43 results about "Riluzole" patented technology

Disclosed are methods of treating cancer using a combination of an immunotherapeutic agent, such as, for example, a PD-1, PD-L1 or CTLA-4 checkpoint inhibitor, and a glutamate modulating agent such as riluzole or trigriluzole. Pharmaceutical compositions and kits including the immunotherapeutic agents and glutamate modulating agents are also disclosed.

An oral film in an individual unit dose for delivery of one or more actives is disclosed herein, the film having a precisely calculated and controlled active dissolution profile. A wide variety of actives may be used, including, for example, clobazam, diazepam, or riluzole. Also disclosed are methods of treating a variety of diseases and conditions, for example, epilepsy and seizures, by administering the oral film disclosed herein.

A pharmaceutical composition includes about 100 mg to about 280 mg of troriluzole, a pharmaceutically acceptable salt thereof, a hydrate thereof, or a hydrate of the salt, wherein the pharmaceutical composition is in a once-a-day oral dosage form, which provides an AUC0-inf for riluzole of about 80% to about 125% of about 791 h•ng / mL to about 2330 h•ng / mL. A method of treating a disease or a condition in a patient in need thereof includes administering to the patient once daily the pharmaceutical composition.

Provided for are prodrugs of riluzole and pharmaceutical compositions and methods of use thereof. The prodrugs have advantageous pharmacological properties for use in methods for treating glutamate-associated diseases or disorders, or other diseases or disorders, against which riluzole is known or expected to be effective, including central nervous system (CNS) disorders, neuropsychiatric disorders, and neurodegenerative disorders.

To provide novel compounds, pharmaceutical compositions and methods for the treatment of Alzheimer's disease which may provide benefits for patients afflicted with the Alzheimer's disease.SOLUTION: Provided is a method of treating Alzheimer's disease in a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a riluzole prodrug.SELECTED DRAWING: None

An oral film in an individual unit dose for delivery of one or more actives is disclosed herein, the film having a precisely calculated and controlled active dissolution profile. A wide variety of actives may be used, including, for example, clobazam, diazepam, or riluzole. Also disclosed are methods of treating a variety of diseases and conditions, for example, epilepsy and seizures, by administering the oral film disclosed herein.

Substances and methods are disclosed for reducing or preventing metastatic behaviour in VGSC expressing cancer by the effect of at least reducing the persistent part of the voltage gated sodium channel current without eliminating the transient part. Inhibition of metastatic cell behaviours such as detachability, lateral motility, transverse migration and invasiveness is demonstrated using the known drugs ranolazine and riluzole.

A method of treating glioblastoma in a patient in need of treatment for glioblastoma, the method comprising administering to the patient a first dosage form comprising a therapeutically effective amount of tolrolizumab or a pharmaceutically acceptable salt thereof is provided.

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

A composition used for preparing a drug for cerebrovascular disease, particularly ischemic cerebrovascular disease, comprising 2-amino-6-trifluoromethoxybenzothiazole or a pharma- ceutical acceptable salt thereof and borneol. The results of non-clinical cell tests and animal efficacy tests show that 2-amino-6-trifluoromethoxybenzothiazole and (+)-2-borneol, when used in combination, have the function of synergistically increasing the efficacy against cerebrovascular disease.

The invention belongs to the technical field of chromatography-mass spectrometry detection, and relates to a method for simultaneously detecting concentrations of riluzole and edaravone. The invention establishes an analysis method for simultaneously detecting riluzole and edaravone based on liquid chromatography-tandem mass spectrometry (LC-MS / MS) for the first time. Mass spectrum response signals of the two drugs are remarkably improved by optimizing key conditions such as mass spectrum ion source parameters, collision energy and declustering voltage. Experimental results show that the quantitation limits of riluzole and edaravone in the method provided by the invention are as low as 1 ng / mL, the monitoring requirement under low blood concentration can be met, and the method is particularly suitable for pharmacokinetic research and trace concentration monitoring of patients taking medicine for a long time.

The present application relates to oral film compositions and dosage forms with precise active dissolution profiles. Disclosed herein are oral membranes for delivering individual unit doses of one or more actives, the membranes having precisely calculated and controlled active dissolution profiles. A wide variety of actives may be used, including, for example, clobazam, diazepam, or riluzole. Also disclosed are methods of treating various diseases and conditions, such as epilepsy and seizures, by administering the oral membranes disclosed herein.

The present invention relates to a process for the preparation of lisethopram. Specifically, the present invention relates to a process for the preparation of 7-(4, 7-diazaspiro [2.5] octane-7-yl)-2-(2, 8-dimethylimidazo [1, 2-b] pyridazin-6-yl) pyrido [1, 2-a] pyrimidin-4-one derivatives, which can be used as pharmaceutically active compounds.

