BR112018071441A2 - métodos para a preparação de ácido obeticólico e derivados do mesmo - Google Patents

métodos para a preparação de ácido obeticólico e derivados do mesmo

Info

Publication number
BR112018071441A2
BR112018071441A2 BR112018071441A BR112018071441A BR112018071441A2 BR 112018071441 A2 BR112018071441 A2 BR 112018071441A2 BR 112018071441 A BR112018071441 A BR 112018071441A BR 112018071441 A BR112018071441 A BR 112018071441A BR 112018071441 A2 BR112018071441 A2 BR 112018071441A2
Authority
BR
Brazil
Prior art keywords
derivatives
preparation
methods
obeticolic acid
obeticolic
Prior art date
Application number
BR112018071441A
Other languages
English (en)
Inventor
List Benjamin
De Chandra
Wang Qinggang
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 BR112018071441A2 publication Critical patent/BR112018071441A2/pt

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
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (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)

Abstract

a presente invenção refere-se a um método de preparação de um derivado de ácidos biliares, ou um sal, solvato ou conjugado de aminoácido farmaceuticamente aceitável do mesmo, que compreende reação do composto 2 com paraldeído para formar o composto 3: fórmula
BR112018071441A 2016-04-19 2017-04-18 métodos para a preparação de ácido obeticólico e derivados do mesmo BR112018071441A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662324405P 2016-04-19 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
BR112018071441A2 true BR112018071441A2 (pt) 2019-02-05

Family

ID=60116337

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018071441A BR112018071441A2 (pt) 2016-04-19 2017-04-18 métodos para a preparação de ácido obeticólico e derivados do mesmo

Country Status (14)

Country Link
US (1) US10550146B2 (pt)
EP (1) EP3445370B1 (pt)
JP (1) JP2019515906A (pt)
KR (1) KR20180134405A (pt)
CN (1) CN109069517A (pt)
AR (1) AR108237A1 (pt)
AU (1) AU2017254480A1 (pt)
BR (1) BR112018071441A2 (pt)
CA (1) CA3021322A1 (pt)
ES (1) ES2907425T3 (pt)
IL (1) IL262405A (pt)
MX (1) MX2018012777A (pt)
TW (1) TW201738254A (pt)
WO (1) WO2017184598A1 (pt)

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

Family Cites Families (8)

* 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
CA2440680C (en) 2001-03-12 2010-06-01 Roberto Pellicciari Steroids as agonists for fxr
EP1568706A1 (en) * 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
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
KR101881245B1 (ko) * 2012-06-19 2018-07-23 인터셉트 파마슈티컬즈, 인크. 오베티콜산의 제조법, 용도 및 고체 형태
DK2912013T3 (en) * 2012-10-26 2018-01-15 Intercept Pharmaceuticals Inc Process for the preparation of bile acid derivatives
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

Also Published As

Publication number Publication date
AR108237A1 (es) 2018-08-01
IL262405A (en) 2018-12-31
CN109069517A (zh) 2018-12-21
KR20180134405A (ko) 2018-12-18
WO2017184598A1 (en) 2017-10-26
US20190211052A1 (en) 2019-07-11
US10550146B2 (en) 2020-02-04
AU2017254480A1 (en) 2018-11-15
JP2019515906A (ja) 2019-06-13
EP3445370B1 (en) 2021-12-01
MX2018012777A (es) 2019-01-28
CA3021322A1 (en) 2017-10-26
EP3445370A1 (en) 2019-02-27
ES2907425T3 (es) 2022-04-25
TW201738254A (zh) 2017-11-01
EP3445370A4 (en) 2019-12-25

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI N? 10196/2001, QUE MODIFICOU A LEI N? 9279/96, A CONCESS?O DA PATENTE EST? CONDICIONADA ? ANU?NCIA PR?VIA DA ANVISA. CONSIDERANDO A APROVA??O DOS TERMOS DO PARECER N? 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL N? 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVID?NCIAS CAB?VEIS.

B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B06I Publication of requirement cancelled [chapter 6.9 patent gazette]

Free format text: ANULADA A PUBLICACAO CODIGO 6.6.1 NA RPI NO 2631 DE 08/06/2021 POR TER SIDO INDEVIDA.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements