32 results about "Glutamate receptor antagonist" patented technology

Tension-type headache is treated by interacting smith neuronal transmission in relation to pain in connection with headache in a way which prevents or decreases sensitization of second order nociceptive neurons. In particular, treatment is performed by administration of an effective amount of a substance which prevents or decreases central sensitization. Important examples of such substances are substances which interact with glutamate neurotransmission, such as glutamate receptor antagonists, such as NMDA receptor antagonists, such as MK-801 or Amitriptylline or Imipramine or Desipramine or Mirtazaprine or Venlafaxine. Other examples are substances which interact with nitric oxide, such as nitric oxide synthase (NOS) inhibitors, such as L-NMMA or L-NAME or L-NIO or L-NNA. According to a broader aspect of the invention tension-type headache is treated by administration of substances which are effective in preventing or decreasing pain in connection with tension-type headache, such as the substances mentioned above. An additional aspect of the invention relates to treatment of tension-type headache by administration of substances which substantially inhibit the activity of nitric oxide synthase (NOS), such as NOS inhibitors, such as L-NMMA or L-NAME or L-NIO or L-NNA.

The present invention describes a novel treatment for movement disorders, including tardive dyskinesia, tic disorders, Tourette's syndrome, and blepharospasm, and other focal dystonias. The treatment of the present invention utilizes agents that simultaneously act as NMDA-type glutamate receptor antagonists and GABA-A receptor agonists. Preferably these two activities are characteristic of a single agent, for example acamprosate. Alternatively, separate agents having these activities can be combined and administered together. The invention also provides a third agent that acts as a non-competitive NMDA-receptor blocking agent or ion channel blocker that augments the effect of the primary treatment. A particularly preferred ion channel blocking agent is magnesium. Alternatively, magnesium can be administered alone for prevention and treatment of movement disorders.

The present invention relates to methods and compositions for modulating platelet activity by inhibiting or activating glutamate receptors. The invention further relates to preventing or treating thrombotic diseases.

Provided herein are compositions, combinations, and methods comprising NMDA antagonists including, but not limited to, NMDA glutamate receptor antagonists such as [2-(8,9-dioxo-2,6-diazabicyclo[5.2.0]non-1-(7)-en-2-yl)alkyl]phosphonic acid and derivatives thereof, which are effective in reducing the amount of anesthetic required to maintain anesthesia (i.e. to achieve an anesthetic-sparing effect).

The present invention describes a novel treatment for movement disorders, including tardive dyskinesia, tic disorders, Tourette's syndrome, and blepharospasm, and other focal dystonias. The treatment of the present invention utilizes agents that simultaneously act as NMDA-type glutamate receptor antagonists and GABA-A receptor agonists. Preferably these two activities are characteristic of a single agent, for example acamprosate. Alternatively, separate agents having these activities can be combined and administered together. The invention also provides a third agent that acts as a non-competitive NMDA-receptor blocking agent or ion channel blocker that augments the effect of the primary treatment. A particularly preferred ion channel blocking agent is magnesium. Alternatively, magnesium can be administered alone for prevention and treatment of movement disorders.

In its many embodiments, the present invention provides tetracyclic compounds of formula I or formula II (wherein the various moieties are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimers disease.

Indole-2,3-dione-3-oxime derivatives, for instance compounds represented by the formulaare capable of antagonizing the effect of excitatory amino acids, such as glutamate. Also disclosed are methods of preparing the compounds, pharmaceutical compositions comprising them, and methods of treatment of disorders or diseases which are responsive to excitatory amino acid receptor antagonists.

Compounds of formula (II), wherein X, Y, and Z are independently selected from N, O, S, C, and CO, and at least one of X, Y, and Z is a heteroatom; Ar1 ​​and Ar2 are independently selected from heterocycles base or fused heterocyclyl and aryl groups; the compounds act as metallotropic glutamate receptor antagonists and can be used to treat neurological diseases and disorders.

