CY1122614T1 - 11-υδροξυλ-6-υποκατεστημενα-παραγωγα χολικων οξεων και συζευγματα αμινοξεων αυτων ως ρυθμιστες υποδοχεων χ φαρνεσοειδων - Google Patents
11-υδροξυλ-6-υποκατεστημενα-παραγωγα χολικων οξεων και συζευγματα αμινοξεων αυτων ως ρυθμιστες υποδοχεων χ φαρνεσοειδωνInfo
- Publication number
- CY1122614T1 CY1122614T1 CY20181100583T CY181100583T CY1122614T1 CY 1122614 T1 CY1122614 T1 CY 1122614T1 CY 20181100583 T CY20181100583 T CY 20181100583T CY 181100583 T CY181100583 T CY 181100583T CY 1122614 T1 CY1122614 T1 CY 1122614T1
- Authority
- CY
- Cyprus
- Prior art keywords
- amino acid
- farnesoid
- hydroxyl
- substituted
- acid derivatives
- Prior art date
Links
- 150000001413 amino acids Chemical class 0.000 title abstract 2
- 102100038495 Bile acid receptor Human genes 0.000 title 1
- 101000603876 Homo sapiens Bile acid receptor Proteins 0.000 title 1
- 239000002812 cholic acid derivative Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 episolvate Chemical class 0.000 abstract 1
- 229940121360 farnesoid X receptor (fxr) agonists Drugs 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (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)
Abstract
Η παρούσα εφεύρεση παρέχει μια ένωση του τύπου (I) ή ένα φαρμακευτικώς αποδεκτό άλας, επιδιαλύτωμα, ή σύζευγμα αμινοξέος αυτής, όπου το R1 είναι μια υδροξυ ομάδα και τα R2, R3, R4, R5, και R6 είναι όπως περιγράφονται στο παρόν. Η παρούσα εφεύρεση αναφέρεται γενικώς σε εκλεκτικούς αγωνιστές FXR και σε μεθόδους παρασκευής και χρήσης αυτών.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361823169P | 2013-05-14 | 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 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1122614T1 true CY1122614T1 (el) | 2020-07-31 |
Family
ID=50721801
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY20181100583T CY1122614T1 (el) | 2013-05-14 | 2018-06-01 | 11-υδροξυλ-6-υποκατεστημενα-παραγωγα χολικων οξεων και συζευγματα αμινοξεων αυτων ως ρυθμιστες υποδοχεων χ φαρνεσοειδων |
Country Status (37)
| Country | Link |
|---|---|
| US (6) | US9611289B2 (el) |
| EP (4) | EP3360881B1 (el) |
| JP (2) | JP6326131B2 (el) |
| KR (1) | KR102229952B1 (el) |
| CN (2) | CN108245523B (el) |
| AU (1) | AU2014267324B2 (el) |
| BR (1) | BR112015028399B1 (el) |
| CA (1) | CA2912139C (el) |
| CL (2) | CL2015003344A1 (el) |
| CR (1) | CR20150643A (el) |
| CY (1) | CY1122614T1 (el) |
| DK (4) | DK3360881T3 (el) |
| EA (1) | EA030152B1 (el) |
| ES (4) | ES2671427T3 (el) |
| GT (1) | GT201500324A (el) |
| HK (2) | HK1221471A1 (el) |
| HR (1) | HRP20180931T1 (el) |
| HU (1) | HUE037996T2 (el) |
| IL (2) | IL242555B (el) |
| LT (1) | LT2997035T (el) |
| MA (1) | MA38647B1 (el) |
| ME (1) | ME03082B (el) |
| MX (1) | MX352065B (el) |
| MY (1) | MY187886A (el) |
| NI (1) | NI201500160A (el) |
| PE (1) | PE20160665A1 (el) |
| PH (1) | PH12015502576B1 (el) |
| PL (3) | PL2997035T3 (el) |
| PT (3) | PT3360882T (el) |
| RS (1) | RS57372B1 (el) |
| SA (1) | SA515370140B1 (el) |
| SG (1) | SG11201509352XA (el) |
| SI (3) | SI3360882T1 (el) |
| TN (1) | TN2015000497A1 (el) |
| TR (1) | TR201809041T4 (el) |
| UA (1) | UA118673C2 (el) |
| WO (1) | WO2014184271A1 (el) |
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| EP2545964A1 (en) | 2011-07-13 | 2013-01-16 | Phenex Pharmaceuticals AG | Novel FXR (NR1H4) binding and activity modulating compounds |
| EP3360881B1 (en) | 2013-05-14 | 2020-12-09 | Intercept Pharmaceuticals, Inc. | 11-hydroxyl-6-substituted-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators |
| US10301268B2 (en) | 2014-03-13 | 2019-05-28 | The Salk Institute For Biological Studies | Analogs of fexaramine and methods of making and using |
| US10077268B2 (en) | 2014-03-13 | 2018-09-18 | Salk Institute For Biological Studies | FXR agonists and methods for making and using |
| US10407462B2 (en) * | 2014-05-29 | 2019-09-10 | Bar Pharmaceuticals S.R.L. | Cholane derivatives for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases |
| CN106999551A (zh) | 2014-11-06 | 2017-08-01 | 英安塔制药有限公司 | 作为fxr/tgr5激动剂的胆汁酸类似物和其使用方法 |
| 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 |
| MX2017006565A (es) | 2014-11-19 | 2018-01-26 | Nzp Uk Ltd | Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la produccion de moduladores esteroides del receptor x farnesoide (fxr). |
| MX2017006564A (es) | 2014-11-19 | 2018-01-26 | Nzp Uk Ltd | Esteroides 5.beta.-6-alquil-7-hidroxi-3-ona como intermedios para la produccion de moduladores esteroideos del receptor x farnesoide (fxr). |
| ES2759725T3 (es) | 2014-11-19 | 2020-05-12 | Nzp Uk Ltd | Esteroides 6-alquil-7-hidroxi-4-en-3-ona como intermediarios para la producción de moduladores de FXR esteroideo |
| RU2017121457A (ru) | 2014-11-26 | 2018-12-26 | Энанта Фармасьютикалс, Инк. | Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения |
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| MA41094A (fr) * | 2014-12-02 | 2017-10-10 | Lilly Co Eli | Procédés de traitement de troubles rénaux |
| 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 |
| CN104523703A (zh) * | 2014-12-24 | 2015-04-22 | 聂飚 | 一种游离脂肪酸转运蛋白小分子抑制物的应用 |
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| CN107249594A (zh) | 2015-02-11 | 2017-10-13 | 英安塔制药有限公司 | 作为fxr/tgr5激动剂的胆汁酸类似物及其使用方法 |
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| KR20180054770A (ko) * | 2015-09-21 | 2018-05-24 | 인터셉트 파마슈티컬즈, 인크. | 간 재생 촉진 방법 |
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| AU2018225255A1 (en) * | 2017-02-23 | 2019-09-05 | Intercept Pharmaceuticals, Inc | Pharmaceutical compositions of a bile acid derivative and microbiome and uses thereof |
| PT3600309T (pt) | 2017-03-28 | 2022-10-03 | Gilead Sciences Inc | Combinações terapêuticas para o tratamento de doenças hepáticas |
| CN110612105B (zh) | 2017-04-07 | 2023-05-02 | 英安塔制药有限公司 | 氨基甲酸酯磺酸胆汁酸衍生物的制备方法 |
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| JP7224307B2 (ja) * | 2017-06-23 | 2023-02-17 | 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 | 胆汁酸誘導体の調製のための方法及び中間体 |
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| GB201812382D0 (en) | 2018-07-30 | 2018-09-12 | Nzp Uk Ltd | Compounds |
| CN109182451B (zh) * | 2018-08-21 | 2021-06-11 | 四川大学 | 细胞色素cyp3a7酶的新型特异性探针反应及其应用 |
| AU2020209564B2 (en) | 2019-01-15 | 2022-12-01 | Gilead Sciences, Inc. | FXR (NR1H4) modulating compounds |
| US11524005B2 (en) | 2019-02-19 | 2022-12-13 | Gilead Sciences, Inc. | Solid forms of FXR agonists |
| CN114144185A (zh) | 2019-05-30 | 2022-03-04 | 英特塞普特医药品公司 | 用于治疗胆汁淤积性肝病的包含fxr激动剂和贝特类的药物组合物 |
| KR20220035365A (ko) | 2019-07-18 | 2022-03-22 | 엔요 파마 | 인터페론의 부작용을 감소시키는 방법 |
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| JP2024502673A (ja) | 2021-01-14 | 2024-01-22 | ウエヌイグレックオ・ファーマ | Ｈｂｖ感染の処置のためのｆｘｒアゴニストとｉｆｎの相乗効果 |
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2014
- 2014-05-14 EP EP18163622.6A patent/EP3360881B1/en active Active
- 2014-05-14 TR TR2018/09041T patent/TR201809041T4/tr unknown
- 2014-05-14 EP EP14723820.8A patent/EP2997035B8/en active Active
- 2014-05-14 LT LTEP14723820.8T patent/LT2997035T/lt unknown
- 2014-05-14 JP JP2016513357A patent/JP6326131B2/ja active Active
- 2014-05-14 PL PL14723820T patent/PL2997035T3/pl unknown
- 2014-05-14 PT PT181636234T patent/PT3360882T/pt unknown
- 2014-05-14 KR KR1020157034951A patent/KR102229952B1/ko active IP Right Grant
- 2014-05-14 ME MEP-2018-159A patent/ME03082B/me unknown
- 2014-05-14 TN TN2015000497A patent/TN2015000497A1/en unknown
- 2014-05-14 PT PT181636226T patent/PT3360881T/pt unknown
- 2014-05-14 EA EA201592055A patent/EA030152B1/ru unknown
- 2014-05-14 CN CN201810162562.4A patent/CN108245523B/zh not_active Expired - Fee Related
- 2014-05-14 HU HUE14723820A patent/HUE037996T2/hu unknown
- 2014-05-14 RS RS20180690A patent/RS57372B1/sr unknown
- 2014-05-14 DK DK18163622.6T patent/DK3360881T3/da active
- 2014-05-14 SG SG11201509352XA patent/SG11201509352XA/en unknown
- 2014-05-14 PT PT147238208T patent/PT2997035T/pt unknown
- 2014-05-14 SI SI201431741T patent/SI3360882T1/sl unknown
- 2014-05-14 BR BR112015028399-3A patent/BR112015028399B1/pt active IP Right Grant
- 2014-05-14 MX MX2015015730A patent/MX352065B/es active IP Right Grant
- 2014-05-14 SI SI201431742T patent/SI3360881T1/sl unknown
- 2014-05-14 US US14/120,366 patent/US9611289B2/en active Active
- 2014-05-14 MA MA38647A patent/MA38647B1/fr unknown
- 2014-05-14 AU AU2014267324A patent/AU2014267324B2/en active Active
- 2014-05-14 SI SI201430701T patent/SI2997035T1/sl unknown
- 2014-05-14 CN CN201480036949.5A patent/CN105377870B/zh active Active
- 2014-05-14 MY MYPI2015002734A patent/MY187886A/en unknown
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