CN112771063B - 氟化胆汁酸衍生物 - Google Patents
氟化胆汁酸衍生物 Download PDFInfo
- Publication number
- CN112771063B CN112771063B CN201980050077.0A CN201980050077A CN112771063B CN 112771063 B CN112771063 B CN 112771063B CN 201980050077 A CN201980050077 A CN 201980050077A CN 112771063 B CN112771063 B CN 112771063B
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- China
- Prior art keywords
- compound
- ethyl
- cholan
- fluoro
- dihydroxy
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Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/64—Sulfonylureas, e.g. glibenclamide, tolbutamide, chlorpropamide
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/575—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
-
- 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
- C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
- C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
- C07J41/0055—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives
- C07J41/0061—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 the 17-beta position being substituted by an uninterrupted chain of at least three carbon atoms which may or may not be branched, e.g. cholane or cholestane derivatives, optionally cyclised, e.g. 17-beta-phenyl or 17-beta-furyl derivatives one of the carbon atoms being part of an amide group
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J11/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
-
- 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
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1812382.8 | 2018-07-30 | ||
| GBGB1812382.8A GB201812382D0 (en) | 2018-07-30 | 2018-07-30 | Compounds |
| PCT/GB2019/052127 WO2020025942A1 (en) | 2018-07-30 | 2019-07-30 | Fluorinated bile acid derivatives |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN112771063A CN112771063A (zh) | 2021-05-07 |
| CN112771063B true CN112771063B (zh) | 2023-10-27 |
Family
ID=63518053
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201980050077.0A Active CN112771063B (zh) | 2018-07-30 | 2019-07-30 | 氟化胆汁酸衍生物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11517577B2 (enExample) |
| EP (1) | EP3830103B8 (enExample) |
| JP (1) | JP2024088648A (enExample) |
| CN (1) | CN112771063B (enExample) |
| ES (1) | ES2968881T3 (enExample) |
| GB (1) | GB201812382D0 (enExample) |
| WO (1) | WO2020025942A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201820887D0 (en) * | 2018-12-20 | 2019-02-06 | Nzp Uk Ltd | Compounds |
| CN118660883A (zh) * | 2021-11-15 | 2024-09-17 | 海湃泰克(北京)生物医药科技有限公司 | 多环化合物及其方法 |
| CN115819491A (zh) * | 2022-12-22 | 2023-03-21 | 江苏佳尔科药业集团股份有限公司 | 7-酮基石胆酸及熊去氧胆酸的合成方法 |
| TW202508555A (zh) * | 2023-07-27 | 2025-03-01 | 大陸商珂闌(上海)醫藥科技有限公司 | 甾類化合物、其製備方法和應用 |
| WO2025020190A1 (zh) * | 2023-07-27 | 2025-01-30 | 珂阑(上海)医药科技有限公司 | 甾类化合物、其制备方法和应用 |
| CN119371475B (zh) * | 2023-07-27 | 2025-11-04 | 珂阑(上海)医药科技有限公司 | 甾类化合物、其制备方法和应用 |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2016073767A1 (en) * | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| WO2016173493A1 (en) * | 2015-04-28 | 2016-11-03 | Shanghai De Novo Pharmatech Co. Ltd. | Sulfonylaminocarbonyl derivative, pharmaceutical composition and uses thereof |
| 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 |
| EP3290429A1 (en) * | 2015-04-28 | 2018-03-07 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Cholic acid derivative, and preparation method and medical use thereof |
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| US5175320A (en) | 1989-04-17 | 1992-12-29 | Giuliani S.P.A. | Fluorinated bile acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them |
| CA2253593C (en) | 1996-05-23 | 2008-07-08 | Novartis Ag | Prevention and treatment of colorectal cancer by 6-fluoroursodeoxycholic acid (6-fudca) |
| IL157816A0 (en) | 2001-03-12 | 2004-03-28 | Roberto Pellicciari | Steroids as agonists for fxr |
| EP1450816A4 (en) | 2001-11-08 | 2008-02-13 | Univ Chicago | METHOD OF TREATING DISORDERS RELATED TO HIGH CHOLESTEROL RATE |
| EP1568706A1 (en) | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for FXR |
| HUE024952T2 (en) | 2004-03-12 | 2016-02-29 | Intercept Pharmaceuticals Inc | Treatment of fibrosis using FXR ligands |
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| 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 |
| JP2010517931A (ja) | 2006-02-14 | 2010-05-27 | 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 | Fxr媒介性の疾患または状態の予防または治療用のfxrリガンドとしての胆汁酸誘導体 |
| CA2656320C (en) | 2006-06-27 | 2015-04-28 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases 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 |
| BRPI0916735B8 (pt) | 2008-07-30 | 2021-05-25 | Intercept Pharmaceuticals Inc | compostos moduladores de tgr5, composições farmacêuticas compreendendo os mesmos e seus usos |
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| EP3336097B1 (en) | 2012-06-19 | 2020-08-19 | Intercept Pharmaceuticals, Inc. | Preparation of the non-crystalline form of obeticholic acid |
| JP6272888B2 (ja) | 2012-10-26 | 2018-01-31 | 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 | 胆汁酸誘導体を調製するためのプロセス |
| US20140206657A1 (en) | 2013-01-18 | 2014-07-24 | City Of Hope | Bile acid analog tgr5 agonists |
| IL286970B2 (en) | 2013-03-13 | 2024-11-01 | Sage Therapeutics Inc | Neuroactive steroids and methods of use thereof |
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| GB201608776D0 (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 |
| GB201608779D0 (en) | 2016-05-18 | 2016-06-29 | Dextra Lab Ltd | Methods and compounds |
-
2018
- 2018-07-30 GB GBGB1812382.8A patent/GB201812382D0/en not_active Ceased
-
2019
- 2019-07-30 US US17/262,915 patent/US11517577B2/en active Active
- 2019-07-30 CN CN201980050077.0A patent/CN112771063B/zh active Active
- 2019-07-30 ES ES19748933T patent/ES2968881T3/es active Active
- 2019-07-30 WO PCT/GB2019/052127 patent/WO2020025942A1/en not_active Ceased
- 2019-07-30 EP EP19748933.9A patent/EP3830103B8/en active Active
-
2024
- 2024-03-13 JP JP2024038682A patent/JP2024088648A/ja active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016073767A1 (en) * | 2014-11-06 | 2016-05-12 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| WO2016173493A1 (en) * | 2015-04-28 | 2016-11-03 | Shanghai De Novo Pharmatech Co. Ltd. | Sulfonylaminocarbonyl derivative, pharmaceutical composition and uses thereof |
| EP3290429A1 (en) * | 2015-04-28 | 2018-03-07 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | Cholic acid derivative, and preparation method and medical use thereof |
| 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 |
Also Published As
| Publication number | Publication date |
|---|---|
| CN112771063A (zh) | 2021-05-07 |
| WO2020025942A1 (en) | 2020-02-06 |
| EP3830103B1 (en) | 2023-11-08 |
| EP3830103A1 (en) | 2021-06-09 |
| US11517577B2 (en) | 2022-12-06 |
| EP3830103B8 (en) | 2023-12-20 |
| JP2024088648A (ja) | 2024-07-02 |
| GB201812382D0 (en) | 2018-09-12 |
| JP2021533206A (ja) | 2021-12-02 |
| EP3830103C0 (en) | 2023-11-08 |
| US20210299148A1 (en) | 2021-09-30 |
| ES2968881T3 (es) | 2024-05-14 |
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Effective date of registration: 20250409 Address after: British Bristow Patentee after: NZP UK Ltd. Country or region after: Britain Address before: British Bristow Patentee before: NZP UK Ltd. Country or region before: Britain Patentee before: University OF SOUTHAMPTON |
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