47 results about "Peroxisome proliferator" patented technology

The present invention provides a method for inducing fat accumulation in a cell of a fish, including contacting a cell obtained or derived from a fish with an effective amount of a composition including: (i) a fat accumulation inducing agent; and (ii) a carrier, wherein the fat accumulation inducing agent consists essentially of a free fatty acid and a peroxisome proliferator-activated receptor gamma (PPARy) agonist. Further provided are a cultured fish cell including an increased amount of a PUFA and a reduced amount of MUFA, compared to a control fish cell, and an edible composition including the same.

Formula I: A compound or its derivative, or its salt or prodrug, having the structure of TIFF2025524142000026.tif2292, wherein m = 2 and n is an odd number between 4 and 20, and Formula II: Disclosed is a compound or its derivative, or its salt or prodrug, having the structure of TIFF2025524142000027.tif2696, wherein m and n are independently integers between 2 and 20. Also provided are compositions and methods of using the compounds for the therapeutic modulation of peroxisome proliferator-activated receptor (PPAR).

Benzyl derivative compounds having peroxisome proliferator-activated receptor alpha (PPARα) agonist activity, kits and compositions containing such compounds, and methods of using them to enhance PPARα activity to treat diseases and / or conditions involving inflammation and / or angiogenesis, particularly diseases and / or conditions of the eye such as, but not limited to, retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema.

Provided are methods of treating subjects in need of an anti-fibroblast growth factor receptor 4 (anti-FGFR4) 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-FGFR4 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 FGFR4 inhibitor, a PPAR alpha agonist, and, optionally, a bile acid sequestrant. The methods attenuate the dysregulation of bile acid biosynthesis caused by FGFR4 inhibition with anti-FGFR4 therapies. The methods reduce the severity and / or incidence of adverse events associated with anti-FGFR4 therapies.

Benzyl derivative compounds having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, kits and compositions containing such compounds, and methods of their use in enhancing PPARα activity for treating diseases and / or conditions involving inflammation and / or angiogenesis, particularly ocular diseases and / or conditions such as but not limited to retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema.

The invention discloses a construction method of a spontaneous lupus adipositis animal model, which comprises the following steps: constructing keratinocytes with genotypes of PPAR [gamma] flox / flox- / -Krt5-CreERT < 2 + > / -Adipoq-Cre < + > / -and PPAR [gamma] flox / flox- / -Krt5-CreERT < 2 + > / -Adipoq-CreERT < 2 + > / -and fat cells into a conditional PPAR [gamma]-active receptor gamma gene knockout mouse, so as to construct the animal model with the spontaneous lupus adipositis animal model. Then knocking out PPAR gamma genes in keratinocytes and adipocytes by using a gene knockout activator, so that the mice spontaneously have the phenotypes of lupus septicaemia, including local skin unhairing, lipoatrophy, persistent skin lesion, proteinuria and serum autoantibodies; histological examination finds that lobular adipositis, glomerular volume increase, mesangial cell hyperplasia, inflammatory cell infiltration, glomerular IgG deposition and the like are mainly caused by dermal immune cell infiltration and subcutaneous fat layer lymphocyte infiltration, clinical symptoms of patients with lupus adipositis are simulated, and an important tool is provided for related research of lupus adipositis.

The present disclosure relates to a method for diagnosing and treating multiple-system atrophy (MSA) in a subject, the method comprising: determining in a subject-derived biological sample an expression level of a gene from the group consisting of: QKI, GGCX, MOCS1, NF1, LINC01572, PRRG3, HMBOX1, PLP1, PPP1CA, C8orf88, TGFB2, MASP1, TIAM1, SYNGAP1, ACTN1, EMP1, NFIL3, GPNMB, PGAM2, ST5, STON1, RFTN1, and MMP14; comparing the subject-derived expression level of the gene with a normal control expression level of the gene obtained from a non-neurodegenerative biological sample; diagnosing the subject as a having MSA by detecting a differential expression of the gene in the subject-derived biological sample as compared to the normal control expression level; and administering a peroxisome proliferator-activated receptor β (PPARβ) agonist or a retinoid X receptor (RXR) agonist to the subject diagnosed as having MSA.

Incorporation of lipids into a growing hair fibre is provided by a composition comprising at least one of: 1) 0.05 to 8 wt % of a lipid precursor selected from the group consisting of a fatty acid having a chain of 6 to 24 carbon atoms, an ester or an acylglycerol thereof and mixtures thereof; 2) 0.05 to 8.0% of a "gene activator material" that modulates the biosynthesis of lipids in the hair follicle or sebaceous gland, selected from a) at least one activator of a peroxisome proliferator-activated receptor (PPAR activator), b) at least one activator of a liver X receptor (LXR), and c) at least one activator of a retinoid X receptor (RXR); and 3) a fatty alcohol having a chain of 6 to 24 carbon atoms, preferably 8 to 20 carbon atoms, most preferably 10 to 18 carbon atoms; and mixtures thereof; and a cosmetically acceptable carrier.

The invention relates to an anti-inflammatory and lipid-lowering-based nano preparation for treating fatty liver and a preparation method of the nano preparation. Galactose modified polyethylene glycol-polylactic acid-glycolic acid copolymer (PEG-PLGA) is used as a targeting carrier, and a lipid-lowering drug fenofibrate and an anti-inflammatory drug curcumin are co-loaded; the particle size of the nano preparation is 150-200nm, and the drug encapsulation efficiency is greater than or equal to 85%. Galactose modified PEG-PLGA is adopted as a carrier, galactose can be specifically combined with an asialoglycoprotein receptor (ASGPR) specifically expressed on the surface of liver cells, active targeting of the liver is achieved, the drug enrichment amount of the liver lesion position is remarkably increased, meanwhile, accumulation of drugs in extrahepatic tissue is reduced, extrahepatic toxicity is effectively reduced, and the drug delivery effect is improved. According to the present invention, the anti-inflammatory drug curcumin and the fenofibrate are combined, such that the biological safety of the preparation is improved, the lipid lowering drug fenofibrate and the anti-inflammatory drug curcumin are innovatively co-loaded, and the fenofibrate and the anti-inflammatory drug curcumin form the synergistic effect system: fenofibrate can activate peroxisome proliferator-activated receptor alpha (PPAR alpha), promote liver lipid catabolism, and reduce lipid deposition;

Prenylated tetrahydroquinolines and quinolines and pharmaceutical compositions comprising the same. Prenylated tetrahydroquinoline and quinolines and pharmaceutical compositions comprising the same, for use in the prevention and / or treatment of peroxisome proliferator-activated receptor (PPAR)-mediated diseases such as metabolic syndrome, type 2 diabetes mellitus, dyslipidemia, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, obesity, dyslipidemic atherosclerosis, metabolic dysfunction- associated fatty liver disease (MAFLD), cardiovascular disease, cardiometabolic disease, neurodegenerative disease, Friedreich's ataxia, Parkinson's disease, multiple sclerosis, Alzheimer's disease, autoimmune disease, rheumatoid arthritis, autoimmune thyroid disease, dermatological disease, and cancer.

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.

The present disclosure relates generally to processes for preparing seladelpar, an agonist of peroxisome proliferator-activated receptor (PPAR)-delta, and compositions thereof.

A compound having the structure of Formula I: wherein m=2 and n is an odd-number between 4 and 20, or a derivative thereof, or a salt, or a prodrug thereof, and a compound having the structure of Formula II: wherein m and n are independently an integer between 2 and 20, or a derivative thereof, or a salt, or a prodrug thereof are described. Compositions and methods of use of the compounds for therapeutically modulating peroxisome proliferator-activated receptors (PPARs) are also provided

The present invention relates to the use of skin benefit agents for enhancing the overnight repair function of skin, wherein the skin benefit agents are selected from the group consisting of: borage oil, farnesol, activators of the peroxisome proliferator-activated receptors, and mixtures thereof; and wherein the skin benefit agents are applied to the skin from about 5 pm to about 12 am at the end of the day.

The present invention is directed to an isotropic wash composition. The composition is stable, comprises alfa olefin sulfonate and a co-anionic surfactant. The composition comprises an amphoteric surfactant, low salt content and can comprise a peroxisome proliferator-activated receptor (PPAR) agonist.

The present disclosure is directed to compounds and methods for the treatment of disorders associated with fluid retention or salt overload, such as heart failure (in particular, congestive heart failure), chronic kidney disease, end-stage renal disease, liver disease, and peroxisome proliferator-activated receptor (PPAR) gamma agonist-induced fluid retention. The present disclosure is also directed to compounds and methods for the treatment of hypertension. The present disclosure is also directed to compounds and methods for the treatment of gastrointestinal tract disorders, including the treatment or reduction of pain associated with gastrointestinal tract disorders.

The disclosure relates to fixed dose combinations of the integrin inhibitor bexotegrast ((S)-4-((2-methoxyethyl)(4-(5,6,7,8-tetrahydro-l,8-naphthyridin-2-yl)butyl)amino)-2- (quinazolin-4-ylamino)butanoic acid) with peroxisome proliferator-activated receptor agonists (PPAR agonists), and methods of treating a subject for a liver fibrotic disease, such as primary sclerosing cholangitis or primary biliary cholangitis, by administration of the fixed dose combinations.

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).

To provide a peroxisome proliferating agent-responsive receptor activation composition that is suitable for adding to food or the like in order to ingest, and is also suitable for continuous ingestion due to its excellent safety.SOLUTION: Provided is a peroxisome proliferating agent-responsive receptor activation composition that contains sucrose fatty acid ester as an active ingredient.SELECTED DRAWING: None

The pharmaceutical compound or the pharmaceutically acceptable salt thereof is used for preventing or treating the following diseases by simultaneously inhibiting autotaxin (ATX) and activating peroxisome proliferator-activated receptor gamma (PPAR gamma): a) fibroproliferative diseases, in particular interstitial lung diseases (ILD) and / or liver diseases, and b) fibroproliferative diseases, in particular interstitial lung diseases (ILD) and / or liver diseases; the present invention relates to a pharmaceutical composition for treating hepatitis, such as various hepatitis and / or non-alcoholic fatty liver disease (NAFLD) and / or non-alcoholic steatohepatitis (NASH) and / or cirrhosis, where said ILD may be a primary disease, preferably idiopathic pulmonary fibrosis and / or sarcoidosis and / or interstitial pneumonia, or said ILD is a complication associated with an autoimmune and / or inflammatory and / or metabolic disease, or a pharmaceutical composition comprising said ILD. Preferably rheumatoid arthritis ILD and / or scleroderma ILD and / or myositis ILD and / or diabetes ILD and / or cardiovascular disease ILD; and / or b) inflammatory and / or autoimmune diseases, preferably rheumatoid arthritis and / or scleroderma; and / or c) cancer, in particular lung and / or hepatocellular carcinoma and / or pancreatic cancer and / or glioblastoma and / or neuroblastoma; and / or d) a metabolic disease, in particular diabetes mellitus type 1 and / or diabetes mellitus type 2 and / or obesity, having a formula selected from the group consisting of formulae (A), (B), (C), (D), (E), (F), (G) and (H).

