WO2004007521A3 - Bile acid derivatives as agonists of the farnesoid x receptor - Google Patents

Bile acid derivatives as agonists of the farnesoid x receptor Download PDF

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Publication number
WO2004007521A3
WO2004007521A3 PCT/EP2003/007512 EP0307512W WO2004007521A3 WO 2004007521 A3 WO2004007521 A3 WO 2004007521A3 EP 0307512 W EP0307512 W EP 0307512W WO 2004007521 A3 WO2004007521 A3 WO 2004007521A3
Authority
WO
WIPO (PCT)
Prior art keywords
agonists
farnesoid
receptor
acid derivatives
bile acid
Prior art date
Application number
PCT/EP2003/007512
Other languages
French (fr)
Other versions
WO2004007521A2 (en
Inventor
Roberto Pellicciari
Original Assignee
Roberto Pellicciari
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Roberto Pellicciari filed Critical Roberto Pellicciari
Priority to AU2003250935A priority Critical patent/AU2003250935A1/en
Publication of WO2004007521A2 publication Critical patent/WO2004007521A2/en
Publication of WO2004007521A3 publication Critical patent/WO2004007521A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J9/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane
    • C07J9/005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of more than two carbon atoms, e.g. cholane, cholestane, coprostane containing a carboxylic function directly attached or attached by a chain containing only carbon atoms to the cyclopenta[a]hydrophenanthrene skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics

Abstract

The invention relates to compounds of formula (I), wherein R is ethyl, propyl or allyl, and to salts, solvates and pharmaceutically acceptable amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
PCT/EP2003/007512 2002-07-12 2003-07-11 Bile acid derivatives as agonists of the farnesoid x receptor WO2004007521A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2003250935A AU2003250935A1 (en) 2002-07-12 2003-07-11 Bile acid derivatives as agonists of the farnesoid x receptor

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IT2002MI001532A ITMI20021532A1 (en) 2002-07-12 2002-07-12 CHEMICAL COMPOUNDS
ITMI2002A001532 2002-07-12

Publications (2)

Publication Number Publication Date
WO2004007521A2 WO2004007521A2 (en) 2004-01-22
WO2004007521A3 true WO2004007521A3 (en) 2004-04-01

Family

ID=30012506

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2003/007512 WO2004007521A2 (en) 2002-07-12 2003-07-11 Bile acid derivatives as agonists of the farnesoid x receptor

Country Status (3)

Country Link
AU (1) AU2003250935A1 (en)
IT (1) ITMI20021532A1 (en)
WO (1) WO2004007521A2 (en)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1392714B1 (en) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroids as agonists for fxr
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
EP2712617B2 (en) 2004-03-12 2020-11-18 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using Fxr ligands
US7618956B2 (en) 2005-05-31 2009-11-17 The Gillette Company Reduction of hair growth
JP5292310B2 (en) 2007-01-19 2013-09-18 インターセプト ファーマシューティカルズ， インコーポレイテッド 23-substituted bile acids as TGR5 modulators and methods of use thereof
US8338628B2 (en) * 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
WO2010014836A2 (en) 2008-07-30 2010-02-04 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
MX2011005295A (en) 2008-11-19 2011-06-24 Intercept Pharmaceuticals Inc Tgr5 modulators and method of use thereof.
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
SG11201408501UA (en) 2012-06-19 2015-01-29 Intercept Pharmaceuticals Inc Preparation, uses and solid forms of obeticholic acid
DK3848038T3 (en) * 2013-05-14 2023-02-06 Intercept Pharmaceuticals Inc 11-Hydroxyl-6-substituted derivatives of bile acids and their amino acid conjugates as farnesoid X receptor modulates.
RS61540B1 (en) 2013-09-11 2021-04-29 Inst Nat Sante Rech Med Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection
CN104672290B (en) * 2015-01-05 2017-06-06 北京普禄德医药科技有限公司 A kind of medicine of disease for preventing or treating FXR mediations and its production and use
MX2019009908A (en) 2017-02-21 2019-10-14 Genfit Combination of a ppar agonist with a fxr agonist.
EP3600293A1 (en) 2017-03-30 2020-02-05 Institut National de la Sante et de la Recherche Medicale (INSERM) Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses
WO2019085963A1 (en) * 2017-11-02 2019-05-09 正大天晴药业集团股份有限公司 Method for preparing cholic acid compound
AU2020312735A1 (en) 2019-07-18 2021-12-16 Enyo Pharma Method for decreasing adverse-effects of interferon
IL293892A (en) 2020-01-15 2022-08-01 Inserm Institut National De La Sant? Et De La Rech M?Dicale Use of fxr agonists for treating an infection by hepatitis d virus
AU2022209084A1 (en) 2021-01-14 2023-08-10 Centre Leon Bérard Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CA3213217A1 (en) 2021-04-28 2022-11-03 Raphael Darteil Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0312867A1 (en) * 1987-10-20 1989-04-26 GIULIANI S.p.A. Billiary acid derivatives, processes for the preparation thereof and phamaceutical compositions containing them
EP0393493A2 (en) * 1989-04-17 1990-10-24 GIULIANI S.p.A. Fluorinated bile acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
WO2002072598A1 (en) * 2001-03-12 2002-09-19 Roberto Pellicciari Steroids as agonists for fxr

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0312867A1 (en) * 1987-10-20 1989-04-26 GIULIANI S.p.A. Billiary acid derivatives, processes for the preparation thereof and phamaceutical compositions containing them
EP0393493A2 (en) * 1989-04-17 1990-10-24 GIULIANI S.p.A. Fluorinated bile acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
WO2002072598A1 (en) * 2001-03-12 2002-09-19 Roberto Pellicciari Steroids as agonists for fxr

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PARKS D J ET AL: "BILE ACIDS: NATURAL LIGANDS FOR AN ORPHAN NUCLEAR RECEPTOR", SCIENCE, AMERICAN ASSOCIATION FOR THE ADVANCEMENT OF SCIENCE, NEW YORK, US, vol. 284, May 1999 (1999-05-01), pages 1365 - 1368, XP000892009, ISSN: 0036-8075 *

Also Published As

Publication number Publication date
WO2004007521A2 (en) 2004-01-22
AU2003250935A8 (en) 2004-02-02
ITMI20021532A1 (en) 2004-01-12
AU2003250935A1 (en) 2004-02-02

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