CN104781272A - 奥贝胆酸的制备、用途和固体形式 - Google Patents

奥贝胆酸的制备、用途和固体形式 Download PDF

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Publication number
CN104781272A
CN104781272A CN201380043964.8A CN201380043964A CN104781272A CN 104781272 A CN104781272 A CN 104781272A CN 201380043964 A CN201380043964 A CN 201380043964A CN 104781272 A CN104781272 A CN 104781272A
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acid
obeticholic acid
cholan
hydroxy
obeticholic
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Chinese (zh)
Inventor
A.施泰纳
H.维纳伦德普尔森
E.乔利博瓦
M.雷沃林斯基
R.格罗斯
E.夏普
F.迪巴斯-费希尔
A.埃伯林
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Intercept Pharmaceuticals Inc
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Intercept Pharmaceuticals Inc
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Application filed by Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Priority to CN202010196448.0A priority Critical patent/CN111228278A/zh
Publication of CN104781272A publication Critical patent/CN104781272A/zh
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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)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (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)
  • Peptides Or Proteins (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicinal Preparation (AREA)
CN201380043964.8A 2012-06-19 2013-06-17 奥贝胆酸的制备、用途和固体形式 Pending CN104781272A (zh)

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US201261661531P 2012-06-19 2012-06-19
US61/661531 2012-06-19
PCT/US2013/046150 WO2013192097A1 (en) 2012-06-19 2013-06-17 Preparation, uses and solid forms of obeticholic acid

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EP (4) EP3992201A1 (enExample)
JP (6) JP2015521621A (enExample)
KR (4) KR20150022974A (enExample)
CN (2) CN104781272A (enExample)
AU (5) AU2013277429B2 (enExample)
BR (2) BR112014031828B1 (enExample)
CA (3) CA2877122C (enExample)
CL (2) CL2014003475A1 (enExample)
CO (1) CO7240414A2 (enExample)
DK (1) DK3336097T3 (enExample)
EA (2) EA201990211A1 (enExample)
ES (1) ES2822375T3 (enExample)
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IL (3) IL236231A0 (enExample)
IN (1) IN2014MN02561A (enExample)
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NZ (3) NZ719360A (enExample)
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PL (1) PL3336097T3 (enExample)
PT (1) PT3336097T (enExample)
SG (3) SG11201408501UA (enExample)
SI (1) SI3336097T1 (enExample)
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Cited By (49)

* Cited by examiner, † Cited by third party
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CN105085597A (zh) * 2015-08-28 2015-11-25 成都百裕科技制药有限公司 一种无定型奥贝胆酸的制备方法
CN105315320A (zh) * 2015-11-30 2016-02-10 山东省药学科学院 一种制备奥贝胆酸的方法
CN105399793A (zh) * 2015-12-24 2016-03-16 北京康立生医药技术开发有限公司 一种胆烷酸的制备方法
CN105481925A (zh) * 2015-12-17 2016-04-13 南京济群医药科技有限公司 一种奥贝胆酸及其中间体的制备方法
