Target and Its Patented Drug(s)

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Target General Information
Patent(s) and the Corresponding Patented Drug(s)
References
Target General Information  Top
Target ID T51426 Target Info
Target Name Farnesoid X-activated receptor (FXR)
Synonyms Retinoid X receptor-interacting protein 14; RXR-interacting protein 14; RIP14; Nuclear receptor subfamily 1 group H member 4; HRR1; Farnesol receptor HRR-1; FXR; Bile acid receptor; BAR
Target Type Successful Target
Gene Name NR1H4
Biochemical Class Nuclear hormone receptor
UniProt ID
NR1H4_HUMAN
Patent(s) and the Corresponding Patented Drug(s)  Top
World Intellectual Property Organization (WIPO)
Patent ID WO2017147047
Title Fxr Modulators and Methods of Their Use.
Abstract The present disclosure is directed to modulators of farnesoid X receptor. Methods of making and using these modulators is also described.
Applicant(s) Alios Biopharma, Inc
Representative Drug(s) D01XIW Drug Info EC50 > 57 nM; EC50 < 10700 nM Click to Show More [1]
2 D0FC0B Drug Info EC50 > 57 nM; EC50 < 10700 nM [1]
Patent ID WO2017143134
Title Fxr Modulators and Methods of Their Use.
Abstract The present disclosure is directed to modulators of farnesoid X receptor. Methods of making and using these modulators is also described.
Applicant(s) Alios Biopharma, Inc
Representative Drug(s) D0N4PL Drug Info EC50 = 9 nM [1]
Patent ID WO2016127924
Title Tricyclic Compounds and Uses Thereof In Medicine.
Abstract The present invention relates to novel tricyclic compounds which can bind to FXR and act as modulators of the FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the uses of the compounds for the treatment of diseases and/or conditions mediated by FXR. The invention further provides a pharmaceutical composition containing the compound disclosed herein and a method of treatment of diseases and/or conditions mediated by FXR comprising administering the compound or the pharmaceutical composition.
Applicant(s) Sunshine Lake Pharma Co., Ltd
Representative Drug(s) D03IMJ Drug Info EC50 = 6 nM Click to Show More [1]
2 D0J4CL Drug Info EC50 = 6 nM [1]
Patent ID WO2016086218
Title Bile Acid Derivatives As Fxr/Tgr5 Agonists and Methods of Use Thereof.
Abstract The present invention provides compounds of amino-substituted bile acid derivatives, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions. In one embodiment the present invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound or combination of compounds of the present invention, or a pharmaceutically acceptable salt form, stereoisomer, solvate, hydrate or combination thereof, in combination with a pharmaceutically acceptable carrier or excipient.
Applicant(s) Enanta Pharmaceuticals, Inc
Representative Drug(s) D07NTP Drug Info EC50 = 100 nM Click to Show More [1]
2 D08ZAW Drug Info EC50 = 100 nM [1]
3 D0BN9E Drug Info EC50 = 100 nM [1]
Patent ID WO2016073767
Title Bile Acid Analogs An Fxr/Tgr5 Agonists and Methods of Use Thereof.
Abstract The present invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, where Ri, R2, R3, R4, R5, R6, R7, Rs and m are as defined herein, pharmaceutical compositions comprising these compounds and methods of use of these compounds for treating a TGR5 mediated disease or condition.
Applicant(s) Enanta Pharmaceuticals, Inc
Representative Drug(s) D0HR8Y Drug Info EC50 < 100 nM Click to Show More [1]
2 D0U0CC Drug Info EC50 < 100 nM [1]
Patent ID WO201696115
Title Hydroxy Containing Fxr (Nr1H4) Modulating Compounds.
Applicant(s) Gilead Sciences
Representative Drug(s) D08MBD Drug Info EC50 = 1 nM Click to Show More [1]
2 D0TL4F Drug Info EC50 = 1.6 nM [1]
Patent ID WO2008002573
Title Bile Acid Derivatives As Fxr Ligands for The Prevention or Treatment of Fxr-Mediated Deseases or Conditions.
