30 results about "SERT Proteins" patented technology

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

The invention relates to a particular substituted heterocycle fused gamma-carboline, in free, or pharmaceutically acceptable salt, and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), and / or pathways involving the dopamine D1 and D2 receptor signaling system.

The invention relates to pharmaceutical compositions comprising compounds of Formula Q:wherein W is —N(CH3)—, and Y is —CH(OH)—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and / or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

Compositions comprising mesembryanol, such as (-) mesembryanol or (-) 6-epi-mesembryanol, are disclosed. The disclosed compositions can be used in methods of inhibiting SERT. Also provided are methods of treatment against anxiety or depression, including methods comprising orally administering to a subject in need thereof a therapeutically effective amount of certain pharmaceutical compositions.

Disclosed are compositions containing mesembranol, such as (-) mesembranol or (-)6-epi-mesembrananol. The disclosed compositions can be used in methods for inhibiting SERT. Also provided are methods for treating anxiety and depression, including methods comprising orally administering a therapeutically effective amount of a particular pharmaceutical composition to a subject in need thereof.

This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

Disclosed herein are compounds, compositions, and methods for promoting neuronal growth, improving neuronal structure, and / or increasing serotonin efflux through the serotonin transporter with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders, such as neurological diseases and disorders, with constrained amine psychoplastogens disclosed herein.

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

The present invention relates to specific deuterium-substituted heterocycle fused gamma-carbolines in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of preparing the same. And methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 and D2 receptor signaling systems, and / or [mu]-opioid receptors.

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

The invention relates to pharmaceutical compositions comprising substituted heterocycle fused gamma carbolines, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and / or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

Compositions and methods are provided that are useful for diagnosing, treating, and monitoring alcohol dependence and disorders, susceptibility to alcohol dependence disorders, as well as drug related dependence and disorders. The methods include treating patients with an antagonist of the serotonin receptor 5-HT3 for such disorders, wherein the patient's serotonin transporter gene SLC6A4 is known to have particular genotypes.

Compounds and method for treating a disease, condition, or disorder associated with serotonin (5-HT) signaling, including gastroenterological disorders, such as colitis, irritable bowel syndrome (IBS), constipation, diarrhea, and gastroparesis, or extra-gastrointestinal disorders, such as asthma, migraine, itching, and osteoporosis. In some aspects, the compounds inhibit serotonin / 5-HIT transporter (SERT).

The present invention relates to specific substituted heterocycle fused gamma-carbolines in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and uses thereof in the treatment of compounds related to the 5-HT2A receptor, serotonin transporter (SERT), or the like. Methods of treating diseases involving pathways of dopamine D1 and D2 receptor signaling systems and / or [mu]-opioid receptors.

Provided herein are ibogaine compounds which can be useful for methods of treating a neuropsychiatric disease or neurological disorder, for increasing neural plasticity, or for modulating the function of a serotonin transporter.

Compositions and methods are provided that are useful for diagnosing, treating, and monitoring alcohol dependence and disorders, susceptibility to alcohol dependence disorders, as well as drug related dependence and disorders. The methods include treating patients with an antagonist of the serotonin receptor 5-HT3 for such disorders, wherein the patient's serotonin transporter gene SLC6A4 is known to have particular genotypes.

The gene responsible for encoding SERT has a functional polymorphism at the 5′-regulatory promoter region, which results in two forms, long (L) and short (S). The LL-genotype is hypothesized to play a key role in the early onset of alcohol use. The present invention discloses the differences in treatment and diagnosis based on the L or short genotypes as well as on a single nucleotide polymorphism of the SERT gene, the 3′ UTR SNP rs1042173. The present invention demonstrates the efficacy of using the drug ondansetron and similar drugs for treatment based on variations in the polymorphisms of the SERT gene as well as methods for diagnosing susceptibility to abuse of alcohol and other addiction-related diseases and disorders.

The invention relates to particular deuterated substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

The invention relates to pharmaceutical compositions comprising the compound of Formula I,and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and / or pathways involving dopamine D2 receptor signaling, sodium channel activity, and / or norepinephrine transporter activity.

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

To provide particular substituted heterocycle fused γ-carbolines, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.SOLUTION: The invention provides compounds represented by the formula I in a free or salt form (e.g., a pharmaceutically acceptable salt form), such as an isolated or purified, free or salt form (e.g., a pharmaceutically acceptable salt form).SELECTED DRAWING: None

The invention relates to particular deuterated substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

This invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

Disclosed are compounds of the formulae (II) and (III), and pharmaceutically acceptable salts thereof: (II) (III) wherein * represents the relative cis- or trans- conformations in formulae (II) and (III) respectively and R1, R2, each R3, each R4, n and m are as defined herein. The compounds are modulators of norepinephrine transporters (NET), dopamine transporters (DAT), serotonin transporters (SERT), sigma-1 receptor (σ1R), muscarinic M1 receptors and / or muscarinic M2 receptors and are expected to be useful in the treatment of pain, neuropsychiatric or neurodegenerative diseases, sleep disorders, as a sedative or as an anaesthetic.

The invention discloses an indole piperidine compound with double / multi-target analgesic activity as well as a preparation method and application thereof. The compound has double-target activity of a mu opioid receptor (MOR) / noradrenaline transporter (NET) and a MOR / 5-serotonin transporter (SERT), has multi-target activity of MOR / NET / SERT, and can be used for preparing medicines for preventing or treating pain-related diseases. Experimental results show that the indole piperidine compound provided by the invention has relatively high affinity to MOR / NET, MOR / SERT or MOR / NE / SERT, and meanwhile, the indole piperidine compound shows good analgesic activity in an experiment of neuralgia induced by acetic acid twisting and paclitaxel. Good safety is shown in an acute toxicity experiment and an open field experiment. # imgabs0 #

The disclosure relates to the field of alcohol use disorder. The disclosure provides methods of treating a subject having alcohol use disorder that includes administering ondansetron to a subject having a specified genotype corresponding to genetic variants that effect the 5-HT3 receptor complexes to which ondansetron binds and / or genetic variants that effect the expression of the serotonin transporter.

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

The invention relates to a particular substituted heterocycle fused gamma-carboline, the compound of Formula I, and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and / or pathways involving dopamine D2 receptor signaling, sodium channel activity, and / or norepinephrine transporter activity.