16 results about "PPAR agonist" patented technology

This invention provides an application of tartary buckwheat antioxidant peptide as a PPARα agonist. The tartary buckwheat antioxidant peptide (SEQ ID NO:1) is used to prepare a PPARα agonist, and this tartary buckwheat antioxidant peptide is used to prepare a drug for improving metabolic dysfunction-related fatty liver disease (MASLD). The tartary buckwheat antioxidant peptide of this invention provides a new drug candidate for improving MASLD and has broad clinical application prospects.

The invention provides an application method of a PPAR gamma agonist in preparation of a medicine for inhibiting ferroptosis of nucleus pulposus cells, and belongs to the technical field of medicine preparation.The PPAR gamma agonist pioglitazone and TAT cell-penetrating peptide are combined to form a compound, the compound is encapsulated in hyaluronic acid modified pH-sensitive lipidosome to construct a nucleus pulposus targeted drug delivery system, and the nucleus pulposus targeted drug delivery system is used for inhibiting ferroptosis of the nucleus pulposus cells. The flow cytometry is utilized to detect the physicochemical properties of the drug delivery system, the optimal drug delivery parameters are determined through a double-layer game optimization model, the drug release kinetics is determined in different pH environments to establish a pH response release model, and finally the PPAR gamma and Axl protein expression levels and the GPX4 protein level are detected through the fluorescence luminescence to verify the ferroptosis resisting effect. The technical problem that a drug carrier system cannot realize dual-function collaborative optimization of targeted delivery and acid-sensitive controlled release of nucleus pulposus cells is solved.

The present invention provides compounds as PPAR agonists and their application, involving a new class of peroxisome proliferator-activated receptor (PPAR) gamma receptor agonist, which can inhibit the production of mitochondrial reactive oxygen species, and most of which can readily cross the blood-brain barrier. The present invention also includes pharmaceutical uses of the compounds.

Microparticulate (MP) formulations formed from one or more poly(hydroxyacid) polymers having a molecular weight ranging from 5kD to 60kD, and one or more active agents are injected into the eye of a subject to address eye disorders. The MP formulations assure high drug loading and extended delivery of the active agent of six to twelve months. The active agents may include peroxisome proliferator-activated receptor alpha (PPARα) signaling agonists such as PPARα agonist A190 (IUPAC name 3-((4-((4-fluorobenzyl)oxy)- 3- methylbenzyl)amino)benzoic acid). The formulations have therapeutic and protective effects against retinal degeneration diseases such as age-related macular degeneration (AMD), but may also be used for treating or relieving the symptoms of retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity (ROP), diabetic retinopathy (DR), and diabetic macular edema (DME).

This specification provides a method for reducing or reversing age-induced insulin resistance and / or fatty acid elevation, comprising a composition comprising a PPAR agonist, or a pharmaceutically acceptable salt or prodrug thereof. This specification also provides a method for extending lifespan, comprising a composition comprising a PPAR agonist, or a pharmaceutically acceptable salt or prodrug thereof, and its use in animal health.

The present application belongs to the technical field of biological medicine, and particularly relates to a composition for promoting synthesis of an OAHFA derivative family, a microneedle patch and application thereof in preventing and treating dry eye syndrome. The present application first selects an OAHFA derivative as a dry eye treatment target and relies on activation of a PPARγ signal pathway to exert drug efficacy. The composition is compounded from 0.2% to 0.5% PPARγ agonists, 2.0% to 4.0% super-long chain fatty acids and 0.3% to 0.8% ceramides, three effective components. The super-long chain fatty acids supply synthesis substrates, and the ceramides stabilize the interface. The three components synergistically improve the curative effect. The composition described in the present application adopts soluble microneedles for local administration, and the drug release rate is not less than 70% in 30 min. The effect is rapid and the puncture is painless, and the patient compliance is excellent. Local administration eliminates systemic exposure of the drug, and the drug safety is high, and there is no serious adverse reaction.

The present invention provides a pharmaceutical composition for use in preventing or treating metabolic diseases comprising a novel pan-PPAR agonist compound or a salt thereof as an active ingredient. As the pan-PPAR agonist, the compound or the salt thereof may be useful in pharmaceutical compositions for preventing or treating metabolic diseases such as obesity, diabetes, fatty liver diseases, dyslipidemia, cardiovascular diseases, and / or metabolic syndrome, and in food or feed compositions for improving metabolic health.

Provided are methods of treating subjects in need of an anti-fibroblast growth factor receptor 3 (anti-FGFR3) therapy. The methods comprise administering to the subjects a therapeutically effective amount of a peroxisome proliferator-activated receptor (PPAR) alpha agonist in combination with the anti-FGFR3 therapy. The methods can comprise administering to the subject a therapeutically effective amount of PPAR alpha agonist and a bile acid sequestrant. Also provided are compositions comprising an FGFR3 inhibitor, a PPAR alpha agonist, and, optionally, a bile acid sequestrant. The methods attenuate the dysregulation of bile acid biosynthesis caused by FGFR3 inhibition with anti-FGFR3 therapies. The methods reduce the severity and / or incidence of adverse events associated with anti-FGFR3 therapies.

The present invention relates to a pharmaceutical compound or a pharmaceutically acceptable salt thereof for use in the prevention or treatment of the following conditions, wherein the pharmaceutical compound or a pharmaceutically acceptable salt thereof is characterized in that it simultaneously inhibits autotaxin (ATX) and agonizes PPARγ, and has a chemical formula selected from the group consisting of formulas (A), (B), (C), (D), (E), (F), (G), and (H): a) fibroproliferative diseases, in particular interstitial lung diseases (ILD) and / or liver diseases such as all types of hepatitis and / or non-alcoholic fatty liver disease (NAFLD) and / or non-alcoholic steatohepatitis (NASH) and / or cirrhosis, where the ILD is a primary disease, preferably idiopathic pulmonary fibrosis and / or sarcoidosis and / or interstitial pneumonia, or where the ILD is associated with an autoimmune and / or inflammatory and / or metabolic disease, preferably rheumatoid arthritis-ILD ​​and / or scleroderma-ILD and / or myositis-ILD ​​and / or diabetes-ILD ​​and / or cardiovascular disease-ILD combination, and / or b) an inflammatory and / or autoimmune disease, preferably rheumatoid arthritis and / or scleroderma, and / or c) cancer, in particular lung cancer and / or hepatocellular carcinoma and / or pancreatic cancer and / or glioblastoma and / or neuroblastoma, and / or d) metabolic diseases, in particular type 1 diabetes and / or type 2 diabetes and / or obesity [Formula 1] TIFF2026503883000014.tif94126

Dendrimer-drug compositions have been developed that not only target the reactive inflammatory cells / macrophages in the plaque, but also in the adipose tissue, delivering drugs in a targeted manner to simultaneously and independently address both atherosclerosis and obesity, and associated metabolic disorders.   The dendrimers are preferably glucose dendrimers, hydroxyl-terminated PAMAM dendrimers, or sugar-modified dendrimers, most preferably glucose dendrimers.   The drugs are preferably a PPAR-α agonist; a PPAR-γ agonist; a dual PPAR agonist (e.g., a PPAR- α / γ agonists); a GLP-1 receptor agonist (e.g., semaglutide); a metformin; an SGLT2 agonist, a GIP-1 receptor agonist or antagonist; a dual GLP-1 / GIP-1 receptor agonist (e.g., tirzepatide); a mitochondrial uncoupler (e.g., niclosamide); or a combination thereof. These compositions have the ability to overcome the side effects of current drugs for obesity and heart disease, and open new avenues in addressing these disorders through targeting of selective cells.

This invention belongs to the field of pharmaceutical technology, specifically relating to a compound, its preparation method, and its application in the preparation of sEH inhibitors and PPARs agonists. This invention provides a compound having the structure shown in Formula II. The compound provided by this invention has a typical urea structure as the primary pharmacophore of soluble epoxide hydrolase (sEH), and a thiazolidinedione moiety as the primary pharmacophore of peroxisome proliferator-activated receptors (PPARs). The sEH inhibitor and PPARs agonist compound provided by this invention exhibits high inhibitory activity against human HsEH and high agonistic activity against PPARs, and can be used as an sEH inhibitor and PPARs agonist compound in the preparation of drugs for treating diseases mediated by soluble epoxide hydrolase and peroxisome proliferator-activated receptors.

The present application relates to the technical field of medicines, and in particular to a compound, and a preparation method therefor and a use thereof in the preparation of a soluble epoxide hydrolase (sEH) inhibitor and a peroxisome proliferators-activated receptors (PPARs) agonist. The present application provides a compound, having a structure represented by formula I, II, III, IV, V or VI. The compound provided by the present application has a typical urea structure as the primary pharmacophore of an sEH, and the thiazolidinedione part serves as the primary pharmacophore of PPARs. The sEH inhibitor and PPARs agonist compound provided by the present application has high inhibitory activity against human-derived HsEH and high agonistic activity against a PPAR, and can be used for the preparation of a drug for treating soluble epoxide enzyme and PPARs-mediated diseases.

The application belongs to the technical field of medicine, and particularly relates to a compound, a preparation method thereof and application of the compound in preparation of sEH inhibitors and PPARs agonists. The application provides a compound with a structure shown in formula V or VI. The compound provided by the application has a typical urea structure as a primary pharmacophore of soluble epoxide hydrolase (sEH) and a thiazolidinedione part as a primary pharmacophore of peroxisome proliferator-activated receptors (PPARs). The sEH inhibitor and PPARs agonist compound provided by the application has high inhibitory activity on human HsEH and high agonistic activity on PPARs, and can be used as an sEH inhibitor and PPARs agonist compound for preparation of a medicine for treating diseases mediated by soluble epoxide hydrolase and peroxisome proliferator-activated receptors.

A method of treating or preventing glomerular disease or chronic kidney disease in a subject is described. The method includes administering to the subject a therapeutically effective amount of PPARγ agonist or a pharmaceutically acceptable salt thereof.