Abstract: The present invention is macrocycles of the formula (X): for treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme for 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:
August 19, 2005
Date of Patent:
November 25, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Shon R. Pulley, James P. Beck, Ruth E. TenBrink, Jon S. Jacobs
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 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 compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
December 11, 2002
Date of Patent:
November 18, 2008
Assignees:
Elan Pharmaceuticals, Inc., Wyeth
Inventors:
Francine S. Grant, Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett
Abstract: The x-ray crystal structure of BACE or BACE-like proteins is useful for solving the structure of other molecules or molecular complexes, and identifying and/or designing potential modifiers of BACE activity.
Type:
Grant
Filed:
May 9, 2003
Date of Patent:
October 28, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Timothy E. Benson, Daisy Danielle Woods, Donald Bryan Prince
Abstract: Disclosed are compounds that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
Type:
Grant
Filed:
April 30, 2004
Date of Patent:
October 7, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Jay S. Tung, Albert W. Garofalo, Michael A. Pleiss, Jing Wu, David W. G. Wone, Ashley C. Guinn, Darren B. Dressen, R. Jeffrey Neitz, Jennifer Marugg, Martin Neitzel
Abstract: Disclosed are various forms of an active, isolated ?-secretase enzyme in purified and recombinant form. This enzyme is implicated in the production of amyloid plaque components which accumulate in the brains of individuals afflicted with Alzheimer's disease. Recombinant cells that produce this enzyme either alone or in combination with some of its natural substrates (?-APPwt and ?-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate ?-secretase. Inhibitors of ?-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease.
Type:
Grant
Filed:
February 28, 2005
Date of Patent:
September 23, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
John P. Anderson, Guriqbal Basi, Minh Tam Doan, Normand Frigon, Varghese John, Michael Power, Sukanto Sinha, Gwen Tatsuno, Jay Tung, Shuwen Wang, Lisa McConlogue
Abstract: This invention provides methods useful in aiding in the diagnosis of Alzheimer's disease. The methods involve measuring the amount of amyloid-? peptide (x??41) in the cerebrospinal fluid of a patient. High levels of the peptide generally are inconsistent with a diagnosis of Alzheimer's. Low levels of the peptide are consistent with the disease and, with other tests, can provide a positive diagnosis. Other methods involve measuring the amounts of both A?(x??41) and tau. Low levels of A?(x??41) and high levels of tau are a positive indicator of Alzheimer's disease, while high levels of A?(x??41) and low levels of tau are a negative indication of Alzheimer's disease.
Type:
Grant
Filed:
June 6, 1995
Date of Patent:
September 23, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Peter A. Seubert, Carmen Vigo-Pelfrey, Dale B. Schenk, Robin Barbour
Abstract: Disclosed are compounds which bind ?4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, preferably VLA-4. Such compounds 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 compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
September 26, 2006
Date of Patent:
September 23, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupi, Jenifer Smith, Michael A. Pleiss, Eugene D. Thorsett
Abstract: Disclosed are compounds of formula I and II that are bradykinin B1 receptor antagonists and are useful for treating diseases, or relieving adverse symptoms associated with disease conditions, in mammals mediated by bradykinin B1 receptor. Certain of the compounds exhibit increased potency and are also expected to exhibit increased duration of action.
Type:
Grant
Filed:
April 30, 2004
Date of Patent:
August 26, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Jay S. Tung, Albert W. Garofalo, Michael A. Pleiss, Jing Wu, David W. G. Wone, Ashley C. Guinn, Darren B. Dressen, R. Jeffrey Neitz, Jennifer Marugg, Martin Neitzel
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:
August 20, 2007
Publication date:
July 24, 2008
Applicants:
Elan Pharmaceuticals, Inc., The Regents of the University of California
Inventors:
Dale B. Schenk, Kate Dora Games, Manuel J. Buttini, Tamie J. Chilcote, Edward Rockenstein, Eliezar Masliah
Abstract: The invention provides agents and methods for treatment of diseases associated with Lewy body diseases (LBDs) in the brain of a patient. Preferred agents include inhibitors of PLK2 and GRK6 kinases.
Type:
Application
Filed:
January 30, 2007
Publication date:
July 3, 2008
Applicant:
Elan Pharmaceuticals, Inc.
