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111 results about "Farnesoid X receptor" patented technology
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The bile acid receptor (BAR), also known as farnesoid X receptor (FXR) or NR1H4 (nuclear receptor subfamily 1, group H, member 4) is a nuclear receptor that is encoded by the NR1H4 gene in humans.
Farnesoid X receptor modulators
The present invention provides a compound of formula (I):or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.
Owner:INTERCEPT PHARMA INC
Heterocyclic farnesoid X receptor modifier
The invention relates to a preparation method of a heterocyclic compound and a composition with components the same as those of the heterocyclic compound and application of the heterocyclic compound as a farnesoid X receptor active modifier. The modifier is the heterocyclic compound shown as the formula I or salt acceptable pharmaceutically or a predrug or a solvent compound or a polycrystal or an isomer or a stable isotope derivative. The compound can be used for treating or preventing related diseases mediated by FXR, and the related diseases are caused by saccharide or lipid or bile metabolic disturbance. The formula I is shown in the specification.
Owner:SHANGHAI DE NOVO PHARMA
Method of reducing drug-induced adverse side effects in a patient
InactiveUS20060252670A1Good treatment effectReduce adverse side effectsBiocideSenses disorderSide effectPeroxisome Proliferation
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
Methods of using farnesoid x receptor (frx) agonists
InactiveUS20050107475A1Increasing leptin releaseFacilitated releaseBiocideAnimal repellantsFarnesoid X receptorAgonist
Treatment of human hepatocytes with farnesoid X receptor (FXR) agonists resulted in increased expression of FGF-19. Methods of using FXR agonists to alter cell metabolism, and in pharmaceutical weight loss methods, are described.
Owner:CURAGEN CORP +1
Treatment of fibrosis using FXR ligands
The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.
Owner:INTERCEPT PHARMA INC
FXR agonist
PendingCN107021957AExcellent FXR receptor agonistic activityGood biological stabilityOrganic active ingredientsOrganic chemistryPrimary biliary cirrhosisFarnesoid X receptor
The invention relates to a compound shown as formula (I), a pharmaceutically acceptable salt, ester or stereoisomer thereof. R1, R2, R3, R4, m, n, W, A, Z, E, F, X and Y are defined as the specification. The invention also relates to a preparation method of the compounds, pharmaceutical preparations and application in drugs for treatment and / or prevention of FXR (farnesoid X receptor) mediated nonalcoholic fatty liver diseases, primary biliary cirrhosis, lipid metabolism disorders, diabetic complications, malignant tumors and other related diseases. (formula (I)).
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
FXR regulator with spirane structure
InactiveCN109053751AExcellent FXR receptor agonistic activityPrevent non-alcoholic fatty liver diseaseOrganic active ingredientsNervous disorderDiseaseHepatic Diseases
The invention provides a new compound which has certain agonist activity on a Farnesoid X receptor (FXR) and is used for treating FXR mediated diseases and / or symptoms such as liver disease and gastrointestinal disease. (The formula is shown in the description.).
Owner:SCINNOHUB PHARM CO LTD
FXR agonist
PendingCN107021958AExcellent FXR receptor agonistic activityGood biological stabilityOrganic active ingredientsNervous disorderPrimary biliary cirrhosisFarnesoid X receptor
The invention relates to a compound shown as formula (I), a pharmaceutically acceptable salt, ester or stereoisomer thereof. R1, R2, R3, R4, m, n, W, A, Z, E, F, X and Y are defined as the specification. The invention also relates to a preparation method of the compounds, pharmaceutical preparations and application in drugs for treatment and / or prevention of FXR (farnesoid X receptor) mediated nonalcoholic fatty liver diseases, primary biliary cirrhosis, lipid metabolism disorders, diabetic complications, malignant tumors and other related diseases. (formula (I)).
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Farnesoid x receptor agonists
The present invention relates to famesoid X receptors (FXR, NR1 H4) FXR is a member of the nuclear receptor class of ligand-activated transcription factors. More particularly, the present invention relates to compounds useful as agonists for FXR, pharmaceutical formulations comprising such compounds, and therapeutic use of the same Novel isoxazole compounds are disclosed as part of pharmaceutical compositions for the treatment of a condition mediated by decreased FXR activity, such as obesity, diabetes, cholestatic liver disease and metabolic syndrome.
