Patent application number | Description | Published |
20100034799 | ANTI-COCAINE COMPOSITIONS AND TREATMENT - Embodiments of the invention disclosed herein generally relate to anti-cocaine therapeutics. Specifically, some embodiments of the invention relate to highly efficient, thermostable, and long-lasting cocaine esterase (CocE) mutants that can protect against the toxic and reinforcing effects of cocaine in subjects. Provided herein are mutant CocE polypeptides displaying thermostable esterase activity. Also provided are methods of treating cocaine-induced conditions in a subject in need via administration of mutant CocE as well as methods for high-throughput screening of candidate esterase polypeptides. | 02-11-2010 |
20100152440 | NOVEL ANTI-ARRHYTHMIC AND HEART FAILURE DRUGS THAT TARGET THE LEAK IN THE RYANODINE RECEPTOR (RyR2) - The present invention provides novel 1,4-benzothiazepine intermediates and derivatives, methods for synthesizing same, and methods for assaying same. The present invention also provides methods for using these novel compounds to limit or prevent a decrease in the level of RyR2-bound FKBP12.6 in a subject; to prevent exercise-induced sudden cardiac death in a subject; and to treat or prevent heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia in a subject. The present invention further provides methods for identifying an agent that enhances binding of RyR2 and FKBP12.6, and agents identified by these methods. Additionally, the present invention provides methods for identifying agents for use in treating or preventing heart failure, atrial fibrillation, or exercise-induced cardiac arrhythmia, and in preventing exercise-induced sudden cardiac death. Also provided are agents identified by such methods. | 06-17-2010 |
20100204258 | METHODS AND COMPOSITIONS FOR MODULATING INSULIN SECRETION AND GLUCOSE METABOLISM - The present invention relates to methods and compositions for treating or ameliorating the effects of diabetes. In addition, the present invention relates to methods and compositions for treating or preventing hyperglycemia, as well as modulating monoamine levels, islet β-cell insulin secretion, insulin and/or glucagon levels in a patient. In certain preferred embodiments, such methods include administering to a patient an effective amount of a vesicular monoamine transporter type 2 (VMAT2) antagonist, such as tetrabenazine (TBZ), dihydrotetrabenazine (DTBZ), tetrahydroberberine (THB), reserpine, emetine, Compound 6, or enantiomers, optical isomers, diastereomers, N-oxides, crystalline forms, hydrates, metabolites or pharmaceutically acceptable salts thereof. | 08-12-2010 |
20110071124 | Compounds that Inhibit Production of sAPPB and AB and Uses Thereof - The present invention relates to compounds with activity as inhibitors of sAPPβ and Aβ production, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease and pharmaceutical compositions containing such candidate compounds. | 03-24-2011 |
20110281899 | METHODS OF PREVENTING AND TREATING LOW BONE MASS DISEASES - The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists. | 11-17-2011 |
20120029022 | Potent Non-Urea Inhibitors Of Soluble Epoxide Hydrolase - The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension. | 02-02-2012 |
20120064099 | COMPOUNDS THAT INHIBIT NFKB AND BACE1 ACTIVITY - The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds. | 03-15-2012 |
20120269828 | ANTI-DRUG VACCINES - The present invention relates to anti-drug vaccines based on conjugates between the drug and a non-immunogenic carrier protein. In preferred embodiments, it provides for anti-cocaine vaccines and their use to diminish the effects and/or use of cocaine in a subject. | 10-25-2012 |
20120295853 | NEURONAL PAIN PATHWAY - The present invention relates to the discovery of a novel molecular pathway involved in long-term hyperexcitability of sensory neurons, which, in higher animals, is associated with persistent pain. It is based on the discovery that, following injury to an axon of a neuron, an increase in nitric oxide synthase activity results in increased nitric oxide production, which, in turn, activates guanylyl cyclase, thereby increasing levels of cGMP. Increased cGMP results in activation of protein kinase G (“PKG”), which then is retrogradely transported along the axon to the neuron cell body, where it phosphorylates MAPKerk. | 11-22-2012 |
20130053343 | COMPOUNDS AND METHODS FOR INHIBITING SEROTONIN SYNTHESIS - Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis. | 02-28-2013 |
20130121919 | HISTONE ACETYLTRANSFERASE ACTIVATORS AND USES THEREOF - The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject. | 05-16-2013 |
20130136728 | ANTI-COCAINE COMPOSITIONS AND TREATMENT - Embodiments of the invention disclosed herein generally relate to anti-cocaine therapeutics. Specifically, some embodiments of the invention relate to highly efficient, thermostable, and long-lasting cocaine esterase (CocE) mutants that can protect against the toxic and reinforcing effects of cocaine in subjects. Provided herein are mutant CocE polypeptides displaying thermostable esterase activity. Also provided are methods of treating cocaine-induced conditions in a subject in need via administration of mutant CocE as well as methods for high-throughput screening of candidate esterase polypeptides. | 05-30-2013 |
20130225592 | ALDOSE REDUCTASE INHIBITORS AND USES THEREOF - The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like. | 08-29-2013 |
20140073668 | N-QUINOLIN-BENZENSULFONAMIDES AND RELATED COMPOUNDS FOR THE TREATMENT OF CANCER, AUTOIMMUNE DISORDERS AND INFLAMMATION - The present invention relates to the NQBS class of molecules. It is based, at least in part, on the discovery that a representative group of compounds have been observed to inhibit nuclear translocation of NF-κB subunits. Without being bound by any particular theory, this inhibition of nuclear translocation may be mediated by either (i) binding of the NQBS or related compound to the C-terminus of the RHD, which specifically mediates the nuclear internalization; or (ii) NQBS-mediated stabilization of the dimer/IκB complex, disallowing dissociation of the active NF-κB monomers, and thus, inhibiting the generation of the subunits necessary to enter the nucleus. The NQBS class of molecules, and related molecules, may be used in therapeutic applications where inhibition of NF-κB translocation is beneficial, including but not limited to the treatment of cancer, autoimmune disorders, and inflammatory states. | 03-13-2014 |
20140275165 | COMPOUNDS THAT INHIBIT NFkB AND BACE1 ACTIVITY - The present invention relates to compounds with activity as BACE1 and NFκB modulators, and methods for treating, preventing, or ameliorating neurodegenerative diseases, such as Alzheimer's disease. The present invention is also directed to the treatment of diseases related to dysfunction of cell proliferation, the immune system and/or inflammation using such compounds or pharmaceutical compositions containing such candidate compounds. | 09-18-2014 |
20140336193 | POTENT NON-UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE - The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension. | 11-13-2014 |
20140349368 | POTENT NON-UREA INHIBITORS OF SOLUBLE EPOXIDE HYDROLASE - The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension. | 11-27-2014 |
20150072989 | ALDOSE REDUCTASE INHIBITORS AND USES THEREOF - The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like. | 03-12-2015 |