EA033427B1 - 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr - Google Patents

6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr

Info

Publication number
EA033427B1
EA033427B1 EA201790884A EA201790884A EA033427B1 EA 033427 B1 EA033427 B1 EA 033427B1 EA 201790884 A EA201790884 A EA 201790884A EA 201790884 A EA201790884 A EA 201790884A EA 033427 B1 EA033427 B1 EA 033427B1
Authority
EA
Eurasian Patent Office
Prior art keywords
intermediates
steroids
hydroxy
alkyl
production
Prior art date
Application number
EA201790884A
Other languages
English (en)
Russian (ru)
Other versions
EA201790884A8 (ru
EA201790884A1 (ru
Inventor
Alexander Weymouth-Wilson
Zofia Komsta
James Boydell
Carl Otter
Laura Wallis
Rhys Batchelor
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 GBGB1505670.8A external-priority patent/GB201505670D0/en
Application filed by Nzp Uk Ltd filed Critical Nzp Uk Ltd
Publication of EA201790884A1 publication Critical patent/EA201790884A1/ru
Publication of EA201790884A8 publication Critical patent/EA201790884A8/ru
Publication of EA033427B1 publication Critical patent/EA033427B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005—Oxygen-containing hetero ring
    • C07J71/001—Oxiranes
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
EA201790884A 2014-11-19 2015-11-19 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr EA033427B1 (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
GBGB1505670.8A GB201505670D0 (en) 2015-04-01 2015-04-01 Compounds
PCT/GB2015/053516 WO2016079517A1 (en) 2014-11-19 2015-11-19 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators

Publications (3)

Publication Number Publication Date
EA201790884A1 EA201790884A1 (ru) 2017-11-30
EA201790884A8 EA201790884A8 (ru) 2019-07-31
EA033427B1 true EA033427B1 (ru) 2019-10-31

Family

ID=54704019

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201790884A EA033427B1 (ru) 2014-11-19 2015-11-19 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr

Country Status (15)

Country Link
US (1) US10301350B2 (enExample)
EP (1) EP3221331B1 (enExample)
JP (1) JP6700274B2 (enExample)
KR (1) KR102526631B1 (enExample)
CN (1) CN107207559B (enExample)
BR (1) BR112017010319B1 (enExample)
CA (1) CA2968309A1 (enExample)
DK (1) DK3221331T3 (enExample)
EA (1) EA033427B1 (enExample)
ES (1) ES2759725T3 (enExample)
MX (1) MX375863B (enExample)
PL (1) PL3221331T3 (enExample)
PT (1) PT3221331T (enExample)
TW (1) TWI690536B (enExample)
WO (1) WO2016079517A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL3221333T3 (pl) 2014-11-19 2020-01-31 NZP UK Limited Steroidy, 6.alfa-alkilo-3,7-diony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
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
MX381239B (es) 2014-11-19 2025-03-12 Nzp Uk Ltd Esteroides de 6.alfa.-alquil-6,7-diona como intermedios para la producción de moduladores esteroideos del receptor x farnesoide (fxr).
CZ2015504A3 (cs) * 2015-07-16 2017-01-25 Zentiva, K.S. Krystalické formy obeticholové kyseliny
WO2017111979A1 (en) * 2015-12-22 2017-06-29 Intercept Pharmaceuticals, Inc. Polymorphic crystalline forms of obeticholic acid
GB201608779D0 (en) * 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
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
MX378555B (es) * 2016-11-29 2025-03-10 Enanta Pharm Inc Proceso para la preparacion de derivados del acido biliar de las sulfonilureas
EP3431486A1 (en) 2017-07-18 2019-01-23 Bionice, S.L.U. Process and intermediates for the synthesis of obeticholic acid and derivatives thereof
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
CN112521438B (zh) * 2020-12-08 2021-11-23 苏利制药科技江阴有限公司 一种β-谷甾醇的合成工艺
WO2023288123A1 (en) * 2021-07-16 2023-01-19 Interecept Pharmaceuticals, Inc. Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid
CN113912661B (zh) * 2021-11-11 2023-04-21 湖南科瑞生物制药股份有限公司 一种7-羟基甾体化合物的合成方法

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
ATE156158T1 (de) 1992-04-14 1997-08-15 Cornell Res Foundation Inc Makromoleküle auf basis von dendritischen polymeren und verfahren zur herstellung
AU6392894A (en) 1993-02-26 1994-09-14 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
EP1446438A2 (en) 2001-11-07 2004-08-18 Nektar Therapeutics Al, Corporation Branched polymers and their conjugates
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
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
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
AU2008209566C1 (en) 2007-01-19 2013-02-14 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as TGR5 modulators and methods of use thereof
AU2009276507B2 (en) 2008-07-30 2015-11-19 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CA2744189C (en) 2008-11-19 2016-10-11 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
US8829213B2 (en) 2009-07-29 2014-09-09 The University Of Chicago Liver X receptor agonists
SG10201607230SA (en) 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
SMT201700602T1 (it) 2012-10-26 2018-03-08 Intercept Pharmaceuticals Inc Processo per la preparazione di derivati dell’acido biliare
US20140206657A1 (en) 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
PT3360882T (pt) 2013-05-14 2021-02-12 Intercept Pharmaceuticals Inc Derivados de 11-hidroxilo substituídos em 6 de ácidos biliares e conjugados de aminoácidos dos mesmos como moduladores do recetor farnesoide x
RU2015155590A (ru) 2013-05-24 2017-06-29 Нестек С.А. Путеспецифичные маркеры для диагностики синдрома раздраженного кишечника
WO2015183794A1 (en) 2014-05-27 2015-12-03 City Of Hope Tgr5 agonist complexes for treating diabetes and cancer
JP6820253B2 (ja) 2014-05-29 2021-01-27 バール ファーマシューティカルズ ソチエタ レスポンサビリタ リミタータ Ｆｘｂ及びｔｇｒ５／ｇｐｂａｒ１介在性疾患の治療及び／又は予防に使用するためのコラン誘導体
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
PL3221333T3 (pl) 2014-11-19 2020-01-31 NZP UK Limited Steroidy, 6.alfa-alkilo-3,7-diony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
MX381239B (es) 2014-11-19 2025-03-12 Nzp Uk Ltd Esteroides de 6.alfa.-alquil-6,7-diona como intermedios para la producción de moduladores esteroideos del receptor x farnesoide (fxr).
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
SG11201703997XA (en) 2014-11-26 2017-06-29 Enanta Pharm Inc Bile acid analogs 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
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
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
AU2016280806B2 (en) 2015-06-19 2021-01-28 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

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 (2)

* Cited by examiner, † Cited by third party
Title
ESPERANZA VELARDE, IRIARTE J., RINGOLD H. J., DJERASSI CARL: "Steroids. CXIII. 6-Methyl Estrogens", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 24, no. 3, 1 March 1959 (1959-03-01), US, pages 311 - 313, XP055245937, ISSN: 0022-3263, DOI: 10.1021/jo01085a006 *
UEKAWA T, ISHIGAMI K, KITAHARA T: "Short-step Synthesis of Chenodiol from Stigmasterol", BIOSCI. BIOTECH. BIOCHEM., vol. 68, no. 6, 1 January 2004 (2004-01-01), pages 1332 - 1337, XP003016017, ISSN: 0916-8451, DOI: 10.1271/bbb.68.1332 *

Also Published As

Publication number Publication date
DK3221331T3 (da) 2019-12-02
NZ731924A (en) 2020-12-18
PL3221331T3 (pl) 2020-03-31
KR20170086604A (ko) 2017-07-26
JP2017534670A (ja) 2017-11-24
US20170327528A1 (en) 2017-11-16
WO2016079517A1 (en) 2016-05-26
EP3221331B1 (en) 2019-09-18
EP3221331A1 (en) 2017-09-27
MX375863B (es) 2025-03-07
MX2017006563A (es) 2018-01-26
US10301350B2 (en) 2019-05-28
JP6700274B2 (ja) 2020-05-27
HK1246801A1 (en) 2018-09-14
BR112017010319A2 (pt) 2017-12-26
CA2968309A1 (en) 2016-05-26
PT3221331T (pt) 2019-12-23
CN107207559B (zh) 2019-10-25
CN107207559A (zh) 2017-09-26
EA201790884A8 (ru) 2019-07-31
BR112017010319B1 (pt) 2023-04-11
EA201790884A1 (ru) 2017-11-30
ES2759725T3 (es) 2020-05-12
KR102526631B1 (ko) 2023-04-27
TW201632537A (zh) 2016-09-16
TWI690536B (zh) 2020-04-11

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