Assignee: Elan Pharmaceuticals, Inc.

Location: South San Francisco, CA
No. of patents: 125

Number	Title	Issue Date
8158642	Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4 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, su...	04/17/2012
8138272	Preparation of polymer conjugates of therapeutic, agricultural, and food additive compounds This invention provides an improved synthesis of polymer conjugates of formula (I), of agricultural, therapeutic, and food additive compounds. In particular, a process is described for the preparation of conjugates by treat...	03/20/2012
8124350	Methods and products for evaluating an immune response to a therapeutic protein The invention relates to methods and products for the identification of a clinically significant immune response in subjects treated with a therapeutic protein. A first aspect of the invention relates to methods and compositions for identifying a clinically signific...	02/28/2012
7993627	Methods for determining whether a compound alters the amount of at least one αβ (X-41) peptide and the amount of either total αβ or at least one αβ (X-40) peptide produced by a non-human mammal This invention provides methods of screening compounds for their ability to alter the production of Aβ(x≧41) alone or in combination with Aβ(x≦40). The methods involve administering compounds to cells, specifically measuring the amounts of Aβ(x≦40) and Aβ(...	08/09/2011
7977368	Pyrazolopyrrolidines as inhibitors of gamma secretase The invention provides compounds of Formula I wherein A, Y, R1, R1a, R2, and R2a are as described in the specification. Compounds of Formula I are useful in treating and/or preven...	07/12/2011
7977316	Prevention and treatment of amyloidogenic diseases 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...	07/12/2011
7968547	Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 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, su...	06/28/2011
7939657	N-substituted benzene sulfonamides 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′,...	05/10/2011
7928203	Chimeric, humanized, or human antibody 2A4 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 aggre...	04/19/2011
7919088	Treatment and delay of onset of synucleinopathic and amyloidogenic disease 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 ...	04/05/2011
7910333	Antibodies to alpha-synuclein The invention provides methods for detecting alpha-synuclein. The invention also identifies preferred epitopes of alpha synuclein for use in such detection, and provides antibodies specifically binding to such epitopes. ...	03/22/2011
7906556	Methods of treating amyloidosis using cyclopropyl derivative aspartyl protease inhibitors 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. ...	03/15/2011
7901683	Methods of inhibiting amyloid toxicity The present invention features methods and compositions for inhibiting amyloidogenic protein toxicity, inhibiting formation of an amyloidogenic protein deposit and/or treating amyloidogenic diseases by administering a pharmaceutically effective amount of one or more...	03/08/2011
7888291	Substrates and assays for β-secretase The present invention is directed to novel substrates for Hu-Asp. More particularly, the invention provides peptide substrates and fusion polypeptide substrates comprising a β-secretase cleavage site. Methods and compositions for making and using the peptides are d...	02/15/2011
7858642	Substituted hydroxyethylamine aspartyl protease inhibitors The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal...	12/28/2010
7829303	Ligand screening method using a crystal of beta secretase 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. ...	11/09/2010
7829087	Methods of treating cognitive impairment Methods and compositions for suppressing amyloid-mediated inhibition of long-term potentiation (LTP) are provided. ...	11/09/2010
7820687	Pyrimidinyl sulfonamide compounds which inhibit leukocyte adhesion mediated by VLA-4 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 a...	10/26/2010
7816114	Methods of using crystals of beta amyloid cleaving enzyme (BACE) Methods of using monoclinic crystals of human beta-secretase (BACE) having unit cell dimensions of a, b, and c, wherein a is about 81±20 Å to about 101 Å, b is 103±20 Å, c is 100±20 Å, and α=γ=90°, and β is 105°±10° for crystals of symmetry P2...	10/19/2010
7812123	Alzheimer's disease secretase The present invention provides the enzyme and enzymatic procedures for cleaving the β secretase cleavage site of the APP protein and associated nucleic acids, peptides, vectors, cells and cell isolates and assays. ...	10/12/2010
7811769	Methods for aiding in the diagnosis of Alzheimer's disease by measuring amyloid-β peptide (x-≧41) and tau This invention provides methods useful in aiding in the diagnosis of Alzheimer's disease. The methods involve measuring the amount of amyloid-β peptide (x−≧41) in the cerebrospinal fluid of a patient. High levels of the peptide generally are inconsistent with a...	10/12/2010
