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39 results about "Peroxisome Proliferation" patented technology

Associated with hepatocellular carcinomas, Peroxisome Proliferation occurs in epigenetic non-genotoxic responses of hepatocytes to diverse peroxisome proliferator chemicals and involves, probably by a steroid superfamily receptor-based mechanism (PPARs), altered expression of cellular growth and/or differentiation genes, induction of peroxisomal enzymes, and possibly oxidative stress.

Method of reducing drug-induced adverse side effects in a patient

The invention relates to the discovery that farnesoid X receptor (FXR) agonists can be used in combination with peroxisome proliferation activated receptor gamma (PPARγ) agonists to reduce drug-induced adverse side effects in patients suffering from conditions such as insulin resistance, Type II diabetes, metabolic syndrome, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and heart disease. Particularly, the present invention encompasses methods for treating patients suffering from drug-induced adverse side effects with selective PPARγ, dual PPARα / γ and pan PPARα / γ / δ agonists in combination with FXR agonists.
Owner:INTERCEPT PHARMA INC

Activating agent for peroxisome proliferator activated receptor delta

A compound represented by the general formula (II) below or a salt thereof is used as an activating agent for PPAR d. (II) (In the formula, G represents O, CH2 or the like; A represents a thiazole, oxazole or thiophene which may have a substituent selected from an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, a halogen atom, an alkyl group having 1-8 carbon atoms and substituted by a halogen atom and the like; B represents an alkylene chain having 1-8 carbon atoms, and when the alkylene chain has two or more carbon atoms, it may have a double bond; and R<1a> and R<2a> respectively represent a hydrogen atom, an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, a halogen atom, an alkyl group having 1-8 carbon atoms and substituted by a halogen atom or the like.
Owner:NIPPON CHEMIPHAR CO LTD

Substituted phenylpropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor (PPAR) alpha

The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor alpha (PPARalpha), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride).It relates to a substituted phenylpropanoic acid derivatives represented by a general formula (1),their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.
Owner:KYORIN PHARMA CO LTD

Modulators of peroxisome proliferator activated receptors

Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W, R1 is (CH2)n—CH(OR2)—(CH2)mE1, —(CH)═C(OR2)—(CH2)mE, —(CH2)n—CH(Y)—(CH2)mE or (CH)═C(Y)—(CH2)mE; wherein E is COOR3, C1–C3 alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1–C6 alkyl, haloalkyl and aryl-C0-4-alkyl; R2 is H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or C(S)NR5R6, R3 is H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is O—, CH2—, —CH2CH2— or CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4–R6 are independently H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2
Owner:ELI LILLY & CO +1

Use of FXR, PPAR 'alpha' and LXR 'alpha' activators to restore barrier function, promote epidermal differentiation and inhibit proliferation

Disorders of the skin and mucous membranes that have a disrupted or dysfunctional epidermal barrier are treated or prevented by topical application of compounds that are either activators of the farnesoid X receptor, activators of the peroxisome proliferator-activated receptor alpha , and oxysterol activators of the LXR alpha receptor. The same compounds are also effective in treating disorders of epidermal differentiation and proliferation.
Owner:RGT UNIV OF CALIFORNIA

Peroxisome proliferator activated receptor modulators

The present invention is directed to compounds of the structural Formula: wherein: R1 is H or —C1-C3 alkyl; R2 is selected from the group consisting of —H, —C1-C4 alkyl, —C1-C3 alkyl-CF3, phenyl, and pyridinyl; and R3 is selected from the group consisting of —H, —C1-C4 alkyl, —C1-C3 alkyl-O—CH3, —CH2-cyclopropyl, CH2—C═CH2, —CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; provided that when R1 and R2 are each H, then R3 is selected from the group consisting of —C1-C4 alkyl, —C1-C3 alkyl-O—CH3, —CH2-cyclopropyl, —CH2—C═CH2, —CH2CH2-(2-F-phenyl), and phenyl substituted with from 1 to 2 fluorines; or stereoisomers and pharmaceutically acceptable salts thereof.
Owner:ELI LILLY & CO

PPAR (Peroxisome Proliferator-Activated Receptor) alpha gene and application thereof as goose fat traits genetic markers

The invention relates to a PPAR (Peroxisome Proliferator-Activated Receptor) alpha gene and application thereof as goose fat traits genetic markers. Genetic markers related to abdomen fat weight and abdomen fat ratio in the PPAR alpha gene are measured; the existence of polymorphism in the PPAR alpha gene in a nucleic acid sample obtained from a goose is measured, wherein the polymorphism is related to the abdomen fat weight and the abdomen fat ratio; and the fat traits selection breeding can be carried out on the goose containing the PPAR alpha gene in a genome DNA according to the single nucleotide polymorphism of the gene, and an advantageous genotype for reducing the abdomen fat weight and the abdomen fat ratio is obtained by the screening. The invention has extremely important application value and economic benefit.
Owner:曲湘勇 +1

Pharmaceutical use of an extended-release composition containing pirfenidone for the treatment and reversal of human steatohepatitis (nafld/nash)

The present invention relates to the use of a pharmaceutical composition in the form of extended-release tablets containing Pirfenidone for treating NAFLD / NASH and advanced liver fibrosis by decreased serum cholesterol and triglycerides as well as reducing the content of hepatic fat accumulation, both in the form of macrosteatosis and microsteatosis. Additionally, its use as an agonist for PPARgamma (peroxisome proliferation receptor activated gamma), PPARalpha (peroxisome proliferation receptor activated alpha), LXR and CPT1, key molecules in the metabolism of fatty degradation and inflammation of the liver. In addition, another use is the induction of decreased expression of NFkB master gene, transcriptional inducer of hepatic inflammatory process factor. All of these events results in the reversal of NAFLD / NASH and advanced liver fibrosis.
Owner:EXCALIBUR PHARM INC

Peroxisome proliferator activated receptor modulators

InactiveUS20050107449A1Lowering fibrinogenRaise HDL levelsBiocideOrganic chemistryThiazolePeroxisome Proliferation
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I. (Formula I); wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, aryl (C0-C4) alkyl, aryloxy (C0-C4) alkyl, arylthio (C0-C4) alkyl, and further wherein when R5 is alkyl, R5 can optionally combine with W to form a 6 membered cycloheteroalkyl ring that is fused with the oxazole or thiazole ring to which the R5 group is attached; (b) R9 is selected from the group consisting of C1-C5 alkyl, C1-C5 alkenyl, and arylC0-C3alkyl. (c) T1 is selected from the group consisting of C and N, (d) W is selected from the group consisting of CH2, C(O)N(R21), N(R21), N(R21)CH2, O, OCH2, S, and SO2; and (e) X is selected from the group consisting of C, CH2C, and CCH2
Owner:ELI LILLY & CO

Modulation of peroxisome proliferation-activated receptors

Method of treating diseases associated with peroxisome proliferator-activated receptors by administering to a subject in need thereof an effective amount of 15-ketoprostaglandin-delta 13 - Reductase modulators. Also disclosed is a method of identifying a compound that inhibits the reductase activity, and a method of lowering blood glucose levels by administering to a subject an effective amount of the reductase inhibitor.
Owner:ABGENOMICS COOPERATIEF U A

Peroxisome proliferator activated receptor alpha agonists

The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
Owner:ELI LILLY & CO

Modulators of peroxisome proliferator activated receptors

Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W. R1 is —(CH2)n—CH(OR2)—(CH2)mE, —(CH)═C(OR2)—(CH2)mE, —(CH2)n—CH(Y)—(CH2)mE or —(CH)═C(Y)—(CH2)mE; wherein E is COOR3, C1-C3-alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1-C6 alkyl, haloalkyl and aryl-C0-4-alkyl; R2 is —H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or —C(S)NR5R6. R3 is —H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is —O—, —CH2—, —CH2CH2— or —CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4-R6 are independently —H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2.
Owner:BROOKS DAWN +12

Peroxisome proliferator activated receptor modulators

InactiveUS20060084663A1Lowering fibrinogenRaise HDL levelsBiocideOrganic chemistryArylHydrogen
The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts thereof, Formula I: wherein: (a) R5 is selected from the group consisting of (C1-C6) alkyl, (C1-C6) alkenyl, substituted aryl(C0-C4)alkyl, substituted aryloxy(C0-C4)alkyl, substituted arylthio(C0-C4)alkyl, unsubstituted aryl(C0-C4)alkyl, unsubstituted aryloxy(C0-C4)alkyl, and unsubstituted arylthio(C0-C4)alkyl; (b) T1 is C or N; (c) Q is selected from the group consisting of O, a single bond, O(CH2)q and C; (d) q is 1 or 2; (e) W is selected from the group consisting of O, S, (CH2)rN(R20)(CH2)k, NHSO2, C(O)N(R20)(CH2)r, (CH2)rN(R20)C(O), and SO2; (f) X is CmH2m; (g) m is 0, 1 or 2; (h) A is an functional group selected from the group consisting of carboxyl, C1-C3 alkylnitrile, carboxamide, and (CH2)nCOOR19; and (i) R19 is selected from the group consisting of hydrogen, optionally substituted C1-C4alkyl and optionally substituted arylmethyl.
Owner:ELI LILLY & CO

Detection method for detecting adipogenic potential of mesenchymal stem cells

PendingCN111057750AAdipogenic potentialMicrobiological testing/measurementMedicineAdipogenesis
A detection method for detecting adipogenic potential of mesenchymal stem cells comprises the following steps: respectively collecting d0 cells and d7 cells, and respectively extracting total RNA of the d0 cells and the d7 cells; synthesizing cDNA from the total RNA of the d0 cell and the d7 cell respectively; and detecting and calculating the relative expression quantity of the peroxisome proliferative activation receptor gamma 2 of the d0 cells and d7 cells by taking peroxisome proliferative activation receptor gamma 2 as a primer and 18S rRNA as an internal reference, and judging that the mesenchymal stem cells have the large adipogenesis potential when the ratio of X7:X0 is larger than or equal to 10. The detection method for detecting the adipogenesis potential of the mesenchymal stemcells can judge that whether the mesenchymal stem cells have large adipogenesis potential or not by detecting the relative expression quantity of the peroxisome proliferative activation receptor gamma 2 on the seventh day of induction, so the detection method has great significance in the adipogenesis induction culture process of the mesenchymal stem cells.
Owner:上海葆年生物科技有限公司

Application of ciglitazone in preparing drugs for treating pulmonary arterial hypertension

InactiveCN109512818APositive and obvious effectThe role is clearOrganic active ingredientsRespiratory disorderPulmonary vasculatureCiglitazone
The invention belongs to the field of medicinal chemistry and provides an application of ciglitazone in preparing drugs for treating pulmonary arterial hypertension. An experiment of the invention proves that ciglitazone is capable of effectively reducing average pulmonary artery pressure and pulmonary vasculature resistance of pulmonary arterial hypertension rats, increasing cardiac output, reducing right ventricular hypertrophy index, improving pulmonary vasculature remodeling and increasing protein expression of Gamma(peroxisome proliferation activated receptor, PPAR Gamma). The experimentproves that ciglitazone has a therapeutic effect on pulmonary arterial hypertension.
Owner:张锐

Novel compounds, their preparation and use

A novel class of dicarboxylic acid derivatives, the use of these compounds as phar-maceutical compositions, pharmaceutical compositions comprising the compounds and meth-ods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and / or prevention of conditions mediated by Peroxisome Prolifera-tor-Activated Receptors (PPAR).
Owner:NOVO NORDISK AS

Dihydronaphthalene devivatives and drugs contanining these compounds as active ingrdeient

Compounds represented by the following general formula (I): (I) wherein each symbol has the meaning as defined in the description; salts thereof and drugs for controlling peroxisome proliferation-activated receptor which contain these compounds as the active ingredient. Because of having an activity of controlling peroxisome proliferation-activated receptor, the compounds of the general formula (I) are useful as hypoglycemics, lipid-lowering agents, preventives and / or remedies for metabolic errors such as diabetes, obesity, syndrome X, hypercholesterolemia and hyperlipoproteinemia, preventives and / or remedies for hyperlipemia, arteriosclerosis, hypertension, circulatory diseases, over-eating, ischemic heart diseases, etc., HDL cholesterol-elevating agents, LDL cholesterol and / or VLDL cholesterol-lowering agents and risk factor relieving agents for diabetes and syndrome X.
Owner:ONO PHARMA CO LTD

Pharmaceutical composition containing pioglitazone and glimepiride

The invention provides a pharmaceutical composition containing pioglitazone and glimepiride. Glimepiride which is one of components of the pharmaceutical composition disclosed by the invention can be used for lowering the blood sugar of a patient with II diabetes by stimulating insulin to release from a functional pancreatic beta cell. By virtue of a non-insulin mechanism, the glimepiride further can be used for increasing the sensitivity of a peripheral tissue to insulin. Another component pioglitazone hydrochloride is a peroxysome proliferator-activated receptor-gamma agonist with strong effect and high selectivity, and capable of lowering the insulin resistance of livers and the peripheral tissue, so that the insulin-dependent glucose utilization is increased, and the output of hepatic glucose is lowered.
Owner:SICHUAN HAISCO PHARMA CO LTD

Composition for activating fatty acid-G protein coupling acceptor route

The invention belongs to the field of medicines, and discloses a composition for activating a fatty acid-G protein coupling acceptor route. The composition contains polysaccharide and / or saponin, wherein the polysaccharide is from an extract of medicinal materials A, and the medicinal materials A are selected from one or more of glossy ganoderma, poria cocos, fungus umbellatus, antrodia cinnamomea, shiitake mushrooms, fungi, Chinese caterpillar fungi and cordyceps militaris; and the saponin is from an extract of medicinal materials B, and the medicinal materials B are selected from one or moreof ginseng and processed products thereof, pseudo-ginseng and fiveleaf gynostemma herbs. The composition disclosed by the invention can effectively increase the abundance of short chain fatty acid generation bacteria in a host body, and increase the contents of short chain fatty acid, protein G coupling acceptors, and activating acceptors and peptide tyrosine of downstream signaling molecule peroxisome proliferation agents. Besides, the expression level of histone deacetylase in intestinal tracts can be reduced, and further important guarantee is provided for maintaining health of the intestinal tracts of the host. In addition, the composition disclosed by the invention is high in safety.
Owner:MACAU UNIV OF SCI & TECH
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