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47 results about "Monoamine transporter" patented technology

Monoamine transporters (MATs) are protein structures that function as integral plasma-membrane transporters to regulate concentrations of extracellular monoamine neurotransmitters. Three major classes of MATs (SERT, DAT, NET) are responsible for the reuptake of their associated amine neurotransmitters (serotonin, dopamine, norepinephrine). MATs are located just outside the synaptic cleft (peri-synaptically), transporting monoamine transmitter overflow from the synaptic cleft back to the cytoplasm of the pre-synaptic neuron. MAT regulation generally occurs through phosphorylation and posttranslational modification. Due to their significance in neuronal signaling, MATs are commonly associated with drugs used to treat mental disorders as well as recreational drugs, a line that can become quite blurred in many cases. Compounds targeting MATs range from medications such as the wide variety of tricyclic antidepressants, selective serotonin reuptake inhibitors such as fluoxetine (Prozac) to stimulant medications such as methylphenidate (Ritalin) and amphetamine in its many forms (Adderall, Dexedrine) and derivatives methamphetamine (Desoxyn) and lisdexamfetamine (Vyvanse). Furthermore, drugs such as MDMA ("ecstasy", "molly") and natural alkaloids such as cocaine exert their effects in part by their interaction with MATs, by blocking the transporters from mopping up dopamine, serotonin, and other neurotransmitters from the synapse.

Dual-action inhbitors and methods of using same

Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.
Owner:AERIE PHARMA

Dual mechanism inhibitors for the treatment of disease

Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
Owner:AERIE PHARMA

Cycloalkylamines as monoamine reuptake inhibitors

The invention relates to novel cyclohexylamine derivatives and their use in the treatment and / or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
Owner:SEPACOR INC

Fluorescent Substrates for Monoamine Transporters as Optical False Neurotransmitters

The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ═O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK

Phenyl substituted cycloalkylamines as monoamine reuptake inhibitors

Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat / prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.
Owner:SUNOVION PHARMA INC

Fluorescent substrates for monoamine transporters as optical false neurotransmitters

The present invention relates to compounds of the general structure: wherein Y is O, X is O, bond α is absent and bond β is present, or Y is H, X is CH, bond α is present, and bond β is absent; atom Z is a carbon and bonds χ, δ and γ are present, or is a nitrogen and bonds χ, δ and γ are absent; R1 is —H, —OH, —O—R7, —N(H)—R8, —N(H)—(CH2)n—NH2, —N(R9)(R10), or a piperazine cation; R2 is either covalently bound to R9, or is —H, or is covalently bound to R3 so as to form a substituted or unsubstituted pyrrole or R2 is covalently bound to R9 or R8 or R7; or R1 and R2 are covalently joined to form an aromatic ring; R3 is either covalently bound to R2 so as to form a pyrrole, or is, inter alia, —H, —OH, alkyl, or when Z is nitrogen R3 is ═O; R4 is, inter alia, —H, —OH, or —R11NH2; R5 is, inter alia, —H, —OH, or —R12NH2, and R6 is either is covalently bound to R10 or is —H, or R6 is covalently bound to R10 or R8 or R7. This invention also provides processes for making the compounds as well as methods for monitoring activity of monoamine transporters or treating monoamine transporter-associated diseases by employing the compounds.
Owner:THE TRUSTEES OF COLUMBIA UNIV IN THE CITY OF NEW YORK

Tetralone-based monoamine reuptake inhibitors

ActiveUS8053603B2Increase synaptic availabilityImprove usabilityBiocideNervous disorderDiseaseSynaptic cleft
The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.
Owner:SUNOVION PHARMA INC

Tetralone-based monoamine reuptake inhibitors

ActiveUS20070197588A1Increase synaptic availabilityImprove usabilityBiocideNervous disorderSynaptic cleftTetralone
The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.
Owner:SUNOVION PHARMA INC

Monoamine reuptake inhibitors

The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.
Owner:RES TRIANGLE INST

P-450-catalyzed enantioselective cyclopropanation of electron-deficient olefins

The present invention pertains to the use of engineered variants of enzyme CYP102A, also known as P450-BM3, for cyclopropanation of olefins containing electron-withdrawing groups. One exemplary enzyme variant, referred to as BM3-HStar, contains five mutations away from wild-type P450-BM3, and demonstrates high activity towards cyclopropanation of olefinic substrates using ethyldiazoacetate (EDA) and other carbene transfer reagents. Products of these reactions are potential precursors of levomilnacipran derivatives, a class of compounds that have been shown to be selective inhibitors of monoamine transporters. In addition, cyclopropanation reactions with the P450-BM3 enzyme variants of the invention can be conducted in whole cells expressing the enzyme variants and can proceed under aerobic conditions.
Owner:CALIFORNIA INST OF TECH

Genetic screening for predicting antidepressant drug response based on the monoamine transporter gene polymorphism combination

InactiveUS20080248470A1Microbiological testing/measurementNoradrenaline reuptake inhibitorBiology
The present invention discloses is a method of selecting a drug based on personal genetic information when prescribing an antidepressant for a depressed patient. According to the invention, either a noradrenaline reuptake inhibitor (NRI) antidepressant or a selective serotonin reuptake inhibitor (SSRI) antidepressant can be selected based on the combination of monoamine transporter gene polymorphisms, that is, NET G1287A polymorphism in a norepinephrine transporter (NET) gene, serotonin transporter gene (5-HTT) promoter polymorphism and 5-HTT gene intron 2 polymorphism. Also, based on the norepinephrine transporter gene NET G1287A polymorphism alone, the noradrenaline reuptake inhibitor (NRI) antidepressant can be selected.
Owner:RES & BUSINESS FOUND SUNGKYUNKWAN UNIV

Substituted Pyran Derivatives

ActiveUS20140309427A1Potent activityOrganic chemistryMonoamine transportBiochemistry
Certain 3,6-disubstituted and 2, 4, 5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3, 6 and 2, 4, 5 pyrans are useful in probing the effects of their binding to monoamine transporter systems and the corresponding relationships to various afflictions affecting the CNS, or as a treatment for various CNS-related disorders in which the monoamine transport and related systems are implicated.
Owner:WAYNE STATE UNIV

Cycloalkylamines as monoamine reuptake inhibitors

The invention relates to novel cyclohexylamine derivatives and their use in the treatment and / or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
Owner:SUNOVION PHARMA INC

Hydroxybupropion analogues for treating drug dependence

InactiveUS8906908B2Organic active ingredientsNervous disorderHydroxybupropionAntagonist
The invention provides hydroxybupropion analogues capable of inhibiting the reuptake of one or more monoamines and / or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and / or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and / or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
Owner:RES TRIANGLE INST +2

Pyrrolidine triple reuptake inhibitors

In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and / or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
Owner:SUNOVION PHARMA INC

Monoamine reuptake inhibitors

The invention provides bupropion analogue compounds capable of inhibiting the reuptake of one or more monoamines. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin. Such compounds may be used to treat conditions that are responsive to inhibition of the reuptake of monoamines, including addiction, depression, and obesity.
Owner:RES TRIANGLE INST

Polypharmacophoric agents

One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.
Owner:MOLECULAR INSIGHT PHARMA

Pyrrolidine triple reuptake inhibitors

In various embodiments, the present invention provides cycloalkyl pyrrolidine compounds and methods for their use in the treatment and / or prevention of various diseases, conditions and syndromes, including central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.
Owner:SUNOVION PHARMA INC

Method for analyzing action of drugs on monoamine transporter based on liquid chromatography-mass spectrometry

The invention belongs to the technical field of biological analysis, and relates to a method for analyzing the action of drugs on monoamine transporters, in particular to a method for analyzing the action of drugs on monoamine transporters based on liquid chromatography-mass spectrometry. The method can be used for researching the action mechanism of drugs on dopamine transporters and 5-hydroxytryptamine transporters. The method is high in sensitivity, strong in specificity and high in safety, and can be used for replacing a traditional radioisotope detection method.
Owner:FUDAN UNIV

Sulfonyl fluoride compound and application thereof

The invention discloses a sulfonyl fluoride compound. Compared with reported PET imaging agents for targeted amino acid transporter, fibroblast activating protein, vesicular monoamine transporter 2, serotonin receptor and prostate specific membrane antigen protein change related diseases, the series of sulfonyl fluoride compounds designed and synthesized by the invention have the advantages of simple labeling conditions, high yield and high affinity. The invention belongs to the technical field of radiopharmaceutical chemistry and nuclear medicine.
Owner:首都医科大学脑重大疾病研究中心

Phenyl substituted cycloalkylamines as monoamine reuptake inhibitors

Phenyl-substituted cyclohexylamine derivatives and method for their synthesis and characterization are disclosed. Use of these compounds to treat / prevent neurological disorders as well as methods for their synthesis are set forth herein. Exemplary compounds of the invention inhibit reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine (e.g., from the synaptic cleft) and modulate one or more monoamine transporter. Pharmaceutical formulations incorporating compounds of the invention are also provided.
Owner:SUNOVION PHARMA INC

Polypharmacophoric agents

One aspect of the present invention relates to polypharmacophoric compounds. In certain embodiments, the polyphamacophore compounds comprise individual pharmacophore units selected from the group consisting of D-1 agonists, D-2 agonists, D-3 agonists, D-4 agonists, irreversible monoamine inhibitors, reversible monoamine inhibitors, monoamine transporter inhibitors, COMT inhibitors, MAO inhibitors, and dopamine transporter inhibitors. Moreover, the present invention also relates to combinatorial libraries of polypharmacophoric compounds. Another aspect of the present invention relates to the use of a polypharmacophoric compound in a method of treating a mammal in need thereof. For example, a polypharmacophoric compound of the present invention may be used in a method of treating a mammal afflicted with Alzheimer's Disease, Huntington's Disease, depression, attention deficit disorder, autism, obesity, or inflammation.
Owner:MOLECULAR INSIGHT PHARMA

Substituted pyran derivatives

ActiveUS9458124B2Potent activityOrganic chemistryMonoamine transportBiochemistry
Certain 3,6-disubstituted and 2,4,5-trisubstituted pyran derivatives that exhibit potent activity on monoamine transport systems are provided. The 3,6 and 2,4,5 pyrans are useful in probing the effects of their binding to monoamine transporter systems and the corresponding relationships to various afflictions affecting the CNS, or as a treatment for various CNS-related disorders in which the monoamine transport and related systems are implicated.
Owner:WAYNE STATE UNIV

Tropane analogs and methods for inhibition of monoamine transport

New tropane analogs that bind to monoamine transporters are described, particularly, 8-aza, 8carbo and 8-oxo tropanes having 6- or 7-hydroxyl or ketone substituents. The compounds of the present invention can be racemic, pure R-enantiomers, or pure S-enantiomers. Certain preferred compounds of the present invention have a high selectivity for the DAT versus the SERT. Also described are pharmaceutical therapeutic compositions comprising the compounds formulated in a pharmaceutically acceptable carrier and a method for inhibiting 5-hydroxy-tryptamine reuptake of a monoamine transporter by contacting the monoamine transporter with a 5-hydroxytryptamine reuptake inhibiting amount of a compound of the present invention. Preferred monoamine transporters for the practice of the present invention include the dopamine transporter, the serotonin transporter and the norepinephrine transporter.
Owner:ORGANIX +1

Dopamine-, norepinephrine- and serotonin-transporter-selective heterocyclic compounds and their therapeutic applications

One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aforementioned compounds in a method of treating a disorder of the central nervous system in a mammal.
Owner:GEORGETOWN UNIV

A kind of crystal form of valbenazine di-p-toluenesulfonate and its preparation method and use

A crystal form of Valbenazine di-p-toluenesulfonate and its preparation method, a pharmaceutical composition containing the crystal form, and the use of the crystal form in the preparation of vesicular monoamine transporter 2 inhibitors and pharmaceutical preparations for treating tardive dyskinesia use in .
Owner:CRYSTAL PHARMA CO LTD
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