70 results about "Tryptamine Receptors" patented technology

A compound, as shown in Formula I, is a multi-heterocyclic compound. It has been verified that the compound provided by this invention integrates a novel compound targeting the calcitonin gene-related peptide (CGRP) based on ephedrine. Upon contact with the skin, due to photoactivated cell biological function regulation and the blocking effect of the multi-heterocyclic compound I structure on serotonin receptors, it achieves therapeutic effects on cutaneous vascular malformations and telangiectasia, improves the effectiveness of phototherapy in improving chronic cutaneous vascular diseases, and promotes skin wound healing.

A single unit oral dose pharmaceutical composition for use as a medicament for separate, sequential or simultaneous administration with an agonist of a 5-hydroxytryptamine (5-HT) receptor;wherein the single unit oral dose pharmaceutical composition comprises a first active ingredient and a second active ingredient;wherein the first active ingredient is for absorption in the gastrointestinal tract from the oesophagus onwards and the second active ingredient is for absorption in the oral cavity; andwherein the first active ingredient is naltrexone in an amount of 0.01 to 10 mg and the second active ingredient is calcitriol in an amount of 80 to 200 ug.

Pharmaceutical compositions of the invention comprise functionalized lactam derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

The invention discloses a heteroarylamine compound as well as a pharmaceutical composition and application thereof. Specifically, the invention discloses a compound shown as a formula (I) or a pharmaceutically acceptable salt thereof. The compound provided by the invention has one or more of the following advantages: (1) the compound has excellent agonistic activity on a 5-hydroxytryptamine 4 receptor; and (2) the inhibitory activity on hERG is relatively weak.

This disclosure relates, in some embodiments, to substituted ergolines such as 14-monosubstituted and 2,14-disubstituted lysergic amides and their quaternated derivatives. In some embodiments, this disclosure relates to methods for using these compounds, including methods for synthesizing these compounds, compositions containing these compounds, and methods for administering them to subjects. In some embodiments, the characteristics of the compounds include neuromodulatory activity, such as activation of serotonin receptors. In some further embodiments, the compounds are useful as therapeutic agents, such as anti-inflammatory agents. [Formula 1] JPEG2026525309000071.jpg5750

This invention belongs to the field of medical technology, and specifically relates to the application of serotonin 3 receptor antagonists in the preparation of antitumor drugs. This invention, through research, demonstrates for the first time that serotonin 3 receptor antagonists can inhibit the activity of tumor cells resistant to third-generation EGFR-TKIs. More importantly, serotonin 3 receptor antagonists can not only reverse HER2 S310F mutation-mediated resistance to third-generation EGFR-TKIs, but also reverse secondary resistance to third-generation EGFR-TKIs, thus enabling their use as antitumor drugs for patients resistant to third-generation EGFR-TKIs. The combined use of serotonin 3 receptor antagonists and third-generation EGFR-TKIs exhibits a significant synergistic effect in inhibiting the proliferation of lung adenocarcinoma cells, with minimal toxic side effects on liver and kidney function, providing an effective treatment strategy for clinically reversing third-generation EGFR-TKI resistance and improving the treatment efficacy of NSCLC.

The present disclosure provides azocino[4,5,6-cd]indoles as serotonin receptor modulators. Uses of said compounds in the treatment of medical disorders, such as neurological or psychiatric disorders, and processes of synthesizing said compounds are also provided.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

Provided herein are ergoline derivatives which modulate serotonin receptors and compositions thereof. Also provided herein are methods of modulating serotonin receptors and methods of treating diseases and disorders (e.g., pain) in a subject in need thereof. (I)

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system diseases. Pharmaceutical compositions and methods of making various benzisoxazole and benzisothiazole compounds are provided. These compounds are considered to be modulators of the serotonin 2A (5-HT2A) receptor.

The present disclosure relates to stable pharmaceutical compositions of amorphous psilocybin and deuterated psilocybin, and to the use of such pharmaceutical compositions in the treatment of diseases associated with a serotonin 5-HT2 receptor. The pharmaceutical compositions are formulated with solid dispersions of psilocybin or deuterated psilocybin in amorphous form dispersed in a polymer.

Pharmaceutical compositions of the invention comprise functionalized lactam derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity.

Hallucinogenic and non-hallucinogenic serotonin receptor agonists are disclosed herein in addition to methods of making and using the same.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system disorders. Pharmaceutical compositions and methods of making various tetrahydropyridine and piperidine compounds are provided. The compounds are expected to be modulators of the serotonin 2A (5-HT2A) receptor.

5-HT2A receptor ligands and receptor-ligand complexes are synthesized. These ligands, which may link two indole containing moieties through an amine, may be used in therapeutically effective amounts, to treat mood disorders and neurologic disorders.

Methods and compositions that treat Alzheimer's disease and other neurodegenerative diseases and / or to ameliorate or improve symptoms associated with Alzheimer's disease. In some aspects, the compositions and methods use a serotonin 4 receptor (5-hydroxytryptamine (serotonin) receptor 4, or 5-HT4R) agonist in combination with: (R,S)-ketamine, a (R,S)-ketamine analog, or a pharmaceutically acceptable salt, derivative, or metabolite thereof; an antagonist of the glutamate N-methyl-D-aspartate (NMDA) receptor (NMDAR); or an agonist of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor (AMPAR).

The present disclosure relates to small molecule compound (SMC), pharmaceutical composition comprising the same, uses thereof in methods for treating brain disease.

The present disclosure relates to stable pharmaceutical compositions of amorphous psilocybin and deuterated psilocybin, and to the use of such pharmaceutical compositions in the treatment of diseases associated with a serotonin 5-HT2 receptor. The pharmaceutical compositions are formulated with solid dispersions of psilocybin or deuterated psilocybin in amorphous form dispersed in a polymer.

The present disclosure relates to compounds useful for activating 5-hydroxytryptamine 2A receptor (5-HT2AR), pharmaceutically acceptable compositions thereof, and methods of using said compounds and compositions. Formula (I).

Described herein are compounds of Formula (I), Formula (II), Formula (III), Formula (III-A), Formula (III-B), Formula (IV), Formula (V), Formula (V-A), Formula (VI), Formula (VII), Formula (VIII), Formula (VIII-A), Formula (IX), or Table 1-15 and their pharmaceutically acceptable salts, deuterated form, or stereoisomers, as well as their uses (e.g., as serotonin receptor agonists).

Provided herein include compounds, compositions, kits and methods for preventing and treating psychiatric disorders. The composition and methods described herein can prophylactically treat a subject prior to and / or after a stressor and / or prior to the recurrence of a stressor, thereby preventing or delaying a relapse of depression or depression-like and / or stress-induced behaviors and disorders. The composition can comprise a serotonin 4 receptor (S-HUR) agonist and an N- methyl-D-aspartate (NMDAR) antagonist and a pharmaceutically acceptable salt, analog, derivative or metabolite thereof.

Disclosed in the present invention are a heteroaromatic amine compound, a pharmaceutical composition thereof and the use thereof. Specifically, disclosed are a compound represented by formula (I), a pharmaceutically acceptable salt thereof, a solvate thereof, or a solvate of the pharmaceutically acceptable salt thereof. The compound of the present invention has one or more of the following advantages: (1) excellent agonistic activity on 5-hydroxytryptamine 4 receptor; (2) good selective agonistic activity on 5-hydroxytryptamine 4 receptor; (3) capability of significantly reducing the risk of cardiotoxicity caused by hERG channel suppression; and (4) excellent intestinal tissue selectivity and low system exposure, which can reduce the safety risk of the circulatory system.

The present disclosure provides methods and compositions for reducing the addictive liability of opioid analgesics in a subject, for example, by co-administering to the subject the opioid and a serotonin receptor type 2 (5HT2) agonist or a serotonin (5HT) releasing agent. The disclosed methods include methods for preventing opioid abuse, methods for reducing the rewarding effect of an opioid, methods for reducing the addictive liability of an opioid, methods for eliminating or substantially reducing the tendency for a subject to develop physical dependence, tolerance, and / or withdrawal symptoms with respect to an opioid, and methods for eliminating or substantially reducing the tendency for a subject to use opioids in ways not prescribed, take opioids more often or in larger amounts than prescribed, and / or use opioids recreationally. The methods can be performed on a subject, such as a patient (e.g., a human patient).

Provided herein are treatment methods including administering a 5-hydroxytryptamine (HT)2C receptor agonist to a patient in need thereof. An exemplary method includes treating or preventing a 5-hydroxytryptamine (HT)2C receptor-associated disorder in a patient in need thereof, wherein the method comprises administering to the patient (R)—N-(2,2-difluoroethyl)-7-methyl-1,2,3,4,6,7-hexahydro-[1,4]diazepino[6,7,1-hi]indole-8-carboxamide (Compound 1), or a pharmaceutically acceptable salt thereof, wherein Compound 1, or a pharmaceutically acceptable salt thereof.

Provided herein are treatment methods including administering a 5-hydroxytryptamine (HT)2C receptor agonist to a patient in need thereof. An exemplary method includes treating or preventing a 5-hydroxytryptamine (HT)2C receptor-associated disorder in a patient in need thereof, wherein the method comprises administering to the patient (R)-N-(2,2-difluoroethyl)-7-methyl-1,2,3,4,6,7-hexahydro-[1,4]diazepino[6,7,1-hi]indole-8-carboxamide (Compound 1), or a pharmaceutically acceptable salt thereof, wherein Compound 1, or a pharmaceutically acceptable salt thereof.

The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and / or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use as agonists or antagonists of the serotonin (5-HT2A) receptor, preferably non-hallucinogenic biased agonists at the serotonin (5-HT2A) receptor, such as having agonism biased towards the beta-arrestin signaling pathway. Such compounds are useful for the treatment of mood disorders, general anxiety, social anxiety, depression, and other neuropsychiatric diseases.

1,1'-Biphenyl-4-yl-(het)arylimino-λ6-sulfanone compounds are 5-HT2A receptor activators, and these compounds and their pharmaceutical compositions are useful for the treatment of neurological or psychiatric disorders.

The present disclosure provides compounds, such as compounds of Formula I, and their use in the treatment of medical diseases or disorders, such as psychiatric and nervous system disorders. Pharmaceutical compositions and methods of making various piperidine compounds are also provided. These compounds are expected to be modulators of the serotonin 2A (5-HT2A) receptor.

This invention provides an apophene derivative, its preparation method, and its application. The general formula of the apophene derivative structure described in this invention is shown below: Among them, R 1 C 1 -C 8 alkoxy or hydrogen, R 2 For hydroxyl or hydrogen; R 3 Selected from C 1 -C 8 Alkyl, C 1 -C 8 Alkoxy, C 2 -C 10 alkynyl group, C 2 -C 10 alkenyl, halogen, C 1 -C 8 Halogenated, cyano, nitro, or aryl. The use of the 5-hydroxytryptamine 2A receptor agonist and 5-hydroxytryptamine 2C receptor agonist described in this invention in the preparation of medicaments for the prevention and / or treatment of obesity, urinary incontinence, depression, anxiety, obsessive-compulsive disorder, epilepsy, schizophrenia, pain, diabetes, and drug addiction.

Pharmaceutical compositions of the invention comprise functionalized lactam derivatives of formula (I) having a disease-modifying action in the treatment of diseases associated with dysregulation of 5-hydroxytryptamine receptor 7 activity, wherein A is selected from a group consisting of: