62 results about "Opioid receptor" patented technology

Disclosed are a peptide amide compound composition, a preparation method therefor and medical use thereof. Specifically, the composition contains a compound of formula (I) and pH regulators, and the pH of the solution thereof is 3-5.5. The composition is stable and requires few excipients, and is stable in clinical use. The composition is used for treating or preventing a disease or condition associated with kappa opioid receptors

Methods and compositions are provided for treating individuals exhibiting opioid withdrawal symptoms with opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of opioid withdrawal symptoms, including respiratory depression, sedation, and hypotension. Methods and compositions are also provided for treating stimulant overdose with a benzodiazepine and beta-adrenergic blocking agent. Methods and compositions are also provided for treating concurrent stimulant and opioid overdose comprising administering to a patient in need thereof a benzodiazepine and an opioid antagonist. Methods and compositions are also provided for treating individuals exhibiting opioid withdrawal symptoms or prophy tactically treating individuals for opioid withdrawal symptoms from opioid, benzodiazepine and other drugs of abuse by administering an opioid receptor antagonist agent together with a respiratory stimulant to reverse the effects of withdrawal, including respiratory depression, sedation, and hypotension.

Problem The purpose of the present invention is to provide a novel method for prevention and / or treatment of opioid tolerance or opioid dependence. Specifically, the purpose of the present invention is to develop peptide-based blockers to block MOR-DOR and KOR-DOR heterodimerization. In addition, the purpose of the present invention is to develop homodimer blockers for MOR, DOR, and KOR which modulate their downstream signaling without affecting their internalization. Solution The present invention is a prophylactic and / or therapeutic agent for the prevention and / or treatment of opioid tolerance or opioid dependence comprising the peptide which inhibits the dimer formation of the opioid receptor, wherein the above opioid receptor dimer is a heterodimer or a homodimer formed from one or two opioid receptors selected from the group consisting of the μ type (MOR), the κ type (KOR), and the δ type (DOR).

The present application discloses a compound of formula (I), compositions comprising said compound, and a method of using said compound as a cannabinoid receptor ligand in the treatment or prevention of diseases associated with a cannabinoid receptor, such as, CB1, CB2, 5HT1A, 5HT2A, GPR18, GPR119, TRPV1, TPRV2, PPARγ or a μ-opioid receptor.

The present disclosure relates to compositions that upregulate the production of one or more sequences of micro-interfering ribonucleic acid (miRNA). The sequences of miRNA may be complimentary to a sequence of target messenger RNA (mRNA) that encodes for translation of a target biomolecule, and the miRNA may cause the target mRNA to be degraded or inactivated, thereby causing a decrease in bioavailability of the target biomolecule because it is degraded or inactivated by the miRNA, thereby decreasing the bioavailability of the target biomolecule within a subject that is administered the one or more compositions. In some embodiments of the present disclosure, the target biomolecule is an opioid receptor. In some embodiments of the present disclosure, the target biomolecule is one or more of the mu opioid receptor, the delta opioid receptor, the kappa opioid receptor and the nociceptin opioid receptor.

A series of non-peptide opioid receptor modulators having the general formula: (I) is provided. In the formula: R = (II) * is a chiral carbon; M is a saturated or unsaturated, branched or unbranched, substituted or unsubstituted alkyl chain from 0-10 atoms in length; X1, X2, X3, X4, or X5 are independently, C, N, O, or S; and R is attached to M by any of X1, X2, X3, X4, or X5. The compounds are used to treat disorders related to opioid receptor functions such as opioid addiction, opioid overdose, pain and constipation caused by opioid use.

The present invention relates to a pharmaceutical composition for treating drug addiction comprising opioid receptor nanodiscs and to a method for preparing opioid receptor nanodiscs. Specifically, the opioid receptor nanodiscs, according to the present invention, inhibit the interaction between an opioid receptor and an opioid-based drug without exhibiting toxicity in the body, are delivered to the brain when administered into the body, and significantly restore the delay in a hot-plate response caused by opioid-based drug addiction, thereby being usefully applicable to treatment of opioid-based drug addiction.

The invention discloses aza-2-ketone derivatives, a synthesis method thereof and application of the aza-2-ketone derivatives in preparation of drugs. According to the invention, an alpha-carbonyl acyl silane compound is taken as a raw material, and under illumination, the alpha-carbonyl acyl silane compound and a vinyl aziridine compound are subjected to [5 + 2] cycloaddition reaction, so that a series of aza-2-ketone derivatives with different structures are simply and efficiently synthesized. The aza-2-ketone derivative disclosed by the invention can be further converted into medicine molecules such as kappa-opioid receptor selective agonist molecules and the like. The method has the advantages of easily available raw materials, simple operation, mild reaction conditions, and diversity of functional groups.

The invention relates to a tetrahydrothebaine derivative as well as a preparation method and application thereof, in particular to a 7alpha-(4 '-substituted amidophenyl)-6alpha, 14alpha-endo-ethylidene (alkenyl)-tetrahydrothebaine derivative as shown in a general formula (I) or pharmaceutically acceptable salts thereof and a preparation method of the 7alpha-(4'-substituted amidophenyl)-6alpha, 14alpha-endo-ethylidene (alkenyl)-tetrahydrothebaine derivative. And to the use of such derivatives in the preparation of medicaments for the treatment and / or prevention of pain, irritable bowel syndrome, pruritus, addiction, depression. The derivative disclosed by the invention has a remarkable improvement effect in the aspects of agonistic activity of the kappa opioid receptor, subtype selectivity of the kappa opioid receptor and central safety.

The subject matter disclosed herein relates generally to cancer therapy and to anticancer compounds and imaging agents. More specifically, the subject matter disclosed herein relates to agents that target DOR and their use in the treatment of cancer.

Disclosed herein are kappa opioid receptor (KOR) antagonist compounds of formula (I) and formula (II) and their pharmaceutically acceptable salts, as well as pharmaceutical compositions thereof. The compounds are useful in methods for treating a variety of diseases and disorders for which KOR antagonism is indicated, including substance abuse disorders, depression, anxiety, and other psychiatric conditions. TIFF2026506965000204.tif34128

Disclosed are tetrahydroisoquinoline compounds useful for treating an opioid receptor-associated condition including pain, immune disease, esophageal reflux, diarrhea, anxiety, or heroin addiction. Also provided are pharmaceutical compositions and treatment methods.

This disclosure relates to using Mu Opioid Receptor (MOR) antagonists.

Disclosed herein are kappa-opioid receptor (KOR) antagonist compounds of Formula (I), Formula (II) and their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds are useful in methods of treating a variety of diseases and disorders adapted to KOR antagonism, including substance abuse disorders, depression, anxiety, and other psychiatric conditions.

The present disclosure is directed to substituted Pyrazole and Imidazole derivatives of compounds that are antagonists and / or modulators of orexin and kappa-opioid receptors, and which are useful in the treatment or prevention of neurological, psychiatric, cardiovascular and cancer disorders and diseases in which orexin and kappa-opioid receptors are involved or implicated. The disclosure is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin and kappa-opioid receptors are involved.

Provided are a novel opioid receptor antagonist and pharmaceutical composition that contain, as an active ingredient, a compound represented by formula (1) or a pharmacologically-acceptable salt of said compound. In formula (1), R1 represents an alkyl group, a heteroaryl group, or the like. R2, R3, and R4 each independently represent a hydrogen atom, an alkyl group, or the like. Note that the two R2 each represent the same group, the two R3 each represent the same group, and the R2 and / or the R3 represent hydrogen atoms. When R2 and R3 are both hydrogen atoms, R4 is a hydrogen atom. R5 is not present, or represents an alkyl group. R6 represents an organic group.

The application discloses a kind of azapine-2-ketone derivatives and synthesis method and application for preparing medicine thereof.The application can α The application uses carbonyl acylsilane compound as raw material, and under light, [5+2] cycloaddition reaction occurs with vinyl aziridine compound, so that a series of different structural azapine-2-ketone derivatives are simply and efficiently synthesized.The azapine-2-ketone derivatives of the application can be further converted into Kappa Opioid receptor selective agonist molecules and other drug molecules.The method of the application has the advantages of easy availability of raw materials, simple operation and mild reaction conditions, and the functional groups have diversity.

The present disclosure is directed to kappa opioid receptor ligands and pharmaceutical compositions thereof and their utility as neurological modulators (e.g., anti-nociceptive agents, antidepressants, anxiolytics, antipruritics). Specifically, the disclosed kappa opioid ligands are G-protein biased kappa opioid agonists containing a core and three different arms as is shown in Formula (A) below.

The present disclosure relates methods of treating psychiatric disorders such as depression and anhedonia with a kappa opioid receptor antagonist.

Described herein are compositions, devices, and methods useful for treating (reversing) and / or preventing fentanyl overdose resulting in respiratory failure or airway obstruction (FIVCC). Compositions are provided that include optimized amounts and / or ratios of two active ingredients, including: an alpha 2 adrenergic receptor agonist (e.g., lofexidine, dexmedetomidine, clonidine) and a short acting mu opioid receptor antagonist (e.g., naloxone); an alpha 2 adrenergic receptor agonist and a long acting mu opioid receptor antagonist (nalmefene); and an alpha 2 adrenergic receptor agonist and a fentanyl opioid analgesic. Methods and devices for concurrent delivery of combined active ingredients are also provided.

The invention relates to a method and a pharmaceutical composition for treating Parkinson's syndrome or Parkinson's disease, in particular to a pharmaceutical composition, application and a method for treating Parkinson's syndrome or Parkinson's disease by using a peripheral mu-opioid receptor antagonist. According to the pharmaceutical composition, the application and the method, the symptoms, including constipation, of the Parkinson's syndrome or the Parkinson's disease can be remarkably improved, and particularly the constipation which is invalid or refractory to treat by using a universal constipation drug can be remarkably improved.

Disclosed are tetrahydroisoquinoline compounds useful for treating an opioid receptor- associated condition including pain, immune disease, esophageal reflux, diarrhea, anxiety, or heroin addiction. Also provided are pharmaceutical compositions and treatment methods.

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 in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and / or the μ-opioid receptor.

The application belongs to the field of pharmacy, discloses a fused ring morphine derivative and a preparation method and application thereof, and relates to N-cyclopropylmethyl-4'-substituted aminonalepotem series derivatives with formula (I) and pharmaceutically acceptable salts. The derivative with formula (I) is prepared by reacting thebaine with a substituted phenyl vinyl ketone reagent and through a series of conversion methods. Among them, N-cyclopropylmethyl-(4'-benzoyl amino) nalepotem (SLL-1062) is a typical high selectivity mu opioid receptor antagonist, and can be applied to the research and development in the fields of diagnosis and treatment of opioid and other narcotic analgesic dependence, opioid drug-induced intestinal dysfunction, sedative hypnotics and acute alcohol poisoning, opioid and other narcotic analgesic poisoning and the like.

The present invention relates to antagonistic peptides specifically binding the µ-opioid receptor (µOR). Said antagonists are mimetic peptides of a single domain antibody ligand having binding affinity to the µOR. The invention furthermore provides pharmaceutical compositions comprising such antagonistic peptides, as well as the use of such antagonistic peptides in methods for treating diseases.

The present application belongs to the technical field of pharmaceutical crystal, and relates to a solid salt type, a crystal form of an opioid receptor antagonist conjugate and a preparation method, a composition and a use thereof. Specifically, the conjugate has a structure as shown in formula I, and can form a stably existing solid phosphate salt, wherein the molar ratio of phosphoric acid to the compound of formula I is 1:1-3:1. The phosphate salt can be an amorphous substance or a polymorph having crystal form 1, 2, 3 or 4, and the preparation method is simple and easy to operate, and is suitable for preventing and treating intestinal function disorders caused by opioid drugs, such as constipation.

Compositions and methods are provided to determine occupancy level of opioid receptors in a subject. The disclosed methods may be performed non-invasively in the inner ear of the subject, and may be performed at a point-of-care location to provide guidance to a practitioner on tapering on pharmacotherapy or on a patient's risk of relapse for substance abuse.

Disclosed herein are kappa-opioid receptor (KOR) antagonist compounds of Formula (I), Formula (II), and their pharmaceutically acceptable salts, and pharmaceutical compositions thereof. The compounds are useful in methods of treatment of various diseases and disorders for which KOR antagonism is indicated, including substance abuse disorders, depression, anxiety, and other psychiatric conditions.

This application relates to a 7α-substituted phenyltetrahydrothebaine derivative, its preparation method, and its uses. Specifically, it relates to a 7α-substituted phenyltetrahydrothebaine derivative as shown in general formula (I) or a pharmaceutically acceptable salt thereof, and its preparation method, and to the use of such derivatives in the preparation of analgesic, anti-anxiety, anti-addiction, and antidepressant drugs. The derivatives of this invention exhibit significantly enhanced agonist activity and subtype selectivity of δ-opioid receptors.

Bivalent ligands which bind to MOR-CCR5 heterodimers are provided. The bivalent ligands comprise two discrete pharmacophores, naltrexone and maraviroc, linked by a spacer and bind to MOR-CCR5 heterodimers, e.g. at the surface of a cell. The bivalent ligands are useful in assays to detect MOR-CCR5 heterodimers, as therapeutic agents to prevent and / or treat diseases characterized by the presence of MOR-CCR5 heterodimers.