. Hawkinson
Abstract: Disclosed are pharmaceutical compositions and methods for preventing or treating a number of amyloid diseases, including Alzheimer's disease, prion diseases, familial amyloid neuropathies and the like. The pharmaceutical compositions include immunologically reactive amounts of amyloid fibril components, particularly fibril-forming peptides or proteins. Also disclosed are therapeutic compositions and methods which use immune reagents that react with such fibril components.
Abstract: Disclosed are pharmaceutical compositions and methods for preventing or treating a number of amyloid diseases, including Alzheimer's disease, prion diseases, familial amyloid neuropathies and the like. The pharmaceutical compositions include immunologically reactive amounts of amyloid fibril components, particularly fibril-forming peptides or proteins. Also disclosed are therapeutic compositions and methods which use immune reagents that react with such fibril components.
Abstract: The invention provides transgenic non-human animals and transgenic non-human mammalian cells harboring a transgene encoding an APP polypeptide comprising the Swedish mutation.
Type:
Grant
Filed:
December 20, 2006
Date of Patent:
October 27, 2009
Assignees:
Elan Pharmaceuticals, Inc., Eli Lilly and Company
Inventors:
Lisa C. McConlogue, Jun Zhao, Sukanto Sinha
Abstract: This application relates to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and an antibody to alpha-4 integrin or an immunologically active antigen binding fragment in therapeutically effective amounts. The application also relates generally to methods and compositions for treating rheumatoid arthritis by administering a combination therapy comprising methotrexate and small molecule alpha-4 integrin antagonist that inhibits the alpha-4 integrin (?4 integrin) interaction with VCAM-1. The invention further relates to methods of preparing the compounds and methods of using the compounds and compositions.
Type:
Grant
Filed:
June 25, 2004
Date of Patent:
October 20, 2009
Assignee:
Elan Pharmaceuticals Inc.
Inventors:
Theodore A. Yednock, Stephen B. Freedman, Ivan Lieberburg, Michael A. Pleiss, Andrei W. Konradi, George Shopp, Elizabeth Messersmith
Abstract: An inhibitor bound form of human beta secretase, also known as memapsin 2 and BACE, particularly in a glycosylated form as expressed in Chinese hamster ovary (CHO), HEK293 cells, or in insect cells as part of a Baculovirus expression system has been crystallized, and the three dimensional x-ray crystal structure has been solved to 3.2 ? resolution. The x-ray crystal structure is useful for solving the structure of other molecules or molecular complexes, and designing inhibitors of human beta secretase activity.
Type:
Grant
Filed:
January 25, 2005
Date of Patent:
October 13, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Timothy E. Benson, Jim D. Durbin, D. Bryan Prince
Abstract: Disclosed are conjugates which bind VLA-4. Certain of these conjugates also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such conjugates are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The conjugates can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
January 24, 2005
Date of Patent:
September 29, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Andrei Konradi, Michael A. Pleiss, Jenifer L. Smith, Christopher M. Semko, Chris Vandevert
Abstract: Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
December 7, 2005
Date of Patent:
September 15, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Andrea Gailunas, John A. Tucker, Ruth TenBrink, John Mickelson
Abstract: Provided are methods of determining a resistance-adjusted dosage regimen of an anti-infective agent for treatment of an infection of a mammal by a resistant infective organism, wherein an effective dosage regimen of the anti-infective agent is known for treatment of an infection of the mammal by a susceptible strain of the infective organism. Methods of treating a cefepime resistant bacterial infection in a patient are also provided.
Abstract: The invention provides highthroughput screening assays to identify agents useful for treatment of Parkinson's Disease. In one embodiment the assay includes exposing a plurality of test samples, each containing a test compound and parkin protein, to thermal destabilization conditions and determining parkin ligase activity in the test samples relative to a control sample not containing a test agent. A test agent contained in a test sample in which parkin ligase activity exceeds the ligase activity in said control sample is identified as a candidate compound for treatment of Parkinson's Disease.
