MX2017006565A - Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la produccion de moduladores esteroides del receptor x farnesoide (fxr). - Google Patents
Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la produccion de moduladores esteroides del receptor x farnesoide (fxr).Info
- Publication number
- MX2017006565A MX2017006565A MX2017006565A MX2017006565A MX2017006565A MX 2017006565 A MX2017006565 A MX 2017006565A MX 2017006565 A MX2017006565 A MX 2017006565A MX 2017006565 A MX2017006565 A MX 2017006565A MX 2017006565 A MX2017006565 A MX 2017006565A
- Authority
- MX
- Mexico
- Prior art keywords
- intermediates
- alpha
- alkyl
- production
- fxr modulators
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title 1
- 230000003637 steroidlike Effects 0.000 title 1
- 150000003431 steroids Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 239000003613 bile acid Substances 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
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)
Abstract
La invención se refiere a compuestos de la fórmula (I) en donde R1, R2, Y1, R4 y R5 son como se definen aquí; los compuestos son intermedios en la síntesis de ácidos biliares sintéticos.(ver Fórmula).
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 |
|---|---|
| MX2017006565A true MX2017006565A (es) | 2018-01-26 |
| MX375865B MX375865B (es) | 2025-03-07 |
Family
ID=54704021
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017006565A MX375865B (es) | 2014-11-19 | 2015-11-19 | Esteroides de 6.alfa-alquil-3,7-diona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr). |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10538550B2 (es) |
| EP (1) | EP3221333B1 (es) |
| JP (1) | JP6735748B2 (es) |
| KR (1) | KR102546748B1 (es) |
| CN (1) | CN107108688B (es) |
| CA (1) | CA2968305A1 (es) |
| DK (1) | DK3221333T3 (es) |
| EA (1) | EA034739B1 (es) |
| ES (1) | ES2748692T3 (es) |
| MX (1) | MX375865B (es) |
| PL (1) | PL3221333T3 (es) |
| TW (1) | TWI686401B (es) |
| WO (1) | WO2016079519A1 (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20170327531A1 (en) | 2014-11-19 | 2017-11-16 | NZP UK Limited | 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators |
| CN107207559B (zh) | 2014-11-19 | 2019-10-25 | Nzp英国有限公司 | 作为制备类固醇fxr调节剂的中间体的6-烷基-7-羟基-4-烯-3-酮类固醇 |
| PL3221332T3 (pl) | 2014-11-19 | 2019-10-31 | Nzp Uk Ltd | Steroidy, 5.beta.-6-alkilo-7-hydroksy-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr |
| 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 |
| 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 |
| GB201608779D0 (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 |
| EP3890745B1 (en) * | 2018-12-04 | 2025-11-19 | President and Fellows of Harvard College | Synthetic derivatives of cholic acid 7-sulfate and uses thereof |
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| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| EP2112995B1 (en) | 2007-01-19 | 2013-07-31 | Intercept Pharmaceuticals, Inc. | 23-substituted bile acids as tgr5 modulators and methods of use thereof |
| 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 |
| EP2376519B1 (en) | 2008-11-19 | 2013-11-13 | Intercept Pharmaceuticals, Inc. | Tgr5 modulators and method of use thereof |
| ES2592452T3 (es) * | 2008-11-19 | 2016-11-30 | Intercept Pharmaceuticals, Inc. | Moduladores de TGR5 y métodos de uso de los mismos |
| US8829213B2 (en) | 2009-07-29 | 2014-09-09 | The University Of Chicago | Liver X receptor agonists |
| SG11201408501UA (en) * | 2012-06-19 | 2015-01-29 | Intercept Pharmaceuticals Inc | Preparation, uses and solid forms of obeticholic acid |
| AU2013334122B2 (en) | 2012-10-26 | 2017-11-02 | Intercept Pharmaceuticals, Inc. | Process for preparing bile acid derivatives |
| NZ708501A (en) * | 2012-11-28 | 2019-03-29 | Intercept Pharmaceuticals Inc | Treatment of pulmonary disease |
| US20140206657A1 (en) * | 2013-01-18 | 2014-07-24 | City Of Hope | Bile acid analog tgr5 agonists |
| PT2997035T (pt) | 2013-05-14 | 2018-07-18 | Intercept Pharmaceuticals Inc | Derivados de 11-hidroxilo substituídos em 6 de ácidos biliares e seus conjugados de aminoácido como moduladores do recetor farnesoide x |
| HK1223361A1 (zh) | 2013-05-24 | 2017-07-28 | Société des Produits Nestlé S.A. | 用於预测肠易激综合征诊断的途径特异性测定 |
| WO2015183794A1 (en) | 2014-05-27 | 2015-12-03 | City Of Hope | Tgr5 agonist complexes for treating diabetes and cancer |
| CN106661079B (zh) | 2014-05-29 | 2019-03-01 | 巴尔制药有限公司 | 用于治疗和/或预防fxr和tgr5/gpbar1介导的疾病的胆烷衍生物 |
| KR20170094184A (ko) | 2014-11-06 | 2017-08-17 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
| CN107207559B (zh) | 2014-11-19 | 2019-10-25 | Nzp英国有限公司 | 作为制备类固醇fxr调节剂的中间体的6-烷基-7-羟基-4-烯-3-酮类固醇 |
| PL3221332T3 (pl) | 2014-11-19 | 2019-10-31 | Nzp Uk Ltd | Steroidy, 5.beta.-6-alkilo-7-hydroksy-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr |
| US20170327531A1 (en) | 2014-11-19 | 2017-11-16 | NZP UK Limited | 6.alpha.-alkyl-6,7-dione steroids as intermediates for the production of steroidal fxr modulators |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| KR20170099909A (ko) | 2014-11-26 | 2017-09-01 | 이난타 파마슈티칼스, 인코포레이티드 | Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법 |
| 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 |
| 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 |
| CN107771180B (zh) | 2015-06-19 | 2021-03-23 | 英特塞普特医药品公司 | Tgr5调节剂及其使用方法 |
| 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 CN CN201580062897.3A patent/CN107108688B/zh active Active
- 2015-11-19 JP JP2017527790A patent/JP6735748B2/ja active Active
- 2015-11-19 KR KR1020177016857A patent/KR102546748B1/ko active Active
- 2015-11-19 TW TW104138185A patent/TWI686401B/zh not_active IP Right Cessation
- 2015-11-19 US US15/528,331 patent/US10538550B2/en active Active
- 2015-11-19 MX MX2017006565A patent/MX375865B/es active IP Right Grant
- 2015-11-19 CA CA2968305A patent/CA2968305A1/en not_active Abandoned
- 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 DK DK15800911.8T patent/DK3221333T3/da active
- 2015-11-19 EA EA201790879A patent/EA034739B1/ru unknown
- 2015-11-19 EP EP15800911.8A patent/EP3221333B1/en active Active
- 2015-11-19 ES ES15800911T patent/ES2748692T3/es active Active
Also Published As
| Publication number | Publication date |
|---|---|
| TWI686401B (zh) | 2020-03-01 |
| US20180340006A1 (en) | 2018-11-29 |
| JP2017538690A (ja) | 2017-12-28 |
| TW201632538A (zh) | 2016-09-16 |
| EA201790879A1 (ru) | 2017-11-30 |
| CA2968305A1 (en) | 2016-05-26 |
| JP6735748B2 (ja) | 2020-08-05 |
| EP3221333B1 (en) | 2019-07-24 |
| US10538550B2 (en) | 2020-01-21 |
| KR102546748B1 (ko) | 2023-06-22 |
| PL3221333T3 (pl) | 2020-01-31 |
| KR20170104453A (ko) | 2017-09-15 |
| EP3221333A1 (en) | 2017-09-27 |
| DK3221333T3 (da) | 2019-09-30 |
| HK1244287A1 (en) | 2018-08-03 |
| WO2016079519A9 (en) | 2018-08-09 |
| CN107108688A (zh) | 2017-08-29 |
| CN107108688B (zh) | 2019-10-29 |
| ES2748692T3 (es) | 2020-03-17 |
| WO2016079519A1 (en) | 2016-05-26 |
| EA034739B1 (ru) | 2020-03-16 |
| MX375865B (es) | 2025-03-07 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |