207 results about "Reuptake" patented technology

The present invention is directed to phenylaminopropanol derivatives of formulae I, II, and III: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, schizophrenia, and combinations thereof.

The present invention relates to a kit and an intervenously administrable preparation, both, with a signal transmitter precursor, an enhancer of precursor uptake, and an inhibitor of neurotransmitter reuptake or signal transmitter catabolism. The kit also contains an appropriate swab for obtaining oral cells suitable for allelic analysis. The intervenous formulation contains similar materials and, in some cases, ethanol. Either the kit composition or the intervenous formulation may be used as guided by a subjects allelic analysis. Collections of particular alleles, especially those relating to neural system are comprehensible in terms of likelihood of success in the administration of an interveinous formulation or ingestion of components of the subject kit.

The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.

The present invention is directed to cyclic sulfonamide derivatives of formula I:or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, vasomotor symptoms, sexual dysfunction, gastrointestinal disorders and genitourinary disorder, depression disorders, endogenous behaviorial disorder, cognitive disorder, diabetic neuropathy, pain, and other diseases or disorders.

The compounds of the present invention are represented by the chemical structure found in Formula (I): wherein: the carbon atom designated * is in the R or S configuration; and X is a fused bicyclic carbocycle or heterocycle selected from the group consisting of benzofuranyl, benzo[b]thiophenyl, benzoisothiazolyl, benzoisoxazolyl, indazolyl, indolyl, isoindolyl, indolizinyl, benzoimidazolyl, benzooxazolyl, benzothiazolyl, benzotriazolyl, imidazo[1,2-a]pyridinyl, pyrazolo[1,5-a]pyridinyl, [1,2,4]triazolo[4,3-a]pyridinyl, thieno[2,3-b]pyridinyl, thieno[3,2-b]pyridinyl, 1H-pyrrolo[2,3-b]pyridinyl, indenyl, indanyl, dihydrobenzocycloheptenyl, tetrahydrobenzocycloheptenyl, dihydrobenzothiophenyl, dihydrobenzofuranyl, indolinyl, naphthyl, tetrahydronaphthyl, quinolinyl, isoquinolinyl, 4H-quinolizinyl, 9aH-quinolizinyl, quinazolinyl, cinnolinyl, phthalazinyl, quinoxalinyl, benzo[1,2,3]triazinyl, benzo[1,2,4]triazinyl, 2H-chromenyl, 4H-chromenyl, and a fused bicyclic carbocycle or fused bicyclic heterocycle optionally substituted with substituents (1 to 4 in number) as defined in R14; with R1, R2, R3, R4, R5, R6, R7, R8, and R14 defined herein.

The present invention is directed to phenylaminopropanol derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromylagia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

The present invention relates to a method of treating disorders by administering to a patient in need of such treatment a therapeutically effective amount of a compound of formula (I): wherein R1—R8 are as described herein, R4 being aryl or heteroaryl.

Methods for treating chronic widespread pain associated with drug therapy or radiation therapy are described. The method generally involves administering a therapeutically effective amount of a dual or tri reuptake inhibitor of a specific type or a pharmaceutically acceptable salt thereof. Preferably the compound is a non-tricyclic dual reuptake inhibitor. The most preferred compound is milnacipran or a bioequivalent or pharmaceutically acceptable salt thereof. Other preferred compounds are duloxetine and venlafaxine or a bioequivalent or pharmaceutically acceptable salt thereof. In yet another embodiment, a therapeutically effective amount of a non-tricyclic triple reuptake inhibitor (“TRI”) compound of a specific type, or a pharmaceutically acceptable salt thereof, is administered. The TRI compounds are characterized by their ability to block the reuptake (and, hence, increase central concentrations of) the three primary brain monoamines: serotonin, noradrenaline, and dopamine.

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.

Compounds of formula (a), (b), (c), or (d), or any mixture thereof, or a pharmaceutically-acceptable salt thereof;wherein R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl or 2-hydroxyethyl; R3 is -CH2-X-R', wherein X is O, S or NR'', wherein R'' is hydrogen or alkyl and R' is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, or -CO-alkyl; R4 is phenyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; 3,4-methylenedioxyphenyl; benzyl optionally substituted with halogen, CF3, CH, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino nitro, heteroaryl, or aryl; heteroaryl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl; or naphthyl optionally substituted with halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino, nitro, heteroaryl, or aryl. The compounds are monoamine neurotransmitter, i.e., dopamine, serotonin, noradrenaline, reuptake inhibitors.

The present invention relates to a kit and an intravenously administrable preparation, both with a signal transmitter precursor, an enhancer of precursor uptake, and an inhibitor of neurotransmitter reuptake or signal transmitter catabolism. The kit also contains an appropriate swab for obtaining oral cells suitable for allelic analysis. The intravenous formulation contains similar materials and, in some cases, ethanol. Either the kit composition or the intravenous formulation may be used as guided by a subjects allelic analysis. Collections of particular alleles, especially those relating to neural system are comprehensible in terms of likelihood of success in the administration of an intraveinous formulation or ingestion of components of the subject kit.

Provided are analogs of methylphenidate (“MPH”) that are useful for the treatment of drug addiction, attention deficit disorder, attention deficit hyperactivity disorder, and depression. The MPH analogs are extended duration compounds that bind to the dopamine transporter and the reuptake of dopamine in the afflicted individual's brain. Because of the extended duration of the MPH analogs, administration of the compounds is only required on a once or twice daily schedule.

This invention is directed to pharmaceutical compositions and methods for treating a disorder or condition selected from the group consisting of depression, anxiety disorders, phobias, avoidant personality disorder, eating disorders, chemical dependencies, Parkinson's diseases, obsessive-compulsive disorder, negative symptoms of schizophrenia, cognitive dysfunction related to schizophrenia, premenstrual syndrome, stress-induced incontinence, headache, neuropathic pain, chronic pain, urinary incontinence, post-traumatic stress disorder, chronic stress, acute stress, fibromyalgia, depression comorbid with fibromyalgia, obesity, migraine and a combination thereof in a mammal. The methods in one embodiment comprise administering to a mammal in need of treatment for the disorder or condition: (i) at least one serotonin reuptake inhibitor or pharmaceutically acceptable salt thereof; (ii) at least one norepinephrine reuptake inhibitor or pharmaceutically acceptable salt thereof, wherein the norepinephrine reuptake inhibitor is selected from the group consisting of Structure II, Structure III, and Structure IV as defined in the specification; and (iii) a pharmaceutically acceptable carrier. The pharmaceutical compositions and methods of the invention are also useful for preventing a relapse associated with one of the foregoing disorders or conditions, and for treating a symptom associated with one of the foregoing disorders or conditions, wherein the symptom is selected from the group consisting of cognitive dysfunctions and somatic complaints.

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.

This invention is directed to methods for preventing or ameliorating sleep-related breathing disorders. The method comprises administration to a patient in need thereof an effective dose of one or a combination of prostanoid receptor antagonists (eg. ramatroban, ifetroban, diphloretin, phosphate, polyphloretin phosphate, seratrodast, SC19220). The prostanoid receptor antagonist or combination of prostanoid receptor antagonists can be administered in conjunction with one or more serotonin receptor agonists, one or more cannabinoids receptor agonists, one or more serotonin reuptake inhibitors, one or more noradrenalin reuptake inhibitors, a combination of reuptake inhibitors, an inhibitor of prostanoid synthesis, or any combination of the foregoing.

The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.

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.

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.

Compounds of the general formula (1), wherein one of W, X, Y and Z is N or CR4 and the others are each CH; and R4 is a specified substituent. These compounds inhibit monocamine reuptake, and are useful in the treatment of pain, emesis depression, post traumatic stress disorders, attention deficit disorders, obsessive compulsive disorders, pre-menstrual syndrome, substance abuse and sexual dysfunction.

The invention provides a new indole compound, pharmaceutically acceptable salts and medicinal preparations thereof, and a use of the new indole compound in selective inhibition of 5-hydroxytryptamine reuptake and / or excitation of a 5-HT1A receptor. The invention also relates to medicinal compositions comprising the compounds, and a method for treating the central nervous system dysfunction of mammals, especially humans by using the medicinal compositions.

The present invention relates to (−)-1-(3,4-dichlorophenyl )-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing a disorder alleviated by inhibiting dopamine reuptake. In certain embodiments the methods and compositions of the invention are effective for treating attention-deficit disorder, depression, obesity, Parkinson's disease, a tic disorder, and / or an addictive disorder. In more detailed embodiments, methods and compositions of the invention are provided for treating an alcohol-related addictive disorder, for example alcohol abuse, alcohol dependence, excess alcohol consumption, and / or alcohol withdrawal. The (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or pharmaceutically acceptable salt thereof may be employed within the methods and compositions of the invention in a form or composition that is substantially free of its corresponding (+)-enantiomer.

A yeast extract or yeast-derived bioactive peptide having an activity of selectively inhibiting reuptake of serotonin and norepinephrine, which can be effectively used in preventing or treating various diseases related to reuptake of serotonin and norepinephrine, especially depression, anxiety, stress, fatigue and obesity are provided. Also, a yeast extract or yeast-derived bioactive peptide having activities as an anti-stress agent, an anti-fatigue agent, premenstrual syndrome (PMS) and menstrual pain relaxants, and a brain-neurotrophic factor, and a method for preparing the bioactive peptide are provided. The yeast extract or yeast-derived bioactive peptide is effective in relieving stress, nervousness, anxiety, tension, insomnia, fatigue, and imbalance in the autonomic nerve regulation. Therefore, the yeast extract or yeast-derived bioactive peptide is vailable as an anti-depression agent, an anti-anxiety agent, an anti-stress agent, an anti-fatigue agent, an anti-obesity agent, premenstrual syndrome and menstrual pain relaxants, a bain-neurotrophin, and a source of active foods having these activities.

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.

The present invention relates to methods of inhibiting native and promiscuous uptake of biogenic amine neurotransmitters with triple reuptake inhibitors in the treatment of conditions affected by monoamine neurotransmitters.

The present invention provides compositions useful for treating and preventing ryanodine receptor associated disorders comprising a PDE-associated agent and a pharmaceutically acceptable carrier. The present invention also provides methods for treating or preventing ryanodine receptor associated disorders including cardiac disorders and diseases, skeletal muscular disorders and diseases, cognitive disorders and diseases malignant hyperthermia, diabetes and sudden infant death syndrome. The present invention further provides methods for regulating PKA phosphorylation of a ryanodine receptor as well as methods for regulating Ca+2 release and reuptake in cells. Also provided are kits for use in delivering a PDE-associated agent to cardiac cells in a subject, comprising the composition of the present invention and a catheter.

The invention relates to the use of compound Laetispicine in the process for preparing pharmaceutical compositions for suppressing central nerve system monoamine transmitter reuptake related diseases, wherein the compound Laetispicine can be used as raw material for preparing pharmaceutical compositions for inhibiting central nerve system monoamine transmitter reuptake related diseases.

Methods are provided for facilitating psychological extinction of a deleterious, high-anxiety response that is disproportionate to the threat offered by a given stimulus. An afflicted subject is treated with a cannabinoid reuptake inhibitor in conjunction with extinction training. The methods are relevant for treatment of anxiety disorders, including phobic disorders and PTSD, in addition to other afflictions such as chronic pain, insomnia, and erectile dysfunction.