EA201891491A1 - POLYMORPHIC CRYSTAL FORMS OF MUTUAL-CHOLIC ACID - Google Patents

POLYMORPHIC CRYSTAL FORMS OF MUTUAL-CHOLIC ACID

Info

Publication number
EA201891491A1
EA201891491A1 EA201891491A EA201891491A EA201891491A1 EA 201891491 A1 EA201891491 A1 EA 201891491A1 EA 201891491 A EA201891491 A EA 201891491A EA 201891491 A EA201891491 A EA 201891491A EA 201891491 A1 EA201891491 A1 EA 201891491A1
Authority
EA
Eurasian Patent Office
Prior art keywords
mutual
cholic acid
crystal forms
acid
polymorphic crystal
Prior art date
Application number
EA201891491A
Other languages
Russian (ru)
Inventor
Андре Штайнер
Хейди Венерлунд Поульсен
Эмили Жолибуа
Мелисса Револински
Ральф Гросс
Эмма Шарп
Фиона Дубас-Фишер
Алекс Иберлин
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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=55650649&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201891491(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US14/979,005 external-priority patent/US9982008B2/en
Application filed by Интерсепт Фармасьютикалз, Инк. filed Critical Интерсепт Фармасьютикалз, Инк.
Publication of EA201891491A1 publication Critical patent/EA201891491A1/en

Links

Classifications

    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J17/00—Normal steroids containing carbon, hydrogen, halogen or oxygen, having an oxygen-containing hetero ring not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Oncology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Настоящая заявка относится к кристаллическим формам A, D, F, G и I обетихолевой кислоты. Данные кристаллические формы применимы в получении обетихолевой кислоты (в частности, при очистке), которая представляет собой лекарственное средство, применимое в лечении или предупреждении FXR-опосредованного заболевания или состояния, сердечно-сосудистого заболевания или холестатического заболевания печени, а также для снижения уровня холестерина HDL, для снижения уровня триглицеридов у млекопитающего или для замедления прогрессирования фиброза.The present application relates to crystalline forms A, D, F, G and I of obestiolic acid. These crystalline forms are applicable in the production of obethiolic acid (in particular, during purification), which is a drug that is applicable in the treatment or prevention of an FXR-mediated disease or condition, cardiovascular disease or cholestatic liver disease, as well as to reduce HDL cholesterol , to reduce triglyceride levels in a mammal or to slow the progression of fibrosis.

EA201891491A 2015-12-22 2016-01-08 POLYMORPHIC CRYSTAL FORMS OF MUTUAL-CHOLIC ACID EA201891491A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14/979,005 US9982008B2 (en) 2012-06-19 2015-12-22 Preparation and uses of obeticholic acid
PCT/US2016/012651 WO2017111979A1 (en) 2015-12-22 2016-01-08 Polymorphic crystalline forms of obeticholic acid

Publications (1)

Publication Number Publication Date
EA201891491A1 true EA201891491A1 (en) 2018-11-30

Family

ID=55650649

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201891491A EA201891491A1 (en) 2015-12-22 2016-01-08 POLYMORPHIC CRYSTAL FORMS OF MUTUAL-CHOLIC ACID

Country Status (15)

Country Link
EP (1) EP3394081A1 (en)
JP (1) JP2018538331A (en)
KR (1) KR20180095070A (en)
CN (1) CN108495858A (en)
AU (1) AU2016375566A1 (en)
BR (1) BR112018012590A2 (en)
CA (1) CA3009149A1 (en)
CL (1) CL2018001720A1 (en)
CO (1) CO2018006701A2 (en)
EA (1) EA201891491A1 (en)
IL (1) IL259998A (en)
MX (1) MX2018007776A (en)
PH (1) PH12018501318A1 (en)
SG (1) SG11201805235XA (en)
WO (1) WO2017111979A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105801653B (en) * 2014-12-30 2018-04-17 苏州晶云药物科技有限公司 Crystal form A of shellfish cholic acid difficult to understand and preparation method thereof
WO2018211413A1 (en) * 2017-05-15 2018-11-22 Dr. Reddy’S Laboratories Limited Solid forms of obeticholic acid and process for preparation
CN109280071A (en) * 2017-07-19 2019-01-29 东莞东阳光药物研发有限公司 The crystal form and preparation method thereof of shellfish cholic acid difficult to understand
CN107383139A (en) * 2017-08-09 2017-11-24 杭州和泽医药科技有限公司 The method that a kind of β cholanic acid new derivatives of 7 oxo of 3 α hydroxyls 5 prepare shellfish cholic acid difficult to understand
CZ31099U1 (en) * 2017-09-05 2017-10-17 Zentiva, K.S. The crystalline forms of (3α,5β,6α,7α)-6-ethyl-3,7-dihydroxycholan-24-oic acid
CN109485687A (en) * 2017-09-12 2019-03-19 成都弘达药业有限公司 The crystal form J and preparation method thereof of shellfish cholic acid difficult to understand
WO2019106043A1 (en) 2017-11-29 2019-06-06 Hexal Ag Pharmaceutical composition comprising obeticholic acid
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
CN113264972A (en) * 2020-02-14 2021-08-17 四川科伦药物研究院有限公司 Method for preparing obeticholic acid

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ITMI20050912A1 (en) * 2005-05-19 2006-11-20 Erregierre Spa PROCESS OF PREPARATION OF ACIDS 3-A-YA (B) -DIDROSSI-6-A (B) -ALCHIL-5B-COLANICI
SG10201607230SA (en) * 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
WO2016045480A1 (en) * 2014-09-28 2016-03-31 上海源力生物技术有限公司 Method for preparing obeticholic acid
CA2968305A1 (en) * 2014-11-19 2016-05-26 NZP UK Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
TWI688571B (en) * 2014-11-19 2020-03-21 英商Ｎｚｐ英國有限公司 Compounds
WO2016079518A1 (en) * 2014-11-19 2016-05-26 Dextra Laboratories Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
DK3221331T3 (en) * 2014-11-19 2019-12-02 Nzp Uk Ltd 6-ALKYL-7-HYDROXY-4-EN-3-ON STEROIDS AS INTERMEDIATES FOR THE MANUFACTURE OF STEROID FXR MODULATORS

Also Published As

Publication number Publication date
IL259998A (en) 2018-07-31
PH12018501318A1 (en) 2019-02-18
CN108495858A (en) 2018-09-04
WO2017111979A1 (en) 2017-06-29
EP3394081A1 (en) 2018-10-31
KR20180095070A (en) 2018-08-24
CO2018006701A2 (en) 2018-07-10
BR112018012590A2 (en) 2018-12-04
JP2018538331A (en) 2018-12-27
CL2018001720A1 (en) 2018-08-10
SG11201805235XA (en) 2018-07-30
MX2018007776A (en) 2018-08-09
AU2016375566A1 (en) 2018-07-05
CA3009149A1 (en) 2017-06-29

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