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)

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 (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3660030A4 (en) * 2017-07-26 2021-04-21 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. METHOD OF MANUFACTURING STEROID-DERIVATIVE FXR AGONISTS
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
BR112022006546A2 (pt) 2019-10-07 2022-08-30 Kallyope Inc Agonistas de gpr119
BR112022023359A2 (pt) 2020-05-19 2023-04-18 Kallyope Inc Ativadores de ampk
EP4172162A1 (en) 2020-06-26 2023-05-03 Kallyope, Inc. Ampk activators
JP2023539828A (ja) 2020-08-21 2023-09-20 サンドヒル ワン，エルエルシー コール酸誘導体およびそのための出発物質を製造する方法
WO2023081657A2 (en) 2021-11-02 2023-05-11 Sandhill One, Llc High purity non-animal derived udca
WO2023081658A2 (en) 2021-11-02 2023-05-11 Sandhill One, Llc High purity non-animal derived tudca
WO2023081166A1 (en) 2021-11-02 2023-05-11 Sandhill One, Llc Stereoselective steroidal reductions

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4021327B2 (ja) * 2001-03-12 2007-12-12 インターセプト ファーマスーティカル インコーポレイテッド Ｆｘｒに対する作用薬としてのステロイド
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
CN104203293A (zh) 2012-02-07 2014-12-10 加利福尼亚大学董事会 具有经钽涂覆的纳米结构的制造产品及其制备与使用方法
CN104781272A (zh) 2012-06-19 2015-07-15 英特塞普特医药品公司 奥贝胆酸的制备、用途和固体形式
MX361653B (es) * 2012-10-26 2018-12-13 Intercept Pharmaceuticals Inc Procedimiento para la preparación de derivados del ácido biliar.
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
CA3004275A1 (en) 2017-05-11
EP3370728A4 (en) 2019-07-10
TW201720839A (zh) 2017-06-16
JP2018532800A (ja) 2018-11-08
AU2016350690B2 (en) 2019-12-12
JP6749406B2 (ja) 2020-09-02
HK1254055A1 (zh) 2019-07-12
CN108348533A (zh) 2018-07-31
WO2017079062A1 (en) 2017-05-11
KR20180067699A (ko) 2018-06-20
US20190062367A1 (en) 2019-02-28
MX2018005520A (es) 2018-08-01
AU2016350690A1 (en) 2018-05-10
AU2016350690C1 (en) 2020-04-23
IL258922A (en) 2018-06-28
EP3370728A1 (en) 2018-09-12
BR112018008936A2 (pt) 2018-11-27
US10604545B2 (en) 2020-03-31

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