CN105541953A (zh) * 2016-03-15 2016-05-04 成都市新功生物科技有限公司 一种高纯度奥贝胆酸的重结晶纯化方法
CN105566429A (zh) * 2016-01-22 2016-05-11 南京长澳医药科技有限公司 一种奥贝胆酸1型的制备方法
CN105646634A (zh) * 2016-01-29 2016-06-08 中国药科大学 奥贝胆酸杂质的制备方法
CN105859817A (zh) * 2016-05-09 2016-08-17 成都宇西医药技术有限公司 一种制备3α-羟基-6-乙烯基-7-酮基-5β-胆烷酸的方法
CN105859818A (zh) * 2016-05-31 2016-08-17 四川瑞希康生物医药有限公司 一种奥贝胆酸α晶型及其制备方法、药物组合物和用途
CN105997909A (zh) * 2016-06-02 2016-10-12 中国药科大学 一种奥贝胆酸口崩片及其制备方法
CN106008639A (zh) * 2016-03-11 2016-10-12 深圳市塔吉瑞生物医药有限公司 用于预防或治疗fxr-介导疾病的胆烷酸化合物
CN106046094A (zh) * 2016-05-30 2016-10-26 福建广生堂药业股份有限公司 一种奥贝胆酸二聚体杂质及其制备方法
CN106279331A (zh) * 2016-07-27 2017-01-04 宋火良 胆酸类肝病治疗药物
CN106279335A (zh) * 2016-08-12 2017-01-04 齐鲁制药有限公司 一种制备奥贝胆酸及其中间体的方法
CN106478757A (zh) * 2016-09-27 2017-03-08 华南理工大学 一种3α,7α‑二羟基‑6α‑乙基胆烷酸的制备方法
CN106478756A (zh) * 2015-09-02 2017-03-08 中美华世通生物医药科技（武汉）有限公司 Oca-e单晶及其制备方法和用途
CN106589039A (zh) * 2015-10-15 2017-04-26 苏州朗科生物技术有限公司 一种奥贝胆酸的制备方法及相关化合物
CN106589038A (zh) * 2015-10-15 2017-04-26 重庆医药工业研究院有限责任公司 一种制备3α,7α-二羟基-6α-乙基-5β-胆烷酸的方法
CN106668027A (zh) * 2015-11-05 2017-05-17 中美华世通生物医药科技（武汉）有限公司 奥贝胆酸药物组合物及其制备方法
CN106749472A (zh) * 2016-12-30 2017-05-31 江苏开元医药化工有限公司 一种3α‑羟基‑6α‑乙基‑7‑酮‑5β‑胆烷‑24‑酸的制备方法
CN106749466A (zh) * 2015-11-23 2017-05-31 南京济群医药科技有限公司 一种高纯度奥贝胆酸的制备方法
CN106810587A (zh) * 2015-12-01 2017-06-09 中美华世通生物医药科技（武汉）有限公司 制备无定型奥贝胆酸的方法
CN106810586A (zh) * 2015-12-01 2017-06-09 中美华世通生物医药科技（武汉）有限公司 奥贝胆酸晶型ⅱ及其制备方法和用途
CN106854229A (zh) * 2015-12-08 2017-06-16 陈剑 一类脂肪酸盐,其制备及其在医药上的应用
CN106892954A (zh) * 2017-02-23 2017-06-27 广州隽沐生物科技有限公司 奥贝胆酸的制备工艺
CN106916195A (zh) * 2015-12-25 2017-07-04 中美华世通生物医药科技（武汉）有限公司 奥贝胆酸中间体的纯化方法
CN106986910A (zh) * 2017-04-19 2017-07-28 成都百特万合医药科技有限公司 奥贝胆酸中间体的制备方法
CN107126419A (zh) * 2016-02-26 2017-09-05 石药集团中诺药业（石家庄）有限公司 一种奥贝胆酸片剂及其制备方法
CN107188917A (zh) * 2016-03-15 2017-09-22 正大天晴药业集团股份有限公司 奥贝胆酸盐及其药物组合物
CN107286160A (zh) * 2017-06-05 2017-10-24 毛佳婧 一种抗肝炎药物的哌啶并吡啶并吡唑‑锌配合物的制备方法
CN107383139A (zh) * 2017-08-09 2017-11-24 杭州和泽医药科技有限公司 一种3α‑羟基‑7‑氧代‑5β‑胆烷酸新衍生物制备奥贝胆酸的方法
CN107400154A (zh) * 2016-05-18 2017-11-28 北京凯因科技股份有限公司 一种制备3α,7α-二-羟基-6α-乙基-5β-胆烷酸的方法
CN107540720A (zh) * 2016-06-29 2018-01-05 常州市第四制药厂有限公司 3α,7α‑二羟基‑6α‑乙基‑5β‑胆烷酸晶型H及其制备方法和应用
CN107648190A (zh) * 2016-07-26 2018-02-02 江苏先声药业有限公司 奥贝胆酸组合物及其制备方法
CN107674106A (zh) * 2016-08-01 2018-02-09 华北制药集团新药研究开发有限责任公司 一种奥贝胆酸二聚体的制备方法
CN107778339A (zh) * 2016-08-29 2018-03-09 鲁南制药集团股份有限公司 一种无定型奥贝胆酸的制备方法
CN107793463A (zh) * 2016-08-29 2018-03-13 鲁南制药集团股份有限公司 一种3α‑羟基‑6α‑乙基‑7‑酮‑5β‑胆‑24‑酸的制备方法
CN108348533A (zh) * 2015-11-06 2018-07-31 英特塞普特医药品公司 制备奥贝胆酸及其衍生物的方法
CN108348543A (zh) * 2015-09-21 2018-07-31 英特塞普特医药品公司 促进肝再生的方法
CN108440629A (zh) * 2018-03-16 2018-08-24 丽珠集团新北江制药股份有限公司 一种制备奥贝胆酸中间体及奥贝胆酸的方法
CN108495858A (zh) * 2015-12-22 2018-09-04 英特塞普特医药品公司 奥贝胆酸的多晶结晶形式
CN108779141A (zh) * 2016-02-10 2018-11-09 雷迪博士实验室有限公司 奥贝胆酸的胺盐
CN108794558A (zh) * 2018-07-03 2018-11-13 丽珠集团新北江制药股份有限公司 一种反应条件温和的奥贝胆酸制备方法
CN109069517A (zh) * 2016-04-19 2018-12-21 英特塞普特医药品公司 制备奥贝胆酸及其衍生物的方法
CN109152787A (zh) * 2016-03-31 2019-01-04 英特塞普特医药品公司 具有优越的溶出性的口服制剂
CN109195607A (zh) * 2016-03-31 2019-01-11 英特塞普特医药品公司 具有活性成分的高化学稳定性的薄膜包衣片剂
CN109280071A (zh) * 2017-07-19 2019-01-29 东莞东阳光药物研发有限公司 奥贝胆酸的晶型及其制备方法
CN109485687A (zh) * 2017-09-12 2019-03-19 成都弘达药业有限公司 奥贝胆酸的晶型j及其制备方法
CN110655550A (zh) * 2018-06-29 2020-01-07 江苏海悦康医药科技有限公司 (E)-3α-羟基-6-亚乙基-7-氧代-5β-胆甾烷-24-酸的制备方法

Families Citing this family (123)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60205891T2 (de) 2001-03-12 2006-06-22 Intercept Pharmaceuticals, Inc. Steroide als agonisten für fxr
WO2011140441A2 (en) 2010-05-06 2011-11-10 Children's Hospital Medical Center Methods and systems for converting precursor cells into intestinal tissues through directed differentiation
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
PT3336097T (pt) 2012-06-19 2020-10-29 Intercept Pharmaceuticals Inc Preparação da forma não cristalina de ácido obeticólico
NZ708501A (en) * 2012-11-28 2019-03-29 Intercept Pharmaceuticals Inc Treatment of pulmonary disease
US9814733B2 (en) * 2012-12-31 2017-11-14 A,arin Pharmaceuticals Ireland Limited Compositions comprising EPA and obeticholic acid and methods of use thereof
US9725481B2 (en) 2013-04-17 2017-08-08 Sage Therapeutics, Inc. 19-nor C3, 3-disubstituted C21-C-bound heteroaryl steroids and methods of use thereof
WO2014169836A1 (en) 2013-04-17 2014-10-23 Sage Therapeutics, Inc. 19-nor neuroactive steroids and methods of use thereof
SI2986624T1 (sl) 2013-04-17 2020-10-30 Sage Therapeutics, Inc. 19-nor nevroaktivni steroidi za metode zdravljenja
EP2986623B1 (en) 2013-04-17 2018-11-07 Sage Therapeutics, Inc. 19-nor c3,3-disubstituted c21-n-pyrazolyl steroids and methods of use thereof
SI3021852T1 (sl) 2013-07-19 2021-07-30 Sage Therapeutics, Inc. Nevroaktivni steroidi, sestavki in uporabe le-teh
JP6466942B2 (ja) 2013-08-23 2019-02-06 セージ セラピューティクス， インコーポレイテッド 向神経活性ステロイド、組成物、及びその使用
EP3149156B1 (en) 2014-05-28 2021-02-17 Children's Hospital Medical Center Methods and systems for converting precursor cells into gastric tissues through directed differentiation
LT3149019T (lt) 2014-05-29 2020-02-25 Bar Pharmaceuticals S.R.L. Cholano dariniai, skirti naudoti fxr ir tgr5/gpbar1 medijuojamų ligų gydymui ir (arba) prevencijai
WO2015195962A1 (en) 2014-06-18 2015-12-23 Sage Therapeutics, Inc. Neuroactive steroids, compositions, and uses thereof
CN106459136B (zh) * 2014-09-28 2018-06-26 江苏盛迪医药有限公司 一种奥贝胆酸的制备方法
EP4527461A3 (en) 2014-10-16 2025-06-25 Sage Therapeutics, Inc. A compound, compositions thereof and this compound for use in methods of treating cns disorders
RS60642B1 (sr) 2014-10-16 2020-09-30 Sage Therapeutics Inc Kompozicije i postupci za lečenje poremećaja cns-a
US11584916B2 (en) 2014-10-17 2023-02-21 Children's Hospital Medical Center Method of making in vivo human small intestine organoids from pluripotent stem cells
EP3215179A4 (en) 2014-11-06 2018-07-25 Enanta Pharmaceuticals, Inc. Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