Type:
Application
Filed:
January 29, 2009
Publication date:
September 10, 2009
Applicant:
Elan Pharmaceuticals, Inc.
Inventors:
Jennifer A. Johnston, Balazs G. Szoke, Lisa McConlogue
Abstract: The present invention relates to methods for preventing cell death in a subject and their application in the treatment of neurodegenerative diseases and conditions, such as Alzheimer's disease, stroke, Parkinson's disease etc. A method for preventing cell death comprises reducing or inhibiting Pyk2 activity.
Abstract: Disclosed are compounds, which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
February 26, 2007
Date of Patent:
August 25, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Jenifer Smith, Christopher Semko, Ying-Zi Xu, Andrei W. Konradi
Abstract: The present invention relates generally to the field of pharmaceutical formulation of immunoglobulins. Specifically, the present invention relates to stable, lyophilized, high concentration immunoglobulin formulations. This invention is exemplified by a stabilized lyophilized formulation of the recombinant humanized anti-alpha-4 integrin antibody natalizumab.
Type:
Application
Filed:
June 12, 2008
Publication date:
August 20, 2009
Applicant:
Elan Pharmaceuticals, Inc.
Inventors:
Barbara Horsey O'Connor, Shaun E. Buckley, David Burke
Abstract: The invention provides improved agents and methods for treatment of diseases associated with synucleinopathic diseases, including Lewy bodies of alpha-synuclein in the brain of a patient. Such methods entail administering agents that induce a beneficial immunogenic response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease.
Type:
Application
Filed:
February 23, 2007
Publication date:
August 20, 2009
Applicant:
Elan Pharmaceuticals, Inc.
Inventors:
Dale B. Schenk, Kate Dora Games, Manuel J. Buttini, Tamie J. Chilcote, Edward Rockenstein, Eliezar Masliah
Abstract: The application provides for methods and compositions for inhibiting demyelination, promoting remyelination and/or treating paralysis in a subject in need thereof. Preferably, such compositions include immunoglobulins (e.g., antibodies, antibody fragments, and recombinantly produced antibodies or fragments), polypeptides (e.g., soluble forms of the ligand proteins for integrins) and small molecules, which when administered in an effective amount inhibits demyelination and/or promotes remyelination in a patient. The compositions and methods described herein can also utilize other anti-inflammatory agents used to palliate conditions and diseases associated with demyelination.
Type:
Grant
Filed:
January 26, 2004
Date of Patent:
August 18, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Stephen J. Karlik, Michael A. Pleiss, Andrei W. Konradi, Francine S. Farouz, Christopher M. Semko, Darren B. Dressen, Elizabeth Messersmith, Stephen Freedman, Ted Yednock
Abstract: Methods useful for effecting prophylaxis or treatment of amyloidosis, including AA Amyloidosis and AL amyloidosis, by administering peptides comprising neoepitopes, such as AA fragments from a C-terminal region of AA, and antibodies specific for neoepitopes of aggregated amyloid proteins, for example, antibodies specific for the C-terminal region of AA fibrils. Antibodies for inhibition of formation and/or increasing clearance of amyloid deposits in a patient thus effecting prophylaxis or treating amyloid disease.
Type:
Application
Filed:
December 29, 2008
Publication date:
August 13, 2009
Applicant:
Elan Pharmaceuticals, Inc.
Inventors:
Dale B. Schenk, Peter A. Seubert, Jonathan Wall, Jose W. Saldanha
Abstract: The invention provides N-substituted heterocyclic-sulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. Compounds of particular interest are defined by Formula (I), wherein R1, R2, Z and n are as described in the specification. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).
Abstract: The invention provides compounds of formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
Type:
Grant
Filed:
September 10, 2003
Date of Patent:
July 28, 2009
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
James P. Beck, Matthew Drowns, Martha A. Warpehoski