Methods, and compositions are provided for inhibition of histamine and non-histamine dependent itch signal transmission or scratch behavior. In one aspect, the present invention further comprises administering to the subject an inhibitor of histamine-dependent itch signal transmission. In some cases, the inhibitor of histamine independent itch signal transmission comprises an NK-1 receptor antagonist or the inhibitor of histamine independent itch signal transmission comprises a GRP receptor antagonist. In some cases, the method comprises administering two inhibitors of histamine independent itch signal transmission. For example, the inhibitors of histamine independent itch signal transmission can comprise an NK-1 receptor antagonist and a GRP receptor antagonist. In another embodiment, the invention provides a method of treating itch comprising administering to a subject suffering from itch an NK-1 receptor antagonist, a GRP receptor antagonist.

Compounds of formula (II), wherein X, Y, and Z are independently selected from N, O, S, C, and CO, and at least one of X, Y, and Z is a heteroatom; Ar 1 and Ar 2 Independently selected from heterocyclyl or fused heterocyclyl and aryl groups; the compounds act as metallotropic glutamate receptor antagonists and are useful in the treatment of neurological diseases and disorders. ∴

The present invention provides brain cells, such as normal brain cells, apolipoprotein E deficient brain cells, or apoE4 containing brain cells, that are treated with a compound which can modulate integrins and / or integrin receptors to produce increased sequestration of and / or accumulation of and / or uptake of Aβ, and / or changes in cathepsin D content and / or lysosomal dysfunction, and / or microglia activation in the brain cells. The present invention also provides methods for producing such cells and methods for using the cells for screening an agent or substance that modulates the sequestration of and / or accumulation of and / or uptake of Aβ, and / or lysosomal dysfunction, and / or changes in cathepsin D content and / or microglia activation in the brain cells. The method further provides a new therapeutic target, antagonism of glutamate receptors, for the treatment of neurodegenerative diseases which are characterized by inter alia, abnormal amyloid uptake and / or accumulation.

The present invention provides novel compounds of Formula I or Formula II, or the pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I or Formula II in combination with a suitable carrier, diluent, or excipient, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine.

The present invention relates to methods and compositions for modulating platelet activity by inhibiting or activating glutamate receptors. The invention further relates to preventing or treating thrombotic diseases.

The present invention provides novel compounds of Formula I or Formula II, or the pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I or Formula II in combination with a suitable carrier, diluent, or excipient, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine.

Methods for inhibiting impaired neurogenesis and / or synaptogenesis in neurons in a subject with or suspected of having Alzheimer's Disease (AD), methods for improving and / or slowing the decline of cognitive function after onset of neuropathology and cognitive dysfunction, which neuropathology and cognitive dysfunction are caused by AD, methods for improving and / or slowing the decline of memory before onset of symptoms of AD, methods for increasing concentration and duration of dantrolene in the brain, and methods for improving and / or slowing the decline of memory after onset of symptoms of AD, the methods comprising intranasally administering to a subject in need thereof an amount of a pharmaceutical composition comprising dantrolene effective to inhibit over-activation of N-methyl-D-aspartate (NMVDA) receptor and / or ryanodine receptor (RyR). Methods further comprise administering a therapeutically effective amount of a glutamate receptor antagonist to the subject.

The present invention provides brain cells, such as normal brain cells, apolipoprotein E deficient brain cells, or apoE4 containing brain cells, that are treated with a compound which can modulate integrins and / or integrin receptors to produce increased sequestration of and / or accumulation of and / or uptake of Aβ, and / or changes in cathepsin D content and / or lysosomal dysfunction, and / or microglia activation in the brain cells. The present invention also provides methods for producing such cells and methods for using the cells for screening an agent or substance that modulates the sequestration of and / or accumulation of and / or uptake of Aβ, and / or lysosomal dysfunction, and / or changes in cathepsin D content and / or microglia activation in the brain cells. The method further provides a new therapeutic target, antagonism of glutamate receptors, for the treatment of neurodegenerative diseases which are characterized by inter alia, abnormal amyloid uptake and / or accumulation.

A novel series of substituted quinoxaline 2,3-diones useful as neuroprotective agents are taught. Novel intermediates, processes of preparation, and pharmaceutical compositions containing the compounds are also taught. The compounds are glutamate antagonists and are useful in the treatment of stroke, cerebral ischemia, or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasms, hypoglycemia, cardiac arrest, status epilepticus, perinatal asphyxia, anoxia, Alzheimer's, Parkinson's, and Huntington's diseases.

Provided is a combination agent that combines N-[(1S)-2,2,5,7-tetrafluoro-2,3-dihydro-1H-inden-1-yl]sulfamide with an AMPA-type glutamate receptor antagonist such as 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridine-2-one or 2-fluoro-6-(3-fluoro-8-oxo-7-(pyridin-3-yl)-7,8-dihydro-6H-pyrano[3,2-b:5,4-b']dipyridin-9-yl]benzonitrile and that can be possibly used as an epilepsy treatment agent.

Disclosed is an RNA aptamer, a synthetic oligonucleotide of 2′-fluoro-modified A, U, and C nucleotides, with improved stability compared to its unmodified counterpart. Like the unmodified aptamer, however, the modified version is a potent glutamate receptor antagonist. Additionally, the RNA aptamers described herein are water soluble by nature, and generally exhibit nano- to micromolar potency making them potential therapeutic agents for the treatment of neurological disorders involving glutamate receptor activity.

The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula (I(a)).

The present invention provides a method for fattening poultry, which is characterized by administering a substance that inhibits motor neurons. Specifically, it provides administration of a substance selected from the group consisting of GABAB receptor agonists, GABAA receptor agonists, substances that enhance the action of GABAA receptors, and kainate-type glutamate receptor antagonists, or a combination thereof , or a method of fattening poultry by administering feed containing these substances or a composition thereof to poultry.

The present invention provides compounds of Formula I or Formula II, or the pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising compounds or Formula I or Formula II, and methods for treating neurological disorders and neurodegenerative diseases, particularly migraine.

The present invention provides novel compounds of Formula (I) and Formula (I(a)), or the pharmaceutically acceptable salts thereof; methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine, comprising administering a compound of Formula (I) or Formula (I(a)); and processes for preparing compounds of Formula (I) or Formula (I(a)).

The present invention provides novel compounds of Formula (I), or the pharmaceutically acceptable salts or prodrugs thereof, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine.

Described herein are compositions, including an oral dosage regimen, for the treatment of N-methyl-D-aspartic acid receptor-related neuropsychiatric disorders such as depression and obsessive-compulsive disorder and that includes an N-methyl-D-aspartic acid receptor antagonist, such as D-cycloserine formulated to produce plasma levels in excess of 25 microgram / mL, combined with more recently developed antidepressants.

Methods for inhibiting impaired neurogenesis and / or synaptic occurrence in neurons of a subject suffering from or suspected of having Alzheimer's disease (AD), methods for ameliorating and / or slowing down a decline in cognitive function following the onset of neuropathology and cognitive dysfunction caused by AD, and methods for improving and / or slowing down a decline in cognitive function following the onset of neuropathology and cognitive dysfunction caused by AD. Methods for ameliorating and / or slowing memory decline prior to the onset of symptoms of AD, methods for increasing the concentration and duration of dantroline in the brain, and methods for ameliorating and / or slowing memory decline after the onset of symptoms of AD, comprising intranasally administering to a subject in need thereof an amount of a pharmaceutical composition, the pharmaceutical composition comprises dantrolin which is effective in inhibiting the excessive activation of the N-methyl-D-aspartic acid (NMDA) receptor and / or the raney receptor (RyR). The method further comprises administering to the subject a therapeutically effective amount of a glutamate receptor antagonist.