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

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  • 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 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
ES2248581T3 (en) 2001-03-12 2006-03-16 Intercept Pharmaceuticals, Inc. STEROIDS AS FXR AGONISTS.
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
PT1734970E (en) 2004-03-12 2015-03-11 Intercept Pharmaceuticals Inc Treatment of fibrosis using fxr ligands
US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
US7618956B2 (en) 2005-05-31 2009-11-17 The Gillette Company Reduction of hair growth
CA2676417C (en) * 2007-01-19 2016-06-28 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
US8796249B2 (en) 2008-07-30 2014-08-05 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
ES2458168T3 (en) 2008-11-19 2014-04-30 Intercept Pharmaceuticals, Inc. TGR5 modulators and their method of use
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
DK3336097T3 (en) 2012-06-19 2020-09-28 Intercept Pharmaceuticals Inc Preparation of non-crystalline obeticholic acid
CA2912139C (en) * 2013-05-14 2021-04-20 Roberto Pellicciari 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
EA031003B1 (en) 2013-09-11 2018-10-31 Инсерм (Энститю Насьональ Де Ля Сантэ Э Де Ля Решерш Медикаль) Methods and pharmaceutical compositions for the treatment of hepatitis b virus infections
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
JP2020508316A (en) 2017-02-21 2020-03-19 ジェンフィＧｅｎｆｉｔ Combination of PPAR agonist and FXR agonist
WO2018178260A1 (en) 2017-03-30 2018-10-04 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses
EP3705487B1 (en) * 2017-11-02 2022-10-26 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Method for preparing cholic acid compound
KR20220035365A (en) 2019-07-18 2022-03-22 엔요 파마 How to reduce the side effects of interferon
WO2021144330A1 (en) 2020-01-15 2021-07-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
EP4277622A1 (en) 2021-01-14 2023-11-22 ENYO Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
TW202308629A (en) 2021-04-28 2023-03-01 法商Ｅｎｙｏ製藥公司 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
AU2003250935A8 (en) 2004-02-02
WO2004007521A2 (en) 2004-01-22
AU2003250935A1 (en) 2004-02-02
ITMI20021532A1 (en) 2004-01-12

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