CN105377870B - 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物 - Google Patents
作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物 Download PDFInfo
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- CN105377870B CN105377870B CN201480036949.5A CN201480036949A CN105377870B CN 105377870 B CN105377870 B CN 105377870B CN 201480036949 A CN201480036949 A CN 201480036949A CN 105377870 B CN105377870 B CN 105377870B
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- 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
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- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
- 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
- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Urology & Nephrology (AREA)
- Pulmonology (AREA)
- Steroid Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810162562.4A CN108245523B (zh) | 2013-05-14 | 2014-05-14 | 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361823169P | 2013-05-14 | 2013-05-14 | |
| US61/823,169 | 2013-05-14 | ||
| PCT/EP2014/059896 WO2014184271A1 (en) | 2013-05-14 | 2014-05-14 | 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810162562.4A Division CN108245523B (zh) | 2013-05-14 | 2014-05-14 | 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105377870A CN105377870A (zh) | 2016-03-02 |
| CN105377870B true CN105377870B (zh) | 2018-04-03 |
Family
ID=50721801
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201480036949.5A Active CN105377870B (zh) | 2013-05-14 | 2014-05-14 | 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物 |
| CN201810162562.4A Expired - Fee Related CN108245523B (zh) | 2013-05-14 | 2014-05-14 | 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810162562.4A Expired - Fee Related CN108245523B (zh) | 2013-05-14 | 2014-05-14 | 作为法尼醇x受体调节剂的胆汁酸的11-羟基衍生物及其氨基酸共轭物 |
Country Status (37)
Families Citing this family (61)
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| DK1392714T3 (da) | 2001-03-12 | 2006-01-09 | Intercept Pharmaceuticals Inc | Steroider som agonister for FXR |
| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| CN105377870B (zh) | 2013-05-14 | 2018-04-03 | 英特塞普特医药品公司 | 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物 |
| US10077268B2 (en) | 2014-03-13 | 2018-09-18 | Salk Institute For Biological Studies | FXR agonists and methods for making and using |
| US10301268B2 (en) | 2014-03-13 | 2019-05-28 | The Salk Institute For Biological Studies | Analogs of fexaramine and methods of making and using |
| SI3626725T1 (sl) | 2014-05-29 | 2023-04-28 | Bar Pharmaceuticals S.R.L. | Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1 |
| BR112017009657A2 (pt) | 2014-11-06 | 2018-01-23 | Enanta Pharmaceuticals, Inc | análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos |
| JP6698085B2 (ja) | 2014-11-19 | 2020-05-27 | エヌゼットピー ユーケー リミテッド | ステロイドＦＸＲモジュレーター製造のための中間体としての６α−アルキル−６，７−ジオン−ステロイド |
| ES2748692T3 (es) | 2014-11-19 | 2020-03-17 | Nzp Uk Ltd | Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la producción de moduladores FXR de esteroides |
| KR102526632B1 (ko) | 2014-11-19 | 2023-04-27 | 엔제트피 유케이 리미티드 | 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드 |
| EA033427B1 (ru) | 2014-11-19 | 2019-10-31 | Nzp Uk Ltd | 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr |
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| ES2905872T3 (es) * | 2015-02-06 | 2022-04-12 | Intercept Pharmaceuticals Inc | Composiciones farmacéuticas para terapia combinada |
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| JP2018507880A (ja) * | 2015-03-09 | 2018-03-22 | 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 | 骨密度を調節する方法 |
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| AU2016233579A1 (en) * | 2015-03-13 | 2017-10-12 | Salk Institute For Biological Studies | Treating latent autoimmune diabetes of adults with farnesoid X receptor agonists to activate intestinal receptors |
| RU2712099C2 (ru) | 2015-03-31 | 2020-01-24 | Энанта Фармасьютикалс, Инк. | Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения |
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| US2802775A (en) * | 1953-05-29 | 1957-08-13 | Merck & Co Inc | 11 alpha-hydroxylation of steroids by aspergillus ochraceus |
| EP0124903A1 (en) * | 1983-05-09 | 1984-11-14 | Kuraray Co., Ltd. | 11-Hydroxypregn-4-en-3-one-20-carbaldehyde and a method for its production |
| WO2004007521A2 (en) * | 2002-07-12 | 2004-01-22 | Roberto Pellicciari | Bile acid derivatives as agonists of the farnesoid x receptor |
| EP1568706A1 (en) * | 2004-02-26 | 2005-08-31 | Intercept Pharmaceuticals, Inc. | Novel steroid agonist for FXR |
| CN101522703A (zh) * | 2006-06-27 | 2009-09-02 | 英特塞普特医药品公司 | 胆酸派生物作为fxr配基预防或治疗fxr-介导的疾病或状况 |
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| CN105377870B (zh) | 2013-05-14 | 2018-04-03 | 英特塞普特医药品公司 | 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物 |
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2014
- 2014-05-14 CN CN201480036949.5A patent/CN105377870B/zh active Active
- 2014-05-14 ES ES20211780T patent/ES2936638T3/es active Active
- 2014-05-14 EP EP18163622.6A patent/EP3360881B1/en active Active
- 2014-05-14 SI SI201431742T patent/SI3360881T1/sl unknown
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- 2014-05-14 MA MA38647A patent/MA38647B1/fr unknown
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- 2014-05-14 PE PE2020000355A patent/PE20200844A1/es unknown
- 2014-05-14 PT PT147238208T patent/PT2997035T/pt unknown
- 2014-05-14 SM SM20180326T patent/SMT201800326T1/it unknown
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- 2014-05-14 EA EA201592055A patent/EA030152B1/ru unknown
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