40 results about "Receptor agonist activity" patented technology

The invention provides a hypoglycemic peptide which is prepared by taking bovine whey protein as a raw material and is stable in gastrointestinal digestion and absorption. In an in-vitro cell experiment, the peptide fragment can improve the uptake of insulin-resistant HepG2 hepatocytes and synthesize glycogen by using glucose, can promote intestinal endocrine cells NCI-H716 to secrete GLP-1, has a certain synergistic effect, and can further play the effects of promoting GLP-1 secretion and activating a GLP-1 receptor through combined use. An insulin resistance mouse model is constructed by utilizing high-fat diet, and the peptide fragment is adopted for intervention, so that the hypoglycemic peptide is further proved to have obvious effects on losing weight, reducing lipid accumulation and assisting in reducing blood fat, and meanwhile, the hypoglycemic peptide can be used for improving insulin resistance related symptoms. The milk peptide provided by the invention has gastrointestinal digestion stability and hypoglycemic activity, can be used as a functional milk base material for developing food, medicines or health care products with the effect of regulating blood sugar, and is wide in application prospect.

To provide pharmaceutical compositions which have the same action as GLP-1 peptide as a GLP-1 receptor agonist, are capable of noninvasive administration, and contain a compound having improved activity, metabolic stability, and bioavailability or a salt thereof or a solvate thereof, and to provide methods for preventing or treating non-insulin-dependent diabetes mellitus or obesity using the pharmaceutical compositions.SOLUTION: The present invention provides a pharmaceutical composition which contains as active ingredient a compound having a base skeleton represented by formula (I) in which an indole ring and a pyrazolopyridine skeleton are linked via a substituent, or a salt thereof or a solvate thereof, and is used in the prevention and treatment of non-insulin-dependent diabetes mellitus (type 2 diabetes mellitus) or obesity.SELECTED DRAWING: None

Peptides exhibiting GIP and GLP-1 receptor agonist activity, as well as prodrug derivatives thereof, are provided. Pharmaceutical compositions comprising such glucagon peptides and therapeutic methods for using such peptides are also provided.

The present invention relates to the medical use of specific long-acting glycemic analogs having dual GLP-1 / glycemic receptor agonist activity for the prevention and / or treatment of metabolic liver diseases, in particular non-alcoholic fatty liver disease (NAFLD), non-alcoholic fatty liver (NAFL), non-alcoholic steatohepatitis (NASH), NAFLD-related hepatic fibrosis and / or cirrhosis.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.A compound represented by the formula (I):wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

Novel compounds are provided with excellent orexin type 2 receptor agonist activity. The compounds are represented by Formula (I) or pharmaceutically acceptable salts thereof.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.A compound represented by the formula (I):wherein each symbol is as described in the description, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.A compound represented by the formula (I):wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

The present invention provides a heterocyclic compound having orexin type 2 receptor agonist activity. A compound represented by formula (I): wherein each symbol is as described in the specification, or a salt thereof, useful as an agent for preventing or treating narcolepsy.

This invention provides a novel κ-opioid receptor (KOR receptor) agonist compound that exhibits excellent efficacy and action. [Solution] In one embodiment, a compound represented by formula IB, its stereoisomer, or a pharmaceutically acceptable salt thereof is provided. Such novel amide bond-containing compounds not only have excellent KOR receptor agonist activity (high affinity for κ opioid receptors), but also have very good hydrophilicity, and therefore have a lower ability to cross the blood-brain barrier and enter the brain. JPEG2026086406000232.jpg3368

The present invention provides heterocyclic compounds having orexin type 2 receptor agonist activity. Formula (I): JPEG2025539434000134.jpg51127 [wherein each symbol is as defined in the specification] The compound or a salt thereof has orexin type 2 receptor agonist activity and is useful as an agent for the prophylaxis or treatment of narcolepsy.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.A compound represented by the formula (I):wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.A compound represented by the formula (I):wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.

To provide: a compound as a GLP-1 receptor agonist which has the same effect as GLP-1 peptide, may be non-invasively administered and is improved in activity, metabolic stability and bioavailability; and a preventive or therapeutic agent for non-insulin-dependent diabetes mellitus (type 2 diabetes) or obesity containing the compound as an active ingredient.SOLUTION: The present invention provides: a compound represented by Formula (I) in the figure, in which an indole ring or pyrrolo[2,3-b]pyridine ring and a pyrazolopyridine skeleton are bound to each other through a substituent; or a salt thereof; or a solvate of them.SELECTED DRAWING: None

The invention provides a GLP-1R / GIPR / GCGR triple receptor agonist and an application of the GLP-1R / GIPR / GCGR triple receptor Specifically, the invention provides a polypeptide with GLP-1 (glucagon-like peptide-1) R / GIPR / GCGR triple receptor agonist activity or a pharmaceutically acceptable salt thereof, and the polypeptide or the pharmaceutically acceptable salt thereof has obvious triple agonist activity of a glucagon-like peptide-1 (GLP-1) receptor, a gastric inhibitory polypeptide (GIP) receptor and a glucagon (GCG) receptor. The compound can be used for preparing pharmaceutical compositions for preventing or treating metabolic diseases such as type I diabetes mellitus, type II diabetes mellitus, gestational diabetes mellitus, obesity, non-alcoholic fatty liver disease (NAFLD), obesity, hyperlipidemia and the like.

The present invention provides a heterocyclic compound having orexin type 2 receptor agonist activity. A compound represented by formula (I): wherein each symbol is as described in the specification, or a salt thereof, useful as an agent for preventing or treating narcolepsy.

This invention discloses a polypeptide analog with GLP-1, NPY2, and NPY4 receptor agonist activity and its applications. The sequence structure of the polypeptide analog is selected from any of the amino acid sequences shown in SEQ ID NO:1-2. This polypeptide analog exhibits excellent hypoglycemic and appetite-suppressing activities by selectively agonizing GLP-1, NPY2, and NPY4 receptors in a certain proportion, with almost no gastrointestinal side effects. This polypeptide analog shows broad application prospects in the field of drug preparation for the prevention and treatment of metabolic syndromes such as diabetes and obesity.

This invention provides a heterocyclic compound, its preparation method, and its use in preparing GLP-1 receptor agonist prodrugs with oral and long-acting pharmacokinetic properties, belonging to the field of medicinal chemistry. The compound provided by this invention can be used as a GLP-1 receptor agonist prodrug, which can release a parent drug with GLP-1 receptor agonist activity through hydrolysis in vivo. The compound provided by this invention can be used as a GLP-1 receptor agonist prodrug compound for the preparation of drugs for the prevention and / or treatment of GLP-1 receptor-related diseases. The compound of this invention exhibits good oral and long-acting pharmacokinetics, resulting in better medication adherence and broad application prospects.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity.A compound represented by the formula (I):wherein each symbol is as described in the specification, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as an agent for the prophylaxis or treatment of narcolepsy.

The application provides a compound as shown in formula (I) and use thereof. The compound as shown in formula (I) provided by the application can be used as an effective glucagon-like peptide-1 (GLP-1) receptor agonist, has excellent GLP-1R receptor agonist activity and obvious blood glucose lowering effect, and has good pharmacokinetic characteristics, thereby providing more choices for the prevention and / or treatment of diseases, conditions or disorders related to GLP-1 activity, and having a good application prospect in clinic.

Peptides and prodrug derivatives thereof exhibiting GIP and GLP-1 receptor agonist activity are provided. Also provided are pharmaceutical compositions comprising such glucagon peptides and methods of treatment using such peptides.

The present invention provides a heterocyclic compound having orexin type 2 receptor agonist activity. A compound represented by formula (I): wherein each symbol is as described in the specification, or a salt thereof, useful as an agent for preventing or treating narcolepsy.

