EA034739B1 - 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr - Google Patents

6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr Download PDF

Info

Publication number
EA034739B1
EA034739B1 EA201790879A EA201790879A EA034739B1 EA 034739 B1 EA034739 B1 EA 034739B1 EA 201790879 A EA201790879 A EA 201790879A EA 201790879 A EA201790879 A EA 201790879A EA 034739 B1 EA034739 B1 EA 034739B1
Authority
EA
Eurasian Patent Office
Prior art keywords
general formula
compound
compounds
acid
ethyl
Prior art date
Application number
EA201790879A
Other languages
English (en)
Russian (ru)
Other versions
EA201790879A1 (ru
Inventor
Александер Уэймаут-Уилсон
Зофиа Комста
Джеймс Бойдэлл
Лаура Уоллис
Риз Батчелор
Карл Оттер
Юань Дэвис
Original Assignee
ЭнЗедПи ЮКей ЛИМИТЕД
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
Priority claimed from GBGB1420593.4A external-priority patent/GB201420593D0/en
Priority claimed from GBGB1420594.2A external-priority patent/GB201420594D0/en
Priority claimed from GBGB1505676.5A external-priority patent/GB201505676D0/en
Application filed by ЭнЗедПи ЮКей ЛИМИТЕД filed Critical ЭнЗедПи ЮКей ЛИМИТЕД
Publication of EA201790879A1 publication Critical patent/EA201790879A1/ru
Publication of EA034739B1 publication Critical patent/EA034739B1/ru

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EA201790879A 2014-11-19 2015-11-19 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr EA034739B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB1420593.4A GB201420593D0 (en) 2014-11-19 2014-11-19 Compounds
GBGB1420594.2A GB201420594D0 (en) 2014-11-19 2014-11-19 Compounds
GBGB1505676.5A GB201505676D0 (en) 2015-04-01 2015-04-01 Compounds
PCT/GB2015/053518 WO2016079519A1 (en) 2014-11-19 2015-11-19 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators

Publications (2)

Publication Number Publication Date
EA201790879A1 EA201790879A1 (ru) 2017-11-30
EA034739B1 true EA034739B1 (ru) 2020-03-16

Family

ID=54704021

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201790879A EA034739B1 (ru) 2014-11-19 2015-11-19 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr

Country Status (13)

Country Link
US (1) US10538550B2 (OSRAM)
EP (1) EP3221333B1 (OSRAM)
JP (1) JP6735748B2 (OSRAM)
KR (1) KR102546748B1 (OSRAM)
CN (1) CN107108688B (OSRAM)
CA (1) CA2968305A1 (OSRAM)
DK (1) DK3221333T3 (OSRAM)
EA (1) EA034739B1 (OSRAM)
ES (1) ES2748692T3 (OSRAM)
MX (1) MX375865B (OSRAM)
PL (1) PL3221333T3 (OSRAM)
TW (1) TWI686401B (OSRAM)
WO (1) WO2016079519A1 (OSRAM)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016079517A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
EA033603B1 (ru) 2014-11-19 2019-11-08 Nzp Uk Ltd 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EA033445B1 (ru) 2014-11-19 2019-10-31 Nzp Uk Ltd 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
AU2016375566A1 (en) * 2015-12-22 2018-07-05 Intercept Pharmaceuticals, Inc. Polymorphic crystalline forms of obeticholic acid
GB201608779D0 (en) * 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
EP3431486A1 (en) 2017-07-18 2019-01-23 Bionice, S.L.U. Process and intermediates for the synthesis of obeticholic acid and derivatives thereof
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
WO2020041673A1 (en) 2018-08-23 2020-02-27 President And Fellows Of Harvard College Compositions and methods related to cholic acid-7-sulfate as a treatment for diabetes
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
US12419897B2 (en) 2018-12-04 2025-09-23 President And Fellows Of Harvard College Synthetic derivatives of cholic acid 7-sulfate and uses thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006122977A2 (en) * 2005-05-19 2006-11-23 Erregierre S.P.A. PROCESS FOR PREPARING 3α(β)-7α(β)-DIHYDROXY-6α(β)-ALKYL-5β-CHOLANIC ACID
WO2010059859A1 (en) * 2008-11-19 2010-05-27 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
US20140148428A1 (en) * 2012-11-28 2014-05-29 Intercept Pharmaceuticals, Inc. Treatment of Pulmonary Disease

