43 results about "Amine receptor" patented technology

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 present invention relates to the field of pharmaceutical chemistry, and discloses a salt of carebastine and its use, which solves the problems of the prior art, such as poor solid form of carebastine, many impurities, instability, difficulty in purification, difficulty in mass synthesis, and inapplicability to medicinal use. The salt of carebastine of the present invention includes, but is not limited to, acid salts or base salts, particularly potassium salt, sodium salt, methanesulfonate salt and p-toluenesulfonate salt. The salt of carebastine of the present invention is used in the preparation of drugs for histamine H1 receptor antagonists. The salt of carebastine of the present invention has the characteristics of easy purification, high stability, simple process, easy industrial production, and good hygroscopicity and convenient storage. And the salt of the present invention can enter the body quickly and exert its medicinal effect, has good oral absorption, and is superior to ebastine in both safety and individual variation, and is a promising anti-allergic disease drug for development.

Provided are methods and compositions for enhancing radiotherapy in various cancers by administering dopamine receptor (DRD2)‐binding phenylpiperazine derivatives such as brexpiprazole, cariprazine, pipamperone, and perospirone. In vitro studies show that combining these agents with ionizing radiation (e.g., 5 Gy) significantly reduces cancer cell survival, suppresses metastatic and stemness markers (e.g., CD44, MMP‑2, Snail, Nanog), and promotes apoptosis. Fractionated or single‐fraction radiation regimens can be paired with DRD2 antagonists to lower treatment‐resistant phenotypes, decrease the likelihood of recurrence, and potentially reduce necessary radiation dosages. The approach applies to breast, prostate, lung, pancreatic, and brain cancers, among others. Depending on tumor characteristics, additional chemotherapeutic or immunotherapeutic agents may further improve outcomes.

The present invention provides the use of phenylquinolinone and flavonoid derivatives for neuropathic pain, and the phenylquinolinone and flavonoid derivatives include pharmaceutically acceptable salts thereof. The compound of the present invention is a histamine H3 receptor antagonist, which has a different mechanism of action from existing drugs and can be used in the preparation of drugs for treating neuropathic pain diseases. The effect of the compound of the present invention in treating neuropathic pain is better than amitriptyline, gabapentin, pregabalin and carbamazepine, indicating that the compound of the present invention has a better therapeutic effect, has the characteristics of small dosage, good efficacy, high bioavailability and safety, and compared with opioid drugs, the compound of the present invention is not addictive and is a very effective drug for treating neuropathic pain diseases. Therefore, the clinical application prospects are huge. The general structural formula is as follows:

The present disclosure generally relates to binding agents that are capable of targeting tumor cells and immune cells. The binding agents of the present disclosure are multispecific and comprise antigen binding domains that are capable of binding to Dopamine Receptor D2 (DR2), to Programmed Cell Death Protein 1 (PD-1) and / or to Cluster of Differentiation 47 (CD47). The multispecific binding agents of the present disclosure may be used to treat subjects in need thereof.

Provided are allyl tryptamines, such as asymmetric allyl tryptamines. In some embodiments, such compounds modulate the activity of monoamine receptors and / or monoamine transporters. Also provided are methods for the preparation of allyl tryptamines and pharmaceutical compositions thereof. Methods of using the allyl tryptamines, alone or in combination with other therapeutic agents, are provided. In some embodiments, allyl tryptamines are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders, or are used for the improvement of mental health or functioning.

[Problem] To provide a substance having an activity of antagonizing the binding of histamine to histamine-H3 receptor, or having an activity of inhibiting the homeostatic activity of histamine-H3 receptor. [Means for Solution] A compound of the following formula (I) is provided: [wherein X, Y, Z and W each independently represent a methine group optionally having 1 or 2 substituents, or a nitrogen atom (provided that a case where all of X, Y, Z and W are an optionallysubstituted methine group); A, B and D represent C(0)-, etc.; Q represents a methine group or a nitrogen atom; R represents an optionallysubstituted group of the following formula (II-1): (wherein R7 and R8 each independently represent a lower alkyl group, etc.)].

The present disclosure aims to provide an exercise effect-mimicking agent capable of producing effects similar to those of exercise without actually exercising. An exercise effect-mimicking agent containing at least one compound selected from the group consisting of (A) an α-adrenergic antagonist, (B) a flavonoid, (C) a dopamine D2 receptor antagonist, and (D) an NF-κB signaling pathway inhibitor.

Provided are allyl tryptamines, such as asymmetric allyl tryptamines. In some embodiments, such compounds modulate the activity of monoamine receptors and / or monoamine transporters. Also provided are methods for the preparation of allyl tryptamines and pharmaceutical compositions thereof. Methods of using the allyl tryptamines, alone or in combination with other therapeutic agents, are provided. In some embodiments, allyl tryptamines are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders, or are used for the improvement of mental health or functioning.

The invention belongs to the technical field of pharmaceutical chemicals, and provides a dopamine D3 receptor radioactive tracer and a preparation method and application thereof. According to the dopamine D3 receptor radiotracer (11C-YQA14) disclosed by the invention, a structure as shown in a formula 1 is used as a precursor compound, and gaseous 11C-CH3I is introduced under a closed condition to obtain the 11C-YQA14. The dopamine D3 receptor radioactive tracer has ideal affinity to a dopamine D3 receptor and has low affinity to a dopamine D2 receptor, so that the dopamine D3 receptor radioactive tracer can selectively recognize the dopamine D3 receptor and has low recognizability to the dopamine D2 receptor.

Disclosed are novel C4-carboxylic acid-substituted tryptamine derivative compounds and pharmaceutical and recreational drug formulations containing the same. The pharmaceutical formulations may be used to treat brain neurological disorders through the modulation of various receptors, such as 5-HT1A receptor, a 5-HT2A receptor, a 5-HT1B receptor, a 5-HT2B receptor, a 5-HT3A receptor, an ADRA1 A receptor, an ADRA2A receptor, CHRM1 receptor, a CHRM2 receptor, a CNR1 receptor, a DRD1 receptor, a DRD2S receptor, or an OPRD1 receptor.

The invention belongs to the technical field of neurobiology, and particularly relates to application of a dopamine D2 receptor G protein antagonist in preparation of a drug for treating drug addiction. Researches show that the dopamine D2 receptor G protein antagonist can inhibit recurrence after drug addiction fading induced by ignition of small-dose drugs. A mouse cocaine self-administration addiction model is adopted, a small dose of cocaine is given after model mice are subjected to regression training, and the recurrence behavior of the mouse cocaine addiction after regression is induced. A signal channel dependent on dopamine D2 receptor downstream G protein is inhibited before addiction recurrence is induced by a small dose of cocaine, and recurrence after drug-induced cocaine fading can be inhibited; however, the signal pathway for inhibiting the dependence of beta-arretin on the downstream of the dopamine D2 receptor cannot inhibit the recurrence after drug-induced cocaine fading. The invention discloses the effect of the G protein biased antagonist of the dopamine D2 receptor in treatment of drug addiction, and provides a new thought and a drug intervention target for treatment of drug addiction of cocaine and the like.

This 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.

This invention provides a method for treating postoperative nausea and vomiting using buccal acupuncture combined with a triple antiemetic regimen. The method employs a combined intervention of buccal acupuncture and a triple antiemetic regimen. The triple regimen consists of a 5-HT3 receptor antagonist, a glucocorticoid, and a dopamine receptor antagonist, administered intravenously in two separate doses. The buccal acupuncture uses CA-2 (upper jiao), CA-3 (middle jiao), and CA-4 (lower jiao) as core acupoints, with auxiliary and reinforcing acupoints added based on the surgical site and high-risk groups. A standardized procedure of pecking stimulation is applied, along with a corresponding postoperative remedial antiemetic medication regimen. This invention organically combines multi-target drug blockade with buccal acupuncture's visceral regulation, synergistically enhancing the antiemetic effect, reducing the incidence of nausea and vomiting, and decreasing the need for remedial medication. The regimen is highly standardized, widely adaptable, and can meet the postoperative nausea and vomiting control needs of various surgeries and high-risk groups. It exhibits good safety, strong repeatability, and high clinical application value.

The present invention provides a piperazine derivative, as shown in formula (I) or its stereoisomers and pharmaceutically acceptable salts thereof; the piperazine derivative provided by the present invention has a strong affinity for dopamine D2, D3, and 5-HT1A, 5-HT2A receptors of 5-hydroxytryptamine, and has a medium affinity for dopamine D4 and 5-HT2C, 5-HT7 of 5-hydroxytryptamine and α1-adrenaline, histamine H1 receptors, and also has a medium affinity for 5-hydroxytryptamine reuptake sites, and has no obvious affinity for cholinergic muscarinic receptors. Functionally, it is a partial agonist of D2 and 5-HT1A receptors and an antagonist of 5-HT2A receptors, and can be used to treat or prevent diseases that require regulation of one or more of dopamine D2 receptors, 5-HT1 receptors, 5-HT2 receptors, 5-HT7 receptors, α1-adrenaline receptors, histamine H1 receptors and 5-hydroxytryptamine reuptake sites.

The invention relates to the technical field of biological medicine, in particular to application of vanillyl alcohol in preparation of a dopamine receptor D2 antagonist, and the application proves that the vanillyl alcohol can be specifically combined with a D2 receptor with micromole-level affinity through micro-thermophoresis and biological layer interference technologies. Cell experiments show that vanillyl alcohol can antagonize D2 receptor mediated ERK signal pathway activation in a concentration-dependent manner, and has no agonist activity. In a PCPA-induced insomnia mouse model, vanillyl alcohol can shorten the sleep latency and prolong the total sleep time in a dose-dependent manner. After a D2 receptor is knocked down in nucleus septum, the sleep promoting effect of vanillyl alcohol disappears, and it is confirmed that the drug effect of vanillyl alcohol has target dependence. As a low-toxicity natural small molecule, vanillyl alcohol provides a new choice for developing a novel insomnia treatment medicine.

The invention belongs to the technical field of biological catalysis, and discloses a method for synthesizing a nitrogen-containing heterocyclic ring compound through multi-enzyme-stage combination, which comprises the following steps: by taking alpha, omega-diamine as a substrate, catalyzing one amino group into aldehyde (carbonyl) through one-step enzyme catalysis, then carrying out ammonia-aldehyde condensation on the intermediate in an aqueous solution, and spontaneously cyclizing to generate cyclic imine, thereby obtaining the nitrogen-containing heterocyclic ring compound. And finally, further catalyzing imine by utilizing imine reductase to obtain the nitrogen-containing heterocyclic ring compound. The nitrogen-containing heterocyclic ring compound is synthesized from alpha, omega-diamine by utilizing two-step enzyme catalysis and constructing different amine receptor and cofactor circulation systems, the method belongs to a biosynthesis method, the raw materials are easy to obtain, the operation is simple and convenient, an efficient method is provided for synthesis of the nitrogen-containing heterocyclic ring compound, and the method is suitable for industrialization.

The present invention generally relates to binding agents capable of targeting tumor cells and immune cells. The binding agents of the present invention are multispecific and comprise antigen binding domains capable of binding to dopamine receptor D2 (DR2), binding to programmed cell death protein 1 (PD-1), and / or binding to cluster of differentiation 47 (CD47). The multispecific binding agents of the present invention are useful for treating an individual in need thereof.

The present invention belongs to the pharmaceutical field, and provides an aryl heterocyclic compound and a preparation method and use thereof, wherein the structural formula is shown in formula (I). The compound provided by the present invention has a monoamine system regulating effect, and has binding activity to monoamine transporter proteins and G protein-coupled receptors such as 5-hydroxytryptamine receptors, dopamine receptors, and trace amine receptors. Such compounds have the potential to be applied to the treatment of various diseases, including but not limited to depression, anxiety, schizophrenia, attention deficit disorder, obesity, pain, and neurodegenerative diseases.

The application provides a compound with histamine H3 receptor protein degradation activity and a preparation method and application thereof, and belongs to the field of medicines. The application provides a compound shown in formula I, the compound has obvious degradation effect on HRH3 protein, the compound can be used for preparing a histamine H3 receptor degrading agent, and is used for treating diseases related to the activity of HRH3 protein. The application further proves through experiments that the compound has the effects of significantly improving cognition, learning and memory and attention, and has a wide application prospect. A-L-B formula I.

The invention comprises a method for treatment of ADHD or ADHD-related disorders by a pharmaceutical agent exhibiting combined serotonergic or noradrenergic reuptake transporters and monoamine receptor activity.

The present application relates to a kind of new isoquinoline alkaloid compound and its preparation method and purposes.The new compound (Corybungine A-L) provided by the present application is extracted and separated from Papaveraceae Corydalis bungeana Turcz., a kind of novel isoquinoline alkaloid with novel structure.Biological activity experiment shows that the alkaloid compound has dopamine D2 receptor antagonistic activity, and can be applied in the preparation of dopamine D2 receptor related pain, schizophrenia, Lesch-Nyhan syndrome and other nervous system diseases.

The present invention discloses a carebastine salt and a use of the carebastine salt, relates to the field of pharmaceutical chemistry, and solves the problems of carebastine in the related art such as poor solid form, excessive impurities, instability, difficulty in purification, difficulty in scale-up synthesis, and unsuitability for medicinal use. The carebastine salt of the present invention includes, but is not limited to, acid addition salts or base addition salts, and particularly includes potassium salts, sodium salts, methanesulfonate and p-toluenesulfonate. The carebastine salt of the present invention has the use of preparing histamine H1 receptor antagonist drugs. The carebastine salt of the present invention has the characteristics such as easy purification, high stability, simple process and easy industrial production, and has good hygroscopicity characteristics and is convenient for storage. At the same time, the salt of the present invention can quickly enter the body to exert the efficacy, has good oral absorption, is superior to ebastine in safety and individual differences, and is a promising anti-allergic disease drug.

To provide methods of treating diseases.SOLUTION: Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of a formula (I) having a disease-modifying action in treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity. A is selected from a group consisting of (group) and (group). As described in detail and specifically demonstrated herein, surprisingly, a remarkable effect is achieved according to the present invention, and this remarkable effect has not been able to be easily predicted from a prior art by those skilled in the art.SELECTED DRAWING: None

An orally disintegrating pharmaceutical tablet comprising: between 0.1 and 21 wt % of cariprazine or its pharmaceutically acceptable salts, between 0.1 and 15 wt % of a disintegrant, between 0.1 and 5 wt % of colloidal silicon dioxide, between 0.1 and 10 wt % of a taste masking agent, between 0.1 and 5 wt % of a lubricant, and up to 100 wt % of a diluent, the percentage being expressed with regard to the total weight of the pharmaceutical tablet. Said composition for use in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors, selected from the group of psychoses, drug abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, dementia, psychotic states associated with dementia, eating disorders, attention deficit disorders, hyperactivity disorders in children, psychotic depression, bipolar disorder, paranoid and delusional disorders, dyskinetic disorders, anxiety, sexual dysfunction, sleep disorders, emesis, aggression and autism.

Provided are phenylalkylamines, such as 2,5-disubstituted and 2,4,5-trisubstituted phenylalkylamines. In some embodiments, the phenylalkylamines are asymmetrically substituted. In some embodiments, such compounds modulate the activity of monoamine receptors and / or monoamine transporters. Also provided are methods for the preparation of phenylalkylamines and pharmaceutical compositions thereof. Methods of using the phenylalkylamines, alone or in combination with other therapeutic agents, are provided. In some embodiments, phenylalkylamines are used to treat CNS disorders, such as mental health conditions and neurodegenerative disorders, or are used for the improvement of mental health or functioning.

The present invention relates to a novel isoquinoline alkaloid compound and a preparation method and use thereof. The novel compound (Corybungine A‑L) provided by the present invention is a novel isoquinoline alkaloid extracted and separated from Corydalis bungeana Turcz. in the genus Corydalis of the family Papaveraceae. Biological activity experiments show that the alkaloid compound has dopamine D2 receptor antagonist activity and can be used in the preparation of drugs for dopamine D2 receptor-related pain, schizophrenia, Lesch‑Nyhan syndrome and other nervous system diseases.

The present disclosure provides conjugates and systems for modulating the activity of a ligand-binding polypeptide such as a D2 dopamine receptor. Such conjugates comprising an affinity agent, a linker; a photoisomerizable group and a ligand that binds to a target ligand-binding polypeptide. The present disclosure provides methods of modulating the activity of a D2 dopamine receptor. The present disclosure provides methods of treating Parkinson's disease in an individual.

The invention belongs to the field of biological medicine. The invention provides a dopamine D2 receptor compound and application thereof in treatment of erectile dysfunction. The dopamine D2 receptor compound provided by the invention has excellent biological activity, and has important application potential in erectile dysfunction treatment drugs.

The present invention relates to an orally disintegrating pharmaceutical tablet comprising between 0.1 and 21% by weight of cariprazine or a pharmaceutically acceptable salt thereof, between 0.1 and 15% by weight of a disintegrating agent, between 0.1 and 5% by weight of colloidal silica, between 0.1 and 10% by weight of a taste masking agent, between 0.1 and 5% by weight of a lubricant, and up to 100% by weight of a diluent, the percentage being expressed relative to the total weight of the pharmaceutical tablet. The present invention relates to a composition for use in the treatment and / or prevention of pathological conditions requiring modulation of dopamine receptors, the composition is selected from the group consisting of psychosis, drug abuse, cognitive impairment associated with schizophrenia, mild to moderate cognitive deficits, dementia, psychotic states associated with dementia, eating disorders, attention deficit disorders, hyperactivity disorders in children, psychotic depression, bipolar disorders, paranotic and delusional disorders, dyskinesia, anxiety, sexual dysfunction, sleep disorders, vomiting, or the like. And attacking behaviors and autism.