To provide a novel process for preparing a diaminopyrimidine derivative or an acid addition salt thereof having an activity as a 5-HT4 receptor agonist, and also to provide novel crystalline forms of a hydrochloride of the diaminopyrimidine derivative and processes for preparing the same.SOLUTION: Provided is crystal A of a hydrochloride of the compound of Chemical Formula 1 having an XRPD pattern having peaks at 2θ of 7.4°, 9.1°, 12.0°, 12.5°, 13.5°, 14.1°, 15.9°, 16.8°, 18.3°, 19.1°, 24.6°, 25.3°, and 26.8°±0.2°.SELECTED DRAWING: None

The present invention relates generally to the field of immunomodulation and more specifically to compounds that exhibit Toll-like receptor 4 (TLR4) agonist activity. The invention provides novel compounds capable of stimulating or promoting an immune response, thereby offering potential therapeutic applications. In particular, the compounds may be useful in methods of promoting and / or maintain gastrointestinal health, as well as treating or preventing gastrointestinal diseases, such as IBD and colitis.

To provide a pharmaceutical composition containing a compound or a salt thereof, or a solvate thereof, which has an action similar to that of a GLP-1 peptide as a GLP-1 receptor agonist, can be noninvasively administered, and has improved activity, metabolic stability and bioavailability. The present invention also provides a method for preventing or treating non-insulin-dependent diabetes mellitus (type 2 diabetes) or obesity using the pharmaceutical composition.SOLUTION: The present invention provides a pharmaceutical composition which contains, as an active ingredient, a compound having a basic skeleton represented by formula (I) in which an indole ring and a pyrazolopyridine skeleton are bonded via a substituent, or a salt thereof, or a solvate thereof, and is used in the prevention or treatment of non-insulin-dependent diabetes mellitus (type 2 diabetes mellitus) or obesity.SELECTED DRAWING: None

The present invention provides a tryptamine prodrug compound. A compound represented by the formula (1)where each symbol is as described in the specification, or a salt or zwitterion thereof, is converted to an active which has 5HT2A receptor agonist activity, and is useful a an agent for the treatment of depression.

Provided is a substituted piperidine compound having an orexin type 2 receptor agonist activity. A compound represented by the formula (I):wherein each symbol is as described in the DESCRIPTION, or a salt thereof has an orexin type 2 receptor agonist activity, and is useful as a prophylactic or therapeutic agent for narcolepsy.

The present invention provides a heterocyclic compound having an orexin type 2 receptor agonist activity. A compound represented by the formula ( I ) : (I) wherein each symbol is as described in the specification, or a salt thereof, is useful as an agent for the prophylaxis or treatment of narcolepsy.

The present invention relates to a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.A compound represented by formula (I):whereinA1 is C(R5) or N,A2 is C(R6) or N,A3 is C(R7) or N,R5, R6, and R7 are each independently a hydrogen atom or the like,R2 is substituted or unsubstituted alkyl or the like,-L- is a group represented by:whereinR1 is a hydrogen atom or the like,R8 is a hydrogen atom or the like,R10s are each independently cyano or the like,m is an integer of 1 to 3, andR3 is phenyl optionally substituted with substituent group F, or the like,the substituent group F: halogen, cyano, alkyl, haloalkyl, alkyloxy, and haloalkyloxy.

The application belongs to the technical field of medicine preparation, and particularly relates to a TRPM8 agonist compound and a preparation method and application thereof. The deuterated TRPM8 agonist compound provided by the application has excellent TRPM8 receptor agonist activity, can effectively improve the symptoms of dry eye, significantly promote tear secretion and repair corneal epithelial damage, and has better curative effect than existing classical TRPM8 agonists, and can be used for preparing a medicine for treating dry eye, thereby providing a new effective selection for clinical treatment of dry eye. The deuterated TRPM8 agonist compound provided by the application is prepared by using a four-step synthesis process, raw materials are easy to obtain, process operation is simple, and the reaction process is stable and controllable, and is suitable for industrialized synthesis.