To solve the following problem: since oral films dissolve rapidly, improved dissolution testing is needed for these rapid dissolving products, which enables precise measurements almost immediately upon placement in a liquid and at very small time intervals.SOLUTION: An oral film in an individual unit dose for delivery of one or more actives is disclosed herein, the film having a precisely calculated and controlled active dissolution profile. A wide variety of actives may be used, including, for example, clobazam, diazepam, or riluzole. Also disclosed are methods of treating a variety of diseases and conditions, for example, epilepsy and seizures, by administering the oral film disclosed herein.SELECTED DRAWING: None

The application discloses a 4-(benzo[d]thiazol-2-yl)benzene-1,2-ethylenediamine compound and a preparation method and application thereof. The structural formula of the compound is: the compound has strong ROS scavenging capacity, inhibits lipid peroxidation, can inhibit ferroptosis caused by an iron death inducer, can reduce brain ischemia and nerve damage caused by brain ischemia, and can relieve symptoms of Parkinson's syndrome and other neurological diseases. Therefore, the ferroptosis inhibitor based on the ferrostain-1 / lirilad structure provided by the application can treat diseases related to ferroptosis through multiple actions and has the potential to be developed into a drug for treating diseases related to ferroptosis. Moreover, the ferroptosis inhibitor can be used as an antioxidant fluorescent probe for high-sensitivity detection of a ferroptosis marker, lipid peroxide (PCOOH / PEOOH), can effectively reverse the ferroptosis process of cells, and has a self-indication capacity. The ferroptosis inhibitor is a solid powder, is convenient to store and use, has a simple synthesis method, high yield, low cost, and good popularization prospect.

Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1Λ2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release rihizole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of rihizole from a pro-drug agent.

The invention discloses a double-drug co-delivery lipidosome and a preparation method and application thereof, and belongs to the technical field of biological medicine and nano-drug delivery, the surface of the double-drug co-delivery lipidosome is modified with Angiopep-2 and COG1410, riluzole is loaded, the Angiopep-2 mediates the lipidosome to cross a blood brain barrier, the COG1410 excites a TREM2 pathway to enhance microglial cell mediated A beta removal, and the riluzole is loaded on the lipidosome. Riluzole inhibits glutamic acid release and promotes removal, so that neuronal hyperactivity is reduced; the preparation method of the liposome comprises the following steps: lipid dissolution, hydration, membrane extrusion and gel column purification. The invention also provides an application of the double-drug co-delivery liposome in medicines for treating Alzheimer's disease, provides a composite nano-drug system with cross-BBB capability, A beta removal and neuroprotection, and overcomes the limitation of the existing therapy.

The invention relates to application of riluzole in preparation of medicines for treating obesity and depression, and particularly discloses application of riluzole or pharmaceutically acceptable salts or derivatives of riluzole, and application of riluzole or pharmaceutically acceptable salts or derivatives of riluzole in preparation of medicines or kits for preventing and / or treating obesity and depression codiseases.

The invention relates to the technical field of pharmaceutical analysis, and particularly discloses a method for detecting related substances of 4-trifluoromethoxyaniline. According to the method disclosed by the invention, a capillary column which takes 2, 3-di-O-acetyl-6-0-TBDMS-gamma-cyclodextrin as a stationary liquid is used for carrying out gas chromatographic analysis on a 4-trifluoromethoxyaniline sample; according to the method, the four related substances in the 4-trifluoromethoxyaniline, namely trifluoromethoxybenzene, p-nitro trifluoromethoxybenzene, 2-trifluoromethoxyaniline and 3-trifluoromethoxyaniline, and the contents of the four related substances are accurately detected at the same time. The detection method is high in specificity, low in detection limit and quantification limit, good in linear relation, high in recovery rate, good in repeatability, high in stability, good in durability, easy and rapid to operate, low in detection cost and accurate and reliable in detection result, and guarantees can be provided for monitoring the quality stability and clinical medication safety of riluzole.

The application relates to the technical field of medicines, and discloses application of a tetra-substituted pyrrole derivative in preparation of a product for treating neurodegenerative diseases. The application provides application of the tetra-substituted pyrrole derivative or a pharmaceutically acceptable salt thereof in preparation of the product for treating neurodegenerative diseases. The tetra-substituted pyrrole derivative has high cell safety, and the neuroprotective effect on glutamic acid damage is far higher than that of atrasentan, edaravone and riluzole which are standard clinical drugs; not only can the tetra-substituted pyrrole derivative effectively correct TDP-43 nuclear and cytoplasmic mislocation, but also has the ability of removing insoluble pathological aggregates which atrasentan does not have; the tetra-substituted pyrrole derivative can more effectively inhibit the co-localization of TDP-43 and stress granule protein G3BP1, and intervene in the formation of pathological granules from the source; on a whole animal model, the tetra-substituted pyrrole derivative successfully converts the advantages at the cell level into significant survival benefits, and significantly prolongs the life span of a disease model fruit fly.

