EA034739B1 - 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 Download PDFInfo
- Publication number
- EA034739B1 EA034739B1 EA201790879A EA201790879A EA034739B1 EA 034739 B1 EA034739 B1 EA 034739B1 EA 201790879 A EA201790879 A EA 201790879A EA 201790879 A EA201790879 A EA 201790879A EA 034739 B1 EA034739 B1 EA 034739B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- general formula
- compound
- compounds
- acid
- ethyl
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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)
- 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)
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 EA201790879A1 (ru) | 2017-11-30 |
| EA034739B1 true 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 (13)
| Country | Link |
|---|---|
| US (1) | US10538550B2 (enExample) |
| EP (1) | EP3221333B1 (enExample) |
| JP (1) | JP6735748B2 (enExample) |
| KR (1) | KR102546748B1 (enExample) |
| CN (1) | CN107108688B (enExample) |
| CA (1) | CA2968305A1 (enExample) |
| DK (1) | DK3221333T3 (enExample) |
| EA (1) | EA034739B1 (enExample) |
| ES (1) | ES2748692T3 (enExample) |
| MX (1) | MX375865B (enExample) |
| PL (1) | PL3221333T3 (enExample) |
| TW (1) | TWI686401B (enExample) |
| WO (1) | WO2016079519A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI686400B (zh) | 2014-11-19 | 2020-03-01 | 英商Nzp英國有限公司 | 化合物(二) |
| MX375863B (es) | 2014-11-19 | 2025-03-07 | Nzp Uk Ltd | Esteroides de 6-alquil-7-hidroxi-4-en-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr) |
| EA033603B1 (ru) | 2014-11-19 | 2019-11-08 | Nzp Uk Ltd | 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
| EA201891491A1 (ru) * | 2015-12-22 | 2018-11-30 | Интерсепт Фармасьютикалз, Инк. | Полиморфные кристаллические формы обетихолевой кислоты |
| 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 |
| 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 |
| US12186329B2 (en) | 2018-08-23 | 2025-01-07 | President And Fellows Of Harvard College | Compositions and methods related to cholic acid 7-sulfate as a treatment for diabetes |
| 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 |
| EP3890745B1 (en) * | 2018-12-04 | 2025-11-19 | President and Fellows of Harvard College | Synthetic derivatives of cholic acid 7-sulfate and uses thereof |
Citations (3)
| 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)
| 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 |
| 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 |
| US7138390B2 (en) * | 2001-03-12 | 2006-11-21 | Intercept Pharmaceuticals | 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 |
| KR100948532B1 (ko) | 2001-11-07 | 2010-03-23 | 넥타르 테라퓨틱스 | 분지형 중합체 및 그의 공액체 |
| 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 |
| WO2008002573A2 (en) | 2006-06-27 | 2008-01-03 | 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 |
| EA020310B1 (ru) * | 2008-07-30 | 2014-10-30 | Интерсепт Фармасьютикалз, Инк. | Модуляторы рецептора tgr5 и их применение |
| AU2009316566B9 (en) | 2008-11-19 | 2014-05-15 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and method of use thereof |
| US8829213B2 (en) | 2009-07-29 | 2014-09-09 | The University Of Chicago | Liver X receptor agonists |
| ES2822375T3 (es) * | 2012-06-19 | 2021-04-30 | Intercept Pharmaceuticals Inc | Preparación de la forma no cristalina del ácido obeticólico |
| WO2014066819A1 (en) | 2012-10-26 | 2014-05-01 | 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 |
| HRP20180931T1 (hr) | 2013-05-14 | 2018-10-05 | Intercept Pharmaceuticals, Inc. | 11-hidroksil-6-supstituirani-derivati žučnih kiselina i njihovi aminokiselinski konjugati kao modulatori receptora za farnezoid x |
| RU2015155552A (ru) | 2013-05-24 | 2017-06-27 | Нестек С.А. | Путеспецифические способы прогнозирования диагноза синдрома раздраженного кишечника |
| WO2015183794A1 (en) | 2014-05-27 | 2015-12-03 | City Of Hope | Tgr5 agonist complexes for treating diabetes and cancer |
| ES2938874T3 (es) | 2014-05-29 | 2023-04-17 | Bar Pharmaceuticals S R L | Derivados de colano para su uso en el tratamiento y/o prevención de enfermedades mediadas por FXR y TGR5/GPBAR1 |
| CA2966885A1 (en) | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| MX375863B (es) | 2014-11-19 | 2025-03-07 | Nzp Uk Ltd | Esteroides de 6-alquil-7-hidroxi-4-en-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr) |
| EA033603B1 (ru) | 2014-11-19 | 2019-11-08 | Nzp Uk Ltd | 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
| TWI686400B (zh) | 2014-11-19 | 2020-03-01 | 英商Nzp英國有限公司 | 化合物(二) |
| WO2016086134A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives 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 |
| 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 |
| HK1244708A1 (zh) | 2014-11-26 | 2018-08-17 | 英安塔制药有限公司 | 作爲fxr/tgr5激动剂的胆汁酸类似物及其使用方法 |
| 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 |
| PL3310801T3 (pl) | 2015-06-19 | 2021-11-22 | Intercept Pharmaceuticals, Inc. | Modulatory tgr5 i sposoby ich stosowania |
| 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 |
-
2015
- 2015-11-19 CN CN201580062897.3A patent/CN107108688B/zh active Active
- 2015-11-19 EA EA201790879A patent/EA034739B1/ru unknown
- 2015-11-19 MX MX2017006565A patent/MX375865B/es active IP Right Grant
- 2015-11-19 EP EP15800911.8A patent/EP3221333B1/en active Active
- 2015-11-19 ES ES15800911T patent/ES2748692T3/es active Active
- 2015-11-19 PL PL15800911T patent/PL3221333T3/pl unknown
- 2015-11-19 WO PCT/GB2015/053518 patent/WO2016079519A1/en not_active Ceased
- 2015-11-19 JP JP2017527790A patent/JP6735748B2/ja active Active
- 2015-11-19 TW TW104138185A patent/TWI686401B/zh active
- 2015-11-19 US US15/528,331 patent/US10538550B2/en active Active
- 2015-11-19 KR KR1020177016857A patent/KR102546748B1/ko active Active
- 2015-11-19 DK DK15800911.8T patent/DK3221333T3/da active
- 2015-11-19 CA CA2968305A patent/CA2968305A1/en not_active Abandoned
Patent Citations (3)
| 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 (1)
| Title |
|---|
| UEKAWA T, ISHIGAMI K, KITAHARA T: "Short-step Synthesis of Chenodiol from Stigmasterol", BIOSCIENCE, BIOTECHNOLOGY AND BIOCHEMISTRY, JAPAN SOCIETY FOR BIOSCIENCE, BIOTECHNOLOGY AND AGROCHEMISTRY, JP, vol. 68, no. 6, 1 January 2004 (2004-01-01), JP, pages 1332 - 1337, XP003016017, ISSN: 0916-8451, DOI: 10.1271/bbb.68.1332 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3221333A1 (en) | 2017-09-27 |
| TWI686401B (zh) | 2020-03-01 |
| TW201632538A (zh) | 2016-09-16 |
| KR102546748B1 (ko) | 2023-06-22 |
| KR20170104453A (ko) | 2017-09-15 |
| US20180340006A1 (en) | 2018-11-29 |
| HK1244287A1 (en) | 2018-08-03 |
| WO2016079519A1 (en) | 2016-05-26 |
| JP6735748B2 (ja) | 2020-08-05 |
| MX2017006565A (es) | 2018-01-26 |
| MX375865B (es) | 2025-03-07 |
| CA2968305A1 (en) | 2016-05-26 |
| US10538550B2 (en) | 2020-01-21 |
| EA201790879A1 (ru) | 2017-11-30 |
| CN107108688B (zh) | 2019-10-29 |
| JP2017538690A (ja) | 2017-12-28 |
| CN107108688A (zh) | 2017-08-29 |
| DK3221333T3 (da) | 2019-09-30 |
| ES2748692T3 (es) | 2020-03-17 |
| WO2016079519A9 (en) | 2018-08-09 |
| PL3221333T3 (pl) | 2020-01-31 |
| EP3221333B1 (en) | 2019-07-24 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EA034739B1 (ru) | 6-альфа-алкил-3,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr | |
| KR102527821B1 (ko) | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드 | |
| KR102526631B1 (ko) | 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드 | |
| KR102526632B1 (ko) | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드 | |
| HK1244285A1 (en) | 5.beta -6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators | |
| EA038224B1 (ru) | Способ и интермедиаты для 6,7-альфа-эпоксидирования стероидных 4,6-диенов | |
| HK1244286B (en) | 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators | |
| HK1244287B (en) | 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators | |
| NZ731924B2 (en) | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators | |
| HK1246801B (en) | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators |