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) |
D0YK9Q |
Drug Info
|
EC50 = 8 nM |
Click to Show More |
[1] |
2
|
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 |
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[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] |
5
|
D0ZG3D
|
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] |
5
|
D0ZG3D
|
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] |
5
|
D0ZG3D
|
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 |
Representative Drug(s) |
D0Y3NZ |
Drug Info
|
EC50 = nM range |
[1] |
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 |
Representative Drug(s) |
D0Y0LI |
Drug Info
|
EC50 < 1000 nM |
[1] |
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 |
Representative Drug(s) |
D0WT7M |
Drug Info
|
N.A. |
[1] |
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 |
Representative Drug(s) |
D0WA9U |
Drug Info
|
N.A. |
[1] |
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 |
Representative Drug(s) |
D0Z0FP |
Drug Info
|
N.A. |
[1] |
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 |
Representative Drug(s) |
D0UW8Q |
Drug Info
|
N.A. |
[1] |
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 |
Representative Drug(s) |
D0WT7M |
Drug Info
|
N.A. |
[1] |
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] |
5
|
D0ZG3D
|
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] |