Abstract The present invention relates to compounds of formula (I) wherein R is hydrogen or alpha-hydroxy, the hydroxyl group in position 7 is in the alpha or beta position; and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof.
Applicant(s) Intercept Pharmaceuticals, Inc
Representative Drug(s) D0E0MH Drug Info EC50 = 30 nM Click to Show More [1]
2 D08LIB Drug Info N.A. [1]
Patent ID WO2017062763
Title Farnesoid X Receptor Modulators.
Abstract The present application provides a compound of formula I: or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, as described herein. The present invention relates generally to FXR modulators and to methods of making and using said compounds.
Applicant(s) Intercept Pharmaceuticals, Inc
Representative Drug(s) D0E5ED Drug Info N.A. Click to Show More [1]
2 D0EB7G Drug Info N.A. [1]
3 D0F3SQ Drug Info N.A. [1]
4 D0JD0G Drug Info N.A. [1]
Patent ID WO2016149111
Title Treating Latent Autoimmune Diabetes of Adults with Farnesoid X Receptor Agonists To Activate Intestinal Receptors.
Abstract Disclosed are embodiments of a method of treating or preventing latent autoimmune diabetes of adults (LADA) in a subject. Such embodiments include administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or farnesoid X receptor (FXR) agonist compounds, thereby activating FXR receptors in the intestines, and treating or preventing latent autoimmune diabetes of adults (LADA) in the subject.
Applicant(s) Salk Institute for Biological Studies
Representative Drug(s) D04QBY Drug Info N.A. Click to Show More [1]
2 D07EDS Drug Info N.A. [1]
3 D08MYA Drug Info N.A. [1]
4 D0OM2M Drug Info N.A. [1]
Patent ID WO2015138986
Title Fxr Agonists and Methods for Making and Using.
Abstract Novel FXR agonists are disclosed, embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.
Applicant(s) Salk Institute for Biological Studies
Representative Drug(s) D04QBY Drug Info N.A. Click to Show More [1]
2 D07EDS Drug Info N.A. [1]
3 D08MYA Drug Info N.A. [1]
4 D0OM2M Drug Info N.A. [1]
Patent ID WO2015138969
Title Analogs of Fexaramine and Methods of Making and Using.
Abstract Novel compounds having a formula embodiments of a method of making the same, and of a composition comprising them are disclosed herein. Also disclosed are embodiments of a method of treating or preventing a metabolic disorder in a subject, comprising administering to a subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and treating or preventing a metabolic disorder in the subject. Additionally disclosed are embodiments of a method of treating or preventing inflammation in an intestinal region of a subject, comprising administering to the subject (e.g., via the gastrointestinal tract) a therapeutically effective amount of one or more of the disclosed compounds, thereby activating FXR receptors in the intestines, and thereby treating or preventing inflammation in the intestinal region of the subject.
Applicant(s) Salk Institute for Biological Studies
Representative Drug(s) D04QBY Drug Info N.A. Click to Show More [1]
2 D07EDS Drug Info N.A. [1]
3 D08MYA Drug Info N.A. [1]
4 D0OM2M Drug Info N.A. [1]
Patent ID WO2011020615
Title Novel Fxr (Nr1H4 ) Binding and Activity Modulating Compounds.
Abstract The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.
Applicant(s) Phenex Pharmaceuticals Ag
Representative Drug(s) D0R8GK Drug Info N.A. [2]
Patent ID WO2017189651
Title Isoxazole Derivatives As Fxr Agonists and Methods of Use Thereof.
Abstract The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated as FXR modulators. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.
Applicant(s) Enanta Pharmaceuticals, Inc
Representative Drug(s) D0A4LL Drug Info EC50 < 100 nM [1]
Patent ID WO2017145041
Title Methods for Using Fxr Agonists.
Abstract The invention provides methods for modulating the activity of farnesoid X receptors (FXRs) using specific FXR agonists, in particular for treating or preventing liver diseases.
Applicant(s) Novartis Ag
Representative Drug(s) D05EUR Drug Info EC50 = 0.2 nM [2]
Patent ID WO2016174616
Title Fused Tricyclic Pyrazole Derivatives Useful for Modulating Farnesoid X Receptors.
Abstract 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).
Applicant(s) Novartis Ag
Patent ID WO2016103037
Title Fused Bicyclic Compounds for The Treatment of Disease.
Abstract Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
Applicant(s) Akarna Therapeutics, Ltd
Patent ID WO2016096116
Title Novel Fxr (Nr1H4) Modulating Compounds.
Abstract The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
Applicant(s) Gilead Sciences, Inc
Representative Drug(s) D0F2OO Drug Info EC50 = 5.2 nM [1]
Patent ID WO2016086169
Title Bile Acid Analogs As Fxr/Tgr5 Agonists and Methods of Use Thereof.
Abstract The present invention relates to compounds of Formula (IA) and Formula (IB), and pharmaceutically acceptable salts thereof, where R1, R2, R3, R4, R5, R6, R7, R8, R9 and m are as defined herein, pharmaceutical compositions comprising these compounds and methods of use of these compounds for treating a TGR5 mediated disease or condition.
Applicant(s) Enanta Pharmaceuticals, Inc
Representative Drug(s) D05QJY Drug Info EC50 = 60 nM [1]
Patent ID WO2015116856
Title Farnesoid X Receptor Antagonists.
Abstract Provided herein are Famesoid X receptor (FXR) antagonists having the structure of formula (I), and pharmaceutical compositions comprising the compound of formula (I) and a pharmaceutically acceptable excipient. Also provided are methods of antagonizing FXR and methods of treating metabolic disease in a subject in need thereof, comprising administering an effective amount of the FXR antagonist of formula (I) to a subject.
Applicant(s) City of Hope Foreman, Barry
Representative Drug(s) D0KB4T Drug Info EC50 = 7.5 nM [1]
Patent ID WO2015069666
Title Compositions and Methods for Modulating Farnesoid X Receptors.
Abstract 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).
Applicant(s) Novartis Ag
Representative Drug(s) D02RCY Drug Info EC50 < 81 nM; EC50 > 0.4 nM [1]
Patent ID WO2009012125
Title Compounds and Methods for Modulating Fxr.
Abstract Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.
Applicant(s) Eli Lilly and Company
Representative Drug(s) D0TH6M Drug Info EC50 = 193 nM [2]
Patent ID WO2017205684
Title Combination Therapies with Farnesoid X Receptor (Fxr) Modulators.
Abstract Described herein are methods of treating a metabolic disorder in an individual in need thereof, comprising co-administering to the individual a therapeutically effective amount of an FXR modulator, and at least one second agent that is an CCR2/CCR5 antagonist, ASKl inhibitor, DPP-IV inhibitor, caspase protease inhibitor, SGLT2 inhibitor, acetyl-CoA carboxylase (ACC) inhibitor, diacyl glycerol acyltransferase-1 inhibitor, sodium -bile acid cotransporter-inhibitor, TLR-4 antagonist, PPAR alpha/delta agonist, or GLP-1 agonist, or a combination thereof.
Applicant(s) Akarna Therapeutics, Ltd
Patent ID WO2017205633
Title Fused Bicyclic Compounds for The Treatment of Disease.
Abstract Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
Applicant(s) Akarna Therapeutics, Ltd
Representative Drug(s) D0K3UO Drug Info N.A. [1]
Patent ID WO2017189652
Title Isoxazole Derivatives As Fxr Agonists and Methods of Use Thereof.
Abstract The present invention provides compounds of Formula I: pharmaceutical compositions comprising these compounds and methods of using these compounds to treat or prevent a disease or disorder mediated as FXR modulators. Specifically, the present invention relates to isoxazole derivatives useful as agonists for FXR, and methods for their preparation and use.
Applicant(s) Enanta Pharmaceuticals, Inc
Representative Drug(s) D02OJH Drug Info N.A. [1]
Patent ID WO2017156024
Title 3-Desoxy Derivative and Pharmaceutical Compositions Thereof.
Abstract The present application provides Compound 1 : or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.
Applicant(s) Intercept Pharmaceuticals, Inc
Patent ID WO2017049177
Title Farnesoid X Receptor Agonists and Uses Thereof.
Abstract Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Applicant(s) Metacrine, Inc
Representative Drug(s) D0RL3M Drug Info N.A. [1]
Patent ID WO2017049176
Title Farnesoid X Receptor Agonists and Uses Thereof.
Abstract Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Applicant(s) Metacrine, Inc
Patent ID WO2017049173
Title Farnesoid X Receptor Agonists and Uses Thereof.
Abstract Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Applicant(s) Metacrine, Inc
Representative Drug(s) D0F5MF Drug Info N.A. [1]
Patent ID WO2017049172
Title Farnesoid X Receptor Agonists and Uses Thereof.
Abstract Described herein are compounds that are farnesoid X receptor agonists, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders associated with farnesoid X receptor activity.
Applicant(s) Metacrine, Inc
Patent ID WO2016161003
Title Bile Acid Derivatives As Fxr/Tgr5 Agonists and Methods of Use Thereof.
Abstract The present invention provides compounds represented by Formula I, or pharmaceutically acceptable salts, stereoisomers, solvates, hydrates or combination thereof, (I). The invention also provides pharmaceutical compositions comprising these compounds and methods of using this compounds for treating FXR-mediated or TGR5-mediated diseases or conditions.
Applicant(s) Enanta Pharmaceuticals, Inc
Representative Drug(s) D01QNX Drug Info N.A. [1]
Patent ID WO2016151403
Title Fused Bicyclic Compounds for The Treatment of Disease.
Abstract Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
Applicant(s) Akarna Therapeutics, Ltd
Representative Drug(s) D0K3UO Drug Info N.A. [1]
Patent ID WO2016081918
Title Fused Bicyclic Compounds for The Treatment of Disease.
Abstract Described herein are fused bicyclic compounds, compositions, and methods for their use for the treatment of disease.
Applicant(s) Akarna Therapeutics, Ltd
Patent ID WO2014184271
Title 11-Hydroxyl-Derivatives of Bile Acids and Amino Acid Conjugates Thereof As Farnesoid X Receptor Modulators.
Abstract The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, solvate, or amino acid conjugate thereof, wherein R1 is a hydroxy group and 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.
Applicant(s) Intercept Pharmaceuticals, Inc
Representative Drug(s) D0AA3P Drug Info N.A. [1]
Patent ID WO2000037077
Title Assays for Ligands for Nuclear Receptors.
Abstract The present invention includes nuclear receptor heterodimer and nuclear receptor-coactivator peptide assays for identifying ligands for nuclear receptors, utilizing scintillation proximity and fluorescence resonance energy transfer (FRET), and methods of using identified ligands.
Applicant(s) Glaxo Group Limited
United States Patent and Trademark Office (USPTO)
Patent ID US20160376279
Title Fxr Agonists and Methods for Making and Using.
Representative Drug(s) D04QBY Drug Info N.A. Click to Show More [1]
2 D07EDS Drug Info N.A. [1]
3 D08MYA Drug Info N.A. [1]
4 D0OM2M Drug Info N.A. [1]
Patent ID US20080299118
Title Fxr Agonists for The Treatment of Malignancies.
Representative Drug(s) D03DZQ Drug Info EC50 = 4 nM [2]
Patent ID US20090137554
Title 1,4,5,6-Tetrahydro-Pyrrolo[2,3-D]Azepines and Imidazo[4,5-D]Azepines As Modulators of Nuclear Receptor Activity.
Representative Drug(s) D09FOM Drug Info N.A. [2]
References  Top
REF 1 Farnesoid X receptor modulators 2014-present: a patent review.Expert Opin Ther Pat. 2018 May;28(5):351-364.
REF 2 FXR modulators for enterohepatic and metabolic diseases.Expert Opin Ther Pat. 2018 Nov;28(11):765-782.

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