CN109069517A - 制备奥贝胆酸及其衍生物的方法 - Google Patents

制备奥贝胆酸及其衍生物的方法 Download PDF

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Publication number
CN109069517A
CN109069517A CN201780029699.6A CN201780029699A CN109069517A CN 109069517 A CN109069517 A CN 109069517A CN 201780029699 A CN201780029699 A CN 201780029699A CN 109069517 A CN109069517 A CN 109069517A
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CN
China
Prior art keywords
compound
oca
reaction
form compound
acid
Prior art date
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Pending
Application number
CN201780029699.6A
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English (en)
Chinese (zh)
Inventor
班杰明·利斯特
钱德拉·德
王青冈
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Ntercept Pharmaceuticals Inc
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Ntercept Pharmaceuticals Inc
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Application filed by Ntercept Pharmaceuticals Inc filed Critical Ntercept Pharmaceuticals Inc
Publication of CN109069517A publication Critical patent/CN109069517A/zh
Pending legal-status Critical Current

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    • 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
    • A61K31/565—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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201780029699.6A 2016-04-19 2017-04-18 制备奥贝胆酸及其衍生物的方法 Pending CN109069517A (zh)

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 (1)

Publication Number Publication Date
CN109069517A true CN109069517A (zh) 2018-12-21

Family

ID=60116337

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201780029699.6A Pending CN109069517A (zh) 2016-04-19 2017-04-18 制备奥贝胆酸及其衍生物的方法

Country Status (14)

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

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110204587A (zh) * 2019-07-19 2019-09-06 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

Families Citing this family (2)

* 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
KR20230044603A (ko) 2021-09-27 2023-04-04 (주) 테라베스트 약물 이합체를 포함하는 나노입자 및 이의 용도

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101203526A (zh) * 2005-05-19 2008-06-18 伊莱吉尔瑞公司 制备3α(β)-7α(β)-二羟基-6α(β)-烷基-5β-胆烷酸的方法
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
CN105102425A (zh) * 2012-10-26 2015-11-25 英特塞普特医药品公司 制备胆汁酸衍生物的方法

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US1895945A (en) * 1928-12-20 1933-01-31 Goodrich Co B F Method of making aldehyde-amines
ES2248581T3 (es) 2001-03-12 2006-03-16 Intercept Pharmaceuticals, Inc. Esteroides como agonistas de fxr.
EP1568706A1 (en) * 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
CN104672290B (zh) * 2015-01-05 2017-06-06 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
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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101203526A (zh) * 2005-05-19 2008-06-18 伊莱吉尔瑞公司 制备3α(β)-7α(β)-二羟基-6α(β)-烷基-5β-胆烷酸的方法
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
CN105102425A (zh) * 2012-10-26 2015-11-25 英特塞普特医药品公司 制备胆汁酸衍生物的方法

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
HISASHI YAMAMOTO: "New reaction and new catalyst-a personal perspective", 《TETRAHEDRON》 *
KAZUAKI ISHIHARA 等: "A High Yield Procedure for the Me3SiNTf2-Induced Carbon-Carbon Bond-Forming Reactions of Silyl Nucleophiles with Carbonyl Compounds:The Importance of Addition Order and Solvent Effects", 《SYNLETT》 *
XINYUAN FAN 等: "Highly Enantioselective Cross-Aldol Reactions of Acetaldehyde Mediated by a Dual Catalytic System Operating under Site Isolation", 《CHEMISTRY A EUROPEAN JOURNAL》 *
XINYUAN FAN 等: "Paraldehyde as an Acetaldehyde Precursor in Asymmetric Michael Reactions Promoted by Site-Isolated Incompatible Catalysts", 《CHEMISTRY A EUROPEAN JOURNAL》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110204587A (zh) * 2019-07-19 2019-09-06 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

Also Published As

Publication number Publication date
AR108237A1 (es) 2018-08-01
JP2019515906A (ja) 2019-06-13
BR112018071441A2 (pt) 2019-02-05
MX374550B (es) 2025-03-06
AU2017254480A1 (en) 2018-11-15
WO2017184598A1 (en) 2017-10-26
EP3445370B1 (en) 2021-12-01
EP3445370A1 (en) 2019-02-27
US10550146B2 (en) 2020-02-04
CA3021322A1 (en) 2017-10-26
ES2907425T3 (es) 2022-04-25
EP3445370A4 (en) 2019-12-25
US20190211052A1 (en) 2019-07-11
IL262405A (en) 2018-12-31
MX2018012777A (es) 2019-01-28
KR20180134405A (ko) 2018-12-18
TW201738254A (zh) 2017-11-01

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