WO2016168553A8 - Deuterated obeticholic acid - Google Patents

Deuterated obeticholic acid Download PDF

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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
Application number
PCT/US2016/027688
Other languages
French (fr)
Other versions
WO2016168553A1 (en
Inventor
I. Robert Silverman
Roger D. Tung
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

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

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 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 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
MX2020000873A (en) 2017-07-24 2020-07-22 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
MX2022000742A (en) 2019-07-18 2022-02-14 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
US20240100125A1 (en) 2021-01-14 2024-03-28 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

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2822375T3 (en) * 2012-06-19 2021-04-30 Intercept Pharmaceuticals Inc Preparation of the non-crystalline form of obeticholic acid
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
DK2997035T3 (en) * 2013-05-14 2018-07-02 Intercept Pharmaceuticals Inc 11-HYDROXY-6-SUBSTITUTED BALIC ACID DERIVATIVES AND AMINO ACID CONJUGATES THEREOF AS FARNESOID X RECEPTOR MODULATORS
WO2015061421A1 (en) * 2013-10-22 2015-04-30 Metselex, Inc. Deuterated bile acids

Also Published As

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

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