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AR106587A1 - Métodos para preparar ácido obeticólico y derivados de este - Google Patents

Métodos para preparar ácido obeticólico y derivados de este

Info

Publication number
AR106587A1
AR106587A1 ARP160103362A ARP160103362A AR106587A1 AR 106587 A1 AR106587 A1 AR 106587A1 AR P160103362 A ARP160103362 A AR P160103362A AR P160103362 A ARP160103362 A AR P160103362A AR 106587 A1 AR106587 A1 AR 106587A1
Authority
AR
Argentina
Prior art keywords
formula
compound
solvate
convert
preparing
Prior art date
Application number
ARP160103362A
Other languages
English (en)
Inventor
M Gavin Gabriel
Original Assignee
Intercept 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 Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Publication of AR106587A1 publication Critical patent/AR106587A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
    • C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La presente solicitud se refiere a un método para preparar un derivado de ácido biliar, o una sal, solvato o conjugado de aminoácidos farmacéuticamente aceptable de este, que comprende la alquilación directa en la posición C-6 de KLCA. Reivindicación 1: Un método para preparar ácido obeticólico (OCA) de fórmula (1), o una sal, solvato, o conjugado de aminoácidos farmacéuticamente aceptable de este, que comprende la alquilación del átomo de carbono en la posición C-6 del Compuesto de fórmula (2) con un agente alquilante para formar el Compuesto de fórmula (3), donde PG es un grupo protector y la reducción del grupo ceto en la posición C-7 del Compuesto de fórmula (3) para formar OCA de fórmula (4). Reivindicación 24: El método de la reivindicación 1, que comprende además preparar 6a-etil-3a,7a-23-trihidroxi-24-nor-5b-colan-23-sulfato (Compuesto de fórmula (10)), o una sal, solvato, o conjugado de aminoácidos farmacéuticamente aceptable de este, que comprende: esterificar OCA de fórmula (4) para formar el Compuesto de fórmula (5), convertir el Compuesto de fórmula (5) para formar el Compuesto de fórmula (6), convertir el Compuesto de fórmula (6) para formar el Compuesto de fórmula (7), convertir el Compuesto de fórmula (7) para formar el Compuesto de fórmula (8), convertir el Compuesto de fórmula (8) para formar el Compuesto de fórmula (9), convertir el Compuesto de fórmula (9) para formar el Compuesto de fórmula (10).
ARP160103362A 2015-11-06 2016-11-04 Métodos para preparar ácido obeticólico y derivados de este AR106587A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562252077P 2015-11-06 2015-11-06

Publications (1)

Publication Number Publication Date
AR106587A1 true AR106587A1 (es) 2018-01-31

Family

ID=58662647

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160103362A AR106587A1 (es) 2015-11-06 2016-11-04 Métodos para preparar ácido obeticólico y derivados de este

Country Status (14)

Country Link
US (1) US10604545B2 (es)
EP (1) EP3370728A4 (es)
JP (1) JP6749406B2 (es)
KR (1) KR20180067699A (es)
CN (1) CN108348533A (es)
AR (1) AR106587A1 (es)
AU (1) AU2016350690C1 (es)
BR (1) BR112018008936A2 (es)
CA (1) CA3004275A1 (es)
HK (1) HK1254055A1 (es)
IL (1) IL258922A (es)
MX (1) MX2018005520A (es)
TW (1) TW201720839A (es)
WO (1) WO2017079062A1 (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2019020067A1 (zh) * 2017-07-26 2019-01-31 正大天晴药业集团股份有限公司 甾体类衍生物fxr激动剂的制备方法
CN107383139A (zh) * 2017-08-09 2017-11-24 杭州和泽医药科技有限公司 一种3α‑羟基‑7‑氧代‑5β‑胆烷酸新衍生物制备奥贝胆酸的方法
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
WO2021029656A1 (ko) * 2019-08-14 2021-02-18 주식회사 바이오톡스텍 하이드로퀴논 유도체, 및 오베티콜릭산을 포함하는 비알콜성 지방간염의 예방 또는 치료용 약학조성물
CN114945560B (zh) 2019-10-07 2024-08-13 卡尔优普公司 Gpr119激动剂
CN115667277A (zh) 2020-02-28 2023-01-31 卡尔优普公司 Gpr40激动剂
UY39222A (es) 2020-05-19 2021-11-30 Kallyope Inc Activadores de la ampk
CA3183575A1 (en) 2020-06-26 2021-12-30 Iyassu Sebhat Ampk activators
CA3190433A1 (en) * 2020-08-21 2022-02-24 Sandhill One, Llc Methods of making cholic acid derivatives and starting materials therefor
WO2023081658A2 (en) 2021-11-02 2023-05-11 Sandhill One, Llc High purity non-animal derived tudca
WO2023081657A2 (en) 2021-11-02 2023-05-11 Sandhill One, Llc High purity non-animal derived udca
CA3235454A1 (en) 2021-11-02 2023-05-11 Sandhill One, Llc Stereoselective steroidal reductions

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH06279488A (ja) * 1993-03-29 1994-10-04 Kuraray Co Ltd 新規なステロイド誘導体および骨粗鬆症治療剤
US7138390B2 (en) * 2001-03-12 2006-11-21 Intercept Pharmaceuticals Steroids as agonists for FXR
ITMI20050912A1 (it) 2005-05-19 2006-11-20 Erregierre Spa Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
US8338628B2 (en) * 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
US10149921B2 (en) 2012-02-07 2018-12-11 The Regents Of The University Of California Implants having tantalum coated nanostructures
SG11201408501UA (en) * 2012-06-19 2015-01-29 Intercept Pharmaceuticals Inc Preparation, uses and solid forms of obeticholic acid
AU2013334122B2 (en) * 2012-10-26 2017-11-02 Intercept Pharmaceuticals, Inc. Process for preparing bile acid derivatives
CN104876995B (zh) * 2014-02-27 2016-09-07 人福医药集团股份公司 鹅去氧胆酸衍生物的制备方法
CN104558086B (zh) * 2014-12-25 2016-10-05 康美（北京）药物研究院有限公司 一种5β-3α,7α-二羟基-6α-乙基-胆烷酸的制备方法

Also Published As

Publication number Publication date
MX2018005520A (es) 2018-08-01
US20190062367A1 (en) 2019-02-28
AU2016350690C1 (en) 2020-04-23
IL258922A (en) 2018-06-28
HK1254055A1 (zh) 2019-07-12
AU2016350690A1 (en) 2018-05-10
WO2017079062A1 (en) 2017-05-11
CA3004275A1 (en) 2017-05-11
EP3370728A4 (en) 2019-07-10
EP3370728A1 (en) 2018-09-12
TW201720839A (zh) 2017-06-16
CN108348533A (zh) 2018-07-31
BR112018008936A2 (pt) 2018-11-27
JP2018532800A (ja) 2018-11-08
KR20180067699A (ko) 2018-06-20
US10604545B2 (en) 2020-03-31
JP6749406B2 (ja) 2020-09-02
AU2016350690B2 (en) 2019-12-12

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