AR105648A1 - Métodos para la preparación de ácidos biliares y derivados de los mismos - Google Patents
Métodos para la preparación de ácidos biliares y derivados de los mismosInfo
- Publication number
- AR105648A1 AR105648A1 ARP160102432A ARP160102432A AR105648A1 AR 105648 A1 AR105648 A1 AR 105648A1 AR P160102432 A ARP160102432 A AR P160102432A AR P160102432 A ARP160102432 A AR P160102432A AR 105648 A1 AR105648 A1 AR 105648A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- solvate
- amino acid
- pharmaceutically acceptable
- Prior art date
Links
- 239000003613 bile acid Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 8
- 150000001413 amino acids Chemical class 0.000 abstract 3
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 239000012453 solvate Substances 0.000 abstract 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 229910052739 hydrogen Inorganic materials 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 229910004727 OSO3H Inorganic materials 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000000304 alkynyl group Chemical group 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 229910052757 nitrogen Inorganic materials 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07J—STEROIDS
- C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
- C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
-
- 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
-
- 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
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Peptides Or Proteins (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Reivindicación 1: Un método para preparar un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable, solvato, o conjugado de aminoácidos del mismo, en donde: R¹ es a-OH o un grupo oxo; R² es H, F, a-alquilo C₁₋₃ opcionalmente sustituido con F o OH, a-alcoxi C₁₋₃, a-alquenilo o alquinilo C₂₋₃, o cicloalquilo; R³ o R⁷ son independientemente H, F, o C₁₋₄ alquilo opcionalmente sustituido con F o OH, o R³ o R⁷ tomado junto con otro R³ o R⁷ en un átomo de carbono adyacente forma un anillo carbocíclico o heterocíclico C₁₋₆ sustituido o no sustituido; R⁴ y R⁵ y R⁸ son cada uno independientemente H, a-OH, o b-OH; R⁶ es CO₂H, OSO₃H, NH₂, NHCO₂(CH₂CHCH)fenilo, NHCO₂CH₂CH₃, C(O)NHOH, C(O)NH(CH₂)₂OH, CONH(CH₂)₂OSO₃H, o un heterociclo de 5 miembros opcionalmente sustituido que comprende 1 - 4 heteroátomos seleccionados de N, S y O; y n es 0, 1, 2 ó 3; que comprende las etapas de: (i) convertir el compuesto de fórmula (2) en el compuesto de fórmula (3) en donde la línea ondulada indica que el OH en la posición C₃ o en la posición C₇ se encuentra en una estereoquímica a o b; y (ii) convertir el compuesto de fórmula (3) en un compuesto de la fórmula (1). Reivindicación 4: El compuesto de la reivindicación 1, en donde el compuesto es de la fórmula (4), o una sal farmacéuticamente aceptable, solvato, o conjugado de aminoácidos del mismo, en donde: R² es a-alquilo C₁₋₃; y R³ es H o alquilo C₁₋₄. Reivindicación 25: Un compuesto que tiene la estructura de fórmula (5), o una sal farmacéuticamente aceptable, solvato, o conjugado de aminoácidos del mismo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562202300P | 2015-08-07 | 2015-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR105648A1 true AR105648A1 (es) | 2017-10-25 |
