ES2968881T3 - Derivados de ácidos biliares fluorados - Google Patents
Derivados de ácidos biliares fluorados Download PDFInfo
- Publication number
- ES2968881T3 ES2968881T3 ES19748933T ES19748933T ES2968881T3 ES 2968881 T3 ES2968881 T3 ES 2968881T3 ES 19748933 T ES19748933 T ES 19748933T ES 19748933 T ES19748933 T ES 19748933T ES 2968881 T3 ES2968881 T3 ES 2968881T3
- Authority
- ES
- Spain
- Prior art keywords
- compound
- ethyl
- cholan
- fluoro
- general formula
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Active
Links
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)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 (1)
| Publication Number | Publication Date |
|---|---|
| ES2968881T3 true ES2968881T3 (es) | 2024-05-14 |
Family
ID=63518053
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ES19748933T Active ES2968881T3 (es) | 2018-07-30 | 2019-07-30 | Derivados de ácidos biliares fluorados |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11517577B2 (https=) |
| EP (1) | EP3830103B8 (https=) |
| JP (2) | JP7805783B2 (https=) |
| CN (1) | CN112771063B (https=) |
| ES (1) | ES2968881T3 (https=) |
| GB (1) | GB201812382D0 (https=) |
| WO (1) | WO2020025942A1 (https=) |
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 |
| TW202333741A (zh) * | 2021-11-15 | 2023-09-01 | 大陸商海湃泰克（北京）生物醫藥科技有限公司 | 多環化合物及其方法 |
| 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 |
| 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 |
| WO2025021195A1 (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 |
Family Cites Families (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| ES2306459T3 (es) | 1996-05-23 | 2008-11-01 | Novartis Ag | Prevencion y tratamiento de adenoma colonico o microadenoma colonico mediante acido 6-fluoroursodesoxicolico (6-fudca). |
| ES2248581T3 (es) | 2001-03-12 | 2006-03-16 | Intercept Pharmaceuticals, Inc. | Esteroides como agonistas de fxr. |
| CA2466033A1 (en) | 2001-11-08 | 2003-05-15 | The University Of Chicago | Method of treating disorder related to high cholesterol concentration |
| EP1568706A1 (en) | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for FXR |
| PL1734970T3 (pl) | 2004-03-12 | 2015-05-29 | Intercept Pharmaceuticals Inc | Leczenie zwłóknienia z zastosowaniem ligandów FXR |
| EP1737890A2 (en) | 2004-03-24 | 2007-01-03 | Xencor, Inc. | Immunoglobulin variants outside the fc region |
| 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 |
| 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 |
| US7932244B2 (en) | 2006-06-27 | 2011-04-26 | Intercept Pharmaceuticals, Inc. | Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions |
| KR101555716B1 (ko) | 2007-01-19 | 2015-09-25 | 인터셉트 파마슈티컬즈, 인크. | Ｔｇｒ5 조절제로서의 23-치환 담즙산 및 이의 사용 방법 |
| WO2010014836A2 (en) | 2008-07-30 | 2010-02-04 | Intercept Pharmaceuticals, Inc. | Tgr5 modulators and methods of use thereof |
| ES2774368T3 (es) | 2008-11-19 | 2020-07-20 | Intercept Pharmaceuticals Inc | Moduladores de TGR5 y métodos de uso de los mismos |
| DK2698375T3 (en) | 2008-11-19 | 2018-05-28 | Intercept Pharmaceuticals Inc | TGR5 modulators and methods for using them |
| SI3336097T1 (sl) | 2012-06-19 | 2021-07-30 | Intercept Pharmaceuticals, Inc. | Priprava nekristalinične oblike obetiholne kisline |
| SG11201503247UA (en) | 2012-10-26 | 2015-06-29 | 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 |
| CN105164161A (zh) | 2013-03-13 | 2015-12-16 | 萨奇治疗股份有限公司 | 神经活性类固醇、组合物、及其用途 |
| TN2015000497A1 (en) | 2013-05-14 | 2017-04-06 | Intercept Pharmaceuticals Inc | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
| CN104938001B (zh) | 2013-12-10 | 2019-04-12 | 华为终端有限公司 | 一种注册方法和相关节点以及注册系统 |
| SG11201703717SA (en) | 2014-11-06 | 2017-06-29 | Enanta Pharm Inc | Bile acid analogs an fxr/tgr5 agonists and methods of use thereof |
| KR102546748B1 (ko) | 2014-11-19 | 2023-06-22 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-3,7-다이온 스테로이드 |
| KR102527821B1 (ko) | 2014-11-19 | 2023-05-02 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드 |
| 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 |
| WO2016086134A1 (en) | 2014-11-26 | 2016-06-02 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| EP3223823A4 (en) | 2014-11-26 | 2018-10-17 | Enanta Pharmaceuticals, Inc. | Bile acid analogs 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 |
| 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 |
| CN105348365A (zh) | 2014-12-03 | 2016-02-24 | 四川百利药业有限责任公司 | 一种胆酸衍生物及其制备方法、药物组合物和用途 |
| TW201628625A (zh) | 2015-02-06 | 2016-08-16 | 英特賽普醫藥品公司 | 組合療法醫藥組成物 |
| EP3256134A4 (en) | 2015-02-11 | 2018-10-03 | Enanta Pharmaceuticals, Inc. | Bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| CN107530361A (zh) | 2015-03-09 | 2018-01-02 | 英特塞普特医药品公司 | 用于调节骨密度的方法 |
| WO2016145216A1 (en) | 2015-03-10 | 2016-09-15 | Metselex, Inc. | Fluorinated and alkylated bile acids |
| US20160279393A1 (en) | 2015-03-25 | 2016-09-29 | Covidien Lp | Guidewire retrieval catheter |
| WO2016161003A1 (en) | 2015-03-31 | 2016-10-06 | Enanta Phamraceuticals, Inc. | Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| US10894054B2 (en) | 2015-04-07 | 2021-01-19 | Intercept Pharmaceuticals, Inc. | FXR agonist compositions for combination therapy |
| PE20180690A1 (es) | 2015-04-27 | 2018-04-23 | Intercept Pharmaceuticals Inc | Composiciones de acido obeticolico y metodos de uso |
| WO2016173493A1 (en) * | 2015-04-28 | 2016-11-03 | Shanghai De Novo Pharmatech Co. Ltd. | Sulfonylaminocarbonyl derivative, pharmaceutical composition and uses thereof |
| JP2018519246A (ja) * | 2015-04-28 | 2018-07-19 | ジエンス ハンセン ファーマセウティカル グループ カンパニー リミテッド | コール酸誘導体、及びその製造方法及び医薬用途 |
| TW201704251A (zh) | 2015-04-29 | 2017-02-01 | 正大天晴藥業集團股份有限公司 | 鵝去氧膽酸衍生物 |
| CN106210599B (zh) | 2015-04-30 | 2021-02-12 | 中兴通讯股份有限公司 | 一种多画面调整方法、装置及多点控制单元 |
| 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 |
| KR20180030204A (ko) | 2015-07-30 | 2018-03-21 | 인터셉트 파마슈티컬즈, 인크. | 담즙산 및 이의 유도체를 제조하는 방법 |
| US10604544B2 (en) | 2015-08-07 | 2020-03-31 | Intercept Pharmaceuticals, Inc. | Methods for preparation of bile acids and derivatives 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 |
| CA2998876A1 (en) | 2015-09-21 | 2017-03-30 | Intercept Pharmaceuticals, Inc. | Methods of promoting hepatic regeneration |
| AU2016325619A1 (en) | 2015-09-24 | 2018-04-12 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation bile acid derivatives |
| MA42339A1 (fr) | 2015-10-07 | 2019-01-31 | Intercept Pharmaceuticals Inc | Modulateurs du récepteur farnésoïde x |
| AU2016350690C1 (en) | 2015-11-06 | 2020-04-23 | Intercept Pharmaceuticals, Inc. | Methods for the preparation of obeticholic acid and derivatives thereof |
| 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 |
| CN105646634A (zh) | 2016-01-29 | 2016-06-08 | 中国药科大学 | 奥贝胆酸杂质的制备方法 |
| WO2017147174A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof |
| US10323060B2 (en) | 2016-02-23 | 2019-06-18 | Enanta Pharmaceuticals, Inc. | Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof |
| WO2017147159A1 (en) | 2016-02-23 | 2017-08-31 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as fxr/tgr5 agonists and methods of use thereof |
| ES2874682T3 (es) | 2016-03-11 | 2021-11-05 | Intercept Pharmaceuticals Inc | Derivados de 3-desoxi y composiciones farmacéuticas de los mismos |
| 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 |
| GB201608776D0 (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 CN CN201980050077.0A patent/CN112771063B/zh active Active
- 2019-07-30 EP EP19748933.9A patent/EP3830103B8/en active Active
- 2019-07-30 WO PCT/GB2019/052127 patent/WO2020025942A1/en not_active Ceased
- 2019-07-30 JP JP2021529531A patent/JP7805783B2/ja active Active
- 2019-07-30 ES ES19748933T patent/ES2968881T3/es active Active
- 2019-07-30 US US17/262,915 patent/US11517577B2/en active Active
-
2024
- 2024-03-13 JP JP2024038682A patent/JP2024088648A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP3830103C0 (en) | 2023-11-08 |
| EP3830103B8 (en) | 2023-12-20 |
| WO2020025942A1 (en) | 2020-02-06 |
| EP3830103A1 (en) | 2021-06-09 |
| US11517577B2 (en) | 2022-12-06 |
| CN112771063A (zh) | 2021-05-07 |
| GB201812382D0 (en) | 2018-09-12 |
| JP2021533206A (ja) | 2021-12-02 |
| US20210299148A1 (en) | 2021-09-30 |
| JP2024088648A (ja) | 2024-07-02 |
| JP7805783B2 (ja) | 2026-01-26 |
| EP3830103B1 (en) | 2023-11-08 |
| CN112771063B (zh) | 2023-10-27 |
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