Disclosed are methods of treating a disease in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a therapeutically effective amount of riluzole, or a pharmaceutically acceptable salt thereof, in the form of an oral solid molded fast-dispersing dosage form. Pharmaceutical compositions and kits are also disclosed.

An oral film in an individual unit dose for delivery of one or more actives is disclosed herein, the film having a precisely calculated and controlled active dissolution profile. A wide variety of actives may be used, including, for example, clobazam, diazepam, or riluzole. Also disclosed are methods of treating a variety of diseases and conditions, for example, epilepsy and seizures, by administering the oral film disclosed herein.

The invention relates to the technical field of medicines, and discloses an application of a tetra-substituted pyrrole derivative in preparation of a product for treating neurodegenerative diseases. According to the tetra-substituted pyrrole derivative or the pharmaceutically acceptable application of the tetra-substituted pyrrole derivative in preparation of products for treating neurodegenerative diseases, the tetra-substituted pyrrole derivative is high in cell safety, and the neuroprotective effect on glutamic acid injury is far better than that of atrasentan and clinical standard drugs edaravone and riluzole; not only can the nucleoplasm dislocation of the TDP-43 be effectively corrected, but also the capability of removing insoluble pathological aggregates, which is not possessed by the atrasentan, is achieved; the co-localization of the TDP-43 and the stress particle protein G3BP1 can be more effectively inhibited, and the formation of pathological particles is intervened from the source; on the whole animal model, the tetra-substituted pyrrole derivative successfully converts the advantage of the cellular level into remarkable survival benefit, and the life of the disease model fruit flies is remarkably prolonged.

Disclosed are methods of treating cancer using a combination of an immunotherapeutic agent, such as, for example, a PD-1, PD-L1 or CTLA-4 checkpoint inhibitor, and a glutamate modulating agent such as riluzole or trigriluzole. Pharmaceutical compositions and kits including the immunotherapeutic agents and glutamate modulating agents are also disclosed.

The application belongs to the technical field of medicine, and provides a riluzole sustained-release tablet and a preparation method thereof. The sustained-release tablet is composed of a tablet core containing riluzole, a filler, a disintegrant, a glidant, a lubricant and a sustained-release skeleton material, and a sustained-release coating layer containing Eudragit RL 30D, Eudragit RS 30D, triethyl citrate, dimethyl silicone oil emulsion and talc. The prepared riluzole sustained-release tablet is a sustained-release preparation combined with a skeleton type and a membrane-controlled type, has slow drug release, avoids the peak-valley phenomenon, has a simple preparation process, low technical difficulty, small batch difference, good release curve reproducibility and is suitable for large-scale production.

An oral film in an individual unit dose for delivery of one or more actives is disclosed herein, the film having a precisely calculated and controlled active dissolution profile. A wide variety of actives may be used, including, for example, clobazam, diazepam, or riluzole. Also disclosed are methods of treating a variety of diseases and conditions, for example, epilepsy and seizures, by administering the oral film disclosed herein.

Disclosed are methods of treating a disease in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a therapeutically effective amount of riluzole, or a pharmaceutically acceptable salt thereof, in the form of an oral solid molded fast-dispersing dosage form. Pharmaceutical compositions and kits are also disclosed.

The invention belongs to the technical field of medicines, and particularly relates to application of Riluzole in preparation of a medicine for treating colon cancer. The invention discloses a drug Riluzole which has very high affinity with GOLGA8B protein, can significantly improve the thermal stability of the GOLGA8B protein and significantly inhibit the growth of colon cancer cells, and the inhibition effect has dose dependence. In addition, the clone formation capability of colon cancer cells can be remarkably inhibited, and the effect of inhibiting the survival of the colon cancer cells is achieved; apoptosis of colon cancer cells can be promoted, and free migration and invasion of the colon cancer cells can be inhibited; the growth of colon cancer tumor (plt; 0.01) can be obviously inhibited, and the tumor volume and the tumor weight are reduced.

The present disclosure relates to a method of treating or ameliorating symptoms of a motor neurone disease and improving motor neuron survival in a subject, more specifically treating or ameliorating symptoms of amyotrophic lateral sclerosis (ALS) and related neurodegenerative disorders. The treatment method comprises administering a Janus kinase (JAK) inhibitor in combination with one or more compounds selected from a glutamate antagonist and an N-methyl-D-aspartate (NMDA) receptor antagonist, in particular baricitinib in combination with riluzole and / or memantine, and compositions and kits thereof for same.

Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.