Inventors:
Tami J. Chilcote, Kelly Banducci, Normand L. Frigon, Guriqbal S. Basi, John P. Anderson, Jason Goldstein, Irene Griswold-Prenner, David Chereau
Abstract: The present invention is directed to methods of producing conjugates of A? peptide immunogens with protein/polypeptide carrier molecules, which are useful as immunogens, wherein peptide immunogens are conjugated to protein carriers via activated functional groups on amino acid residues of the carrier or of the optionally attached linker molecule, and wherein any unconjugated reactive functional groups on amino acid residues are inactivated via capping, thus retaining the immunological functionality of the carrier molecule, but reducing the propensity for undesirable reactions that could render the conjugate less safe or effective. Furthermore, the invention also relates to such immunogenic products and immunogenic compositions containing such immunogenic products made by such methods.
Type:
Application
Filed:
August 20, 2007
Publication date:
June 19, 2008
Applicants:
Elan Pharmaceuticals, Inc., Wyeth
Inventors:
Rasappa G. Arumugham, A. Krishna Prasad
Abstract: The invention relates to novel compounds and methods of treating diseases, disorders, and conditions associated with amyloidosis. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.
Type:
Grant
Filed:
July 11, 2005
Date of Patent:
June 10, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Varghese John, Michel Maillard, Barbara Jagodzinska, Jose Aquino, Gary Probst, Jay Tung
Abstract: Disclosed are certain 3-(heteroaryl)alanine derivatives which bind VLA-4 and inhibit leukocyte adhesion mediated by VLA-4. Such compounds 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 compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.
Type:
Grant
Filed:
July 23, 2004
Date of Patent:
April 29, 2008
Assignees:
Elan Pharmaceuticals, Inc., Wyeth
Inventors:
Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Darren B. Dressen, Francine S. Farouz, Christopher Semko, Ying-Zi Xu, Frank Stappenbeck
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.
Abstract: The application identifies novel fragments of alpha-synuclein in patients with Lewy Body Disease (LBD) and transgenic animal models thereof. These diseases are characterized by aggregations of alpha-synuclein. The fragments have a truncated C-terminus relative to full-length alpha-synuclein. Some fragments are characterized by a molecular weight of about 12 kDa as determined by SDS gel electrophoresis in tricine buffer and a truncation of at least ten contiguous amino acids from the C-terminus of natural alpha-synuclein. The site of cleavage preferably occurs after residue 117 and before residue 126 of natural alpha-synuclein. The identification of these novel fragments of alpha-synuclein has a number of application in for example, drug discovery, diagnostics, therapeutics, and transgenic animals.
Type:
Grant
Filed:
July 29, 2005
Date of Patent:
April 15, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Tamie J Chilcote, Jason Goldstein, John P Anderson, Donald Walker
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:
November 26, 2003
Date of Patent:
April 1, 2008
Assignees:
Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
Abstract: The invention provides N-cyclic sulfonamido compounds and salts of Formula I: wherein A is as described in the specification and R1 and R2 combine to form a [3.3.1] or a [3.2.1] ring system, where the nitrogen is attached to the two bridgehead carbons, and the [3.3.1] or [3.2.1] ring systems are optionally fused with an heteroaryl or heterocycloalkyl ring. Compounds of Formula I are useful in treating or preventing cognitive disorders, such as Alzheimer's Disease. The invention also encompasses pharmaceutical compositions comprising compounds of Formula I, methods of treating cognitive disorders, such as Alzheimer's disease, and the intermediates useful in preparing the compounds of Formula I.
Type:
Grant
Filed:
August 18, 2006
Date of Patent:
March 18, 2008
Assignee:
Elan Pharmaceuticals, Inc.
Inventors:
Simeon Bowers, Albert W. Garofalo, Roy K. Hom, Andrei W. Konradi, Matthew N. Mattson, Martin L. Neitzel, Christopher M. Semko, Anh P. Truong, Jing Wu, Ying-zi Xu
Abstract: The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure: where Z is CR or N, and R1, R2 and R3 are as described in the specification.
Type:
Grant
Filed:
November 19, 2002
Date of Patent:
March 4, 2008
Assignees:
Pharmacia & Upjohn Company, Elan Pharmaceuticals, Inc.
Inventors:
Joseph B. Moon, Shon R. Pulley, Daniel H. Rich, David L. Brown, Barbara Jagodzinska, Varghese John, John Jacobs