JP2015521621A - オベチコール酸の調製、使用および固体形態 - Google Patents

オベチコール酸の調製、使用および固体形態 Download PDF

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Publication number
JP2015521621A
JP2015521621A JP2015518485A JP2015518485A JP2015521621A JP 2015521621 A JP2015521621 A JP 2015521621A JP 2015518485 A JP2015518485 A JP 2015518485A JP 2015518485 A JP2015518485 A JP 2015518485A JP 2015521621 A JP2015521621 A JP 2015521621A
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Prior art keywords
acid
cholan
hydroxy
keto
obeticholic
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Pending
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JP2015518485A
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Japanese (ja)
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JP2015521621A5 (enExample
Inventor
アンドレ シュタイナー，
アンドレ シュタイナー，
ポールセン ハイディ ヴェネルルント，
ポールセン ハイディ ヴェネルルント，
エミリー ジョリボア，
エミリー ジョリボア，
メリッサ リーウォーリンスキ，
メリッサ リーウォーリンスキ，
ラルフ グロス，
ラルフ グロス，
エマ シャープ，
エマ シャープ，
フィオナ ドバス−フィッシャー，
フィオナ ドバス−フィッシャー，
アレックス エーベルリーン，
アレックス エーベルリーン，
Original Assignee
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
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
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Application filed by 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, 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 filed Critical 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
Publication of JP2015521621A publication Critical patent/JP2015521621A/ja
Publication of JP2015521621A5 publication Critical patent/JP2015521621A5/ja
Pending legal-status Critical Current

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    • 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
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/04—Drugs for disorders of the urinary system for urolithiasis
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • C07J—STEROIDS
    • C07J51/00—Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • 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

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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)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Vascular Medicine (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2015518485A 2012-06-19 2013-06-17 オベチコール酸の調製、使用および固体形態 Pending JP2015521621A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261661531P 2012-06-19 2012-06-19
US61/661,531 2012-06-19
PCT/US2013/046150 WO2013192097A1 (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid

Related Child Applications (1)

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JP2015521621A true JP2015521621A (ja) 2015-07-30
JP2015521621A5 JP2015521621A5 (enExample) 2015-09-10

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JP2015518485A Pending JP2015521621A (ja) 2012-06-19 2013-06-17 オベチコール酸の調製、使用および固体形態
JP2015238204A Active JP6527077B2 (ja) 2012-06-19 2015-12-07 オベチコール酸の調製、使用および固体形態
JP2016244217A Withdrawn JP2017075169A (ja) 2012-06-19 2016-12-16 オベチコール酸の調製、使用および固体形態
JP2018137553A Active JP6877389B2 (ja) 2012-06-19 2018-07-23 オベチコール酸の調製、使用および固体形態
JP2018137552A Withdrawn JP2018172438A (ja) 2012-06-19 2018-07-23 オベチコール酸の調製、使用および固体形態
JP2020071677A Active JP6978544B2 (ja) 2012-06-19 2020-04-13 オベチコール酸の調製、使用および固体形態

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JP2016244217A Withdrawn JP2017075169A (ja) 2012-06-19 2016-12-16 オベチコール酸の調製、使用および固体形態
JP2018137553A Active JP6877389B2 (ja) 2012-06-19 2018-07-23 オベチコール酸の調製、使用および固体形態
JP2018137552A Withdrawn JP2018172438A (ja) 2012-06-19 2018-07-23 オベチコール酸の調製、使用および固体形態
JP2020071677A Active JP6978544B2 (ja) 2012-06-19 2020-04-13 オベチコール酸の調製、使用および固体形態

Country Status (25)

Country Link
US (10) US9238673B2 (enExample)
EP (4) EP2861613A1 (enExample)
JP (6) JP2015521621A (enExample)
KR (4) KR20150022974A (enExample)
CN (2) CN111228278A (enExample)
AU (5) AU2013277429B2 (enExample)
BR (2) BR122016011808B1 (enExample)
CA (3) CA3028207A1 (enExample)
CL (2) CL2014003475A1 (enExample)
CO (1) CO7240414A2 (enExample)
DK (1) DK3336097T3 (enExample)
EA (2) EA032347B1 (enExample)
ES (1) ES2822375T3 (enExample)
HK (1) HK1211296A1 (enExample)
IL (3) IL236231A0 (enExample)
IN (1) IN2014MN02561A (enExample)
MX (2) MX365059B (enExample)
NZ (3) NZ719360A (enExample)
PH (1) PH12014502835A1 (enExample)
PL (1) PL3336097T3 (enExample)
PT (1) PT3336097T (enExample)
SG (3) SG10201607230SA (enExample)
SI (1) SI3336097T1 (enExample)
TW (1) TWI673284B (enExample)
WO (1) WO2013192097A1 (enExample)

Cited By (9)

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WO2017170858A1 (ja) * 2016-03-31 2017-10-05 大日本住友製薬株式会社 溶出性に優れた経口製剤
WO2017170434A1 (ja) * 2016-03-28 2017-10-05 大日本住友製薬株式会社 Ｆｘｒアゴニストとａｒｂの組み合わせ医薬
WO2017170854A1 (ja) * 2016-03-31 2017-10-05 大日本住友製薬株式会社 有効成分の化学的安定性に優れたフィルムコーティング錠
JP2018538331A (ja) * 2015-12-22 2018-12-27 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 オベチコール酸の多型結晶形態
JP2019515906A (ja) * 2016-04-19 2019-06-13 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 オベチコール酸およびその誘導体の調製方法
JP2020502095A (ja) * 2016-12-09 2020-01-23 カディラ・ヘルスケア・リミテッド 原発性胆汁性胆管炎の治療
JP2020534246A (ja) * 2016-02-04 2020-11-26 シンリックス ファーマ、エルエルシー 重水素化ドンペリドン組成物、方法、及び調製
US11364226B2 (en) 2017-06-30 2022-06-21 Cinrx Pharma, Llc Deuterated domperidone compositions, methods, and preparation
US12478612B2 (en) 2017-06-30 2025-11-25 Cindome Pharma, Inc. Deuterated domperidone compositions, methods, and preparation

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