Owner:GLAXOSMITHKLINE LC
Farnesoid X receptor modulators
The present invention provides a compound of formula (I):or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1, R2, R3, R4, R5, and R6 are as described herein. The present invention relates generally to selective FXR agonists and to methods of making and using them.
Owner:INTERCEPT PHARMA INC
Use of FXR, PPAR 'alpha' and LXR 'alpha' activators to restore barrier function, promote epidermal differentiation and inhibit proliferation
InactiveCN1248916AHydrocarbon active ingredientsHydroxy compound active ingredientsDiseaseFarnesoid X receptor
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
Treatment of fibrosis using FXR ligands
The present invention relates to a method for inhibiting fibrosis that occurs in an organ where the farnesoid X receptor (FXR) is expressed. This method involves the step of administering a high potency, activating ligand of FXR in an effective amount to a patient who is not suffering from a cholestatic condition. The invention also provides pharmaceutical compositions containing an effective amount of an FXR ligand and kits for dispensing the pharmaceutical compositions.
Owner:INTERCEPT PHARMA INC
Preventive and/or therapeutic agent for diabetes
InactiveCN101039697AInhibit receptor activityOrganic active ingredientsMetabolism disorderDiabetes mellitusFarnesoid X receptor
A preventive and / or therapeutic agent for diabetes, comprising a substance capable of inhibiting the activity of farnesoid X receptor as an active ingredient.
Owner:MITSUBISHI TANABE PHARMA CORP
Compositions and methods for modulating farnesoid x receptors
ActiveCN105682656AHigh trafficOrganic active ingredientsOrganic chemistryEnantiomerFarnesoid X receptor
The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).
Owner:NOVARTIS AG
Farnesoid X receptor (FXR) stimulant
ActiveCN109320517AExcellent FXR receptor agonistic activityPrevent non-alcoholic fatty liver diseaseOrganic active ingredientsSenses disorderDiseaseStimulant
The invention belongs to the technical field of medicines, and particularly relates to a compound as shown in the formula (I), and pharmaceutically acceptable salt and ester or a stereisomer thereof.R1, R2, R3, M1, M2, m, n, Q, L, ring A, ring B and ring C are as defined in the specification. The invention further relates to a preparation method of the compounds, and application in preparing medicines for treating and / or preventing related diseases such as non-alcoholic fatty liver disease, primary biliary cirrhosis, lipid metabolism disorders, diabetic complication and malignant tumors mediated by an FXR. The formula (I) is shown in the description.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Composition containing SUMO inhibitor and application
InactiveCN109432431AInhibition of activationReduce depositionSalicyclic acid active ingredientsDigestive systemFiberHigh activation
The invention provides a composition containing an SUMO inhibitor, and belongs to the technical field of medicines. The composition is prepared from an FXR (farnesoid X receptor) agonist and the SUMOinhibitor. According to the composition, in the high-activation state of hepatic stellate cells, the FXR (farnesoid X receptor) agonist does not have the effect of inhibiting the activation of the hepatic stellate cells; after the FXR (farnesoid X receptor) agonist and the SUMO inhibitor are compounded, the activation of the hepatic stellate cells can also be inhibited in the high-activation stateof the hepatic stellate cells; and the hepatic stellate cells of an individual with fibrosis symptoms are in an activated state, using the FXR (farnesoid X receptor) agonist alone cannot generate a good anti-fibrosis effect. The composition of the FXR (farnesoid X receptor) agonist and the SUMO inhibitor has the advantages that the activation of the hepatic stellate cells can be obviously inhibitd, deposition of collagenous fibers can be reduced, and therefore a remarkable anti-fibrosis effect can be achieved.
Owner:CHINA PHARM UNIV
Modulators of farnesoid x receptor and methods for the use thereof
InactiveUS20180116993A1Metabolism disorderDigestive systemLiver diseaseReceptor for activated C kinase 1
Owner:XIAMEN UNIV
Application of FXR expression interference reagent in preparation of anti-hepatic fibrosis drugs
InactiveCN108079316AIntegrity guaranteedLower serum transaminasesDigestive systemNon-active genetic ingredientsFarnesoid X receptorHepatic fibrosis
The present invention relates to the field of biomedicine. The present invention provides application of a farnesoid X receptor (FXR) expression interference reagent in preparation of anti-hepatic fibrosis drugs. Specifically, the present invention relates to application of FXR for treatment of hepatic fibrosis, by tail intravenous injection of the farnesoid X receptor (FXR) expression interference reagent (namely, an adenovirus carrying FXR plasmid) to mice, the expression level of the FXR in hepatocytes is significantly increased, CCl4-induced hepatic fibrosis can be significantly countered,hepatocyte morphology and structural integrity can be maintained, and serum transaminase level can be reduced. A new approach for clinical treatment of liver diseases especially hepatic fibrosis is provided.
Owner:CHINA PHARM UNIV
Inhibitors of inflammatory gene activity and cholesterol biosynthesis
InactiveUS20050221328A1Improve efficiencyCost-effectiveBiocideCompound screeningFarnesoid X receptorCholesterol biosynthesis
Methods of identifying agents effective as inhibitors of short heterodimer protein (SHP) and farnesoid X receptor (FXR) and promoters, cell lines and vectors used in said methods. Methods of preparing and using the agents effective as inhibitors of short heterodimer protein (SHP), including methods of using same to prevent and / or treat a condition associated with inflammatory gene activity and / or cholesterol biosynthesis in a subject. Agents effective as inhibitors of short heterodimer protein (SHP) and farnesoid X receptor (FXR) and compositions comprising same, including compositions effective in reducing inflammatory gene activity and / or cholesterol biosynthesis in a subject.
Owner:WYETH HOLDINGS CORP
Carboxylic acid derivative and application of carboxylic acid derivative serving as FXR (farnesoid X receptor) antagonist
The invention relates to preparation of carboxylic acid derivatives and application of the carboxylic acid derivatives serving as an FXR (farnesoid X receptor) antagonist and particularly provides a compound shown as a formula (I), or a pharmaceutically acceptable salt of the compound and a preparation method of the compound. In the formula (I) as shown in the specification, R1 is selected from hydrogen, methyl, methoxyl, halogen, nitryl and carboxyl; X is selected from NH or O; n1 is 0 or 1; n2 is 0 or 1; R1 and a radical as shown in the specification are positioned at any substitution positions of a benzene ring. The compound shown as the formula (I) or the pharmaceutically acceptable salt thereof has a pharmacological effect of blood fat reduction and can be used as the FXR antagonist.
Owner:SHANGHAI INST OF PHARMA IND +1
Farnesoid X receptor (FXR) stimulant
ActiveCN109320509AExcellent FXR receptor agonistic activityPrevent non-alcoholic fatty liver diseaseOrganic active ingredientsSenses disorderDiseaseStimulant
The invention belongs to the technical field of medicines, and particularly relates to a compound as shown in the formula (I), and pharmaceutically acceptable salt and ester or a stereisomer thereof.R1, R2, R3, R4, W, A, Z, E, X, Y and n are as defined in the specification and the claims. The invention further relates to a preparation method of the compounds, pharmaceutical preparation and application in preparing medicines for treating and / or preventing related diseases such as non-alcoholic fatty liver disease, primary biliary cirrhosis, lipid metabolism disorders, diabetic complication andmalignant tumors mediated by an FXR. The formula (I) is shown in the description.
Owner:XUANZHU BIOPHARMACEUTICAL CO LTD
Methods for using fxr agonists
ActiveUS20190046518A1Good potencyStrong specificityDigestive systemPharmaceutical delivery mechanismDiseaseFarnesoid X receptor
Owner:NOVARTIS AG
Action mechanism of silybin for preventing liver apoptosis through FXR (Farnesoid X Receptor) path
The invention relates to the field of natural medicines, and in particular relates to an action mechanism of silybin for preventing liver apoptosis through an FXR (Farnesoid X Receptor) path. According to the invention, the silybin prevents apoptosis of HepG2 cells caused by ActD / TNF alpha through an FXR dependent path. Within human hepatoma cell line HepG2 cells, silybin can induce up-regulation of mRNA level and protein level of FXR in a dose-dependent manner, and can reverse down-regulation of FXR expression in a HepG2 cell apoptosis model caused by ActD / TNFalpha remarkably; the silybin has remarkable protective effect on the HepG2 cell apoptosis caused by the ActD / TNFalpha, but the anti-apoptosis function of the silybin is lost after the FXR SiRNA is used for silencing endogenous FXR genes.
Owner:CHINA PHARM UNIV
Application of nuclear FXR (Farnesoid X Receptor) in targeted therapy of liver cancer stem cells
InactiveCN106237332ARealize regulationReduce carcinogenicityDigestive systemAntineoplastic agentsBiological activationTargeted therapy
The invention belongs to the field of biomedicines, and relates to application of a nuclear FXR (Farnesoid X Receptor) in targeted therapy of liver cancer stem cells. The nuclear FXR is used as a target for diagnosing or assisting in diagnosis of the liver cancer stem cells, and a gene medicine or a chemical medicine is designed to be applied to treatment of the liver cancer stem cells. According to the application of the nuclear FXR in the targeted therapy of the liver cancer stem cells, the gene medicine is an FXR-containing expression vector or interference vector; the chemical medicine contains a ligand for regulating the FXR and a ligand for regulating a target gene of the FXR. According to the application, by virtue of cell transfection and activation of the nuclear FXR, the tumor ball formation capacity of a hepatoma cell line can be obviously reduced, and the tumorigenicity of the liver cancer stem cells is reduced; a new molecular target is supplied to identification of the liver cancer stem cells and diagnosis and treatment of the liver cancer, so that the problem that a conventional molecular marker of tumor stem cells is hard to regulate is solved.
Owner:HENAN UNIVERSITY
Application of combination of FXR (Farnesoid X Receptor) agonist and SIRT1 (Sirtuin1) agonist for preparing anti-hepatic fibrosis drug
ActiveCN109303921AReduced expression levelHydroxy compound active ingredientsDigestive systemFarnesoid X receptorPharmaceutical drug
The invention discloses application of combination of FXR (Farnesoid X Receptor) agonist and SIRT1 (Sirtuin1) agonist for preparing an anti-hepatic fibrosis drug. Compared with the prior art, the invention discloses the application of the combination of FXR agonist and SIRT1 agonist for preparing the anti-hepatic fibrosis drug. Under a liver injury state, an FXR expression level is obviously lowered, in addition, the SIRT1 agonist can obviously inhibit FXR protein reduction, and therefore, the FXR agonist and the SIRT1 agonist are combined for treating hepatic fibrosis so as to perform an important role.
Owner:CHINA PHARM UNIV
Novel benzimidazole derivatives
The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to Farnesoid-X-receptors (FXR) and can be used to treat diseases which are modulated by FXR agonists such as diabetes and dyslipidemia.
Owner:F HOFFMANN LA ROCHE INC
Agent for prophylactic and/or therapeutic treatment of diabetes
InactiveUS20100055066A1Organic active ingredientsMetabolism disorderDiabetes mellitusFarnesoid X receptor
According to the present invention, an agent for prophylactic and / or therapeutic treatment of diabetes comprising a substance inhibiting activity of farnesoid X receptor as an active ingredient can be provided.
Owner:MITSUBISHI TANABE PHARMA CORP
Combination compositions comprising fxr agonists for treating or preventing a fibrotic, cirrhotic disease or disorder
InactiveUS20190231770A1Reduce developmentDipeptide ingredientsDigestive systemDiseaseFarnesoid X receptor
The invention provides pharmaceutical compositions comprising a farnesoid X receptor (FXR) agonist and another therapeutic agent, in particular for treating or preventing liver diseases or disorders.
Owner:NOVARTIS AG
Application of FXR antagonist in preparing anti-HBV medicines
InactiveCN107441098AEasy to removeImprove the quality of lifeOrganic active ingredientsDigestive systemLymphatic SpreadFarnesoid X receptor
According to the invention, a farnesoid X receptor (FXR) antagonist is applied to treatment of HBV infected persons. Serum bile acid in the HBV infected persons can promote HBV replication and expression through the FXR, and the FXR receptor antagonist can inhibit the HBV replication and expression, promote HBV cleaning, improve hepatic functions, inhibit hepatic fibrosis and hepatic cirrhosis and reduce risk of metastasis of liver cancer.
Owner:HENAN UNIVERSITY
Methods for using fxr agonists
ActiveUS20190083481A1Good potencyStrong specificityDigestive systemPharmaceutical delivery mechanismDiseaseHepatic Diseases
Owner:NOVARTIS AG
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