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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
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/EP2003/007512
Other languages
French (fr)
Other versions
WO2004007521A2 (en
Inventor
Roberto Pellicciari
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
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 Individual filed Critical Individual
Priority to AU2003250935A priority Critical patent/AU2003250935A1/en
Publication of WO2004007521A2 publication Critical patent/WO2004007521A2/en
Publication of WO2004007521A3 publication Critical patent/WO2004007521A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Obesity (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)

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 Ceased 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
ITMI2002A001532 2002-07-12
IT2002MI001532A ITMI20021532A1 (en) 2002-07-12 2002-07-12 CHEMICAL COMPOUNDS

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 Ceased 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
US7138390B2 (en) 2001-03-12 2006-11-21 Intercept Pharmaceuticals 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
PT1734970E (en) 2004-03-12 2015-03-11 Intercept Pharmaceuticals Inc Treatment of fibrosis using fxr ligands
US7618956B2 (en) 2005-05-31 2009-11-17 The Gillette Company Reduction of hair growth
CA2928178C (en) 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. 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
EA020310B1 (en) 2008-07-30 2014-10-30 Интерсепт Фармасьютикалз, Инк. Tgr5 modulators and use thereof
AU2009316566B9 (en) 2008-11-19 2014-05-15 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
ES2822375T3 (en) 2012-06-19 2021-04-30 Intercept Pharmaceuticals Inc Preparation of the non-crystalline form of obeticholic acid
HRP20180931T1 (en) * 2013-05-14 2018-10-05 Intercept Pharmaceuticals, Inc. 11-HYDROXYL-6-SUBSTITUTED-Bile ACID DERIVATIVES AND THEIR AMINO ACID CONJUGATES AS FARNEZOID RECEPTOR MODULATORS X
LT3043865T (en) 2013-09-11 2021-04-26 Institut National De La Santé Et De La Recherche Médicale (Inserm) 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
CA3051776A1 (en) 2017-02-21 2018-08-30 Genfit Combination of a ppar and fxr agonist for the treatment of liver disorders
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
US11111265B2 (en) * 2017-11-02 2021-09-07 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Method for preparing cholic acid compound
WO2021009332A1 (en) 2019-07-18 2021-01-21 Enyo Pharma Method for decreasing adverse-effects of interferon
CA3159163A1 (en) 2020-01-15 2021-07-22 Raphael Darteil Use of fxr agonists for treating an infection by hepatitis d virus
CA3204800A1 (en) 2021-01-14 2022-07-21 Raphael Darteil Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
US20240216364A1 (en) 2021-04-28 2024-07-04 Enyo Pharma 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
AU2003250935A1 (en) 2004-02-02
ITMI20021532A1 (en) 2004-01-12
AU2003250935A8 (en) 2004-02-02
WO2004007521A2 (en) 2004-01-22

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