The present invention provides the use of albiflorin in the preparation of a medicament for treating ulcerative colitis. The research of the present invention finds that albiflorin has a therapeutic effect on ulcerative colitis and can significantly inhibit inflammation-induced pyroptosis of colonic epithelial cells. Further experiments find that the specific mechanism by which albiflorin inhibits the pyroptosis of colonic epithelial cells is achieved by activating the peroxisome proliferator-activated receptor γ-related signaling pathway. Therefore, albiflorin can significantly reduce intestinal damage in a DSS-induced colitis animal model and is a potential drug for treating inflammatory diseases such as ulcerative colitis. The present invention provides a new drug option for the treatment of patients with inflammatory bowel disease, and the drug source is extensive, the composition and dosage are clear, the drug use is safe, and there are no obvious side effects.

Benzyl derivative compounds having peroxisome proliferator-activated receptor alpha (PPAR alpha) agonistic activity, kits and compositions comprising such compounds, and methods of their use to enhance PPAR alpha activity for the treatment of diseases and / or disorders involving inflammation and / or angiogenesis, in particular ocular diseases and / or disorders, such as inflammatory diseases and / or angiogenesis. Such as, but not limited to, retinal inflammation, retinal neovascularization, retinal vascular leakage, preterm retinopathy, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema.

The present invention is directed to an isotropic and pearlescent wash composition. The composition is stable, comprises pearlescent agent and peroxisome proliferator-activated receptor (PPAR) agonist. The pearlescent agent is homogeneously dispersed when the wash composition is substantially free of polymeric thickening agent and suspending agent.

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.

Benzyl derivative compounds having peroxisome proliferator-activated receptor α (PPARα) agonistic activity, kits and compositions containing such compounds, and methods of their use in enhancing PPARα activity for treating diseases and / or conditions involving inflammation and / or angiogenesis, particularly ocular diseases and / or conditions such as but not limited to retinal inflammation, retinal neovascularization, retinal vascular leakage, retinopathy of prematurity, diabetic retinopathy, age-related macular degeneration, and diabetic macular edema.

The present invention relates to methods for treating an ophthalmic condition in a defined patient in need of treatment thereof. The methods comprise inducing the activity of peroxisome proliferator–activated receptor gamma coactivator-1 alpha (PGC1α) in a defined patient that needs treatment of an ophthalmic condition. The defined patient in these methods has been previously identified as having reduced carboxylesterase 1 (CES1) activity, compared to normal activity levels of CES1.

The present disclosure provides compounds of the formulas described herein (e.g., Formula (I)), and pharmaceutically acceptable salts and prodrugs thereof, which are non-agonist modulators of peroxisome proliferator-activated receptor gamma (PPARγ). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts or prodrugs thereof, and methods of treating or preventing diseases or disorders by administering the compounds, or pharmaceutically acceptable salts or prodrugs thereof, or pharmaceutical compositions thereof to a subject in need of treatment or prevention.

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.

There are provided compounds, agents, compositions and preparations which may be used to treat conditions such as colorectal cancer. Activity may be achieved through agonism of Peroxisome Proliferator-Activated Receptors. An exemplary compound is Formula (I):

The present disclosure provides (S)-enantiomers of 7-(3-chloro-6-methyl-5, 5-dioxo-6, 11-dihydrodibenzo [c, f] [1, 2] thiaza-11-ylamino) heptanoic acid ((S)-tianeptine) and (S)-enantiomers of deuterated tianeptine (11-D-(S)-tianeptine), both of which are characterized by comprising no more than 2%, or no more than about 0.1%, of the corresponding (R)-enantiomer. The present disclosure also provides salts, amides, esters, co-crystals, crystals, analogs, and pharmaceutical compositions thereof, and the use of (S)-enantiomers and those compounds and compositions for the treatment of diseases, disorders or conditions of CNS as well as diseases, disorders and disorders associated with, aggravated by, or modulated by altered activity of peroxisome proliferator-activated receptors (PPAR-beta / delta) and / or PPAR-gamma, and at the same time minimizes or eliminates the likelihood of opioid abuse. The present disclosure also provides methods of making the (S)-enantiomers and 11-D-(S)-enantiomers of the present disclosure, as well as related compounds.