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
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- EA
- Eurasian Patent Office
- Prior art keywords
- general formula
- compound
- compounds
- acid
- ethyl
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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
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- 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 |
|---|---|---|---|
| GBGB1420593.4A GB201420593D0 (en) | 2014-11-19 | 2014-11-19 | Compounds |
| GBGB1420594.2A GB201420594D0 (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 (OSRAM) |
| EP (1) | EP3221333B1 (OSRAM) |
| JP (1) | JP6735748B2 (OSRAM) |
| KR (1) | KR102546748B1 (OSRAM) |
| CN (1) | CN107108688B (OSRAM) |
| CA (1) | CA2968305A1 (OSRAM) |
| DK (1) | DK3221333T3 (OSRAM) |
| EA (1) | EA034739B1 (OSRAM) |
| ES (1) | ES2748692T3 (OSRAM) |
| MX (1) | MX375865B (OSRAM) |
| PL (1) | PL3221333T3 (OSRAM) |
| TW (1) | TWI686401B (OSRAM) |
| WO (1) | WO2016079519A1 (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016079517A1 (en) | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators |
| 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 |
| 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 |
| AU2016375566A1 (en) * | 2015-12-22 | 2018-07-05 | Intercept Pharmaceuticals, Inc. | Polymorphic crystalline forms of obeticholic acid |
| 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 |
| GB201608776D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and 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 |
| WO2020041673A1 (en) | 2018-08-23 | 2020-02-27 | 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 |
| US12419897B2 (en) | 2018-12-04 | 2025-09-23 | 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 |
| DE69312700T2 (de) | 1992-04-14 | 1998-02-19 | Cornell Res Foundation Inc | Makromoleküle auf basis von dendritischen polymeren und verfahren zur herstellung |
| 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 |
| DE60205891T2 (de) * | 2001-03-12 | 2006-06-22 | 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 |
| JP2007210888A (ja) | 2006-01-12 | 2007-08-23 | Mitsubishi Chemicals Corp | ステロイド化合物の製造方法 |
| BRPI0707794A2 (pt) | 2006-02-14 | 2011-05-10 | Intercept Pharmaceuticals Inc | compostos derivados de Ácido biliar, formulaÇÕes e composiÇÕes farmacÊuticas, bem como uso de ditos compostos |
| 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 |
| BRPI0808684B1 (pt) | 2007-01-19 | 2021-08-10 | Intercept Pharmaceuticals, Inc | Compostos moduladores de tgr5, composição e seus usos |
| US8796249B2 (en) | 2008-07-30 | 2014-08-05 | Intercept Pharmaceuticals, Inc. | TGR5 modulators and methods of use thereof |
| PL2698375T3 (pl) | 2008-11-19 | 2018-08-31 | Intercept Pharmaceuticals, Inc. | Modulatory TGR5 i sposób ich zastosowania |
| EP2459581A4 (en) | 2009-07-29 | 2012-12-26 | Univ Chicago | LIVER X-RECEPTOR AGONISTS |
| PT3336097T (pt) | 2012-06-19 | 2020-10-29 | Intercept Pharmaceuticals Inc | Preparação da forma não cristalina de ácido obeticólico |
| CN108250264A (zh) | 2012-10-26 | 2018-07-06 | 英特塞普特医药品公司 | 制备胆汁酸衍生物的方法 |
| US20140206657A1 (en) * | 2013-01-18 | 2014-07-24 | City Of Hope | Bile acid analog tgr5 agonists |
| EA030152B1 (ru) | 2013-05-14 | 2018-06-29 | Интерсепт Фармасьютикалз, Инк | 11-гидроксилпроизводные желчных кислот и их аминокислотные конъюгаты в качестве модуляторов фарнезоидных х-рецепторов |
| RU2015155552A (ru) | 2013-05-24 | 2017-06-27 | Нестек С.А. | Путеспецифические способы прогнозирования диагноза синдрома раздраженного кишечника |
| US10166246B2 (en) | 2014-05-27 | 2019-01-01 | City Of Hope | TGR5 agonist complexes for treating diabetes and cancer |
| LT3149019T (lt) | 2014-05-29 | 2020-02-25 | Bar Pharmaceuticals S.R.L. | Cholano dariniai, skirti naudoti fxr ir tgr5/gpbar1 medijuojamų ligų gydymui ir (arba) prevencijai |
| EP3215179A4 (en) | 2014-11-06 | 2018-07-25 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| 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 |
| WO2016079517A1 (en) | 2014-11-19 | 2016-05-26 | Dextra Laboratories Limited | 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators |
| 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 |
| 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 |
| WO2016086134A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| JP2017535570A (ja) | 2014-11-26 | 2017-11-30 | エナンタ ファーマシューティカルズ インコーポレイテッド | Fxr/tgr5アゴニストとしての胆汁酸類似体およびその使用方法 |
| 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 |
| 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 |
-
2015
- 2015-11-19 WO PCT/GB2015/053518 patent/WO2016079519A1/en not_active Ceased
- 2015-11-19 CA CA2968305A patent/CA2968305A1/en not_active Abandoned
- 2015-11-19 DK DK15800911.8T patent/DK3221333T3/da active
- 2015-11-19 TW TW104138185A patent/TWI686401B/zh active
- 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 JP JP2017527790A patent/JP6735748B2/ja active Active
- 2015-11-19 PL PL15800911T patent/PL3221333T3/pl unknown
- 2015-11-19 US US15/528,331 patent/US10538550B2/en active Active
- 2015-11-19 CN CN201580062897.3A patent/CN107108688B/zh active Active
- 2015-11-19 KR KR1020177016857A patent/KR102546748B1/ko active Active
- 2015-11-19 EA EA201790879A patent/EA034739B1/ru unknown
- 2015-11-19 ES ES15800911T patent/ES2748692T3/es active Active
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 |
| US10538550B2 (en) | 2020-01-21 |
| EA201790879A1 (ru) | 2017-11-30 |
| CA2968305A1 (en) | 2016-05-26 |
| MX2017006565A (es) | 2018-01-26 |
| PL3221333T3 (pl) | 2020-01-31 |
| JP6735748B2 (ja) | 2020-08-05 |
| JP2017538690A (ja) | 2017-12-28 |
| US20180340006A1 (en) | 2018-11-29 |
| KR20170104453A (ko) | 2017-09-15 |
| MX375865B (es) | 2025-03-07 |
| TW201632538A (zh) | 2016-09-16 |
| CN107108688B (zh) | 2019-10-29 |
| KR102546748B1 (ko) | 2023-06-22 |
| HK1244287A1 (en) | 2018-08-03 |
| WO2016079519A1 (en) | 2016-05-26 |
| ES2748692T3 (es) | 2020-03-17 |
| DK3221333T3 (da) | 2019-09-30 |
| CN107108688A (zh) | 2017-08-29 |
| TWI686401B (zh) | 2020-03-01 |
| EP3221333B1 (en) | 2019-07-24 |
| WO2016079519A9 (en) | 2018-08-09 |
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