42 results about "Norepinephrine reuptake" patented technology

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject comprising administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and a greater inhibition of norepinephrine reuptake than serotonin reuptake, and wherein said compound is not administered adjunctively with phenylalanine or tyrosine. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Compositions, and methods of use thereof, are provided for the prevention or treatment of side effects associated with the use of drugs that act as 5HT2 / 5HT3 serotonin receptor antagonists and alpha-2 adrenergic receptor antagonists (5HT2 / 5HT3 antagonist / alpha-2 antagonist). The method involves using dopamine-releasing compounds, such as amantadine, anticonvulsants, such as zonisamide, or dopamine / norepinephrine reuptake inhibitors, such as bupropion, in combination with 5HT2 / 5HT3 antagonist / alpha-2 antagonists, such as mirtazapine, to reduce the excessive daytime drowsiness and / or weight gain associated with 5HT2 / 5HT3 antagonist / alpha-2 antagonist use for the treatment of disorders, such as, depression, schizophrenia, anxiety disorders, sleep-related breathing disorders, insomnia, migraine headache, chronic tension-type headache, hot flashes, lower back pain, neuropathic pain and functional somatic syndromes. Formulations of dopamine-releasing compounds or anticonvulsants with 5HT2 / 5HT3 antagonist / alpha-2 antagonists are provided. In particular embodiments, combination therapy with mirtazapine and zonisamide provides relief from chronic low back pain, while reducing or avoiding side effects associated with monotherapy with mirtazapine or zonisamide.

The present invention relates to inhibitors of serotonin and / or norepinephrine reuptake and specifically provides compounds of formula (I): wherein A is selected from —O— and —S—; X is selected from C1-C8 alkyl, C2-C8 alkenyl, and C4-C8 cycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from phenyl, pyrrolidinyl, piperidinyl, morpholinyl, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, —CF3, —CN and —CONH2; Y is selected from (a), (b), (c), (d), (e), (f) where R3, R4 and R5 are independently selected from hydrogen, halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R6 and R7 are independently selected from halo, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R8 is selected from chloro, bromo, iodo, C1-C4alkyl, C1-C4 alkoxy, C1-C4 alkyl-S(O)n— where n is 0, 1 or 2, nitro, acetyl, —CF3, —SCF3 and cyano; R1 and R2 are each independently hydrogen or C1-C4 alkyl; or pharmaceutically acceptable salts thereof; or compositions thereof and methods of using the same.

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

Selective norepinephrine reuptake inhibitors are useful for the prevention or treatment of hot flashes, vasomotor symptoms, impulse control disorders or personality change due to a general medical condition.

Highly selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agorophobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, visceral pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.

The present invention relates to novel 3,5-substituted indole compounds of Formula (I) having nitric oxide synthase (NOS) inhibitory activity together with inhibitory activity at the norepinephrine transporter (NET), to pharmaceutical and diagnostic compositions containing them, and to their medical use.

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 provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject. The method generally involves administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and an equal or greater inhibition of norepinephrine reuptake than serotonin reuptake. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

The present invention provides a method of treating fibromyalgia syndrome (FMS), chronic fatigue syndrome (CFS), and pain in an animal subject comprising administering a therapeutically effective amount of a dual serotonin norepinephrine reuptake inhibitor compound or a pharmaceutically acceptable salt thereof, wherein said dual serotonin norepinephrine reuptake inhibitor compound is characterized by a non-tricyclic structure and a greater inhibition of norepinephrine reuptake than serotonin reuptake, and wherein said compound is not administered adjunctively with phenylalanine or tyrosine. In particular, the use of milnacipran to treat FMS, CFS, and pain is disclosed.

The present invention relates to selective adrenergica2B antagonists alone, selective adrenergicα2B antagonists in combination with norepinephrine reuptake inhibitors (NRI) (as a single compound or as a combination of two or more compounds), or selective adrenergicα2B antagonists in combination with dual norepinephrine reuptake inhibitors / serotonin reuptake inhibitors (NRI / SRI) (as a single compound or as a combination of two or more compounds) and methods of their use in the treatment of vasomotor symptoms.

In one aspect, the invention relates to compounds of formula I:where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

A reduction in the side effects of treating with an agent having combined 5HT2 / 5HT3 and alpha-2 antagonistic activity is obtained by administering an agent having selective norepinephrine reuptake inhibitory or histamine H1 agonist activity. In some embodiments, the invention provides synergistic combinations of 5HT2 / 5HT3 antagonist / alpha-2 antagonist and selective norepinephrine reuptake inhibitor or histamine H1 agonist.

Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agoraphobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.

The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and / or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Selective dual serotonin and norepinephrine reuptake inhibitors are provided. These compounds have a lower side-effect profile and are useful in compositions and products for use in treatment of a variety of conditions including depression, fibromyalgia, anxiety, panic disorder, agorophobia, post traumatic stress disorder, premenstrual dysphoric disorder, attention deficit disorder, obsessive compulsive disorder, social anxiety disorder, generalized anxiety disorder, autism, schizophrenia, obesity, anorexia nervosa, bulimia nervosa, Gilles de la Tourette Syndrome, vasomotor flushing, cocaine and alcohol addiction, sexual dysfunction, borderline personality disorder, fibromyalgia syndrome, diabetic neuropathic pain, chronic fatigue syndrome, pain, Shy Drager syndrome, Raynaud's syndrome, Parkinson's Disease, and epilepsy.

The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.

The present invention relates to aniline derivatives of the general formula I and their use as serotonin reuptake inhibitors and preferably also norepinephrine reuptake inhibitors in the treatment of depression, anxiety, affective disorders, pain disorders, attention deficit hyperactivity disorder (ADHD) and stress urinary incontinence.

Many medications, herbal remedies and procedures have side affects that contribute to cognitive dysfunction. Because of these side effects patients may choose to discontinue medication or treatment (such as ECT) which has a detrimental effect on treatment. Currently, there are no medications approved for helping to alleviate these symptoms. The invention describes a novel treatment for individuals who experience various side effects of cognitive dysfunction. The invention additionally describes how these medications may enhance cognitive function in individuals with normal cognitive functioning who might benefit from this type of enhancement. The subject invention further provides materials and methods for the treatment, prevention, or ameliorate medication-induced cognitive dysfunction comprising the administration of medications or compositions comprising at least one selective norepinephrine reuptake inhibitors (SNR1) and / or buproprion.

In one aspect, the invention relates to compounds of formula (I): where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula (I) are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and / or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

The present invention develops methods for treating or preventing depression secondary to atypical pain (DSP). The methods generally comprise administering an effective amount of a monoamine reuptake inhibitor to treat or prevent the symptoms of DSP. In a preferred embodiment, a therapeutically effective dose of a specific type of dual serotonin norepinephrine reuptake inhibitor (SRNI) compound or a pharmaceutically acceptable salt thereof is administered. Most preferably the SNRI compounds are non-tricyclic SNRIs, wherein the serotonin reuptake inhibition is stronger than norepinephrine reuptake inhibition; NSRIs, wherein the norepinephrine reuptake inhibition is stronger than serotonin reuptake inhibition inhibition. The most preferred compound is milnacipran or a bioequivalent or pharmaceutically acceptable salt thereof. Other preferred compounds are duloxetine, venlafaxine or bioequivalent or pharmaceutically acceptable salts thereof. In another embodiment, a therapeutically effective amount of a particular type of non-tricyclic triple reuptake inhibitor ("TRI") compound, or a pharmaceutically acceptable salt thereof, is administered. TRI compounds are characterized by blocking the reuptake (and thus increasing central concentrations) of three major brain monoamines: serotonin, norepinephrine and dopamine.

The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.

The present invention relates to the use of compounds and composition of compounds that modulate norepinephrine levels for the prevention and treatment of vasomotor symptoms, such as hot flush, caused by, inter alia, thermoregulatory dysfunctions.

The invention refers to a synergistic combination comprising a Sigma ligand of general formula (I), and a Serotonin-Norepinephrine Reuptake Inhibitor (SNRI), a medicament comprising said active substance combination, and the use of said active substance combination for the manufacture of a medicament, particularly for the prophylaxis and / or treatment of pain.

The present invention provides compounds, specifically novel tropane analogs, capable of acting as inhibitors of reuptake of monoamines. In preferred embodiments, these compositions are selective inhibitors of serotonin and / or norepinephrine reuptake. Also provided herein are pharmaceutical compositions comprising novel tropane analogs and a pharmaceutically acceptable carrier, and methods for treating conditions in which inhibition of reuptake of monoamines is desired. The inventive compositions as described herein are also useful for medical therapy and diagnosis.

Provided are methods and medicaments for treating stuttering or another communication disorder, comprising administering to a patient in need of such treatment an effective amount of a selective norepinephrine reuptake inhibitor.

The present invention provides a method for treating or preventing a disease or disorder treatable by the inhibition of serotonin reuptake in a patient, and / or norepinephrine reuptake and / or dopamine reuptake in a patient, the method comprising administering to the patient a neurotransmitter reuptake inhibiting-effective amount of at least one compound of the formula A-L-B (I) or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein A is a psychotropic derivative; L is a linking group comprising two carbon atoms; and B is an alkyl, alkenyl, alkynyl or aralkyl comprising at least one substituent of the formula Q, wherein: the alkyl, alkenyl, alkynyl or aralkyl is optionally substituted with one or more halogean halogens, hydroxyl, cyano, nitro, amino or thiol; and Q is OR6, OC(O)R6, C(O)R6, C(S)R6, CO2R6, C(O)SR6, C(O)NR6R7, C(S)NR6R7, NR6R7, NR6C(O)R7, NR6C(S)R7, NR6C(O)NR7R8, NR6C(S)NR7R8, NR6SO2R7, NR6SO2NR7R8, SR6, SC(O)R6, SC(O)NR6R7, S(O)R6, SO2R6, SO2NR6R7, or NR6SO2NR7R8.