BR112018073488A2 - intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólico - Google Patents

intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólico

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Publication number
BR112018073488A2
BR112018073488A2 BR112018073488-8A BR112018073488A BR112018073488A2 BR 112018073488 A2 BR112018073488 A2 BR 112018073488A2 BR 112018073488 A BR112018073488 A BR 112018073488A BR 112018073488 A2 BR112018073488 A2 BR 112018073488A2
Authority
BR
Brazil
Prior art keywords
intermediates
synthesis
obeticolic
acid
acid derivatives
Prior art date
Application number
BR112018073488-8A
Other languages
English (en)
Inventor
Weymouth-Wilson Alexander
Komsta Zofia
WALLIS Laura
Evans Tim
DAVIES Ieuan
Otter Carl
BATCHELOR Rhys
Original Assignee
NZP UK Limited
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 NZP UK Limited filed Critical NZP UK Limited
Publication of BR112018073488A2 publication Critical patent/BR112018073488A2/pt

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J17/00Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/006Ketals at position 3
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J21/00Normal steroids containing carbon, hydrogen, halogen or oxygen having an oxygen-containing hetero ring spiro-condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J21/005Ketals
    • C07J21/008Ketals at position 17
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J33/00Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J33/00Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J33/002Normal steroids having a sulfur-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • C07J41/0061Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0088Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0094Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing nitrile radicals, including thiocyanide radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J13/00Normal steroids containing carbon, hydrogen, halogen or oxygen having a carbon-to-carbon double bond from or to position 17
    • C07J13/007Normal 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)
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003

Abstract

a invenção refere-se a compostos de fórmula geral (i): (i) em que r1, r2, r3, r4, r5, r6 e y são como definidos aqui. os compostos são intermediates na síntese de ácidos biliares sintéticos que são úteis no tratamento de condições tal como doença hepática.
BR112018073488-8A 2016-05-18 2017-05-18 intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólico BR112018073488A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1608777.7A GB201608777D0 (en) 2016-05-18 2016-05-18 Compounds
GB1608777.7 2016-05-18
PCT/GB2017/051385 WO2017199033A1 (en) 2016-05-18 2017-05-18 Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid

Publications (1)

Publication Number Publication Date
BR112018073488A2 true BR112018073488A2 (pt) 2019-04-09

Family

ID=56320629

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018073488-8A BR112018073488A2 (pt) 2016-05-18 2017-05-18 intermediários para a síntese de derivados de ácido biliar, em particular de ácido obeticólico

Country Status (16)

Country Link
US (2) US10968250B2 (pt)
EP (2) EP3458469B1 (pt)
JP (1) JP7034093B2 (pt)
KR (1) KR102458265B1 (pt)
CN (1) CN109415407B (pt)
AU (1) AU2017266539B2 (pt)
BR (1) BR112018073488A2 (pt)
CA (1) CA3024281A1 (pt)
EA (1) EA037584B1 (pt)
ES (1) ES2878577T3 (pt)
GB (1) GB201608777D0 (pt)
HR (1) HRP20211128T1 (pt)
HU (1) HUE054851T2 (pt)
MX (1) MX2018014164A (pt)
PT (1) PT3458469T (pt)
WO (1) WO2017199033A1 (pt)

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GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
CN111138509B (zh) * 2018-11-02 2022-12-06 东莞东阳光药物研发有限公司 奥贝胆酸的制备方法
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
CN114315945A (zh) * 2020-09-28 2022-04-12 四川澄华生物科技有限公司 一种胆甾酸及其衍生物的除杂方法
CN112341516B (zh) * 2020-11-14 2022-07-15 湖南科瑞生物制药股份有限公司 5,6-环氧类固醇类化合物及其制备方法和应用
WO2023081657A2 (en) * 2021-11-02 2023-05-11 Sandhill One, Llc High purity non-animal derived udca

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Also Published As

Publication number Publication date
ES2878577T3 (es) 2021-11-19
EA037584B1 (ru) 2021-04-16
EA201892514A1 (ru) 2019-05-31
EP3848382B1 (en) 2023-11-29
CN109415407A (zh) 2019-03-01
US20210179661A1 (en) 2021-06-17
HRP20211128T1 (hr) 2022-01-07
AU2017266539A1 (en) 2018-11-15
CA3024281A1 (en) 2017-11-23
KR102458265B1 (ko) 2022-10-25
MX2018014164A (es) 2019-04-01
EP3458469B1 (en) 2021-04-14
EP3848382A1 (en) 2021-07-14
GB201608777D0 (en) 2016-06-29
US10968250B2 (en) 2021-04-06
US11479577B2 (en) 2022-10-25
AU2017266539B2 (en) 2021-04-15
EP3458469A1 (en) 2019-03-27
KR20190009322A (ko) 2019-01-28
JP7034093B2 (ja) 2022-03-11
CN109415407B (zh) 2021-08-17
HUE054851T2 (hu) 2021-10-28
US20190284227A1 (en) 2019-09-19
WO2017199033A1 (en) 2017-11-23
EP3848382C0 (en) 2023-11-29
JP2019516720A (ja) 2019-06-20
PT3458469T (pt) 2021-06-11

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Legal Events

Date Code Title Description
B350 Update of information on the portal [chapter 15.35 patent gazette]
B15K Others concerning applications: alteration of classification

Free format text: AS CLASSIFICACOES ANTERIORES ERAM: C07J 71/00 , C07J 9/00 , C07J 17/00 , C07J 33/00 , C07J 41/00 , C07J 43/00 , C07J 51/00 , C07J 13/00 , C07J 21/00 , C07J 31/00

Ipc: C07J 71/00 (2006.01), C07J 9/00 (2006.01), C07J 17

B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]