JP2019515906A - オベチコール酸およびその誘導体の調製方法 - Google Patents

オベチコール酸およびその誘導体の調製方法 Download PDF

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Publication number
JP2019515906A
JP2019515906A JP2018554539A JP2018554539A JP2019515906A JP 2019515906 A JP2019515906 A JP 2019515906A JP 2018554539 A JP2018554539 A JP 2018554539A JP 2018554539 A JP2018554539 A JP 2018554539A JP 2019515906 A JP2019515906 A JP 2019515906A
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Prior art keywords
compound
reaction
present application
acid
form compound
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JP2018554539A
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Japanese (ja)
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JP2019515906A5 (OSRAM
Inventor
ベンヤミン リスト，
ベンヤミン リスト，
チャンドラ デ，
チャンドラ デ，
チンガン ワン，
チンガン ワン，
Original Assignee
インターセプト ファーマシューティカルズ， インコーポレイテッド
インターセプト ファーマシューティカルズ， インコーポレイテッド
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Publication of JP2019515906A publication Critical patent/JP2019515906A/ja
Publication of JP2019515906A5 publication Critical patent/JP2019515906A5/ja
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    • 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
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
JP2018554539A 2016-04-19 2017-04-18 オベチコール酸およびその誘導体の調製方法 Ceased JP2019515906A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662324405P 2016-04-19 2016-04-19
US62/324,405 2016-04-19
PCT/US2017/028130 WO2017184598A1 (en) 2016-04-19 2017-04-18 Methods for the preparation of obeticholic acid and derivatives thereof

Publications (2)

Publication Number Publication Date
JP2019515906A true JP2019515906A (ja) 2019-06-13
JP2019515906A5 JP2019515906A5 (OSRAM) 2020-05-28

Family

ID=60116337

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018554539A Ceased JP2019515906A (ja) 2016-04-19 2017-04-18 オベチコール酸およびその誘導体の調製方法

Country Status (14)

Country Link
US (1) US10550146B2 (OSRAM)
EP (1) EP3445370B1 (OSRAM)
JP (1) JP2019515906A (OSRAM)
KR (1) KR20180134405A (OSRAM)
CN (1) CN109069517A (OSRAM)
AR (1) AR108237A1 (OSRAM)
AU (1) AU2017254480A1 (OSRAM)
BR (1) BR112018071441A2 (OSRAM)
CA (1) CA3021322A1 (OSRAM)
ES (1) ES2907425T3 (OSRAM)
IL (1) IL262405A (OSRAM)
MX (1) MX374550B (OSRAM)
TW (1) TW201738254A (OSRAM)
WO (1) WO2017184598A1 (OSRAM)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108299539B (zh) * 2018-03-09 2021-07-06 中山百灵生物技术股份有限公司 利用连续流微反应器生产6-亚乙基鹅去氧胆酸的方法
CN110204587B (zh) * 2019-07-19 2020-05-12 中山百灵生物技术有限公司 一种奥贝胆酸的合成方法
CN113387992A (zh) * 2020-03-11 2021-09-14 成都倍特药业股份有限公司 奥贝胆酸杂质及其制备方法和检测方法
KR20230044603A (ko) 2021-09-27 2023-04-04 (주) 테라베스트 약물 이합체를 포함하는 나노입자 및 이의 용도

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005082925A2 (en) * 2004-02-26 2005-09-09 Intercept Pharmaceuticals Inc. Novel steroid agonist for fxr
JP2008540612A (ja) * 2005-05-19 2008-11-20 エレジーレ ソシエタ ペル アチオニ ３α（β）−７α（β）−ジヒドロキシ−６α（β）−アルキル−５β−コラン酸の調製方法
US20130345188A1 (en) * 2012-06-19 2013-12-26 Intercept Pharmaceuticals, Inc. Preparation and Uses of Obeticholic Acid
CN104672290A (zh) * 2015-01-05 2015-06-03 北京普禄德医药科技有限公司 一种用于预防或治疗fxr-介导的疾病的药物及其制备方法和用途

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US1895945A (en) * 1928-12-20 1933-01-31 Goodrich Co B F Method of making aldehyde-amines
DE60205891T2 (de) 2001-03-12 2006-06-22 Intercept Pharmaceuticals, Inc. Steroide als agonisten für fxr
CN108250264A (zh) * 2012-10-26 2018-07-06 英特塞普特医药品公司 制备胆汁酸衍生物的方法
CN106046095B (zh) 2016-06-06 2017-02-22 南京理工大学 奥贝胆酸的合成方法

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005082925A2 (en) * 2004-02-26 2005-09-09 Intercept Pharmaceuticals Inc. Novel steroid agonist for fxr
JP2008540612A (ja) * 2005-05-19 2008-11-20 エレジーレ ソシエタ ペル アチオニ ３α（β）−７α（β）−ジヒドロキシ−６α（β）−アルキル−５β−コラン酸の調製方法
US20130345188A1 (en) * 2012-06-19 2013-12-26 Intercept Pharmaceuticals, Inc. Preparation and Uses of Obeticholic Acid
JP2015521621A (ja) * 2012-06-19 2015-07-30 インターセプト ファーマシューティカルズ， インコーポレイテッド オベチコール酸の調製、使用および固体形態
CN104672290A (zh) * 2015-01-05 2015-06-03 北京普禄德医药科技有限公司 一种用于预防或治疗fxr-介导的疾病的药物及其制备方法和用途

Also Published As

Publication number Publication date
BR112018071441A2 (pt) 2019-02-05
AU2017254480A1 (en) 2018-11-15
US10550146B2 (en) 2020-02-04
AR108237A1 (es) 2018-08-01
IL262405A (en) 2018-12-31
ES2907425T3 (es) 2022-04-25
EP3445370B1 (en) 2021-12-01
CN109069517A (zh) 2018-12-21
WO2017184598A1 (en) 2017-10-26
MX2018012777A (es) 2019-01-28
EP3445370A1 (en) 2019-02-27
US20190211052A1 (en) 2019-07-11
MX374550B (es) 2025-03-06
CA3021322A1 (en) 2017-10-26
EP3445370A4 (en) 2019-12-25
KR20180134405A (ko) 2018-12-18
TW201738254A (zh) 2017-11-01

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