32 results about "Anti psychotic" patented technology

The present invention relates to the use of one or more cannabinoids in combination with one or more anti-psychotic medicaments for use in the prevention or treatment of psychosis and psychotic disorders. Preferably the one or more cannabinoids are taken from the group: cannabidiol (CBD); cannabidiolic acid (CBDA); tetrahydrocannbidivarin (THCV); tetrahydrocannbidivarinin acid (THCVA); cannabichromene (CBC); cannabichromenic acid (CBCA); cannabigerol (CBG) and cannabigerolic acid (CBGA). Preferably the anti-psychotic medication is an atypical anti-psychotic medication.

The present invention is an improvement in the treatment of mania and depression by administering topiramate in a sustained-release formulation. The sustained-release formulation of the present invention may also be co-administered with anti-psychotics and anti-depressants.

Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.

The present invention relates to a pharmaceutical composition comprising sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.

Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-psychotic agent. Disclosed herein are also methods of treating psychotic disorders using the disclosed pharmaceutical compositions.

Disclosed herein are pharmaceutical compositions comprising an inverse serotonin receptor agonist or a serotonin receptor antagonist and an anti-psychotic agent. Disclosed herein are also methods of treating psychotic disorders using the disclosed pharmaceutical compositions.

The present invention relates to a pharmaceutical composition comprising benzyl alcohol and polyoxyethylene derivatives of sorbitan esters of carboxylic acids that are useful for the delivery of anti-psychotic drugs.

An subcutaneously implantable device for delivering Risperidone to a patient includes a pump, a compartment configured to store a pharmaceutical formulation, and a volume of the pharmaceutical formulation loaded in the compartment, the pharmaceutical formulation including Risperidone solvated or suspended in a pharmaceutically acceptable solvent in concentration of at least 50 milligrams per milliliter. The implanted pump may then deliver a therapeutically effective dose of Risperidone to the patient.

Disclosed herein is the use of N-desmethylclozapine (NDMC) and related compounds to treat a variety of neuropsychiatric diseases including psychosis. It is shown that NDMC and related compounds are agonists or partial agonists at D2 and D3 dopamine receptors and thus may be effective as a dopamine stabilizing agent, allowing it to be used to treat or provide reduced incidence of Extrapyramidal symptoms (EPS) and/or tardive dyskinesias (TD). Also disclosed is administering NDMC and related compounds in combination with other anti-psychotic agents.

The present invention provides a method for identifying an agent to be tested for an ability to treat a psychotic disorder in a patient in need of such treatment. The invention provides a method for screening candidate drugs for anti-psychotic drug activity, preferably atypical anti-psychotic activity, comprising contacting cells or tissues with a candidate drug, determining levels of phosphorylation of the intracellular signaling proteins, DARPP-32, ERK1, ERK2 and CREB, in said cells or tissues and determining the pattern of the levels of phosphorylation of the proteins. The pattern of the levels of phosphorylation of DARPP-32, ERK1, ERK2 and CREB is, in certain embodiments, compared with the pattern of the levels of phosphorylation of DARPP-32, ERK1, ERK2 and CREB in the presence of an atypical anti-psychotic drug.

A process for the preparation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one of the formula IIB:

where X may be halo, acyloxy, or sulfonyloxy such as tosyloxy or mesyloxy, an intermediate in the synthesis of the anti-psychotic risperidone. The process comprises hydrogenation of 3-substituted ethyl-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one in aqueous inorganic acid medium at atmospheric to 60 psi at 0-100° C. in the presence of a metal catalyst and the product is isolated. A process for the preparation of risperidone of the formula I:

comprising condensation of 3-substituted ethyl-6,7,8,9-tetrahydro-2-methyl-4H-pyrido[1,2,-a]pyrimidin-4-one with 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole in water in the presence of an inorganic base at 25-100° C. and the product is isolated.

Pharmaceutical composite compositions comprising tetrahydroindolones linked to arylpiperazines and derivatives thereof are disclosed. Specifically, composite compositions useful in treating anti-psychotic disorders are disclosed. The composite compositions disclosed herein can effectively ameliorate symptoms and treat psychotic disorders without causing a decrease in cognitive function. Generally, the composite compounds consist of two moieties, moiety A and B in which a tetrahydroindolone comprises a moiety A linked through a linker L to a moiety B, where B is an arylpiperazinyl moiety. The composite compound provides anti-psychotic actively by interaction with GABA, seratoninne and dopamine receptors. The composite molecules with the combined activities will provide treat psychiatric and neurological diseases without cognitive impairment.

The present invention relates to the development of a virtual screening model for predicting antipsychotic activity using quantitative structure activity relationship (QSAR), molecular docking, oral bioavailability, ADME and Toxicity studies. The present invention also relates to the development of QSAR model using forward stepwise method of multiple linear regression with leave-one-out validation approach. QSAR model showed activity-descriptors relationship correlating measure (r²) 0.87 (87%) and predictive accuracy of 81% (rCV²=0.81). The present invention specifically showed strong binding affinity of the untested (unknown) novel compounds against anti-psychotic targets viz., Dopamine D2 and Serotonin (5HT_2A) receptors through molecular docking approach. Theoretical results were in accord with the in vitro and in vivo experimental data. The present invention further showed compliance of Lipinski's rule of five for oral bioavailability and toxicity risk assessment for all the active Yohimbine derivatives. Therefore, use of developed virtual screening model will definitely facilitate the screening of more effective antipsychotic leads/drugs with improved antipsychotic activity and also reduced the drug discovery cost and duration.

A high throughput neurophysiological assay for identifying anti-psychotic compounds is disclosed. In particular, a high throughput neurophysiological assay using information obtained from injecting a neural activity blocker, such as tetrodotoxin (TTX), into one hippocampus persistently coactivated pyramidal cells in the uninjected hippocampus that initially discharged independently. In accord with the definition of cognitive disorganization, pyramidal cell firing rates only changed for 15 min and did not accompany the coactivation. The disclosed assay uses the TTX-induced coactivity of hippocampal pyramidal cell discharge to identify compounds that may prevent or attenuate the changes in the hippocampal pyramidal cell discharge observed when a neural activity blocker is administered. The assays of the invention are useful for high throughput screening of targets in the discovery of drugs that have anti-psychotic properties. Also disclosed is a method of inducing and measuring neural activity normally associated with a psychotic state.

The 4-aryl-1-(biarylmethylene)piperidine compounds are piperadine compounds having a biaryl substituent linked to the nitrogen atom of the piperidine ring by a methylene (—CH₂—) group, and an aryl moiety attached to the 4-position of the piperidine ring. The aryl moiety may be a methoxy quinoline group, a 2-oxo quinoline group, or a 2-oxo, 3,4-dihydroxy quinoline group. The biaryl substituent may be biphenyl, fluorophenyl benzene, 3-phenyl pyridine, 3-(4-fluorophenyl) pyridine, phenyl cyclopentene, or 3-(1-cyclopenten-1-yl) pyridine. The compounds are believed to be suitable for anti-psychotic medication, since they are structurally related to SLV-313, a potential atypical antipsychotic having potent D₂ receptor antagonist and 5-HT_1A receptor agonist properties.