CN110869381A - 甾体类衍生物fxr激动剂的制备方法 - Google Patents
甾体类衍生物fxr激动剂的制备方法 Download PDFInfo
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- CN110869381A CN110869381A CN201880047098.2A CN201880047098A CN110869381A CN 110869381 A CN110869381 A CN 110869381A CN 201880047098 A CN201880047098 A CN 201880047098A CN 110869381 A CN110869381 A CN 110869381A
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- FGZJXVSDDHVZAH-UHFFFAOYSA-N ethoxyethane silane Chemical group [SiH4].CCOCC FGZJXVSDDHVZAH-UHFFFAOYSA-N 0.000 claims description 16
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- C07J—STEROIDS
- C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
- C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
-
- 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
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
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
属于药物化学领域，涉及甾体类衍生物FXR激动剂的制备方法及相关中间体。具体而言，涉及一种制备式I化合物的方法，其包括使式8化合物和式9化合物反应以获得式10化合物，从式10化合物反应以获得式11化合物，从式11化合物反应以获得式I化合物，以及所用中间体、中间体的制备方法和中间体的用途。该制备方法反应条件温和，部分步骤可以同时转变多个基团，有效缩短步骤，适合工业化生产。(I)
Description
PCT国内申请，说明书已公开。
Claims (20)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2017106194201 | 2017-07-26 | ||
| CN201710619420 | 2017-07-26 | ||
| PCT/CN2018/097158 WO2019020067A1 (zh) | 2017-07-26 | 2018-07-26 | 甾体类衍生物fxr激动剂的制备方法 |
Publications (2)
| Publication Number | Publication Date |
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| CN110869381A true CN110869381A (zh) | 2020-03-06 |
| CN110869381B CN110869381B (zh) | 2021-11-19 |
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| Country | Link |
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| US (1) | US11059854B2 (zh) |
| EP (1) | EP3660030A4 (zh) |
| JP (1) | JP7308811B2 (zh) |
| CN (1) | CN110869381B (zh) |
| WO (1) | WO2019020067A1 (zh) |
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| WO2019020068A1 (zh) * | 2017-07-26 | 2019-01-31 | 正大天晴药业集团股份有限公司 | 甾体类衍生物fxr激动剂的结晶或无定型物、其制备方法和用途 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105102425A (zh) * | 2012-10-26 | 2015-11-25 | 英特塞普特医药品公司 | 制备胆汁酸衍生物的方法 |
| WO2016161003A1 (en) * | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| CN106083978A (zh) * | 2015-04-28 | 2016-11-09 | 上海迪诺医药科技有限公司 | 磺酰基氨基羰基衍生物、其药物组合物及应用 |
| CN106661079A (zh) * | 2014-05-29 | 2017-05-10 | 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 |
| WO2017129125A1 (zh) * | 2016-01-28 | 2017-08-03 | 正大天晴药业集团股份有限公司 | 甾体类衍生物fxr激动剂 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2326850T3 (es) | 1998-12-23 | 2009-10-20 | Glaxo Group Limited | Ensayos para ligandos de receptores nucleares. |
| CN111574577B (zh) * | 2015-04-29 | 2025-02-25 | 正大天晴药业集团股份有限公司 | 鹅去氧胆酸衍生物 |
| AU2016306297A1 (en) | 2015-08-07 | 2018-02-22 | Intercept Pharmaceuticals, Inc. | Methods for preparation of bile acids and derivatives thereof |
| JP6824966B2 (ja) | 2015-09-21 | 2021-02-03 | 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 | 肝臓の再生を促進する方法 |
| US11072631B2 (en) | 2015-09-24 | 2021-07-27 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation bile acid derivatives |
| WO2017079062A1 (en) * | 2015-11-06 | 2017-05-11 | Intercept Pharmaceuticals, Inc. | Methods for the preparation of obeticholic acid and derivatives thereof |
| WO2017147137A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as fxr/tgr5 agonists and methods of use thereof |
| WO2019020068A1 (zh) | 2017-07-26 | 2019-01-31 | 正大天晴药业集团股份有限公司 | 甾体类衍生物fxr激动剂的结晶或无定型物、其制备方法和用途 |
-
2018
- 2018-07-26 JP JP2020504103A patent/JP7308811B2/ja active Active
- 2018-07-26 EP EP18837478.9A patent/EP3660030A4/en not_active Withdrawn
- 2018-07-26 US US16/633,122 patent/US11059854B2/en active Active
- 2018-07-26 WO PCT/CN2018/097158 patent/WO2019020067A1/zh not_active Ceased
- 2018-07-26 CN CN201880047098.2A patent/CN110869381B/zh active Active
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105102425A (zh) * | 2012-10-26 | 2015-11-25 | 英特塞普特医药品公司 | 制备胆汁酸衍生物的方法 |
| CN106661079A (zh) * | 2014-05-29 | 2017-05-10 | 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 |
| WO2016161003A1 (en) * | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| CN106083978A (zh) * | 2015-04-28 | 2016-11-09 | 上海迪诺医药科技有限公司 | 磺酰基氨基羰基衍生物、其药物组合物及应用 |
| WO2017129125A1 (zh) * | 2016-01-28 | 2017-08-03 | 正大天晴药业集团股份有限公司 | 甾体类衍生物fxr激动剂 |
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| Title |
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| ACS: "RN1612191-84-0", 《REGISTRY》 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3660030A1 (en) | 2020-06-03 |
| US20200231622A1 (en) | 2020-07-23 |
| WO2019020067A1 (zh) | 2019-01-31 |
| JP7308811B2 (ja) | 2023-07-14 |
| US11059854B2 (en) | 2021-07-13 |
| EP3660030A4 (en) | 2021-04-21 |
| CN110869381B (zh) | 2021-11-19 |
| JP2020528068A (ja) | 2020-09-17 |
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