EA201790879A1 - 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

Info

Publication number
EA201790879A1
EA201790879A1 EA201790879A EA201790879A EA201790879A1 EA 201790879 A1 EA201790879 A1 EA 201790879A1 EA 201790879 A EA201790879 A EA 201790879A EA 201790879 A EA201790879 A EA 201790879A EA 201790879 A1 EA201790879 A1 EA 201790879A1
Authority
EA
Eurasian Patent Office
Prior art keywords
fxr
alpha
alkyl
obtaining
intermediate connections
Prior art date
Application number
EA201790879A
Other languages
English (en)
Other versions
EA034739B1 (ru
Inventor
Александер Уэймаут-Уилсон
Зофиа Комста
Джеймс Бойдэлл
Лаура Уоллис
Риз Батчелор
Карл Оттер
Юань Дэвис
Original Assignee
ЭнЗиПи 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 GBGB1420594.2A external-priority patent/GB201420594D0/en
Priority claimed from GBGB1420593.4A external-priority patent/GB201420593D0/en
Priority claimed from GBGB1505676.5A external-priority patent/GB201505676D0/en
Application filed by ЭнЗиПи Юкей ЛИМИТЕД filed Critical ЭнЗиПи Юкей ЛИМИТЕД
Publication of EA201790879A1 publication Critical patent/EA201790879A1/ru
Publication of EA034739B1 publication Critical patent/EA034739B1/ru

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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)

Abstract

Изобретение относится к соединениям формулы (I)где R, R, Y, Rи Rтакие, как определено в описании изобретения. Эти соединения представляют собой промежуточные соединения в синтезе синтетических желчных кислот.
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
GBGB1420594.2A GB201420594D0 (en) 2014-11-19 2014-11-19 Compounds
GBGB1420593.4A GB201420593D0 (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 true EA201790879A1 (ru) 2017-11-30
EA034739B1 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 (14)

Country Link
US (1) US10538550B2 (ru)
EP (1) EP3221333B1 (ru)
JP (1) JP6735748B2 (ru)
KR (1) KR102546748B1 (ru)
CN (1) CN107108688B (ru)
CA (1) CA2968305A1 (ru)
DK (1) DK3221333T3 (ru)
EA (1) EA034739B1 (ru)
ES (1) ES2748692T3 (ru)
HK (1) HK1244287A1 (ru)
MX (1) MX2017006565A (ru)
PL (1) PL3221333T3 (ru)
TW (1) TWI686401B (ru)
WO (1) WO2016079519A1 (ru)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20170327531A1 (en) 2014-11-19 2017-11-16 NZP UK Limited 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
CA2968309A1 (en) 2014-11-19 2016-05-26 NZP UK Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
EP3221332B1 (en) 2014-11-19 2019-04-24 NZP UK Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
EP3394081A1 (en) * 2015-12-22 2018-10-31 Intercept Pharmaceuticals, Inc. Polymorphic crystalline forms of obeticholic acid
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
GB201608779D0 (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
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
US20220016138A1 (en) * 2018-12-04 2022-01-20 President And Fellows Of Harvard College Synthetic derivatives of cholic acid 7-sulfate and uses thereof

Family Cites Families (42)

* 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
ATE156158T1 (de) 1992-04-14 1997-08-15 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
JP4021327B2 (ja) 2001-03-12 2007-12-12 インターセプト ファーマスーティカル インコーポレイテッド Fxrに対する作用薬としてのステロイド
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
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
JP2007210888A (ja) 2006-01-12 2007-08-23 Mitsubishi Chemicals Corp ステロイド化合物の製造方法
JP2010517931A (ja) 2006-02-14 2010-05-27 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 Fxr媒介性の疾患または状態の予防または治療用のfxrリガンドとしての胆汁酸誘導体
SI2040713T1 (sl) 2006-06-27 2014-11-28 Intercept Pharmaceuticals, Inc. Derivati žolčne kisline kot FXR ligandi za preprečevanje ali zdravljenje bolezni ali stanj, posredovanih s FXR
MX2009007728A (es) 2007-01-19 2009-12-15 Intercept Pharmaceuticals Inc Acidos biliares 23-sustituidos como moduladores de tgr5 y metodos de uso de los mismos.
WO2010014836A2 (en) * 2008-07-30 2010-02-04 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
KR101789960B1 (ko) 2008-11-19 2017-10-25 인터셉트 파마슈티컬즈, 인크. Tgr5 조절제 및 그의 사용 방법
ES2592452T3 (es) * 2008-11-19 2016-11-30 Intercept Pharmaceuticals, Inc. Moduladores de TGR5 y métodos de uso de los mismos
US8829213B2 (en) 2009-07-29 2014-09-09 The University Of Chicago Liver X receptor agonists
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
MX361653B (es) 2012-10-26 2018-12-13 Intercept Pharmaceuticals Inc Procedimiento para la preparación de derivados del ácido biliar.
EP2925328A1 (en) 2012-11-28 2015-10-07 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
DK2997035T3 (en) 2013-05-14 2018-07-02 Intercept Pharmaceuticals Inc 11-HYDROXY-6-SUBSTITUTED BALIC ACID DERIVATIVES AND AMINO ACID CONJUGATES THEREOF AS FARNESOID X RECEPTOR MODULATORS
EP3004892B1 (en) 2013-05-24 2018-10-10 Nestec S.A. Method for diagnosing irritable bowel syndrome
WO2015183794A1 (en) 2014-05-27 2015-12-03 City Of Hope Tgr5 agonist complexes for treating diabetes and cancer
PL3626725T3 (pl) 2014-05-29 2023-04-03 Bar Pharmaceuticals S.R.L. Pochodne cholanu do zastosowania w leczeniu i/lub zapobieganiu chorobom, w których pośredniczy fxr i tgr5/gpbar1
RU2017118569A (ru) 2014-11-06 2018-12-06 Энанта Фармасьютикалс, Инк. Аналоги желчных кислот как агонисты fxr/tgr5 и способы их применения
US20170327531A1 (en) 2014-11-19 2017-11-16 NZP UK Limited 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators
CA2968309A1 (en) 2014-11-19 2016-05-26 NZP UK Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
EP3221332B1 (en) 2014-11-19 2019-04-24 NZP UK Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
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
WO2016086169A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives 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
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
CA2989167A1 (en) 2015-06-19 2016-12-22 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
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

Also Published As

Publication number Publication date
HK1244287A1 (zh) 2018-08-03
TWI686401B (zh) 2020-03-01
KR102546748B1 (ko) 2023-06-22
JP6735748B2 (ja) 2020-08-05
TW201632538A (zh) 2016-09-16
ES2748692T3 (es) 2020-03-17
WO2016079519A1 (en) 2016-05-26
CN107108688B (zh) 2019-10-29
JP2017538690A (ja) 2017-12-28
CA2968305A1 (en) 2016-05-26
DK3221333T3 (da) 2019-09-30
PL3221333T3 (pl) 2020-01-31
CN107108688A (zh) 2017-08-29
WO2016079519A9 (en) 2018-08-09
EP3221333B1 (en) 2019-07-24
EA034739B1 (ru) 2020-03-16
US20180340006A1 (en) 2018-11-29
US10538550B2 (en) 2020-01-21
EP3221333A1 (en) 2017-09-27
MX2017006565A (es) 2018-01-26
KR20170104453A (ko) 2017-09-15

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