7807167	Administration of agents for the treatment of inflammation A method of chronically reducing a patient's pathological inflammation via the administration of an agent that specifically binds to an alpha-4 integrin or a dimer comprising an alpha-4 integrin is disclosed. The agent provided must have a binding affinity such that...	10/05/2010
7806980	Method for crystallizing human beta secretase in complex with an inhibitor 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, an...	10/05/2010
7803739	Substrates and assays for β-secretase The present invention is directed to novel substrates for Hu-Asp. More particularly, the invention provides peptide substrates and fusion polypeptide substrates comprising a β-secretase cleavage site. Methods and compositions for making and using the peptides are d...	09/28/2010
7763632	Pyrimidinyl amide compounds which inhibit leukocyte adhesion mediated by VLA-4 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 as...	07/27/2010
7759382	Acylated amino acid amidyl pyrazoles and related compounds This invention is directed to acylated amino acid amidyl pyrazoles and related compounds of Formula I. The invention is also directed to a pharmaceutical formation comprising such compound or in a pharmaceutically acceptable salt form thereof. The invention is furth...	07/20/2010
7754712	Bridged N-cyclic sulfonamido inhibitors of gamma secretase 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 ni...	07/13/2010
7745454	Alpha amino acid derivatives-inhibitors of leukocyte adhesion mediated by VLA-4 Disclosed are certain alpha amino acid 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...	06/29/2010
7741328	Heteroaryl, heterocyclic and aryl compounds which inhibit leukocyte adhesion mediated by VLA-4 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, su...	06/22/2010
7732609	5-(arylsulfonyl)-pyrazolopiperidines The invention provides N-cyclic sulfonamido compounds of Formula I wherein A, B, R1, R1a, R2, R2a, R3 and R3a are as described in the specification. Compound...	06/08/2010
7732183	Method for refolding enzymes The invention provides methods for efficient recombinant expression, refolding, and purification of Beta-site APP cleaving enzyme (BACE) polypeptides. In various aspects, the method includes the steps of expressing a recombinant construct in bacteria, dissolving inc...	06/08/2010
7727996	Carbamate compounds which inhibit leukocyte adhesion mediated by VLA-4 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, su...	06/01/2010
7718413	Glycosylation variants of BACE Human BACE polypeptides having modifications to the N-linked glycosylation sites including one or more of the following amino acid substitutions: S174I, N223A, N153Q and N354S. DNA sequences, vectors, and host cells for producing the polypeptides. Crystalline protei...	05/18/2010
7700309	Methods for aiding in the diagnosis of alzheimer's disease by measuring amyloid-β peptide (X->41) and tau This invention provides methods useful in aiding in the diagnosis of Alzheimer's disease. The methods involve measuring the amount of amyloid-β peptide (x-≧41) in the cerebrospinal fluid of a patient. High levels of the peptide generally are inconsistent with a d...	04/20/2010
7674599	Methods of using antibodies to detect alpha-synuclein in fluid samples The invention provides methods for detecting alpha-synuclein. The invention also identifies preferred epitopes of alpha synuclein for use in such detection, and provides antibodies specifically binding to such epitopes. ...	03/09/2010
7674597	Signaling intermediates in an in vitro model of Alzheimer's disease The invention provides a novel human protein, FISH adaptor protein, involved in amyloid β-protein-mediated cell death. Also provided are methods for modulating amyloid β-protein-mediated cell death using agents that interfere with the activity of FISH adaptor prot...	03/09/2010
7645780	Acetyl 2-hydroxy-1, 3-diaminoalkanes 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 ar...	01/12/2010
7635775	Sulfonylquinoxalone derivatives and related compounds as bradykinin antagonists Disclosed are sulfonylquinoxalone acetamide derivatives useful as bradykinin antagonists. ...	12/22/2009
7608749	Monitoring APP cleavage in transgenic rodents comprising an APP Swedish mutation The invention provides transgenic non-human animals and transgenic non-human mammalian cells harboring a transgene encoding an APP polypeptide comprising the Swedish mutation. ...	10/27/2009
7601528	Crystallization and structure determination of glycosylated human beta secretase, an enzyme implicated in alzheimer's disease 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, an...	10/13/2009

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Assignee: Elan Pharmaceuticals, Inc.