Patents Assigned to Elan Pharmaceuticals, Inc.
  • ?-secretase enzyme compositions and methods
    Patent number: 7252963
    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: March 25, 2005
    Date of Patent: August 7, 2007
    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
  • Acetyl 2-hydroxy-1, 3-diaminoalkanes
    Patent number: 7244725
    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: September 10, 2003
    Date of Patent: July 17, 2007
    Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
    Inventors: Varghese John, Michel Maillard, James P. Beck, Eric T. Baldwin, Robert Hughes, Shon R. Pulley, Ruth TenBrink
  • Modified BACE
    Patent number: 7244606
    Abstract: The present invention relates to recombinant human BACE polypeptides. More particularly, the invention relates to recombinant human BACE polypeptides that have a modified amino acid sequence at position 33 of the BACE sequence, as well as to polynucleotides, expression vectors, host cells, and methods for producing the modified recombinant human BACE polypeptides.
    Type: Grant
    Filed: October 31, 2005
    Date of Patent: July 17, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Kuo-Chen Chou, W. Jeffrey Howe
  • 4-Bromo-5-(2-chloro-benzoylamino)-1h-pyrazole-3-carboxylic acid (1-aminocarbonyl)eth-1-yl) amide derivatives and related compounds as bradykinin b1 receptor antagonists for the treatment of inflammatory diseases
    Publication number: 20070161633
    Abstract: Disclosed are compounds of formulae (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. Wherein Z is selected from O, S and NH; Q of formula (III) and the other substituents are as defined in claim 1.
    Type: Application
    Filed: April 30, 2004
    Publication date: July 12, 2007
    Applicant: Elan Pharmaceuticals, Inc.
    Inventors: Jay Tung, Albert Garofalo, Michael Pleiss, Jing Wu, David Wone, Ashley Guinn, Darren Dressen, Jennifer Marugg, Martin Neitzel
  • Beta immunogenic peptide carrier conjugates and methods of producing same
    Publication number: 20070161088
    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: December 17, 2004
    Publication date: July 12, 2007
    Applicants: ELAN PHARMACEUTICALS, INC., WYETH
    Inventors: Rasappa Arumugham, A. Krishana Prasad
  • Carbamyloxy compounds which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 7229970
    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: May 13, 2005
    Date of Patent: June 12, 2007
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Eugene D. Thorsett, Christopher M. Semko, Dimitrios Sarantakis, Michael A. Pleiss, Anthony Kreft, Andrei W. Konradi, Francine S. Grant, Darren B. Dressen, Susan Ashwell, Reinhardt B. Baudy, Louis J. Lombardo
  • Beta-amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4
    Patent number: 7223762
    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: April 14, 2005
    Date of Patent: May 29, 2007
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Andrei W. Konradi, Michael A. Pliess, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher M. Semko, Ying-Zi Xu
  • Benzamide 2-hydroxy-3-diaminoalkanes
    Patent number: 7223774
    Abstract: The present invention relates to 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 also useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.
    Type: Grant
    Filed: April 21, 2004
    Date of Patent: May 29, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Jose Aquino, Varghese John, John Tucker, Roy Hom, Shon Pulley, Ruth Tenbrink
  • N-substituted benzene sulfonamides
    Patent number: 7208488
    Abstract: Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. In Formula (I), R1, R2, R3, R4, R3?, R10 and R11 are as described herein. The invention also encompasses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of treating cognitive disorders using compounds of Formula (I).
    Type: Grant
    Filed: October 29, 2004
    Date of Patent: April 24, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Martin Neitzel, Michael S. Dappen, Jennifer Marugg
  • Pyrimidine hydantoin analogues which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 7205310
    Abstract: Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. 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: April 29, 2005
    Date of Patent: April 17, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Andrei W. Konradi, Frank Stappenbeck, Michael A. Pleiss, Christopher Semko, Jenifer L. Smith
  • Testing compounds for effects on synaptophysin in transgenic mice expressing an Alzheimer's disease FAD DNA sequence
    Patent number: 7186881
    Abstract: The construction of transgenic animal models of human Alzheimer's disease, and methods of using the models to screen potential Alzhe## disease therapeutics, are described. The models are characterized by pathologies similar to pathologies observed in Alzheimer's disease, based on expression of all three forms of the ?-amyloid precursor protein (APP), APP695, APP751, and APP770, as well as various point mutations based on naturally occurring mutations, such as the London and Indiana familial Alzheimer's disease (FAD) mutations at amino acid 717, predicted mutations in the APP gene, and truncated forms of APP that contain the A? region. Animal cells can be isolated from the transgenic animals or prepared using the same constructs with standard techniques such as lipofection or electroporation.
    Type: Grant
    Filed: December 23, 2003
    Date of Patent: March 6, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Kate Dora Games, Dale B. Schenk, Lisa C. McConlogue, Peter A. Seubert, Russell E. Rydel
  • Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists
    Patent number: 7183281
    Abstract: Disclosed are sulfonylquinoxalone derivatives of the general formula: These compounds are useful as bradykinin antagonists.
    Type: Grant
    Filed: May 2, 2003
    Date of Patent: February 27, 2007
    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
  • Monitoring APP cleavage in transgenic rodents comprising an APP-Swedish mutation
    Patent number: 7179953
    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: June 27, 2003
    Date of Patent: February 20, 2007
    Assignees: Elan Pharmaceuticals, Inc., Eli Lilly and Company
    Inventors: Lisa C. McConlogue, Jun Zhao, Sukanto Sinha
  • N,N?-substituted-1,3-diamino-2-hydroxypropane derivatives
    Patent number: 7176242
    Abstract: Disclosed are compounds of the formula wherein the variables RN, RC, R1, R25, R2, and R3 are as defined herein. These compounds have activity as inhibitors of beta-secretase and are therefore useful in treating a variety of discorders such as Alzheimer's Disease.
    Type: Grant
    Filed: November 8, 2002
    Date of Patent: February 13, 2007
    Assignees: Elan Pharmaceuticals, Inc., Pharmacia & Upjohn Company
    Inventors: Varghese John, Michel Maillard, Barbara Jagodzinska, James Beck, Andrea Gailunas, John Freskos, John Mickelson, Lakshman Samala, Jennifer Sealy, Ruth TenBrink, Lawrence Fang, Roy Hom
  • Tetrapeptide inhibitors of ?-secretase
    Patent number: 7169759
    Abstract: Statine-derived peptide inhibitors of the ?-secretase enzyme are provided which are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A? peptide in a mammal. The compounds of the invention provide useful methods of treatment by administration of these inhibitors to reduce A? peptide formation and pharmaceutical compositions.
    Type: Grant
    Filed: June 15, 2000
    Date of Patent: January 30, 2007
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Varghese John, Jay Tung, Lawrence Fang, Shumeye S. Mamo
  • Compounds which inhibit leukocyte adhesion mediated by VLA-4
    Patent number: 7166580
    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: October 7, 2002
    Date of Patent: January 23, 2007
    Assignees: Elan Pharmaceuticals, Inc., Wyeth
    Inventors: Michael S. Dappen, Darren B. Dressen, Francine S. Grant, Michael A. Pleiss, Cynthia Y. Robinson, Dimitrios Sarantakis, Eugene D. Thorsett
  • Truncated fragments of alpha-synuclein in Lewy Body Disease
    Publication number: 20060259986
    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: Application
    Filed: July 29, 2005
    Publication date: November 16, 2006
    Applicant: Elan Pharmaceuticals, Inc.
    Inventors: Tamie Chilcote, Jason Goldstein, John Anderson, Donald Walker
  • Heterocyclic compounds which inhibit leukocyte adhesion mediated by ?integrins
    Patent number: 7135477
    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: May 27, 2003
    Date of Patent: November 14, 2006
    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
  • Methods to treat alzheimer's disease
    Patent number: 7119085
    Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: October 10, 2006
    Assignee: Elan Pharmaceuticals, Inc.
    Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
  • Methods and compounds for inhibiting beta-amyloid peptide release and/or its synthesis
    Publication number: 20060223761
    Abstract: Disclosed are compounds which inhibit ?-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease Also disclosed pharmaceutical compositions comprising a compound which inhibits ?-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
    Type: Application
    Filed: February 2, 2004
    Publication date: October 5, 2006
    Applicants: Elan Pharmaceuticals, Inc., Eli Lilly & Company
    Inventors: James Audia, Thomas Britton, James Droste, Beverly Folmer, George Huffman, Varghese John, Lee Latimer, Thomas Mabry, Jeffrey Nissen, Warren Porter, Jon Reel, Eugene Thorsett, Jay Tung, Jing Wu, Clark Eid, William Scott