Elan Pharmaceuticals, Inc. Patent applications |
Patent application number | Title | Published |
20150284337 | INHIBITORS OF LRRK2 KINASE ACTIVITY - The present invention provides compounds having a structure according to Formula I: (I) or a salt or solvate thereof, wherein R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease. | 10-08-2015 |
20140243422 | METHODS OF TREATING BEHAVIORAL AND PSYCHIATRIC DISORDERS - The invention relates to the treatment of disorders associated with elevated myo-inositol levels in brain, in particular behavioural and neuropsychiatry disorders such as dementia, mild Alzheimer's disease, mild cognitive impairment or bipolar disorder by administering an effective amount of scyllo-inositol to a subject. | 08-28-2014 |
20140194428 | Combination treatments for bipolar disorders - The invention relates generally to novel compositions and methods comprising a scyllo-inositol compound and one or both of valproic acid compound and lamotrigine. The compositions and methods provide beneficial effects in the treatment of bipolar disorders. | 07-10-2014 |
20140186294 | PHAGOCYTIC ACTIVITY AS A MARKER OF SYNUCLEINOPATHIC DISEASE - The invention provides methods of screening for agents useful in treating or prophylaxis of synucleinopathic disease, methods of diagnosis or prognosis of the same and methods of treatment and prophylaxis. The invention is based in part on the result that cells with phagocytic activity from subjects with synucleinopathic disease have increased levels of alpha synuclein and reduced phagocytic activity and that these processes can be reversed (i.e., synuclein levels decreased and phagocytic levels increased) by treatment with IL-4 among other agents. The increase in phagocytic activity is readily amenable to detection and provides a basis for a screening assay in which an agent is contacted with phagocytic cells and the effect of the agent on phagocytic activity is detected, which is an indicator that the agent has the ability to reduce alpha synuclein levels. | 07-03-2014 |
20140134103 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 05-15-2014 |
20140073788 | Preparation of Polymer Conjugates of Therapeutic, Agricultural, and Food Additive Compounds - Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions. | 03-13-2014 |
20140051655 | METHODS OF TREATING INFLAMMATORY AND AUTOIMMUNE DISEASES WITH ALPHA-4 INHIBITORY COMPOUNDS - Alpha 4 inhibitors are used in treatment of inflammatory and autoimmune diseases, such as multiple sclerosis, Crohn's Disease, rheumatoid arthritis and asthma. Rare occurrences of progressive multifocal leucoencephalopathy during treatment with an alpha-4 agent suggest the possibility that it may be related to such treatment. Monitoring for the JC virus and educating caregivers and patients about the manifestations of progressive multifocal leucoencephalopathy can improve the safety of alpha 4 inhibitor therapy. | 02-20-2014 |
20130338164 | Multimeric VLA-4 Antagonists Comprising Polymers Moieties - 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. | 12-19-2013 |
20130317199 | 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. | 11-28-2013 |
20130252957 | PYRIDINONE ANTAGONISTS OF ALPHA-4 INTEGRINS - The present invention provides compounds that are alpha4 integrin antagonists having a structure according to the following formula: | 09-26-2013 |
20130231335 | INHIBITORS OF POLO-LIKE KINASE - The present invention provides compounds having a structure according to Formula (I): | 09-05-2013 |
20130072663 | Antibodies to Alpha Synuclein - 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. | 03-21-2013 |
20130072494 | INHIBITORS OF JUN N-TERMINAL KINASE - The present disclosure provides inhibitors of c-Jun N-terminal kinases (JNK) having a structure according to the following formula: | 03-21-2013 |
20130059337 | Therapeutic Uses of Humanized Antibodies Against ALPHA-4 Integrin - The invention provides method of treatment using humanized immunoglobulins that specially bind to alpha-4 integrin. The methods are useful for treatment of asthma, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, transplant rejection, graft versus host disease, tumor metastasis, nephritis, atopic dermatitis, psoriasis, myocardial ischemia, and acute leukocyte mediated lung injury. | 03-07-2013 |
20130018187 | Preparation of Polymer Conjugates of Therapeutic, Agricultural, and Food Additive Compounds - Disclosed is a process for preparing polymer conjugates of agricultural, therapeutic, and food additive compounds using Mitsunobu conditions. | 01-17-2013 |
20120329807 | Multimeric VLA-4 Antagonists Comprising Polymers Moieties - 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. | 12-27-2012 |
20120328614 | Immunoglobulin Formulation and Method of Preparation Thereof - A stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, polysorbate 80, a buffer which inhibits polysorbate oxidation is described along with methods of making the preparation. Also described are formulations with high antibody concentrations which maintain fixed volumes and which may be used on patients of variable weight. | 12-27-2012 |
20120321555 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 12-20-2012 |
20120270902 | N-substituted benzene sulfonamides - The invention provides N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. | 10-25-2012 |
20120201842 | PREVENTION AND TREATMENT 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 response against the Lewy body. The methods are particularly useful prophylactic and therapeutic treatment of Parkinson's disease. | 08-09-2012 |
20120195884 | 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. Aspects of the invention relate to methods and compositions for identifying a clinically significant immune response in patients treated with therapeutic amounts of a VLA4 binding antibody (e.g., natalizumab). A second aspect of the invention concerns the chronological details of sample collection for determining the titre of antibodies against the therapeutic protein, e.g. the collection of at least two samples at two different time points. A third aspect of the invention relates to the selection of the critical threshold level, which corresponds to the antibody titre of untreated patients increased by the double of the standard deviation of this control antibody titre. | 08-02-2012 |
20120189624 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 07-26-2012 |
20120142902 | Prevention and Treatment 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 response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease. | 06-07-2012 |
20120115848 | Inhibitors of Polo-Like Kinase - The present invention provides compounds having a structure according to Formula (I): | 05-10-2012 |
20120059029 | SELECTIVE INTEGRIN INHIBITORS - This invention provides methods for selectively antagonizing the α4β1 integrin heterodimer in a subject in need thereof, and preferably in a human subject. The methods of the invention utilize conjugates comprising two or more α4β1 small molecule antagonists covalently attached to a biocompatible polymer. These methods of selectively inhibiting α4β1 may be used modulate both normal and pathological biological processes mediated at least in part through α4β1 activity. | 03-08-2012 |
20120039878 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 02-16-2012 |
20110306071 | Compositions and Methods for Identifying Substrate Specificity of Inhibitors of Gamma Secretase - The invention provides assays and methods for determining the substrate specificity of gamma secretase inhibitors and for identifying substrate-selective (and substrate isoform-selective) inhibitors of gamma secretase. The invention provides assays and methods for determining whether a compound inhibits gamma secretase in a site specific or substrate specific manner. The invention provides isolated polypeptide sequences comprising modified gamma secretase substrates, and polynucleotide sequences encoding the polypeptide sequences. The invention also provides compounds that inhibit gamma secretase, pharmaceutical compositions comprising such compounds, and methods of treating Alzheimer's disease using such compounds. | 12-15-2011 |
20110294149 | Alzheimer's Disease Secretase, APP Substrates Therefor, and Uses Therefor - 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. The invention further provides a modified APP protein and associated nucleic acids, peptides, vectors, cells, and cell isolates, and assays that are particularly useful for identifying candidate therapeutics for treatment or prevention of Alzheimer's disease. | 12-01-2011 |
20110287049 | PREVENTION AND TREATMENT OF AMYLOIDOGENIC DISEASES - Active immunotherapy methods for treating a human patient having an amyloid disease characterized by the presence of amyloid fibrils comprising islet amyloid polypeptide (IAPP). | 11-24-2011 |
20110281752 | BETA-SECRETASE ENZYME COMPOSITIONS AND METHODS - Disclosed are various forms of an active, isolated β-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 (β-APPwt and β-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease. | 11-17-2011 |
20110224408 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 09-15-2011 |
20110218328 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 09-08-2011 |
20110178119 | Bridged N-Bicyclic Sulfonamido Inhibitors of Gamma Secretase - The invention provides N-bicyclic sulfonamido compounds of Formula (I) wherein A is as described in the specification and R | 07-21-2011 |
20110064734 | PREVENTION AND TREATMENT OF AMYLOIDOGENIC DISEASE - 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. | 03-17-2011 |
20110064729 | 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 administration is sufficient to suppress pathological inflammation, and the agent is administered chronically to provide long-term suppression of pathological inflammation. | 03-17-2011 |
20110003802 | Bridged N-Cyclic Sulfonamido Inhibitors of Gamma Secretase - The invention provides N-cyclic sulfonamido compounds and salts of Formula I: | 01-06-2011 |
20100303824 | 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 protein. | 12-02-2010 |
20100278814 | Prevention and treatment 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 response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease. | 11-04-2010 |
20100267747 | 5-(Arylsulfonyl)-Pyrazolopiperidines - The invention provides N-cyclic sulfonamido compounds of Formula I | 10-21-2010 |
20100261715 | 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, 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. | 10-14-2010 |
20100203631 | 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. | 08-12-2010 |
20100160343 | 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, 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. | 06-24-2010 |
20100160341 | 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, 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. | 06-24-2010 |
20100113434 | 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, 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. | 05-06-2010 |
20100086545 | Prevention and Treatment 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 response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease. | 04-08-2010 |
