50 results about "Reuptake inhibitor" patented technology

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.

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.

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.

The invention relates to a medicament containing selective 5-hydroxytryptamine reuptake inhibitor which mainly refers to a composition taking paroxetine or a pharmaceutically acceptable salt of the paroxetine as main curing integrant, in particular to an intestinal-dissolved sustained-release composition slowly released by passing through stomach via oral taking. The medicament comprises four layers, namely, a drug pellet containing the paroxetine as an active integrant, a sustained-release layer coating on the exterior layer of the drug pellet and presenting sustained-release function, an isolated layer and an intestinal-dissolved layer, wherein, the weight ratio of paroxetine, adjuvant, the sustained-release layer and the intestinal-dissolved layer is 0.5- 5.0: 3-30: 0.5-3.0: 0.8-3.0. The drug preferentially selects a pellet, and can reduce a side effect due to the use of a common sustained-release preparation and individual difference caused by an internal environment factor.

This invention is directed in one embodiment to pharmaceutical compositions and methods for treating depression in a mammal. To a mammal in need of such treatment are administered: (i) at least one serotonin reuptake inhibitor or pharmaceutically acceptable salt thereof; and (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 herein.

The present invention relates to fused bicyclic pyrimidine containing zinc-binding moiety based derivatives that have unique properties as protein tyrosine kinase (PTK) inhibitors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

The present invention relates to substituted 2-indolinone containing zinc-binding moiety based derivatives that have enhanced or unique properties as inhibitors of protein tyrosine kinase (PTK) receptors and their use in the treatment of PTK related diseases and disorders such as cancer. The said derivatives may further act as HDAC inhibitors.

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.

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.

The present invention is directed to methods for providing long-term treatment of fibromyalgia syndrome (FMS) by administering a dual re-uptake inhibitor to a patient with FMS. More particularly, the present invention is directed to the long-term treatment of FMS by administering a norepinephrine-serotonin reuptake inhibitor (NSRI) to a patient with FMS.

The invention discloses a compound preparation for treating cardiovascular and cerebrovascular diseases. The compound preparation comprises a cholesterol reuptake inhibitor, an HMG-CoA (3-hydroxy-3-methyl-glutaryl) reductase inhibitor and a calcium ion antagonist, and has the effect of jointly lowering blood pressure and lipid. According to the compound preparation, isolating layers or / and coatings are arranged for active ingredients or a part of active ingredients, and the usage amount of antioxidants in a precipitation is reduced, therefore, the medicine therapeutic range is expanded, the stability and safety of the medicine are improved; simultaneously, the medication compliance of a patient suffering from hypertension and hyperlipemia is improved.

Benzofuranyl-and benzothienyl-piperzinyl quinoline derivatives and compositions containing such compounds are disclosed. Methods of using benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives and compositions containing such composition in the treatment and / or prevention of serotonin-related disorders, such as depression and anxiety, are also disclosed. In addition, processes for the preparation of benzofuranyl- and benzothienyl-piperzinyl quinoline derivatives are disclosed.

A new treatment methodology and pharmacological composition for the treatment and remission of Parkinson's Disease and other neurological diseases are provided. The medication and treatment are based on the use of a combination of a phosphodiesterase inhibitor medication, commonly used to treat male erectile dysfunction, and a high-dose of serotonergic synaptic reuptake inhibitor medication, commonly used to treat depression, anxiety disorders, obsessive compulsive disorder and various panic phobias.The treatment regime is based upon the discovery that the primary cause of PD and various other related neurological conditions is dysfunction in the serotonergic pathways involving the brainstem, nucleus of Raphe, and various projecting serotonergic fibers. It has been determined that this dysfunction can be overcome by increasing the levels of the ligands and neurotransmitters cyclic-GMP and serotonin and the consequential increased binding of these ligands and neurotransmitters to efferent neuron receptors in the synapse. Testing indicates that the inventive treatment changes Parkinson's Disease from a debilitating, progressive, frightening, and previously untreatable pre-morbid condition to one that is rapidly reversible.

The invention discloses an improved and optimized preparation method of piper laetispicum extractive, extractive obtained by the method and application of the extractive used as a neurotransmitters reuptake inhibitor in treating and / or preventing nervous and mental diseases associated with monamine transmitter in the fields of medical treatment, healthcare and food additive and the like. Compared with the piper laetispicum extractive obtained by the existing preparation method, the piper laetispicum extractive obtained by the preparation method of the invention remarkably increases the antidepressant activity and synchronously reduces the acute toxicity to a mouse further; and moreover, the extractive obtained by the method provided by the invention remarkably increases the security when being used as medicine, and further strengthens the effectiveness.

There is provided a selective serotonin reuptake inhibitor having affinity for serotonin 1A receptors which comprises a cyclic amine represented by the formula: wherein G represents a formula (2): a prodrug of said cyclic amine, or a pharmaceutically acceptable salt of said cyclic amine or prodrug, as an active ingredient.

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 novel combination of a serotonin selective re-uptake inhibitor (SSRI) and an agonist of the serotonin 4 (5-HT4) receptor to augment and / or provide faster onset of the therapeutic effect of the SSRI alone or administered with any other compound which causes an elevation in the level of extracellular serotonin (5-HT). The present invention also relates to a pharmaceutical formulation comprising said combination and to a method and use of said combination in the treatment of depression, anxiety, obsessive compulsive disorder (OCD) or other disease or disorder responsive to a SSRI.

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.

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 relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.

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.

The present invention relates to an azetidine derivative or a pharmaceutically acceptable salt thereof, and an antidepressant agent or a composition for the prevention or treatment of psychiatric disorders including the same. The azetidine derivative is useful as a triple reuptake inhibitor capable of inhibiting reuptake of the neurotransmitters, dopamine, serotonin, and norepinephrine at the same time.

The invention discloses compositions, and provides a method for preventing and / or treating depression by using the compositions, and applications of the compositions in preparing medicines for preventing and / or treating depression. The compositions contain cannabidiol, a 5-HT2A receptor antagonist, and a 5-HT reuptake inhibitor or medicinal salt thereof, and also can comprise one or more medicinalcarriers or excipients, wherein the use amount of cannabidiol and the use amount of the 5-HT2A receptor antagonist and the 5-HT reuptake inhibitor or the medicinal salt thereof enable the effect of the composition to be superior to that obtained when the medicines with the corresponding dosages are independently used.

The invention discloses a compound preparation for treating depression with the traditional antidepressant and curcumin as active components; the traditional antidepressant is a nonselective reuptake inhibitor or a selective 5-hydroxytryptamine reuptake inhibitor, wherein the nonselective reuptake inhibitor is desipramine, the selective 5-hydroxytryptamine reuptake inhibitor is fluoxetine, and the mass ratio of the traditional antidepressant to the curcumin can concretely be 2:1 or 4:1. In the compound preparation for treating the depression, low dosage curcumin and low dosage desipramine or fluoxetine are combined, thereby counteracting the adverse effects caused by blood sugar rise and displaying stronger antidepressant activity, and therefore, the compound preparation has good application prospect.

The invention relates to a solid pharmaceutical preparation containing one or more solid carriers and / or excipients and an active substance selected from among the Monoamine Neurotransmitter Re-uptake Inhibitors which have a 2,3-disubstituted tropane structure, the preparation thereof and use thereof for preparing a pharmaceutical composition for the treatment or prevention of central-nervous diseases or disorders.

Provided is a highly potent and selective endocannabioid cellular reuptake inhibitor represented by formula (I):or a pharmaceutically acceptable solvate or co-crystal thereof as well as to a formulation comprising this inhibitor, and to methods of treatment in which this inhibitor is used.

The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

The invention relates to an application of fluoxetine in an anti-mycobacterium tuberculosis drug. The fluoxetine hydrochloride is a first antidepressant known as a selective 5-hydroxytryptamine reuptake inhibitor (SSRIs), and the fluoxetine is a racemic mixture of R- and S- enantiomers, which have the same pharmacological activity; and the fluoxetine has anti-tuberculosis effect and has good development value. The use of fluoxetine in the anti-mycobacterium tuberculosis drug and the significant anti-tuberculosis effect of fluoxetine are disclosed for the first time.

The present applications discloses novel 8-aza-bicyclo[3.2.1]oct-3-yloxy)-chromen-2-one derivatives and their use as monoamine neurotransmitter re-uptake inhibitors. In other aspects the applications discloses the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

The invention discloses compounds of the following formula (I) wherein R<1> R<2>, n, Ar<1> and A<2> are as defined in the specification, in vivo-hydrolysable precursors thereof, pharmaceutically acceptable salts thereof, the use in therapy and pharmaceutical compositions and methods of treatment using the same. The example compounds are 1-(2-(naphthylmethoxy)-1-phenylethyl)piperazine derivatives. The compounds are neurokinin 1 (NK1) receptor antagonist and / or serotonin reuptake inhibitors, with medical indications for depression and other disorders.