Family Cites Families (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2624748A (en) 1950-09-09 1953-01-06 Upjohn Co Bisnorchola-4, 6-dien-3-one-22-al
US4289872A (en) 1979-04-06 1981-09-15 Allied Corporation Macromolecular highly branched homogeneous compound based on lysine units
US5229490A (en) 1987-05-06 1993-07-20 The Rockefeller University Multiple antigen peptide system
DE69312700T2 (de) 1992-04-14 1998-02-19 Cornell Res Foundation Inc Makromoleküle auf basis von dendritischen polymeren und verfahren zur herstellung
WO1994019366A1 (en) 1993-02-26 1994-09-01 Magainin Pharmaceuticals Inc. Chemical synthesis of squalamine
US5643575A (en) 1993-10-27 1997-07-01 Enzon, Inc. Non-antigenic branched polymer conjugates
US5932462A (en) 1995-01-10 1999-08-03 Shearwater Polymers, Inc. Multiarmed, monofunctional, polymer for coupling to molecules and surfaces
DE60205891T2 (de) * 2001-03-12 2006-06-22 Intercept Pharmaceuticals, Inc. Steroide als agonisten für fxr
US20090062256A1 (en) * 2001-06-01 2009-03-05 Bristol-Myers Squibb Pharma Company LACTAMS SUBSTITUTED BY CYCLIC SUCCINATES AS INHIBITORS OF Abeta PROTEIN PRODUCTION
JP4758608B2 (ja) 2001-11-07 2011-08-31 ネクター セラピューティックス 分枝ポリマーおよびそれらの結合体
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
JP2007210888A (ja) 2006-01-12 2007-08-23 Mitsubishi Chemicals Corp ステロイド化合物の製造方法
BRPI0707794A2 (pt) 2006-02-14 2011-05-10 Intercept Pharmaceuticals Inc compostos derivados de Ácido biliar, formulaÇÕes e composiÇÕes farmacÊuticas, bem como uso de ditos compostos
PL2040713T3 (pl) 2006-06-27 2014-11-28 Intercept Pharmaceuticals Inc Pochodne kwasów żółciowych jako ligandy FXR do zapobiegania lub leczenia chorób lub stanów, w których pośredniczy FXR
BRPI0808684B1 (pt) 2007-01-19 2021-08-10 Intercept Pharmaceuticals, Inc Compostos moduladores de tgr5, composição e seus usos
US8796249B2 (en) 2008-07-30 2014-08-05 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
PL2698375T3 (pl) 2008-11-19 2018-08-31 Intercept Pharmaceuticals, Inc. Modulatory TGR5 i sposób ich zastosowania
EP2459581A4 (en) 2009-07-29 2012-12-26 Univ Chicago LIVER X-RECEPTOR AGONISTS
PT3336097T (pt) 2012-06-19 2020-10-29 Intercept Pharmaceuticals Inc Preparação da forma não cristalina de ácido obeticólico
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
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
EA030152B1 (ru) 2013-05-14 2018-06-29 Интерсепт Фармасьютикалз, Инк 11-гидроксилпроизводные желчных кислот и их аминокислотные конъюгаты в качестве модуляторов фарнезоидных х-рецепторов
RU2015155552A (ru) 2013-05-24 2017-06-27 Нестек С.А. Путеспецифические способы прогнозирования диагноза синдрома раздраженного кишечника
US10166246B2 (en) 2014-05-27 2019-01-01 City Of Hope TGR5 agonist complexes for treating diabetes and cancer
LT3149019T (lt) 2014-05-29 2020-02-25 Bar Pharmaceuticals S.R.L. Cholano dariniai, skirti naudoti fxr ir tgr5/gpbar1 medijuojamų ligų gydymui ir (arba) prevencijai
EP3215179A4 (en) 2014-11-06 2018-07-25 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
EA033445B1 (ru) 2014-11-19 2019-10-31 Nzp Uk Ltd 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
WO2016079517A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
EA033603B1 (ru) 2014-11-19 2019-11-08 Nzp Uk Ltd 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
US11578097B2 (en) 2014-11-26 2023-02-14 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as FXR/TGR5 agonists and methods of use thereof
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
JP2017535570A (ja) 2014-11-26 2017-11-30 エナンタ ファーマシューティカルズ インコーポレイテッド Fxr/tgr5アゴニストとしての胆汁酸類似体およびその使用方法
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
CN106279328A (zh) 2015-05-20 2017-01-04 重庆药友制药有限责任公司 一种制备6α-烷基鹅去氧胆酸的方法
JP6861703B2 (ja) 2015-06-19 2021-04-21 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 Tgr5修飾物質およびその使用方法
CN106397522A (zh) 2015-07-31 2017-02-15 中国人民解放军军事医学科学院毒物药物研究所 3,7‑二(叔丁基二甲基硅基氧基)‑6‑烯‑5β‑胆烷‑24‑酸甲酯
CN106478759A (zh) 2015-08-31 2017-03-08 陕西合成药业股份有限公司 奥贝胆酸衍生物及其制备方法和用途
CN106478756A (zh) 2015-09-02 2017-03-08 中美华世通生物医药科技(武汉)有限公司 Oca-e单晶及其制备方法和用途
CN106518946A (zh) 2015-09-10 2017-03-22 上海迪诺医药科技有限公司 磺酰脲衍生物、其药物组合物及应用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2006122977A2 (en) * 2005-05-19 2006-11-23 Erregierre S.P.A. PROCESS FOR PREPARING 3α(β)-7α(β)-DIHYDROXY-6α(β)-ALKYL-5β-CHOLANIC ACID
WO2010059859A1 (en) * 2008-11-19 2010-05-27 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
US20140148428A1 (en) * 2012-11-28 2014-05-29 Intercept Pharmaceuticals, Inc. Treatment of Pulmonary Disease

