96 results about "Cns disease" patented technology

Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.

Provided herein are substituted pyrrolopyridine heterocycles and substituted pyrazolopyridine heterocycles, pharmaceutical compositions comprising said heterocycles and methods of using said heterocycles in the treatment of disease. The heterocycles disclosed herein function as kinase modulators and have utility in the treatment of diseases such as cancer, allergy, asthma, inflammation, obstructive airway disease, autoimmune diseases, metabolic disease, infection, CNS disease, brain tumor, obesity, asthma, hematological disorder, degenerative neural disease, cardiovascular disease, or disease associated with angiogenesis, neovascularization, or vasculogenesis.

Methods, compositions and kits for producing functional neurons, astroctyes, oligodendrocytes and progenitor cells thereof are provided. These methods, compositions and kits find use in producing neurons, astrocytes, oligodendrocytes, and progenitor cells thereof for transplantation, for experimental evaluation, as a source of lineage- and cell-specific products, and the like, for example for use in treating human disorders of the CNS. Also provided are methods, compositions and kits for screening candidate agents for activity in converting cells into neuronal cells, astrocytes, oligodendrocytes, and progenitor cells thereof.

The present invention relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a sample of a subject, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP. The method further comprises of treating the disease in the subject with the PARP modulators. The methods relate to identifying up-regulated PARP in a disease and making a decision regarding the treatment of the disease with PARP inhibitors. The extent of PARP up-regulation in a disease can also help in determining the efficacy of the treatment with PARP inhibitors. The present invention discloses various diseases that have up-regulated or down-regulated PARP and can be treated with PARP inhibitors or PARP activators, respectively. The examples of the diseases include cancer, inflammation, metabolic disease, CVS disease, CNS disease, disorder of hematolymphoid system, disorder of endocrine and neuroendocrine, disorder of urinary tract, disorder of respiratory system, disorder of female reproductive system, and disorder of male reproductive system.

The present invention relates to methods of identifying a disease treatable with PARP modulators by identifying a level of PARP in a plurality of samples from a population, making a decision regarding identifying the disease treatable by the PARP modulators wherein the decision is made based on the level of PARP. The method further comprises of treating the disease in a subject population with the PARP modulators. The methods relate to identifying up-regulated PARP in a disease and making a decision regarding the treatment of the disease with PARP inhibitors. The extent of PARP up-regulation in a disease can also help in determining the efficacy of the treatment with PARP inhibitors.The present invention discloses various diseases that have up-regulated or down-regulated PARP and can be treated with PARP inhibitors or PARP activators, respectively. The examples of the diseases include cancer, inflammation, metabolic disease, CVS disease, CNS disease, disorder of hematolymphoid system, disorder of endocrine and neuroendocrine, disorder of urinary tract, disorder of respiratory system, disorder of female reproductive system, and disorder of male reproductive system.

Brain-penetrating polymeric nanoparticles that can be loaded with drugs and are optimized for intracranial convection-enhanced delivery (CED) have been developed. In the preferred embodiment, these are loaded with FDA-approved compounds, identified through library screening to target brain cancer stem cells (BSCSs). The particles are formed by emulsifying a polymer-drug solution, then removing solvent and centrifuging at a first force to remove the larger particles, then collecting the smaller particles using a second higher force to sediment the smaller particles having a diameter of less than 100 nm, more preferably less than 90 nanometers average diameter, able to penetrate brain interstitial spaces.

Substituted quinolone carboxylic acids and their derivatives are described. These compounds modulate the effect of γ-aminobutyric acid (GABA) via a novel site on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

Isolated human cells and populations thereof are provided comprising at least one oligodendrocyte phenotype and at least one mesenchymal stem cell phenotype, wherein the mesenchymal stem cell phenotype is not an oligodendrocyte phenotype. Methods of generating and using same are also provided.

A data acquisition system for use in conducting functional magnetic resonance imaging studies. fMRI studies can provide clues to the neurobiological basis of CNS disorders and reliable and quantifiable data relating to their symptoms. The data acquisition system includes a control station, a patient stimulus and response system and fMRI data acquisition software for controlling the operation of the system in response to operator input and acquiring fMRI data comprising MR images and associated behavioral response data. The stimulus and response system presents visual or auditory or other stimuli to the patient under direction of the control station while functional MRI scanning takes place. The MRI image data is collected from the MRI scanner and combined with the behavioral data generated as the patient responds to the stimuli and archived for later analysis and use. The system includes quality control measures for properly setting up the equipment and preparing and training the patient and for verifying data quality during the different steps in the process.

An isolated human cell and populations thereof is provided comprising at least one astrocytic phenotype and at least one mesenchymal stem cell phenotype, wherein the mesenchymal stem cell phenotype is not an astrocytic phenotype.

KATP channel closers (KCCs) are useful for the prophylactic and / or therapeutic treatment of a CNS acute damage in a mammal, including a human, because their administration, particularly in the case of glibenclamide, potientates the neuroprotector microglial effect. Therefore, they may be useful in treating the acute phase of CNS diseases such as stroke, seizure, axonal injury, traumatic damage, neurodegeneration, spinal cord injury, infectious and autoimmune CNS diseases. KCCs, isotopically modified, are also useful for the preparation of diagnostic agents for detection and follow-up of CNS acute damage.

The present invention provides a damaged part treatment composition for repairing a damaged part of a target tissue that includes a stem cell-conditioned medium obtained by culturing stem cells; a damaged part treatment method for repairing or restoring a damaged part of a target tissue that includes administering the damaged part treatment composition to a patient having the target tissue for the damaged part treatment composition in an amount therapeutically effective for repairing the damaged part of the target tissue; a method of treating cerebral infarction that includes administering the damaged part treatment composition to a cerebral infarct patient in an amount effective for repairing a damaged part of the brain; and a method of treating a CNS disease that includes administering, as a CNS disease treatment composition, the damaged part treatment composition to a CNS disease patient in a therapeutically effective amount.

Methods and small molecule compounds for smoking and CNS disease harm reduction are provided. One example of a class of compounds that may be used is represented by the compound having the structure IA or IB in the form of free base or a pharmaceutically acceptable salt, hydrate or solvate thereof:

An isolated human cell is disclosed comprising at least one mesenchymal stem cell phenotype and secreting brain-derived neurotrophic factor (BDNF), wherein a basal secretion of the BDNF is at least five times greater than a basal secretion of the BDNF in a mesenchymal stem cell. Methods of generating same and uses of same are also disclosed.

The present invention relates to a neuronal differentiation method of adult stem cells using small molecules, more particularly to a method for inducing differentiation of adult stem cells into nerve cells using small molecules, which enables effective differentiation into nerve cells and, thus, is useful in treating intractable CNS disorders such as Parkinson's disease, dementia, Alzheimer's disease and spinal cord injury.

The invention relates to methods for treatment of CNS disease and pathologies using non-racemic mixtures of lofexidine enantiomers. The invention also relates to processes for the manufacture of chirally pure enantiomers of lofexidine.

The invention-provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): in which Ar, R2, R3, R4 and R5 are as defined in the specification. The compounds bind to the 5-HT6 receptor and are useful for the treatment and prophylaxis of disorders mediated by the 5-HT6 receptor, such as obesity and CNS disorders.

An isolated human cell is disclosed comprising at least one mesenchymal stem cell phenotype and secreting brain-derived neurotrophic factor (BDNF), wherein a basal secretion of the BDNF is at least five times greater than a basal secretion of the BDNF in a mesenchymal stem cell. Methods of generating same and uses of same are also disclosed.

Compositions and methods are disclosed that relate to improved treatments for nervous system diseases and disorders using CNS-implanted semi-permeable biocompatible capsules containing encapsulated pathogen-free xenogeneic choroid plexus (CP) cells that are induced to produce altered (and in certain embodiments increased) levels of one or more cerebrospinal fluid (CSF) components. Capsules are selected as disclosed to be capable of induction of elevated CSF production levels by CP cells that are remarkably (>16 months post implant) long-lived, without eliciting immunological rejection, inflammation or foreign body response reactions.

The present invention relates to phosphodiesterase (PDE) type 4, phosphodiesterase (PDE) type 7 and dual PDE type 4 / PDE type 7 inhibitors. Compounds disclosed herein having the structure of Formula 1: can be useful in the treatment, prevention, inhibition or suppression of CNS diseases, for example, multiple sclerosis; various pathological conditions such as diseases affecting the immune system, including AIDS, rejection of transplant, auto-immune disorders such as T-cell related diseases, for example, rheumatoid arthritis; inflammatory diseases such as respiratory inflammation diseases including chronic obstructive pulmonary disease (COPD), asthma, bronchitis, allergic rhinitis, adult respiratory distress syndrome (ARDS) and other inflammatory diseases including but not limited to psoriasis, shock, atopic dermatitis, eosinophilic granuloma, allergic conjunctivitis, osteoarthritis; gastrointestinal inflammation diseases such as Crohn's disease, colitis, pancreatitis as well as different types of cancers including leukaemia; especially in humans. Processes for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds and their use as PDE type 4, PDE type 7 and dual PDE type 4 / PDE type 7 inhibitors are provided.

The present disclosure relates to surface-modified mesoporous silica nanoparticles for blood-brain barrier penetration, tumor targeting, and cancer metastasis treatment, methods of making and uses thereof. Specifically, the invention relates to mesoporous silica nanoparticles MSN with specific modification, which have tumor targeting and blood-brain barrier BBB penetration properties as a drug delivery system, and are suitable for cancer treatment and / or CNS disease treatment. The present disclosure also relates to a method of preparing an MSN and an MSN prepared by the method as described herein.

Disclosed are novel A2A adenosine receptor antagonists of the formula:wherein:R1 is optionally substituted aryl or optionally substituted heteroaryl;R2 is optionally substituted lower alkyl or optionally substituted cycloalkyl;R3 is hydrogen, halogen, optionally substituted alkoxy, optionally substituted aryl, optionally substituted heteroaryl, or optionally substituted heterocyclyl;X is —O—, —S—, or —NH—; andY is optionally substituted alkylene;and the pharmaceutically acceptable salts thereof;which are useful for treating various disease states, for example cardiovascular disorders, including tissue damage due to ischemia, CNS diseases, including Parkinson's disease, depression, and the like.

This invention provides the compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent hydrogen or the like; R3 and R4 independently represents hydrogen or the like; R5 represents aryl or the like; —X—Y— represents —CH2O— or the like; and n represents 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.

Disclosed are methods for identifying individuals suffering from a CNS disorder (including Alzheimer's Disease, ALS, behavioral disorders, and the like) that could be treated with a CNS drug with greater therapeutic efficacy and lower side effects and the compounds useful for such treatment. Also disclosed are methods for predicting the efficacy of a drug candidate for the treatment of a CNS disorder. The technology is also applicable to drug discovery for evaluation in animal models of neurodegenerative diseases.

Ghrelin antagonists can be used for the treatment of certain CNS disorders. For example, certain oxadiazoles, preferably such being ghrelin antagonists, can be used to treat obesity, e.g., drug-induced obesity.