EA038632B1 - 7,11-дигидрокси-6-этил-5-холан-24-овая кислота и фармацевтические композиции на ее основе для лечения или предупреждения заболевания или состояния, опосредованных фарнезоидным х-рецептором (fxr) - Google Patents

7,11-дигидрокси-6-этил-5-холан-24-овая кислота и фармацевтические композиции на ее основе для лечения или предупреждения заболевания или состояния, опосредованных фарнезоидным х-рецептором (fxr) Download PDF

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Publication number
EA038632B1
EA038632B1 EA201892007A EA201892007A EA038632B1 EA 038632 B1 EA038632 B1 EA 038632B1 EA 201892007 A EA201892007 A EA 201892007A EA 201892007 A EA201892007 A EA 201892007A EA 038632 B1 EA038632 B1 EA 038632B1
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EA
Eurasian Patent Office
Prior art keywords
disease
compound
present
liver
fxr
Prior art date
Application number
EA201892007A
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English (en)
Russian (ru)
Other versions
EA201892007A1 (ru
Inventor
Роберто Пелличари
Антимо Джойелло
Original Assignee
Интерсепт Фармасьютикалз, Инк.
Priority date (The priority date 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 date listed.)
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Application filed by Интерсепт Фармасьютикалз, Инк. filed Critical Интерсепт Фармасьютикалз, Инк.
Publication of EA201892007A1 publication Critical patent/EA201892007A1/ru
Publication of EA038632B1 publication Critical patent/EA038632B1/ru

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J11/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 3
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/542Carboxylic acids, e.g. a fatty acid or an amino acid
    • 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
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Cephalosporin Compounds (AREA)
EA201892007A 2016-03-11 2017-03-07 7,11-дигидрокси-6-этил-5-холан-24-овая кислота и фармацевтические композиции на ее основе для лечения или предупреждения заболевания или состояния, опосредованных фарнезоидным х-рецептором (fxr) EA038632B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201662306914P 2016-03-11 2016-03-11
PCT/US2017/021194 WO2017156024A1 (en) 2016-03-11 2017-03-07 3-desoxy derivative and pharmaceutical compositions thereof

Publications (2)

Publication Number Publication Date
EA201892007A1 EA201892007A1 (ru) 2019-01-31
EA038632B1 true EA038632B1 (ru) 2021-09-27

Family

ID=59787771

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201892007A EA038632B1 (ru) 2016-03-11 2017-03-07 7,11-дигидрокси-6-этил-5-холан-24-овая кислота и фармацевтические композиции на ее основе для лечения или предупреждения заболевания или состояния, опосредованных фарнезоидным х-рецептором (fxr)

Country Status (20)

Country Link
US (3) US10815267B2 (https=)
EP (1) EP3426348B1 (https=)
JP (1) JP6892457B2 (https=)
KR (1) KR102359191B1 (https=)
CN (1) CN108883305B (https=)
AR (1) AR107864A1 (https=)
AU (1) AU2017229481B2 (https=)
BR (1) BR112018068278B1 (https=)
CA (1) CA3016875C (https=)
EA (1) EA038632B1 (https=)
ES (1) ES2874682T3 (https=)
IL (1) IL261548B (https=)
MX (1) MX384800B (https=)
PH (1) PH12018501956A1 (https=)
PL (1) PL3426348T3 (https=)
PT (1) PT3426348T (https=)
SG (1) SG11201807784SA (https=)
SI (1) SI3426348T1 (https=)
TW (1) TWI772289B (https=)
WO (1) WO2017156024A1 (https=)

Families Citing this family (19)

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WO2016073767A1 (en) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an 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
JP2017535570A (ja) 2014-11-26 2017-11-30 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類似体およびその使用方法
MX2017010376A (es) 2015-02-11 2017-12-20 Enanta Pharm Inc Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.
CA2981503C (en) 2015-03-31 2023-09-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
EP3981779A1 (en) 2015-10-07 2022-04-13 Intercept Pharmaceuticals, Inc. Farnesoid x receptor modulators
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
EP3426348B1 (en) 2016-03-11 2021-05-05 Intercept Pharmaceuticals, Inc. 3-desoxy derivative and pharmaceutical compositions thereof
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
CA3058754A1 (en) 2017-04-07 2018-10-11 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
US20230165853A1 (en) * 2021-01-14 2023-06-01 Enyo Pharma Method for treating chronic kidney diseases
WO2023288123A1 (en) 2021-07-16 2023-01-19 Interecept Pharmaceuticals, Inc. Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid
US20250288600A1 (en) * 2022-04-21 2025-09-18 Intercept Pharmaceuticals, Inc. Uses of farnesoid x receptor agonists
EP4611888A1 (en) * 2022-10-31 2025-09-10 Intercept Pharmaceuticals, Inc. Uses of farnesoid x receptor agonists

Citations (2)

* Cited by examiner, † Cited by third party
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US20130261317A1 (en) * 2010-09-27 2013-10-03 Kythera Biopharmaceuticals, Inc. Methods for preparing synthetic bile acids and compositions comprising the same
US20140371190A1 (en) * 2013-05-14 2014-12-18 TES Pharma SrI. Farnesoid X receptor modulators

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EP1734970B1 (en) * 2004-03-12 2014-12-31 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
CN110041399B (zh) 2011-12-29 2023-12-12 诺沃—诺迪斯克有限公司 包含非成蛋白质性的氨基酸的二肽
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
CN108137643A (zh) 2015-08-07 2018-06-08 英特塞普特医药品公司 制备胆汁酸及其衍生物的方法
EP3426348B1 (en) 2016-03-11 2021-05-05 Intercept Pharmaceuticals, Inc. 3-desoxy derivative and pharmaceutical compositions thereof

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130261317A1 (en) * 2010-09-27 2013-10-03 Kythera Biopharmaceuticals, Inc. Methods for preparing synthetic bile acids and compositions comprising the same
US20140371190A1 (en) * 2013-05-14 2014-12-18 TES Pharma SrI. Farnesoid X receptor modulators

Also Published As

Publication number Publication date
KR20180117702A (ko) 2018-10-29
TW201734031A (zh) 2017-10-01
PT3426348T (pt) 2021-06-28
CN108883305B (zh) 2021-03-16
HK1259145A1 (zh) 2019-11-29
ES2874682T3 (es) 2021-11-05
EP3426348A1 (en) 2019-01-16
CA3016875C (en) 2023-08-22
CN108883305A (zh) 2018-11-23
BR112018068278A2 (pt) 2019-04-02
IL261548B (en) 2021-02-28
SI3426348T1 (sl) 2021-11-30
KR102359191B1 (ko) 2022-02-04
PL3426348T3 (pl) 2022-01-03
PH12018501956A1 (en) 2019-06-17
EP3426348A4 (en) 2019-11-20
WO2017156024A1 (en) 2017-09-14
BR112018068278B1 (pt) 2023-12-19
TWI772289B (zh) 2022-08-01
IL261548A (en) 2018-11-29
EP3426348B1 (en) 2021-05-05
SG11201807784SA (en) 2018-10-30
AU2017229481A1 (en) 2018-09-20
US11319337B2 (en) 2022-05-03
JP6892457B2 (ja) 2021-06-23
AR107864A1 (es) 2018-06-13
CA3016875A1 (en) 2017-09-14
MX2018010983A (es) 2019-01-21
JP2019507781A (ja) 2019-03-22
US20210101927A1 (en) 2021-04-08
US20190002493A1 (en) 2019-01-03
MX384800B (es) 2025-03-14
US10815267B2 (en) 2020-10-27
AU2017229481B2 (en) 2022-06-16
US20170260225A1 (en) 2017-09-14
EA201892007A1 (ru) 2019-01-31
NZ745980A (en) 2025-03-28

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