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AR105555A1 - Métodos para preparar ácidos biliares y derivados de los mismos - Google Patents

Métodos para preparar ácidos biliares y derivados de los mismos

Info

Publication number
AR105555A1
AR105555A1 ARP160102334A ARP160102334A AR105555A1 AR 105555 A1 AR105555 A1 AR 105555A1 AR P160102334 A ARP160102334 A AR P160102334A AR P160102334 A ARP160102334 A AR P160102334A AR 105555 A1 AR105555 A1 AR 105555A1
Authority
AR
Argentina
Prior art keywords
formula
compound
derivatives
prepare
convert
Prior art date
Application number
ARP160102334A
Other languages
English (en)
Inventor
Gioiello Antimo
Pellicciari Roberto
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 AR105555A1 publication Critical patent/AR105555A1/es

Links

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J1/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0003—Androstane derivatives
    • C07J1/0011—Androstane derivatives substituted in position 17 by a keto group
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/005—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 16 (17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J13/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007—Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17 with double bond in position 17 (20)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0005—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring the nitrogen atom being directly linked to the cyclopenta(a)hydro phenanthrene skeleton
    • 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
    • C07J41/005—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 only two carbon atoms, e.g. pregnane derivatives
    • 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
    • C07J7/0025—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 substituted in position 16
    • C07J7/0035—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 substituted in position 16 by a hydroxy group free esterified or etherified
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Obesity (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicación 1: Un método para preparar un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable, solvato, o aminoácido conjugado del mismo, donde R¹ es H, a-OH, b-OH, o un grupo oxo, que comprende los pasos de: (i) convertir el compuesto de fórmula (2) en el compuesto de fórmula (3); (ii) oxidar selectivamente el compuesto de fórmula (3) para proporcionar el compuesto de fórmula (4); (iii) convertir el compuesto de fórmula (4) en el compuesto de fórmula (5); (iv) convertir el compuesto de fórmula (5) en oxima de fórmula (6); (v) convertir la oxima de fórmula (6) en el compuesto de fórmula (7); (vi) convertir el compuesto de fórmula (7) en cetona de fórmula (9); (vii) desproteger la cetona de fórmula (8) para formar cetona de fórmula (9); (viii) olefinar el compuesto de fórmula (9) para proporcionar el compuesto de fórmula (10); (ix) alquilar la olefina de fórmula (10) regioselectivamente y estereoselectivamente para proporcionar el compuesto de fórmula (11), donde P¹ es un grupo protector o H; (x) convertir el compuesto de fórmula (11) para proporcionar el compuesto de fórmula (12), donde P² es un grupo protector; (xi) regioselectivamente y estereoselectivamente reducir el compuesto de fórmula (12) para proporcionar el compuesto de fórmula (13); y (xii) desproteger y selectivamente reducir el compuesto de fórmula (13) para proporcionar el compuesto de la fórmula (1).
ARP160102334A 2015-07-30 2016-08-01 Métodos para preparar ácidos biliares y derivados de los mismos AR105555A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201562198733P 2015-07-30 2015-07-30

Publications (1)

Publication Number Publication Date
AR105555A1 true AR105555A1 (es) 2017-10-18

Family

ID=57885146

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP160102334A AR105555A1 (es) 2015-07-30 2016-08-01 Métodos para preparar ácidos biliares y derivados de los mismos

Country Status (15)

Country Link
US (1) US10414791B2 (es)
EP (1) EP3328817A4 (es)
JP (1) JP6830096B2 (es)
KR (1) KR20180030204A (es)
CN (1) CN108025994A (es)
AR (1) AR105555A1 (es)
AU (1) AU2016297821B2 (es)
BR (1) BR112018001869A2 (es)
CA (1) CA2993540A1 (es)
IL (1) IL256971A (es)
MA (1) MA43066A (es)
MX (1) MX2018001145A (es)
NZ (1) NZ739219A (es)
TW (1) TW201710280A (es)
WO (1) WO2017019524A1 (es)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3305799A3 (en) * 2016-10-07 2018-06-20 Lupin Limited Salts of obeticholic acid
JP6987967B2 (ja) * 2017-04-20 2022-01-05 デーウン・バイオ・インコーポレイテッド 連続フロー反応を利用した胆汁酸誘導体の製造方法
CN107200763B (zh) * 2017-06-01 2019-05-03 江苏佳尔科药业集团有限公司 一种以鹅去氧胆酸为原料合成石胆酸的方法
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
CN111072744B (zh) * 2019-12-03 2021-09-14 江苏佳尔科药业集团股份有限公司 一种以ba为原料合成熊去氧胆酸的方法
EP4200311A4 (en) * 2020-08-21 2024-11-20 Sandhill One, LLC Methods of making cholic acid derivatives and starting materials therefor
CN112220792A (zh) * 2020-09-30 2021-01-15 浙江大学 石胆酸用于制备缓解肝纤维化的药物中的应用
EP4423105A2 (en) * 2021-11-02 2024-09-04 Sandhill One, LLC High purity non-animal derived udca
EP4423106A2 (en) * 2021-11-02 2024-09-04 Sandhill One, LLC High purity non-animal derived tudca
CN114276397A (zh) * 2021-12-28 2022-04-05 湖北武当安泰药业有限公司 醋酸去氢表雄酮的制备方法
EP4499107A1 (en) 2022-03-31 2025-02-05 NZP UK Limited 7-ketolithocholic acid for use in the treatment of gut dysbiosis and as a prebiotic

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4360470A (en) 1980-10-22 1982-11-23 Hoffmann-La Roche Inc. Process and intermediates for the synthesis of Vitamin D3 metabolites and chenodeoxycholic acid
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
WO2008130449A2 (en) 2006-11-20 2008-10-30 Satori Pharmaceuticals, Inc. Modulators of amyloid-beta production
US20080318870A1 (en) 2007-06-19 2008-12-25 Kythera Biopharmaceuticals, Inc. Synthetic bile acid compositions and methods
KR101598402B1 (ko) * 2007-06-19 2016-03-03 키쎄라 바이오파마슈티컬즈 인코포레이티드 합성 담즙산 조성물, 방법 및 제조물
US20130261317A1 (en) * 2010-09-27 2013-10-03 Kythera Biopharmaceuticals, Inc. Methods for preparing synthetic bile acids and compositions comprising the same
CN107936076B (zh) * 2011-09-08 2021-10-15 萨奇治疗股份有限公司 神经活性类固醇、组合物、及其用途
CN102746356B (zh) * 2012-07-17 2014-03-05 湖北芳通药业股份有限公司 均相法生产醋酸去氢表雄酮的工艺方法
JP2016514967A (ja) 2013-03-13 2016-05-26 セージ セラピューティクス， インコーポレイテッド 神経刺激性ステロイド、組成物およびそれらの使用
CN103145784B (zh) 2013-03-25 2015-03-11 浙江仙琚制药股份有限公司 醋酸去氢表雄酮的制备方法
CN104045676A (zh) * 2013-12-13 2014-09-17 成都丽璟科技有限公司 一种生产双烯醇酮醋酸酯的方法

Also Published As

Publication number Publication date
AU2016297821A1 (en) 2018-02-15
AU2016297821B2 (en) 2020-03-12
MX2018001145A (es) 2018-06-15
EP3328817A4 (en) 2019-04-03
BR112018001869A2 (pt) 2018-09-18
KR20180030204A (ko) 2018-03-21
WO2017019524A1 (en) 2017-02-02
MA43066A (fr) 2018-06-06
JP2018523654A (ja) 2018-08-23
CN108025994A (zh) 2018-05-11
IL256971A (en) 2018-03-29
CA2993540A1 (en) 2017-02-02
EP3328817A1 (en) 2018-06-06
US10414791B2 (en) 2019-09-17
US20190010184A1 (en) 2019-01-10
NZ739219A (en) 2019-03-29
TW201710280A (zh) 2017-03-16
JP6830096B2 (ja) 2021-02-17

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