71 results about "Amine receptor" patented technology

The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

The present invention relates to spiroazacyclic compounds as monoamine receptor modulators; compositions comprising the same; methods of inhibiting an activity of a monoamine receptor with said compounds; methods of treating a disease condition associated with a monoamine receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

Compositions and methods for providing relief from pain and / or discomfort associated with gastrointestinal disorders, including, for example, bloating, crying, gas, cramping, regurgitation, diarrhea and gastrointestinal pain, associated with colic comprising, at least one antiflatulent, at least one histamine H1-receptor antagonist, and optionally, one or more prebiotic and / or one or more probiotic.

The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

The invention pertains to a composition and a method for the treatment of mood disorders, in particular of treating, preventing or alleviate depression, mood disorders or insufficient mood, obesity, overweight, premenstrual syndrome, craving, carbohydrate craving, chocolate craving, menopausal complaints, erectile dysfunction and / or reduced libido. The composition contains cocoa or one or more of its pharmacologically active components, and a dopamine D2 receptor agonist.

The invention is directed to compositions comprising at least one nanoparticulate H1-histamine receptor antagonist, such as ebastine or a salt or derivative thereof, having improved dissolution rate providing a faster onset of drug availability. The nanoparticulate H1-histamine receptor antagonist particles, such as ebastine, have an effective average particle size of less than about 2000 nm and are useful in the treatment of seasonal and perennial allergic rhinitis and related diseases.

The present invention relates to a dopamine D3 receptor portion excitant or its pharmaceutically acceptable salt and its application for curing diseases of central nervous system. Said invention also provides its chemical structure general formula, and provides detailed description.

The invention provides application of a compound with the structure as shown in the formula (I) in the specification, or a medical salt, a hydrate or a solvate, of the compound, in preparation of a medicine for treating nervous system diseases relevant to the dopamine receptor, and a preparation method of the compound with the structure as shown in the formula (I) in the specification or the medical salt, the hydrate or the solvate, of the compound. The compound has multiple pharmacologic functions such as mu-opioid receptor excitation and dopamine D2 receptor blocking, and has good physicochemical properties and oral bioavailability, and integral animal experiment shows that the compound has remarkable and long-lasting analgesia and calm activity and can be applied to treatment on pain and other mental diseases.

Disclosed are methods for treating cancer by administering an inhibitor of the interaction of glutamate with the NMDA / glycine / polyamine receptor / ion channel complex.

The invention relates to particular substituted deuterated heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and / or pathways involving dopamine D1 / D2 receptor signaling systems, and / or the treatment of residual symptoms.

The disclosure provides compounds having formula (I), wherein the substituents are as defined herein. The compounds are useful for modulating the dopamine D3 receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.

The present invention provides the application of clove oil, eugenol and derivatives thereof in the preparation of antagonists or inverse agonists of histamine H3 receptors, and also provides a method of using clove oil, eugenol or eugenol derivatives as The main active ingredient, together with other active ingredients, forms a new H3 receptor antagonist or inverse agonist drug, which can be used to prevent and treat senile dementia and depression. The H3 receptor antagonist or inverse agonist medicine provided by the invention has clear efficacy, controllable quality and safety, and provides a new choice for clinical practice.

The invention provides pyrrolidine compounds, salts thereof, applications of the compounds or the salts thereof in nuclear magnetic probes and medicines, a reagent, and a medicine. The benzamide methylpyrrolidine compounds have a chemical structure represented by general formula (I); and in the formula (I), R<1> is selected from a methyl group, an ethyl group, a methoxy group, an ethoxy group and halogen, R<2> is selected from a methyl group, an ethyl group, a methoxy group, an ethoxy group and halogen, R<3> is selected from C1-5 alkyl groups and H, X<1> is selected from C1-10 alkylene groups or is deleted, X<2> is selected from -(CH2CH2O)n- (n is 1-5) or is deleted, X<3> is selected from C1-5 alkyl groups, X<4> is selected from oxygen, sulfur and a methylene group, and Ln is selected from Gd and Eu. The compounds have a gadolinium and europium chelating structure formed by combining with a dopamine D2 receptor and depending on intramolecular chelating groups, and specifically enhance the contrast of dopamine D2 receptor expression tissues on images in magnetic resonance imaging.

The present invention is directed to N-linked quinoline amide compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.

One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

The present invention relates to novel dopamine D2 receptor ligands. The invention further relates to functionally-biased dopamine D2 receptor ligands and the use of these compounds for treating or preventing central nervous system and systemic disorders associated with dysregulation of dopammode inergic activity. The present invention relates to novel compounds that modulate dopamine D2 receptors. In particular, compounds of the present invention show functional selectivity at the dopamine D2 receptors and exhibit selectivity downstream of the D2 receptors, on the 0-arrestin pathway and / or on the cAMP pathway.

The invention relates oral phamiaceuticai compositions for the modified release delivery of cariprazine (trans-N-{4-[2-[4-(2,3-dichlorophenyl)-piperazin-l-yl]-ethyl]-cyclohexyl}-N',N'- dimethylurea) or pharmaceutically acceptable salts thereof for less than daily dosing. The invention also relates to the use of said compositions in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors. The invention also relates to the process for the preparation of said modified release pharmaceutical compositions.

The invention discloses a domperidone oral disintegrating tablet, and a method for preparing the same and a method for quality control. The domperidone oral disintegrating tablet is prepared from domperidone and auxiliary materials, and the quality thereof is controllable and stable. The domperidone oral disintegrating tablet is a peripheral dopamine receptor agonist which is safe and effective. Compared with the prior art, the domperidone oral disintegrating tablet has the advantages of rapid disintegration, convenient taking, no vomiting, rapid effect, and low side effect.

The present invention relates to an ophthalmic composition comprising at least two active pharmaceutical ingredients. In particular, the active pharmaceutical ingredients are selected from the group consisting of: an alpha 2 adrenergic receptor agonist; a beta-adrenergic receptor agonist; an immunosuppressant; a lymphocyte associated antigen antagonist; an anti-inflammatory; a beta-blocker; a prostaglandin analog; a histamine receptor antagonist; a carbonic anhydrase inhibitor; and an antibiotic. In some embodiments, the composition of the invention is a nanoemulsion formulation. In one particular embodiment, the first active pharmaceutical ingredient is an alpha 2 adrenergic receptor agonist. The present invention also provides a method for treating various clinical conditions associated with an eye disorder or eye disease using the composition of the invention.

This invention relates to novel diazabicyclic biaryl derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

The present invention relates to a novel piperazine derivative represented by Formula I having an activity for regulating dopamine D3 receptor, stereoisomers thereof, pharmaceutically acceptable salts or solvates, and a pharmaceutical composition comprising the compound, a process for preparing the same, and use thereof in the prevention or treatment of a disease associated with central nervous system dysfunction, such as Parkinson's disease, schizophrenia, drug addiction and relapse, as well as kidney protection and immunoregulation, or as a tool for researching D3R function or diseases associated with D3R dysfunction.

The invention relates oral pharmaceutical compositions for the modified release delivery of cariprazine (trans-N-{4[2-[4-(2,3-dichlorophenyl)-piperazin-1-yl]-ethyl]-cyclohexyl}-N′,N′-dimethylurea) or pharmaceutically acceptable salts thereof for less than daily dosing. The invention also relates to the use of said compositions in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors. The invention also relates to the process for the preparation of said modified release pharmaceutical compositions.

Novel dopamine receptor ligands of the formula: pharmaceutical formulations of such compounds, and a method using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system, are described. The compounds are expected to be useful in treating Parkinson's disease, improving cognition, improving memory, improving the negative symptoms of schizophrenia, improving attention-deficit hyperactivity disorder and related developmental disorders, treating substance abuse disorders, and in treating various peripheral conditions where changes in dopamine receptor occupation affects physiological function, including organ perfusion, cardiovascular function, and selected endocrine and immune system functions.

Provided are a posttraumatic stress disorder (PTSD) animal model in which dopamine receptor subtype 4 (D4R) is damaged or deficient, a method for preparing the same, a method for screening a drug for treating PTSD using the same, and a pharmaceutical composition for treating PTSD comprising a drug detected by the screening method. As it is identified that a specific type of dopamine receptor is associated with a mechanism for fear memory expression induced by long-term depression (LTD), the understanding of pathogenesis of PTSD may be heightened, the animal model exhibiting similar clinical conditions of PTSD and the method for preparing the same may be applied in analyses for stability and effectiveness of a therapeutic agent for PTSD and screening of a therapeutic drug. Further, an agonist of D4R contained in the composition has been approved by the US FDA and clinically used for psychiatric diseases such as schizophrenia, and thus may be immediately used for clinical applications for PTSD symptoms.

The invention belongs to the technical field of biomedicine and particularly relates to a novel pharmaceutical use of a dopamine receptor 1 antagonist, and to a novel use of the dopamine receptor 1 antagonist in preparing drugs for the treatment of ketamine-induced schizoid symptoms in mice. The dopamine receptor 1 antagonist is selected from SCH23390 having a molecular formula of C17H18ClNO.HCl,and is one or only one effective ingredient to the drugs. A drug for the treatment of ketamine-induced schizoid symptoms in mice comprises the dopamine receptor 1 antagonist having the effective amount (5 mg / kg). The dopamine receptor 1 antagonist is used as one means to treat ketamine-induced schizoid behaviors of mice, and scientific basis is provided for the research and development of a methodto effectively relieve schizoid symptoms in mice.

The present invention provides for prevention and / or treatment of neurological or neuropsychiatric disorders involving abnormal D1-D2 dopamine receptor coupling and / or activation. Methods and agents are provided for modulating dopamine receptor function arising from D1-D2 coupling and / or activation. Agents of the present invention include fragments of D2 receptor or D1 receptor that can disrupt D1-D2 coupling.

Compositions and methods for providing relief from pain and / or discomfort associated with gastrointestinal disorders, including, for example, bloating, crying, gas, cramping, regurgitation, diarrhea and gastrointestinal pain, associated with colic comprising, at least one antiflatulent, at least one histamine H1-receptor antagonist, and optionally,one or more prebiotic and / or one or more probiotic.