EA201592055A1 - 11-гидроксилпроизводные желчных кислот и их аминокислотные конъюгаты в качестве модуляторов фарнезоидных х-рецепторов - Google Patents

11-гидроксилпроизводные желчных кислот и их аминокислотные конъюгаты в качестве модуляторов фарнезоидных х-рецепторов

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Publication number
EA201592055A1
EA201592055A1 EA201592055A EA201592055A EA201592055A1 EA 201592055 A1 EA201592055 A1 EA 201592055A1 EA 201592055 A EA201592055 A EA 201592055A EA 201592055 A EA201592055 A EA 201592055A EA 201592055 A1 EA201592055 A1 EA 201592055A1
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EA
Eurasian Patent Office
Prior art keywords
amino acid
pharnesoid
receptor modulators
acid conjugates
hydroxyl derivatives
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EA201592055A
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English (en)
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EA030152B1 (ru
Inventor
Роберто Пелличчари
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Интерсепт Фармасьютикалз, Инк.
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Application filed by Интерсепт Фармасьютикалз, Инк. filed Critical Интерсепт Фармасьютикалз, Инк.
Publication of EA201592055A1 publication Critical patent/EA201592055A1/ru
Publication of EA030152B1 publication Critical patent/EA030152B1/ru

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • C07J41/0061Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J71/00Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0005Oxygen-containing hetero ring
    • C07J71/001Oxiranes

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  • 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)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (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

Настоящее изобретение предусматривает соединение формулы (I) или его фармацевтически приемлемую соль, сольват или аминокислотный конъюгат, где Rпредставляет собой гидроксигруппу, a R, R, R, Rи Rявляются такими, как описано в настоящем документе. Настоящее изобретение, в целом, относится к селективным агонистам FXR и способам их получения и применения.
EA201592055A 2013-05-14 2014-05-14 11-гидроксилпроизводные желчных кислот и их аминокислотные конъюгаты в качестве модуляторов фарнезоидных х-рецепторов EA030152B1 (ru)

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 (2)

Publication Number Publication Date
EA201592055A1 true EA201592055A1 (ru) 2016-11-30
EA030152B1 EA030152B1 (ru) 2018-06-29

Family

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Family Applications (1)

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EA201592055A EA030152B1 (ru) 2013-05-14 2014-05-14 11-гидроксилпроизводные желчных кислот и их аминокислотные конъюгаты в качестве модуляторов фарнезоидных х-рецепторов

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US (6) US9611289B2 (ru)
EP (4) EP2997035B8 (ru)
JP (2) JP6326131B2 (ru)
KR (1) KR102229952B1 (ru)
CN (2) CN108245523B (ru)
AU (1) AU2014267324B2 (ru)
BR (1) BR112015028399B1 (ru)
CA (1) CA2912139C (ru)
CL (2) CL2015003344A1 (ru)
CR (1) CR20150643A (ru)
CY (1) CY1122614T1 (ru)
DK (4) DK3360881T3 (ru)
EA (1) EA030152B1 (ru)
ES (4) ES2847002T3 (ru)
GT (1) GT201500324A (ru)
HK (2) HK1253326A1 (ru)
HR (1) HRP20180931T1 (ru)
HU (1) HUE037996T2 (ru)
IL (2) IL242555B (ru)
LT (1) LT2997035T (ru)
MA (1) MA38647B1 (ru)
ME (1) ME03082B (ru)
MX (1) MX352065B (ru)
MY (1) MY187886A (ru)
NI (1) NI201500160A (ru)
PE (1) PE20160665A1 (ru)
PH (1) PH12015502576A1 (ru)
PL (3) PL3360882T3 (ru)
PT (3) PT3360881T (ru)
RS (1) RS57372B1 (ru)
SA (1) SA515370140B1 (ru)
SG (1) SG11201509352XA (ru)
SI (3) SI3360882T1 (ru)
TN (1) TN2015000497A1 (ru)
TR (1) TR201809041T4 (ru)
UA (1) UA118673C2 (ru)
WO (1) WO2014184271A1 (ru)

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TR201809041T4 (tr) 2018-07-23
US20190209586A1 (en) 2019-07-11
US10532061B2 (en) 2020-01-14
CR20150643A (es) 2016-06-01
US20170216316A1 (en) 2017-08-03
CA2912139A1 (en) 2014-11-20
CN108245523A (zh) 2018-07-06
BR112015028399A2 (pt) 2017-07-25
AU2014267324A1 (en) 2015-11-26
EP3848038B1 (en) 2022-11-09
HUE037996T2 (hu) 2018-09-28
MY187886A (en) 2021-10-26
RS57372B1 (sr) 2018-08-31
US20210228599A1 (en) 2021-07-29
SI3360882T1 (sl) 2021-06-30
TN2015000497A1 (en) 2017-04-06
SG11201509352XA (en) 2015-12-30
US20140371190A1 (en) 2014-12-18
ES2936638T3 (es) 2023-03-21
EP3360882A1 (en) 2018-08-15
EP3360881B1 (en) 2020-12-09
IL272718A (en) 2020-04-30
JP2016518429A (ja) 2016-06-23
PL2997035T3 (pl) 2018-10-31
SA515370140B1 (ar) 2017-04-11
EP3360882B1 (en) 2020-12-09
US20200297739A1 (en) 2020-09-24
MX352065B (es) 2017-11-08
PH12015502576B1 (en) 2016-02-29
EP3360881A1 (en) 2018-08-15
DK3360882T3 (da) 2021-03-08
JP6326131B2 (ja) 2018-05-16
CL2016001809A1 (es) 2017-01-27
WO2014184271A1 (en) 2014-11-20
HRP20180931T1 (hr) 2018-10-05
CN108245523B (zh) 2021-03-26
SI3360881T1 (sl) 2021-06-30
LT2997035T (lt) 2018-08-10
MA38647B1 (fr) 2019-05-31
PT3360882T (pt) 2021-02-12
EP2997035A1 (en) 2016-03-23
IL242555A0 (en) 2016-02-01
KR102229952B1 (ko) 2021-03-22
CY1122614T1 (el) 2020-07-31
ES2671427T3 (es) 2018-06-06
PH12015502576A1 (en) 2016-02-29
PE20160665A1 (es) 2016-08-07
EP2997035B1 (en) 2018-03-28
IL242555B (en) 2020-04-30
PT2997035T (pt) 2018-07-18
US11000532B2 (en) 2021-05-11
KR20160007586A (ko) 2016-01-20
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EA030152B1 (ru) 2018-06-29
ME03082B (me) 2019-01-20
PL3360882T3 (pl) 2021-10-25
CA2912139C (en) 2021-04-20
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PL3360881T3 (pl) 2021-11-15
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US20230233581A1 (en) 2023-07-27
DK3360881T3 (da) 2021-03-15
CN105377870B (zh) 2018-04-03
EP3848038A1 (en) 2021-07-14
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CL2015003344A1 (es) 2016-07-15
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UA118673C2 (uk) 2019-02-25
EP2997035B8 (en) 2018-05-23
SI2997035T1 (sl) 2018-10-30
NI201500160A (es) 2016-01-04
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