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WO2016168553A8 - Deuterated obeticholic acid - Google Patents

Deuterated obeticholic acid Download PDF

Info

Publication number
WO2016168553A8
WO2016168553A8 PCT/US2016/027688 US2016027688W WO2016168553A8 WO 2016168553 A8 WO2016168553 A8 WO 2016168553A8 US 2016027688 W US2016027688 W US 2016027688W WO 2016168553 A8 WO2016168553 A8 WO 2016168553A8
Authority
WO
WIPO (PCT)
Prior art keywords
obeticholic acid
deuterated
deuterated obeticholic
compositions
farnesoid
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/US2016/027688
Other languages
French (fr)
Other versions
WO2016168553A1 (en
Inventor
I. Robert Silverman
Roger D. Tung
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.)
Concert Pharmaceuticals Inc
Original Assignee
Concert Pharmaceuticals Inc
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 Concert Pharmaceuticals Inc filed Critical Concert Pharmaceuticals Inc
Publication of WO2016168553A1 publication Critical patent/WO2016168553A1/en
Publication of WO2016168553A8 publication Critical patent/WO2016168553A8/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/001—Acyclic or carbocyclic compounds
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J7/00—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms
    • C07J7/0005—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21
    • C07J7/001—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group
    • C07J7/0015—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa
    • C07J7/002—Normal steroids containing carbon, hydrogen, halogen or oxygen substituted in position 17 beta by a chain of two carbon atoms not substituted in position 21 substituted in position 20 by a keto group not substituted in position 17 alfa not substituted in position 16

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

This invention relates to deuterated forms of obeticholic acid, and pharmaceutically acceptable salts thereof. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering an agonist of the farnesoid X receptor (FXR).
PCT/US2016/027688 2015-04-17 2016-04-15 Deuterated obeticholic acid Ceased WO2016168553A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562148900P 2015-04-17 2015-04-17
US62/148,900 2015-04-17

Publications (2)

Publication Number Publication Date
WO2016168553A1 WO2016168553A1 (en) 2016-10-20
WO2016168553A8 true WO2016168553A8 (en) 2016-11-24

Family

ID=57127023

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2016/027688 Ceased WO2016168553A1 (en) 2015-04-17 2016-04-15 Deuterated obeticholic acid

Country Status (1)

Country Link
WO (1) WO2016168553A1 (en)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106645497A (en) * 2017-01-03 2017-05-10 山东省药学科学院 Obeticholic acid and detection method for related substances in preparation of obeticholic acid
BR112020001362A2 (en) * 2017-07-24 2020-08-11 Intercept Pharmaceuticals, Inc. isotopically labeled bile acid derivatives
TW202021595A (en) 2018-08-10 2020-06-16 德商菲尼克斯製藥股份有限公司 Isolithocholic acid or isoallolithocholic acid and deuterated derivatives thereof for preventing and treating clostridium difficile-associated diseases
CA3139291A1 (en) 2019-07-18 2021-01-21 Jacky Vonderscher 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 to treat hepatitis d virus infection
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
WO2022229302A1 (en) 2021-04-28 2022-11-03 Enyo Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013192097A1 (en) * 2012-06-19 2013-12-27 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
CN105377870B (en) * 2013-05-14 2018-04-03 英特塞普特医药品公司 11‑Hydroxy derivatives of bile acids and their amino acid conjugates as farnesoid X receptor modulators
US20150112089A1 (en) * 2013-10-22 2015-04-23 Metselex, Inc. Deuterated bile acids

Also Published As

Publication number Publication date
WO2016168553A1 (en) 2016-10-20

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