Family
ID=57983768
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP160102432A AR105648A1 (es) | 2015-08-07 | 2016-08-08 | Métodos para la preparación de ácidos biliares y derivados de los mismos |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US10604544B2 (es) |
| EP (1) | EP3331896A4 (es) |
| JP (1) | JP2018522054A (es) |
| KR (1) | KR20180028544A (es) |
| CN (1) | CN108137643A (es) |
| AR (1) | AR105648A1 (es) |
| AU (1) | AU2016306297A1 (es) |
| BR (1) | BR112018002499A2 (es) |
| CA (1) | CA2994687A1 (es) |
| HK (1) | HK1252688A1 (es) |
| IL (1) | IL257235A (es) |
| MX (1) | MX2018001491A (es) |
| TW (1) | TW201714891A (es) |
| WO (1) | WO2017027396A1 (es) |
Families Citing this family (33)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015343025A1 (en) | 2014-11-06 | 2017-06-08 | Enanta Pharmaceuticals, Inc. | Bile acid analogs an 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 |
| US10208081B2 (en) | 2014-11-26 | 2019-02-19 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| MX2017006833A (es) | 2014-11-26 | 2018-02-13 | Enanta Pharm Inc | Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos. |
| US10246483B2 (en) | 2015-02-11 | 2019-04-02 | Enanta Pharmaceuticals, Inc. | Bile acid analogs as FXR/TGR5 agonists and methods of use thereof |
| JP6785788B2 (ja) | 2015-03-31 | 2020-11-18 | 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誘導体およびその使用方法 |
| AU2016325619A1 (en) | 2015-09-24 | 2018-04-12 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation bile acid derivatives |
| US10323061B2 (en) | 2016-02-23 | 2019-06-18 | 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 |
| US10364267B2 (en) | 2016-02-23 | 2019-07-30 | Enanta Pharmaceuticals, Inc. | Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof |
| CN108883305B (zh) * | 2016-03-11 | 2021-03-16 | 英特塞普特医药品公司 | 3-脱氧衍生物及其药物组合物 |
| MX2019003684A (es) * | 2016-09-30 | 2019-08-05 | Intercept Pharmaceuticals Inc | Formas cristalinas de un derivado de acido biliar. |
| EP3305799A3 (en) * | 2016-10-07 | 2018-06-20 | Lupin Limited | Salts of obeticholic acid |
| CA3045023A1 (en) | 2016-11-29 | 2018-06-07 | Enanta Pharmaceuticals, Inc. | Process for preparation of sulfonylurea bile acid derivatives |
| US10472386B2 (en) | 2017-02-14 | 2019-11-12 | Enanta Pharmaceuticals, Inc. | Bile acid derivatives as FXR agonists and methods of use thereof |
| JP7136802B2 (ja) | 2017-04-07 | 2022-09-13 | 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 | スルホニルカルバマート胆汁酸誘導体の調製のためのプロセス |
| CN107298694A (zh) * | 2017-04-21 | 2017-10-27 | 华东师范大学 | 奥贝胆酸的合成方法及其中间体 |
| AU2018288883B2 (en) | 2017-06-23 | 2022-06-02 | Intercept Pharmaceuticals, Inc. | Methods and intermediates for the preparation of bile acid derivatives |
| CN110869381B (zh) * | 2017-07-26 | 2021-11-19 | 正大天晴药业集团股份有限公司 | 甾体类衍生物fxr激动剂的制备方法 |
| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| PH12022550852A1 (en) | 2019-10-07 | 2023-05-03 | Kallyope Inc | Gpr119 agonists |
| US20240325458A1 (en) * | 2020-01-16 | 2024-10-03 | Keio University | Composition for producing bile acids |
| CA3173731A1 (en) | 2020-02-28 | 2021-09-02 | Kallyope, Inc. | Gpr40 agonists |
| KR20230012597A (ko) | 2020-05-19 | 2023-01-26 | 칼리오페, 인크. | Ampk 활성화제 |
| AU2021297323A1 (en) | 2020-06-26 | 2023-02-16 | Kallyope, Inc. | AMPK activators |
| CN112831536B (zh) * | 2021-03-02 | 2022-07-15 | 江南大学 | 细胞色素p450单加氧酶在催化石胆酸生产熊去氧胆酸中的应用 |
| CN113528606B (zh) * | 2021-07-22 | 2023-05-05 | 湖州颐盛生物科技有限公司 | 一种酶催化制备17β-羟基类固醇的方法 |
| CN115806578B (zh) * | 2021-09-15 | 2024-11-15 | 成都百泉生物医药科技有限公司 | Nor-UDCA中间体、Nor-UDCA及其中间体的制备方法 |
| CN113968891B (zh) * | 2021-11-15 | 2023-04-07 | 湖南科瑞生物制药股份有限公司 | 一种植物源7-酮基石胆酸的制备方法 |
| CN114276401A (zh) * | 2021-12-27 | 2022-04-05 | 中山百灵生物技术股份有限公司 | 一种24-去甲熊去氧胆酸的合成方法 |
| EP4615461A1 (en) * | 2022-11-11 | 2025-09-17 | Intercept Pharmaceuticals, Inc. | Crystalline forms of a farnesoid x receptor agonist |
| CN117510567B (zh) * | 2023-10-26 | 2025-10-28 | 长沙启晟合研医药科技有限公司 | 一种制备高纯度阿法沙龙的方法 |
| CN119320419A (zh) * | 2024-10-28 | 2025-01-17 | 苏州恩泰新材料科技有限公司 | 一种24-去甲熊去氧胆酸的合成方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2757156A1 (de) | 1977-12-19 | 1979-06-21 | Schering Ag | Verfahren zur herstellung von 21-hydroxy-20-methyl-pregnan-derivaten |
| US4212940A (en) | 1978-12-19 | 1980-07-15 | Schering Aktiengesellschaft | Process for the preparation of 21-hydroxy-20-methylpregnane derivatives |
| US4230625A (en) * | 1979-04-12 | 1980-10-28 | Hoffmann-La Roche Inc. | Process for chenodeoxycholic acid and intermediates therefore |
| EA017714B1 (ru) | 2007-01-19 | 2013-02-28 | Интерсепт Фармасьютикалз, Инк. | Модуляторы tgr5 и способы их применения |
| US20130261317A1 (en) | 2010-09-27 | 2013-10-03 | Kythera Biopharmaceuticals, Inc. | Methods for preparing synthetic bile acids and compositions comprising the same |
| CN105348354A (zh) * | 2014-12-03 | 2016-02-24 | 四川百利药业有限责任公司 | 一类鹅去氧胆酸类化合物及其制备方法和用途 |
-
2016
- 2016-08-05 MX MX2018001491A patent/MX2018001491A/es unknown
- 2016-08-05 BR BR112018002499A patent/BR112018002499A2/pt not_active Application Discontinuation
- 2016-08-05 KR KR1020187006277A patent/KR20180028544A/ko not_active Withdrawn
- 2016-08-05 EP EP16835703.6A patent/EP3331896A4/en not_active Withdrawn
- 2016-08-05 HK HK18111996.1A patent/HK1252688A1/zh unknown
- 2016-08-05 WO PCT/US2016/045831 patent/WO2017027396A1/en not_active Ceased
- 2016-08-05 CA CA2994687A patent/CA2994687A1/en not_active Abandoned
- 2016-08-05 AU AU2016306297A patent/AU2016306297A1/en not_active Abandoned
- 2016-08-05 CN CN201680054598.XA patent/CN108137643A/zh active Pending
- 2016-08-05 US US15/750,683 patent/US10604544B2/en active Active
- 2016-08-05 JP JP2018506143A patent/JP2018522054A/ja active Pending
- 2016-08-08 AR ARP160102432A patent/AR105648A1/es unknown
- 2016-08-08 TW TW105125130A patent/TW201714891A/zh unknown
-
2018
- 2018-01-30 IL IL257235A patent/IL257235A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| TW201714891A (zh) | 2017-05-01 |
| BR112018002499A2 (pt) | 2018-09-18 |
| MX2018001491A (es) | 2018-04-24 |
| KR20180028544A (ko) | 2018-03-16 |
| IL257235A (en) | 2018-03-29 |
| CA2994687A1 (en) | 2017-02-16 |
| WO2017027396A1 (en) | 2017-02-16 |
| AU2016306297A1 (en) | 2018-02-22 |
| US10604544B2 (en) | 2020-03-31 |
| EP3331896A4 (en) | 2019-08-14 |
| US20180222937A1 (en) | 2018-08-09 |
| JP2018522054A (ja) | 2018-08-09 |
| EP3331896A1 (en) | 2018-06-13 |
| HK1252688A1 (zh) | 2019-05-31 |
| CN108137643A (zh) | 2018-06-08 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |