104 results about "Orciprenaline" patented technology

Devices, systems and methods are disclosed for treating or preventing dementia, such as Alzheimer's disease. The methods comprise transmitting impulses of energy non-invasively to selected nerve fibers, particularly those in a vagus nerve, that modulate the activity of a patient's locus ceruleus. The transmitted energy impulses, comprising magnetic and / or electrical energy, stimulate the selected nerve fibers to cause the locus ceruleus to release norepinephrine into regions of the brain that contain beta-amyloids. The norepinephrine counteracts neuroinflammation that would damage neurons in those regions and the locus ceruleus, thereby arresting or slowing the progression of the disease in the patient.

Provided herein are compounds of the formula (I): wherein R1-R8 are as described herein, R4 being phthalazinyl, pyrazinyl, pyridazinyl, or quinoxalinyl. Such compounds are particularly useful in the treatment of a disorder which is created by or is dependent upon decreased availability of serotonin, norepinephrine, or dopamine.

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 relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (−)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient. Finally, the present invention relates to methods of treating mammals suffering from various afflictions, e.g., depression, chronic pain, or fibromyalgia, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of the present invention.

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 present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic and / or serotonin neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient.

The invention relates to the treatment of cardiac dysfunction. In particular, certain compounds, believed to be glucagon-GLP-1 dual agonist compounds, exert a positive inotropic effect while preserving the energy balance of the heart, and so may be superior to known inotropic agents such as dobutamine, norepinephrine and glucagon.

A method of treating a human subject suffering from obesity or who simply desires to lose weight is disclosed, which comprises administering to the subject an effective amount of a compound which enhances serotonin, noradrenaline, and adrenaline activity. The formula is comprised of effective amounts of caffeine, L-phenylalanine, and one or more of L-tryptophan and 5-hydroxytryptophan.

The present invention relates to combinatorial therapies for treating anxiety, depression or psychotic conditions using a lithium salt and a psychoactive drug selected from the group consisting of serotonin reuptake inhibitor, a 5HT2 receptor antagonist, an anticonvulsant, a norepinephrine reuptake inhibitor, an α-adrenoreceptor antagonist, an NK-3 antagonist, an NK-1 receptor antagonist, a PDE4 inhibitor, an Neuropeptide Y5 Receptor Antagonists, a D4 receptor antagonist, a 5HT1A receptor antagonist, a 5HT1D receptor antagonist, a CRF antagonist, a monoamine oxidase inhibitor, a sedative-hypnotic drug, and an atypical antipsychotic.

The invention relates to a medicinal composition taking a medicinal indianmulberry root oligosaccharide extract and a non-saccharide antidepressant medicament as active ingredients. The medicinal composition is characterized in that: the total content of inulin type oligosaccharide in the medicinal indianmulberry root oligosaccharide extract is 50 to 70 percent, and the content of inulin type penta-polyoligosaccharide is 5 to 15 percent; the non-saccharide antidepressant medicament comprises monoamine oxidase inhibitor type antidepressant medicaments such as moclobemide and the like, norepinephrine reuptake inhibitor type antidepressant medicaments such as imipramine, amitriptyline, maprotiline, doxepin, chlorimipramine or reboxetine and the like, selective 5-serotonin reuptake inhibitor type antidepressant medicaments such as fluoxetine, paroxetine, sertraline or citalopram and the like, or methylepinephrine / selective 5-serotonin dual reuptake inhibitor type non-saccharide antidepressant medicaments such as mirtazapine, duloxetine, venlafaxine or demethyl venlafaxine and the like. The invention also relates to the application of the medicinal composition taking the medicinal indianmulberry root oligosaccharide extract and the non-saccharide antidepressant medicament as the active ingredients in treating nervous and mental diseases such as depression, anxiety disorders, neuropathic pains and the like.

The invention provides a method of producing oligodendrocytes by in vitro differentiation of human multi-potent progenitor cells (MLPCs). The method comprises culturing isolated MLPCs on a first surface in a serum-free defined culture medium; replacing the culture medium with serum-free culture medium supplemented with bFGF, EGF and PDGF-AA for approximately 24 hours; changing the cultured MLPCs into the supplemented serum-free culture medium further supplemented with differentiation factors norepinephrine, forskolin. and K252a; establishing a 3D environment by covering the culture with a second surface opposite and spaced apart from the first surface, so as to contain the MLPCs therebetween; and continuing to culture until a majority of the MLPCs have differentiated into oligodendrocytes. Additionally included is a method of treatment for a subject afflicted by a disease characterized by central or peripheral nervous system demyelination, the method comprising transplanting into the subject oligodendrocytes produced according to the method disclosed.

The invention discloses an application of daylily and total flavonoids thereof in preparing antidepressant drug, in particular discloses an application of daylily and the total flavonoids thereof in preparing medicines for increasing 5-hydroxytryptamine, noradrenalin, dopamine and 5-dydroxy group indoleacetic acid in cerebral cortex. The application of daylily and the total flavonoids thereof in preparing antagonism reserpine medicine is also disclosed. The applications are testified by pharmacological experiment.

The present invention is directed to a method of treating a patient suffering from the metabolic syndrome and / or related disorders including obesity, Type 2 diabetes, pre-diabetes, hypertension, dyslipidemia, insulin resistance, endothelial dysfunction, pro-inflammatory state, and pro-coagulative state, and comprising the steps of (a) providing to the patient a dietary regimen that decreases overactive CNS noradrenergic tone; followed by (b) providing to the patient a dietary regimen that increases dopaminergic tone while maintaining the above decreased overactive CNS noradrenergic tone. The present invention is also directed to food products useful in implementing the dietary regimens.

In a first aspect, the present invention relates to a process for producing a stable, injectable solution with low content of noradrenaline, which includes dissolving noradrenaline and optionally an excipient in deoxygenated or degassed water, filtrating the resulting noradrenaline solution in a nitrogen current, distributing the solution in a nitrogen current, and sterilization, preferably hot. The invention further provides a stable, injectable solution with low content of noradrenaline, substantially free of anti-oxidizing and preservative agents, as well as uses thereof in the medical and pharmaceutical fields.

The compounds of the present invention are represented by the following 2,5-methano- and 2,5-ethano-tetrahydrobenzazepine derivatives having formula (I):where the carbon atom designated * is in the R or S configuration when n is 1 and the substituents X and R1-R7 are 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 invention belongs to the technical field of clinical biological sample detection. The invention specifically relates to a technology for detecting catecholamine and metabolites thereof in blood plasma, in particular to a method for detecting catecholamine and metabolites thereof (epinephrine, norepinephrine, dopamine, metanephrine, normetaneprine and 3-methoxytyramine) by high-throughput liquid chromatography-tandem mass spectrometry. The method comprises the steps of standard solution preparation, sample treatment, sample detection and formula calculation. The method can be used for simultaneously detecting six substances including catecholamine and metabolites thereof, and has the advantages of high accuracy, high sensitivity, high specificity, small required sample volume, simple sample pretreatment, good tolerance and the like.

The present invention is directed to phenylaminopropanol derivatives of formula (I): or a pharmaceutically acceptable salt thereof; wherein: the dotted line between Y and Z represents an optional double bond; the dotted line between the two R4 groups represents an optional heterocyclic ring of 4 to 6 ring atoms that may be formed between the two R4 groups, together with the nitrogen through which they are attached; Y is N, CR6, or C=O; Z is N, CR7, CR5, or C(R5)2; R2 is aryl substituted with 0-3 R1 or heteroaryl substituted with 0-3 R1; R3 is H or C1-C4 alkyl; n is an integer form 0 to 4; x is an integer from 1 to 2; and the other substituents are defined in the claims; 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 form the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

The aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepine derivative compounds of the present invention are represented by formulae 1(A-D) having the following structure: where the substituents X and R1-R8 are as defined herein.

Crystalline forms of 4-[2-(4-methylphenylsulfanyl)-phenyl]piperidine and salts thereof are provided e.g. for the treatment of neuropathic pain.

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 invention provides alkyne compounds as well as a preparation method and an application thereof and belongs to the technical field of extraction of alkyne compounds and effective ingredients of traditional Chinese medicines. Specifically, new compounds I, II and IV as well as a reported compound III are obtained from dried roots of Umbeliferae Bupleurum Radix Bupleuri through extraction and separation. In-vitro monoamine neurotransmitter reuptake inhibition experiments are conducted on the compounds, results indicate that the compounds I, II, III and IV have inhibition effects on reuptake of NA (noradrenaline), have the inhibition effects equivalent to that of positive control drug desipramine and have different degrees of inhibition effects on reuptake of 5-HT (5-hydroxytryptophan). The four compounds have anti-depression activity and are expected to be developed into drugs or prodrugs for preventing and treating anti-depression related diseases.

The invention discloses new medicinal application of 3,6'-disinapoyl sucrose (DISS), in particular the application of the 3,6'-disinapoyl sucrose (DISS) in preparing a product for treating tristimania. The 3,6'-disinapoyl sucrose (DISS) has better therapeutic effect on treating the tristimania caused by various reasons and obvious anti-depression activity to a pharmacological depression model, and the anti-depression activity of the 3,6'-disinapoyl sucrose is relative to the enhancement of the functions of 5-hydroxytryptamine (5-HT) and noradrenergic (NE) nerves. The DISS has no central excitation or inhibitive action within the range of an effective dosage of anti-depression.

The invention relates to a traditional Chinese medicine composition used for treating depression after apoplexy. The traditional Chinese medicine composition comprises the following bulk drugs in parts by weight: 20-50 parts of vinegar-processed radix bupleuri, 20-50 parts of grass-leaved sweetflag rhizome, 20-50 parts of Cyperus Rotundus L, 20-50 parts of white peony root, 20-50 parts of curcuma tuber, 20-60 parts of Poria cocos, 10-35 parts of prepared pinellia tuber, 20-60 parts of red sage root, 30-90 parts of oyster, and 20-60 parts of spine date seed. The traditional Chinese medicine composition can be prepared to any dosage form of a particulate agent, a mixture, a capsule, pills and a tablet, which are used for treating depression after apoplexy, and the traditional Chinese medicine composition has the effect for adjusting 5-hydroxytryptamine, norepinephrine and dopamine levels in brain, can be conveniently used, and is easily accepted by patients.

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 invention discloses an autism diagnosis kit, the autism diagnosis kit comprises a reagent for detecting the intestinal microbial metabolite concentration, wherein the intestinal microbial metabolite comprises at least one of acetic acid, tyramine, histamine, gamma-aminobutyric acid, dihydroxyphenylalanine and norepinephrine. The acetic acid content and the score of the severity degree of the autism are in a negative correlation relationship; the contents of tyramine, histamine, gamma-aminobutyric acid, dihydroxyphenylalanine and norepinephrine are respectively in positive correlation withthe severity of autism, and the autism is diagnosed through the intestinal microbial metabolite level of an excrement sample, so that the kit has relatively high accuracy. Therefore, the intestinal microorganism metabolite combination level of a subject can be used as an index for screening and diagnosing autism under the conditions of scientific research and clinical application.