EA033603B1 - 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr - Google Patents

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

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Publication number
EA033603B1
EA033603B1 EA201790885A EA201790885A EA033603B1 EA 033603 B1 EA033603 B1 EA 033603B1 EA 201790885 A EA201790885 A EA 201790885A EA 201790885 A EA201790885 A EA 201790885A EA 033603 B1 EA033603 B1 EA 033603B1
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EA
Eurasian Patent Office
Prior art keywords
general formula
alkyl
compound
compounds
ethyl
Prior art date
Application number
EA201790885A
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English (en)
Russian (ru)
Other versions
EA201790885A1 (ru
Inventor
Alexander Weymouth-Wilson
Zofia Komsta
James Boydell
Laura Wallis
Carl Otter
Ieuan Davies
Rob Clarkson
Original Assignee
Nzp Uk Ltd
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 GBGB1505675.7A external-priority patent/GB201505675D0/en
Application filed by Nzp Uk Ltd filed Critical Nzp Uk Ltd
Publication of EA201790885A1 publication Critical patent/EA201790885A1/ru
Publication of EA033603B1 publication Critical patent/EA033603B1/ru

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    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EA201790885A 2014-11-19 2015-11-19 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr EA033603B1 (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
GBGB1505675.7A GB201505675D0 (en) 2015-04-01 2015-04-01 Compounds
PCT/GB2015/053519 WO2016079520A1 (en) 2014-11-19 2015-11-19 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators

Publications (2)

Publication Number Publication Date
EA201790885A1 EA201790885A1 (ru) 2017-11-30
EA033603B1 true EA033603B1 (ru) 2019-11-08

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201790885A EA033603B1 (ru) 2014-11-19 2015-11-19 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr

Country Status (10)

Country Link
US (2) US20170327531A1 (OSRAM)
EP (1) EP3221334B1 (OSRAM)
JP (1) JP6698085B2 (OSRAM)
KR (1) KR102527821B1 (OSRAM)
CN (1) CN107207558B (OSRAM)
CA (1) CA2968310A1 (OSRAM)
EA (1) EA033603B1 (OSRAM)
MX (1) MX381239B (OSRAM)
TW (1) TWI688571B (OSRAM)
WO (1) WO2016079520A1 (OSRAM)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI688571B (zh) 2014-11-19 2020-03-21 英商Nzp英國有限公司 化合物(四)
PL3221331T3 (pl) 2014-11-19 2020-03-31 NZP UK Limited Steroidy, 6-alkilo-7-hydroksy-4-en-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
WO2016079518A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
CN107108688B (zh) 2014-11-19 2019-10-29 Nzp英国有限公司 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇
CA3009149A1 (en) * 2015-12-22 2017-06-29 Intercept Pharmaceuticals, Inc. Polymorphic crystalline forms of obeticholic acid
GB201608776D0 (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
GB201608779D0 (en) * 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
CN106046093A (zh) * 2016-05-30 2016-10-26 华东师范大学 一种石胆酸的合成方法
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
CN111285914B (zh) * 2018-12-10 2023-02-17 江西青峰药业有限公司 一种奥贝胆酸的制备方法

Citations (5)

* 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
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
WO2015183794A1 (en) * 2014-05-27 2015-12-03 City Of Hope Tgr5 agonist complexes for treating diabetes and cancer

Family Cites Families (38)

* 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
JPH07505915A (ja) 1992-04-14 1995-06-29 コーネル リサーチ ファウンデーション、インコーポレーテッド 樹枝状巨大分子およびその製造法
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
AU2002308295B2 (en) 2001-03-12 2007-08-23 Intercept Pharmaceuticals, Inc. Steroids as agonists for 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
CN101395170A (zh) 2006-02-14 2009-03-25 英特塞普特药品公司 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物
EP2040713B1 (en) 2006-06-27 2014-06-18 Intercept Pharmaceuticals Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions
CA2928178C (en) 2007-01-19 2019-09-10 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
EP2324046B1 (en) 2008-07-30 2014-09-03 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
NO2698375T3 (OSRAM) 2008-11-19 2018-07-21
US8829213B2 (en) 2009-07-29 2014-09-09 The University Of Chicago Liver X receptor agonists
CA2877122C (en) 2012-06-19 2020-04-28 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
KR102068381B1 (ko) 2012-10-26 2020-01-20 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체의 제조 방법
EP2997035B8 (en) 2013-05-14 2018-05-23 Intercept Pharmaceuticals, Inc. 11-hydroxyl-6-substituted-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
BR112015029318A2 (pt) 2013-05-24 2017-07-25 Nestec Sa marcadores específicos de caminhos para diagnóstico da síndrome do intestino irritável
EP3149019B1 (en) 2014-05-29 2019-12-04 Bar Pharmaceuticals S.r.l. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
HK1243930A1 (zh) 2014-11-06 2018-07-27 英安塔制药有限公司 作爲fxr/tgr5激动剂的胆汁酸类似物和其使用方法
CN107108688B (zh) 2014-11-19 2019-10-29 Nzp英国有限公司 作为制备类固醇FXR调节剂的中间体的6α-烷基-3,7-二酮类固醇
WO2016079518A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
PL3221331T3 (pl) 2014-11-19 2020-03-31 NZP UK Limited Steroidy, 6-alkilo-7-hydroksy-4-en-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
TWI688571B (zh) 2014-11-19 2020-03-21 英商Nzp英國有限公司 化合物(四)
MX2017006833A (es) 2014-11-26 2018-02-13 Enanta Pharm Inc Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.
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
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
TW201700447A (zh) 2015-06-19 2017-01-01 英特賽普醫藥品公司 Tgr5調控劑及其用法
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 (5)

* 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
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
WO2015183794A1 (en) * 2014-05-27 2015-12-03 City Of Hope Tgr5 agonist complexes for treating diabetes and cancer

Also Published As

Publication number Publication date
US10597423B2 (en) 2020-03-24
US20170327531A1 (en) 2017-11-16
HK1244286A1 (en) 2018-08-03
WO2016079520A1 (en) 2016-05-26
TWI688571B (zh) 2020-03-21
EP3221334B1 (en) 2020-02-19
MX381239B (es) 2025-03-12
JP2017534669A (ja) 2017-11-24
JP6698085B2 (ja) 2020-05-27
CN107207558B (zh) 2019-10-29
KR102527821B1 (ko) 2023-05-02
CA2968310A1 (en) 2016-05-26
CN107207558A (zh) 2017-09-26
US20190077827A1 (en) 2019-03-14
KR20170099896A (ko) 2017-09-01
MX2017006567A (es) 2018-01-26
EA201790885A1 (ru) 2017-11-30
TW201632539A (zh) 2016-09-16
EP3221334A1 (en) 2017-09-27

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