Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
Abstract: The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Abstract: Process for preparing 3?-7?(?)-dihydroxy-6?(?)-alkyl-5?-cholanic acid (I) in which R is a linear or branched C1-C5 alkyl and the relative intermediates 3?-hydroxy-6?-alkyl-7-keto-5?-cholanic (VIII) and 3?-hydroxy-6?-alkyl-7-keto-5?-cholanic (IX).
Abstract: The invention relates to compounds of Formula A: (A) or a salt, solvate, or hydrate thereof. The compounds of formula A are TGR5 modulators useful for the treatment of disease.
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.
Type:
Grant
Filed:
June 27, 2007
Date of Patent:
April 26, 2011
Assignee:
Intercept Pharmaceuticals, Inc.
Inventors:
Roberto Pellicciari, Stefano Fiorucci, Mark Pruzanski
Abstract: The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.
Type:
Grant
Filed:
May 4, 2009
Date of Patent:
December 28, 2010
Assignee:
Intercept Pharmaceuticals, Inc.
Inventors:
Roberto Pellicciari, Stefano Fiorucci, Mark Pruzanski
Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Abstract: The invention relates to compounds of Formula A: or a salt, solvate, hydrate, or prodrug thereof. The compounds of Formula A are TGR5 modulators useful for the treatment of various diseases, including metabolic disease, inflammatory disease, liver disease, autoimmune disease, cardiac disease, kidney disease, cancer, and gastrointestinal disease.
Abstract: The present invention relates to compounds of formula (I) wherein: R1 is hydrogen or an alkyl group; R2 is hydrogen or a halogen, nitro, alkyloxy, amino or carboxy group; Y is CH2, oxygen or sulfur; n is an integer from 1 to 4, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof for the treatment of FXR-mediated diseases or conditions.
Type:
Application
Filed:
May 4, 2009
Publication date:
March 11, 2010
Applicant:
Intercept Pharmaceuticals, Inc.
Inventors:
Roberto Pellicciari, Stefano Fiorucci, Mark Pruzanski
Abstract: The invention relates to compounds of formula (I): wherein R is ethyl and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
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.
Type:
Application
Filed:
June 27, 2007
Publication date:
July 31, 2008
Applicant:
Intercept Pharmaceuticals, Inc.
Inventors:
Roberto Pellicciari, Stefano Fiorucci, Mark Pruzanski
Abstract: The invention relates to compounds of formula (I): wherein R is ethyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
Abstract: The invention relates to the discovery that farnesoid X receptor (FXR) agonists can be used in combination with peroxisome proliferation activated receptor gamma (PPAR?) 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 PPAR?, dual PPAR?/? and pan PPAR?/?/? agonists in combination with FXR agonists.
Type:
Application
Filed:
October 13, 2005
Publication date:
November 9, 2006
Applicant:
Intercept Pharmaceuticals Inc.
Inventors:
Stefano Fiorucci, Roberto Pellicciari, Mark Pruzanski
Abstract: 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.
Type:
Application
Filed:
March 14, 2005
Publication date:
March 30, 2006
Applicant:
Intercept Pharmaceuticals, Inc.
Inventors:
Stefano Fiorucci, Roberto Pellicciari, Mark Pruzanski