EA201790884A1 - 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
EA201790884A1
EA201790884A1 EA201790884A EA201790884A EA201790884A1 EA 201790884 A1 EA201790884 A1 EA 201790884A1 EA 201790884 A EA201790884 A EA 201790884A EA 201790884 A EA201790884 A EA 201790884A EA 201790884 A1 EA201790884 A1 EA 201790884A1
Authority
EA
Eurasian Patent Office
Prior art keywords
fxr
steroids
hydroxy
alkyl
obtaining
Prior art date
Application number
EA201790884A
Other languages
English (en)
Other versions
EA201790884A8 (ru
EA033427B1 (ru
Inventor
Александер Уэймаут-Уилсон
Зофиа Комста
Джеймс Бойдэлл
Карл Оттер
Лаура Уоллис
Риз Батчелор
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 GBGB1505670.8A external-priority patent/GB201505670D0/en
Application filed by ЭнЗиПи Юкей ЛИМИТЕД filed Critical ЭнЗиПи Юкей ЛИМИТЕД
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
    • 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
    • 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

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)

Abstract

Данное изобретение относится к соединениям формулы (I)где R, R, Y, Rи Rявляются такими, как описано в описании изобретения. Эти соединения являются промежуточными соединениями в синтезе синтетических желчных кислот.
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 true EA201790884A1 (ru) 2017-11-30
EA201790884A8 EA201790884A8 (ru) 2019-07-31
EA033427B1 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 (16)

Country Link
US (1) US10301350B2 (ru)
EP (1) EP3221331B1 (ru)
JP (1) JP6700274B2 (ru)
KR (1) KR102526631B1 (ru)
CN (1) CN107207559B (ru)
BR (1) BR112017010319B1 (ru)
CA (1) CA2968309A1 (ru)
DK (1) DK3221331T3 (ru)
EA (1) EA033427B1 (ru)
ES (1) ES2759725T3 (ru)
HK (1) HK1246801A1 (ru)
MX (1) MX2017006563A (ru)
PL (1) PL3221331T3 (ru)
PT (1) PT3221331T (ru)
TW (1) TWI690536B (ru)
WO (1) WO2016079517A1 (ru)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2968305A1 (en) 2014-11-19 2016-05-26 NZP UK Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
TWI688571B (zh) 2014-11-19 2020-03-21 英商Ｎｚｐ英國有限公司 化合物（四）
CZ2015504A3 (cs) * 2015-07-16 2017-01-25 Zentiva, K.S. Krystalické formy obeticholové kyseliny
BR112018012590A2 (pt) * 2015-12-22 2018-12-04 Intercept Pharmaceuticals Inc formas cristalinas polimórficas do ácido obeticólico
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
GB201608777D0 (en) * 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
AU2017368069B2 (en) * 2016-11-29 2021-07-08 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
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

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
WO1993021259A1 (en) 1992-04-14 1993-10-28 Cornell Research Foundation Inc. Dendritic based macromolecules and method of production
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
ATE303399T1 (de) 2001-03-12 2005-09-15 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
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
AU2007215207A1 (en) 2006-02-14 2007-08-23 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
AU2007265457C1 (en) 2006-06-27 2012-11-29 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
ES2438271T3 (es) 2007-01-19 2014-01-16 Intercept Pharmaceuticals, Inc. Ácidos biliares 23-sustituidos como moduladores de TGR5 y métodos de uso de los mismos
CN105037476B (zh) 2008-07-30 2018-06-12 英特塞普特医药品公司 Tgr5调节剂及其使用方法
CN106380502A (zh) * 2008-11-19 2017-02-08 英特塞普特医药品公司 G蛋白偶联受体5(tgr5)调节剂及其使用方法
DK2698375T3 (en) 2008-11-19 2018-05-28 Intercept Pharmaceuticals Inc TGR5 modulators and methods for using them
CN102482315A (zh) 2009-07-29 2012-05-30 芝加哥大学 肝x受体激动剂
SG10201607230SA (en) 2012-06-19 2016-10-28 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
CA2891348C (en) 2012-11-28 2020-04-28 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
MY187886A (en) 2013-05-14 2021-10-26 Intercept Pharmaceuticals Inc 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
KR20160013163A (ko) 2013-05-24 2016-02-03 네스텍 소시에테아노님 과민성 대장 증후군 진단을 예측하기 위한 경로 특이적 검정법
US10166246B2 (en) 2014-05-27 2019-01-01 City Of Hope TGR5 agonist complexes for treating diabetes and cancer
DK3626725T3 (da) 2014-05-29 2023-02-27 Bar Pharmaceuticals S R L Cholan-derivater til anvendelse ved behandlingen og/eller forebyggelsen af fxr- og tgr5/gpbar1-medierede sygdomme
WO2016073767A1 (en) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
TWI688571B (zh) 2014-11-19 2020-03-21 英商Ｎｚｐ英國有限公司 化合物（四）
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
CA2968305A1 (en) 2014-11-19 2016-05-26 NZP UK Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
WO2016086134A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
WO2016086115A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Tetrazole derivatives of bile acids as fxr/tgr5 agonists and methods of use thereof
CN107231795A (zh) 2014-11-26 2017-10-03 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸类似物及其使用方法
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
SI3310801T1 (sl) 2015-06-19 2021-10-29 Intercept Pharmaceuticals Inc Modulatorji TGR5 in postopki za uporabo le-teh
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
BR112017010319A2 (pt) 2017-12-26
JP6700274B2 (ja) 2020-05-27
US10301350B2 (en) 2019-05-28
EA201790884A8 (ru) 2019-07-31
TWI690536B (zh) 2020-04-11
BR112017010319B1 (pt) 2023-04-11
CN107207559B (zh) 2019-10-25
HK1246801A1 (zh) 2018-09-14
KR20170086604A (ko) 2017-07-26
US20170327528A1 (en) 2017-11-16
ES2759725T3 (es) 2020-05-12
WO2016079517A1 (en) 2016-05-26
MX2017006563A (es) 2018-01-26
EA033427B1 (ru) 2019-10-31
CA2968309A1 (en) 2016-05-26
DK3221331T3 (da) 2019-12-02
EP3221331B1 (en) 2019-09-18
KR102526631B1 (ko) 2023-04-27
JP2017534670A (ja) 2017-11-24
NZ731924A (en) 2020-12-18
TW201632537A (zh) 2016-09-16
PT3221331T (pt) 2019-12-23
EP3221331A1 (en) 2017-09-27
PL3221331T3 (pl) 2020-03-31
CN107207559A (zh) 2017-09-26

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