20100081793 | THERAPEUTIC USES OF HUMANIZED ANTIBODIES AGAINST ALPHA-4 INTEGRIN - The invention provides methods of treatment using humanized immunoglobulins that specifically bind to alpha-4 integrin. The methods are useful for treatment of asthma, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, transplant rejection, graft versus host disease, tumor metastasis, nephritis, atopic dermatitis, psoriasis, myocardial ischemia, and acute leukocyte mediated lung injury. | 04-01-2010 |
20100031377 | Prevention and treatment 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 response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease. | 02-04-2010 |
20100021461 | IMMUNOGLOBULIN FORMULATION AND METHOD OF PREPARATION THEREOF - A stable aqueous pharmaceutical formulation comprising a therapeutically effective amount of an antibody, polysorbate 80, a buffer which inhibits polysorbate oxidation is described along with methods of making the preparation. Also described are formulations with high antibody concentrations which maintain fixed volumes and which may be used on patients of variable weight. | 01-28-2010 |
20090285822 | PREVENTION AND TREATMENT OF AMYLOIDOGENIC DISEASE - 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. | 11-19-2009 |
20090285809 | 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 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. | 11-19-2009 |
20090208492 | Lyophilized Immunoglobulin Formulations and Methods of Preparation - 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. | 08-20-2009 |
20090208487 | Prevention and treatment 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 response against the Lewy body. The methods are particularly useful for prophylactic and therapeutic treatment of Parkinson's disease. | 08-20-2009 |
20090202432 | TREATMENT AND PROPHYLAXIS OF AMYLOIDOSIS - 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. | 08-13-2009 |
20090192181 | 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 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. | 07-30-2009 |
20090163594 | Triple Assay System for Identifying Substrate Selectivity of Gamma Secretase Inhibitors - The invention provides assays and methods for determining whether a compound inhibits gamma secretase in a substrate specific manner. The invention provides an isolated cell wherein the cell stably expresses APP and at least one gamma secretase substrate other than APP. The invention provides assays and methods comprising contacting a cell with gamma secretase and detecting production of Abeta, detecting production of intracellular domain (ICD), and detecting a signal from a reporter gene under transcriptional control of the ICD. The invention also provides compounds that inhibit gamma secretase, pharmaceutical compositions comprising such compounds, and methods of treating Alzheimer's disease using such compounds. | 06-25-2009 |
20090144840 | Beta-secretase enzyme compositions and methods - Disclosed are various forms of an active, isolated β-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 (β-APPwt and β-APPsw) are also disclosed, as are antibodies directed to such proteins. These compositions are useful for use in methods of selecting compounds that modulate β-secretase. Inhibitors of β-secretase are implicated as therapeutics in the treatment of neurodegenerative diseases, such as Alzheimer's disease. | 06-04-2009 |
20090035217 | Truncated Fragments of Alpha-Synuclein in Lewy Body Disease - 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. | 02-05-2009 |
20090023178 | Parkin Substrate and Assay - The invention provides in vitro, ex vivo, and in vivo assays for Parkin activity, in which Parkin-mediated ubiquitination of a Sept4 protein is measured. The assays may be used to screen for agents that modulate Parkin protein ligase activity. | 01-22-2009 |
20090023158 | Compositions and Methods for Identifying Substrate Specificity of Inhibitors of Gamma Secretase - The invention provides assays and methods for determining the substrate specificity of gamma secretase inhibitors and for identifying substrate-selective (and substrate isoform-selective) inhibitors of gamma secretase. The invention provides assays and methods for determining whether a compound inhibits gamma secretase in a site specific or substrate specific manner. The invention provides isolated polypeptide sequences comprising modified gamma secretase substrates, and polynucleotide sequences encoding the polypeptide sequences. The invention also provides compounds that inhibit gamma secretase, pharmaceutical compositions comprising such compounds, and methods of treating Alzheimer's disease using such compounds. | 01-22-2009 |
20080306136 | Substituted Ureas and Carbamates - The invention provides compounds of formula I: | 12-11-2008 |
20080300206 | Alpha-Synuclein Kinase - 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 kinase. | 12-04-2008 |
20080299074 | A-BETA IMMUNOGENIC PEPTIDE CARRIER CONJUGATES AND METHODS OF PRODUCING SAME - The present invention is directed to methods of producing conjugates of Aβ 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. | 12-04-2008 |
20080293089 | Assays for Modulators of Parkin Activity Using Novel Substrates - The invention provides in vitro and cell-based assays for parkin activity, in which parkin-mediated ubiquitination of the S5a subunit of the 26S proteasome is measured, or ubiquitination of troponin 1. The assays may be used to screen for agents that modulate parkin protein ligase activity. | 11-27-2008 |