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
UEKAWA T, ISHIGAMI K, KITAHARA T: "Short-step Synthesis of Chenodiol from Stigmasterol", BIOSCIENCE, BIOTECHNOLOGY AND BIOCHEMISTRY, JAPAN SOCIETY FOR BIOSCIENCE, BIOTECHNOLOGY AND AGROCHEMISTRY, JP, vol. 68, no. 6, 1 January 2004 (2004-01-01), JP, pages 1332 - 1337, XP003016017, ISSN: 0916-8451, DOI: 10.1271/bbb.68.1332 *

Also Published As

Publication number Publication date
EP3221333A1 (en) 2017-09-27
US10538550B2 (en) 2020-01-21
EA201790879A1 (ru) 2017-11-30
CA2968305A1 (en) 2016-05-26
MX2017006565A (es) 2018-01-26
PL3221333T3 (pl) 2020-01-31
JP6735748B2 (ja) 2020-08-05
JP2017538690A (ja) 2017-12-28
US20180340006A1 (en) 2018-11-29
KR20170104453A (ko) 2017-09-15
MX375865B (es) 2025-03-07
TW201632538A (zh) 2016-09-16
CN107108688B (zh) 2019-10-29
KR102546748B1 (ko) 2023-06-22
HK1244287A1 (en) 2018-08-03
WO2016079519A1 (en) 2016-05-26
ES2748692T3 (es) 2020-03-17
DK3221333T3 (da) 2019-09-30
CN107108688A (zh) 2017-08-29
TWI686401B (zh) 2020-03-01
EP3221333B1 (en) 2019-07-24
WO2016079519A9 (en) 2018-08-09

Similar Documents

Publication Publication Date Title
EA034739B1 (ru) 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
KR102527821B1 (ko) 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드
KR102526631B1 (ko) 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드
KR102526632B1 (ko) 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드
HK1244285A1 (en) 5.beta -6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
EA038224B1 (ru) Способ и интермедиаты для 6,7-альфа-эпоксидирования стероидных 4,6-диенов
HK1244286B (en) 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
HK1244287B (en) 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
NZ731924B2 (en) 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
HK1246801B (en) 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators