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
EA201790884A1 (ru
EA201790884A8 (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 (https=)
EP (1) EP3221331B1 (https=)
JP (1) JP6700274B2 (https=)
KR (1) KR102526631B1 (https=)
CN (1) CN107207559B (https=)
BR (1) BR112017010319B1 (https=)
CA (1) CA2968309A1 (https=)
DK (1) DK3221331T3 (https=)
EA (1) EA033427B1 (https=)
ES (1) ES2759725T3 (https=)
MX (1) MX375863B (https=)
PL (1) PL3221331T3 (https=)
PT (1) PT3221331T (https=)
TW (1) TWI690536B (https=)
WO (1) WO2016079517A1 (https=)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR102546748B1 (ko) 2014-11-19 2023-06-22 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-3,7-다이온 스테로이드
KR102527821B1 (ko) 2014-11-19 2023-05-02 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드
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
CZ2015504A3 (cs) * 2015-07-16 2017-01-25 Zentiva, K.S. Krystalické formy obeticholové kyseliny
JP2018538331A (ja) * 2015-12-22 2018-12-27 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 オベチコール酸の多型結晶形態
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
CN110121347A (zh) * 2016-11-29 2019-08-13 英安塔制药有限公司 制备磺酰脲胆汁酸衍生物的方法
EP3431486A1 (en) * 2017-07-18 2019-01-23 Bionice, S.L.U. Process and intermediates for the synthesis of obeticholic acid and derivatives thereof
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
CA2118130A1 (en) 1992-04-14 1993-10-28 Jean M. J. Frechet Dendritic based macromolecules and method of production
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
ES2248581T3 (es) 2001-03-12 2006-03-16 Intercept Pharmaceuticals, Inc. Esteroides como agonistas de 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
AU2002352524B2 (en) 2001-11-07 2007-10-04 Nektar Therapeutics 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
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
US7932244B2 (en) 2006-06-27 2011-04-26 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
KR101555716B1 (ko) 2007-01-19 2015-09-25 인터셉트 파마슈티컬즈, 인크. Ｔｇｒ5 조절제로서의 23-치환 담즙산 및 이의 사용 방법
WO2010014836A2 (en) 2008-07-30 2010-02-04 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
DK2698375T3 (en) 2008-11-19 2018-05-28 Intercept Pharmaceuticals Inc TGR5 modulators and methods for using them
EP2459581A4 (en) 2009-07-29 2012-12-26 Univ Chicago LIVER X-RECEPTOR AGONISTS
SI3336097T1 (sl) 2012-06-19 2021-07-30 Intercept Pharmaceuticals, Inc. Priprava nekristalinične oblike obetiholne kisline
SG11201503247UA (en) 2012-10-26 2015-06-29 Intercept Pharmaceuticals Inc Process for preparing bile acid derivatives
US20140206657A1 (en) * 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
TN2015000497A1 (en) 2013-05-14 2017-04-06 Intercept Pharmaceuticals Inc 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
SG11201509371XA (en) 2013-05-24 2015-12-30 Nestec Sa Pathway specific markers for diagnosing irritable bowel syndrome
US10166246B2 (en) 2014-05-27 2019-01-01 City Of Hope TGR5 agonist complexes for treating diabetes and cancer
SMT202000070T1 (it) 2014-05-29 2020-03-13 Bar Pharmaceuticals S R L Derivati del colano per l'uso del trattamento e/o la prevenzione di malattie mediate da fxr e tgr5/gpbar1
SG11201703717SA (en) 2014-11-06 2017-06-29 Enanta Pharm Inc Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
KR102527821B1 (ko) 2014-11-19 2023-05-02 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드
KR102546748B1 (ko) 2014-11-19 2023-06-22 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-3,7-다이온 스테로이드
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
EP3223823A4 (en) 2014-11-26 2018-10-17 Enanta Pharmaceuticals, 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
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 (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
BR112017010319B1 (pt) 2023-04-11
EA201790884A1 (ru) 2017-11-30
CA2968309A1 (en) 2016-05-26
EP3221331B1 (en) 2019-09-18
MX375863B (es) 2025-03-07
HK1246801A1 (en) 2018-09-14
BR112017010319A2 (pt) 2017-12-26
JP6700274B2 (ja) 2020-05-27
TW201632537A (zh) 2016-09-16
PT3221331T (pt) 2019-12-23
KR20170086604A (ko) 2017-07-26
EA201790884A8 (ru) 2019-07-31
TWI690536B (zh) 2020-04-11
CN107207559A (zh) 2017-09-26
WO2016079517A1 (en) 2016-05-26
CN107207559B (zh) 2019-10-25
US10301350B2 (en) 2019-05-28
US20170327528A1 (en) 2017-11-16
EP3221331A1 (en) 2017-09-27
NZ731924A (en) 2020-12-18
ES2759725T3 (es) 2020-05-12
DK3221331T3 (da) 2019-12-02
PL3221331T3 (pl) 2020-03-31
JP2017534670A (ja) 2017-11-24
KR102526631B1 (ko) 2023-04-27
MX2017006563A (es) 2018-01-26

Similar Documents

Publication Publication Date Title
EA033427B1 (ru) 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EA033445B1 (ru) 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
MX2020001278A (es) Sintesis de compuestos de carbamoilpiridona policiclica.
EA201790879A1 (ru) 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EA201790885A1 (ru) 6α-АЛКИЛ-6,7-ДИОНОВЫЕ СТЕРОИДЫ В КАЧЕСТВЕ ПРОМЕЖУТОЧНЫХ СОЕДИНЕНИЙ ДЛЯ ПОЛУЧЕНИЯ СТЕРОИДНЫХ МОДУЛЯТОРОВ FXR
MX2015012401A (es) Composiciones y metodos de alterar niveles de colesterol.
GR20140100479A (el) Συνθεση λιραγλουτιδης
PH12016501192A1 (en) Tetrahydropyridopyrazines modulators of gpr6
MX2017003301A (es) Producto refractario, relleno para fabricar el producto, procedimiento para fabricar el producto y uso del producto refractario.
PH12016501613B1 (en) Pyrazines modulators of gpr6
IN2013MU03070A (https=)
NZ720106A (en) A process for the preparation of regadenoson
MX389099B (es) Proceso para la preparación de 3-cloro-2-vinilfenilsulfonatos.
IN2013MU01113A (https=)
IN2014MU00171A (https=)
IN2013MU01524A (https=)
IN2014MU00069A (https=)
IN2013MU01305A (https=)
IN2014MU01191A (https=)
IN2013CH05395A (https=)
IN2013MU03769A (https=)

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM