EA201791511A1 - Способы синтеза и очистки дезоксихолевой кислоты - Google Patents

Способы синтеза и очистки дезоксихолевой кислоты

Info

Publication number
EA201791511A1
EA201791511A1 EA201791511A EA201791511A EA201791511A1 EA 201791511 A1 EA201791511 A1 EA 201791511A1 EA 201791511 A EA201791511 A EA 201791511A EA 201791511 A EA201791511 A EA 201791511A EA 201791511 A1 EA201791511 A1 EA 201791511A1
Authority
EA
Eurasian Patent Office
Prior art keywords
methods
synthesis
acid
dezoxyleic
cleaning
Prior art date
Application number
EA201791511A
Other languages
English (en)
Other versions
EA035380B1 (ru
Inventor
Роберт М. Мориарти
Джон Грегори Рейд
мл. Рой А. Сваринген
Original Assignee
Китера Биофармасьютикалз, Инк.
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 Китера Биофармасьютикалз, Инк. filed Critical Китера Биофармасьютикалз, Инк.
Publication of EA201791511A1 publication Critical patent/EA201791511A1/ru
Publication of EA035380B1 publication Critical patent/EA035380B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • 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
    • 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
    • C07J21/00—Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005—Ketals
    • C07J21/008—Ketals at position 17
    • 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
    • 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
    • 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
    • C07J5/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond
    • C07J5/0046—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa
    • C07J5/0053—Normal steroids containing carbon, hydrogen, halogen or oxygen, substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane and substituted in position 21 by only one singly bound oxygen atom, i.e. only one oxygen bound to position 21 by a single bond substituted in position 17 alfa not substituted in position 16
    • 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)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Engineering & Computer Science (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Steroid Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

В настоящем изобретении предложены способы синтеза для получения дезоксихолевой кислоты и промежуточных соединений, синтетическая дезоксихолевая кислота высокой чистоты, композиции и способы применения. Также предложены способы синтеза 12-кето или 12-α-гидроксистероидов из Δ-9,11-ен, 11-кето или 11-гидрокси-β-стероидов. Настоящее изобретение также относится к новым соединениям, полученным в ходе синтеза. Настоящее изобретение также относится к синтезу дезоксихолевой кислоты, начиная с гидрокортизона.
EA201791511A 2009-12-18 2010-12-17 Способ и композиция для уменьшения подкожных жировых отложений EA035380B1 (ru)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US28813209P 2009-12-18 2009-12-18
US30200710P 2010-02-05 2010-02-05
US30381610P 2010-02-12 2010-02-12
GB1008726A GB2480632A (en) 2010-05-25 2010-05-25 Preparation of 12-keto and 12-alpha-hydroxy steroids
US34868610P 2010-05-26 2010-05-26

Publications (2)

Publication Number Publication Date
EA201791511A1 true EA201791511A1 (ru) 2018-03-30
EA035380B1 EA035380B1 (ru) 2020-06-04

Family

ID=42341289

Family Applications (2)

Application Number Title Priority Date Filing Date
EA201290334A EA031768B1 (ru) 2009-12-18 2010-12-17 Способы синтеза промежуточных соединений для применения в синтезе дезоксихолевой кислоты
EA201791511A EA035380B1 (ru) 2009-12-18 2010-12-17 Способ и композиция для уменьшения подкожных жировых отложений

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EA201290334A EA031768B1 (ru) 2009-12-18 2010-12-17 Способы синтеза промежуточных соединений для применения в синтезе дезоксихолевой кислоты

Country Status (16)

Country Link
US (5) US20130137884A1 (ru)
EP (2) EP2513132B9 (ru)
JP (2) JP6393023B2 (ru)
KR (3) KR102058420B1 (ru)
CN (3) CN106955287A (ru)
AU (1) AU2010330760B2 (ru)
CA (1) CA2782478A1 (ru)
EA (2) EA031768B1 (ru)
ES (1) ES2575559T3 (ru)
GB (1) GB2480632A (ru)
IL (2) IL220225A0 (ru)
MY (1) MY167891A (ru)
NZ (1) NZ700195A (ru)
SG (3) SG181768A1 (ru)
WO (1) WO2011075701A2 (ru)
ZA (1) ZA201204388B (ru)

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CN114478676B (zh) * 2022-02-18 2024-05-10 国药集团化学试剂有限公司 一种脱氧胆酸钠的制备方法

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Also Published As

Publication number Publication date
KR101862599B1 (ko) 2018-05-31
JP2013515006A (ja) 2013-05-02
US20190135855A1 (en) 2019-05-09
CA2782478A1 (en) 2011-06-23
GB201008726D0 (en) 2010-07-07
SG10201509046TA (en) 2015-12-30
EP2513132B1 (en) 2016-03-09
GB2480632A (en) 2011-11-30
EA031768B1 (ru) 2019-02-28
SG181768A1 (en) 2012-07-30
JP6568025B2 (ja) 2019-08-28
KR20120107982A (ko) 2012-10-04
US20170320905A1 (en) 2017-11-09
US20130137884A1 (en) 2013-05-30
IL261526A (en) 2018-10-31
ES2575559T3 (es) 2016-06-29
SG10201803507YA (en) 2018-05-30
US10472384B2 (en) 2019-11-12
JP6393023B2 (ja) 2018-09-19
US20200095274A1 (en) 2020-03-26
EA035380B1 (ru) 2020-06-04
US20150141679A1 (en) 2015-05-21
CN106955287A (zh) 2017-07-18
CN102812035A (zh) 2012-12-05
EP2513132B9 (en) 2017-12-27
MY167891A (en) 2018-09-26
AU2010330760B2 (en) 2015-01-22
EP2513132A2 (en) 2012-10-24
IL220225A0 (en) 2012-07-31
EA201290334A1 (ru) 2013-06-28
ZA201204388B (en) 2013-07-31
KR101787719B1 (ko) 2017-10-18
AU2010330760A1 (en) 2012-06-21
JP2016193948A (ja) 2016-11-17
KR102058420B1 (ko) 2019-12-24
CN107011401A (zh) 2017-08-04
WO2011075701A2 (en) 2011-06-23
WO2011075701A4 (en) 2012-09-13
KR20170049635A (ko) 2017-05-10
US9683007B2 (en) 2017-06-20
US10005813B2 (en) 2018-06-26
US10981946B2 (en) 2021-04-20
KR20180059568A (ko) 2018-06-04
WO2011075701A3 (en) 2012-07-26
NZ700195A (en) 2016-03-31
EP3040342A1 (en) 2016-07-06

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