WO2016079517A1 (en) 2014-11-19 2016-05-26 Dextra Laboratories Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
EA033603B1 (ru) 2014-11-19 2019-11-08 Nzp Uk Ltd 6-альфа-алкил-6,7-дионовые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
EA033445B1 (ru) 2014-11-19 2019-10-31 Nzp Uk Ltd 5-бета-6-алкил-7-гидрокси-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
WO2016079519A1 (en) * 2014-11-19 2016-05-26 Dextra Laboratories Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
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
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
SMT202000276T1 (it) 2014-11-27 2020-07-08 Sage Therapeutics Inc Composizioni e metodi per trattare disturbi del snc
CN105777835B (zh) * 2014-12-25 2020-02-14 重庆药友制药有限责任公司 一种制备鹅去氧胆酸类似物的方法
CN105801653B (zh) 2014-12-30 2018-04-17 苏州晶云药物科技有限公司 奥贝胆酸的晶型a及其制备方法
CN105859814A (zh) * 2015-01-23 2016-08-17 江苏奥赛康药业股份有限公司 一种奥贝胆酸化合物及其药物组合物
SMT202100113T1 (it) 2015-01-26 2021-05-07 Sage Therapeutics Inc Composizioni e metodi per trattare disturbi del snc
EA036404B1 (ru) 2015-02-06 2020-11-06 Интерсепт Фармасьютикалз, Инк. Фармацевтические композиции для комбинированной терапии
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.
CN105985395A (zh) * 2015-02-13 2016-10-05 江苏奥赛康药业股份有限公司 一种奥贝胆酸化合物及含有该化合物的药物组合物
CN105985396A (zh) * 2015-02-16 2016-10-05 苏州泽璟生物制药有限公司 氘代鹅去氧胆酸衍生物以及包含该化合物的药物组合物
JP6875996B2 (ja) 2015-02-20 2021-05-26 セージ セラピューティクス， インコーポレイテッド 神経刺激性ステロイド、組成物、およびその使用
MX2017011399A (es) * 2015-03-09 2018-03-16 Intercept Pharmaceuticals Inc Métodos para modular la densidad ósea.
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
EA036757B1 (ru) 2015-04-07 2020-12-17 Интерсепт Фармасьютикалз, Инк. Фармацевтические композиции для комбинированной терапии
CN105777836A (zh) * 2015-04-09 2016-07-20 厦门蔚扬药业有限公司 奥贝胆酸的多晶型物及其制备方法
WO2016168553A1 (en) * 2015-04-17 2016-10-20 Concert Pharmaceuticals, Inc. Deuterated obeticholic acid
PE20180690A1 (es) * 2015-04-27 2018-04-23 Intercept Pharmaceuticals Inc Composiciones de acido obeticolico y metodos de uso
CN106290594B (zh) * 2015-05-27 2020-07-17 中美华世通生物医药科技（武汉）有限公司 测定奥贝胆酸片溶出含量的方法
CN105294801A (zh) * 2015-07-02 2016-02-03 扬子江药业集团南京海陵药业有限公司 6-乙基鹅去氧胆酸异构体的合成及其分离测定方法
CZ2015504A3 (cs) 2015-07-16 2017-01-25 Zentiva, K.S. Krystalické formy obeticholové kyseliny
EP3124080A1 (en) * 2015-07-28 2017-02-01 Merz Pharma GmbH & Co. KGaA Semisynthetic bile acids for injection lipolysis
KR20180052756A (ko) 2015-09-24 2018-05-18 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체 제조를 위한 방법 및 중간체
DK3359160T3 (da) 2015-10-07 2021-11-22 Intercept Pharmaceuticals Inc Farnesoid x receptor modulatorer
CN106632564B (zh) * 2015-10-30 2021-04-13 苏州泽璟生物制药股份有限公司 奥贝胆酸盐及其无定形物和药物组合物
CN106822005A (zh) * 2015-12-03 2017-06-13 江苏先声药业有限公司 奥贝胆酸组合物及其制备方法
WO2017115324A1 (en) * 2016-01-01 2017-07-06 Lupin Limited Solid forms of obeticholic acid and processes thereof
CN105646633B (zh) * 2016-01-22 2020-05-26 南京长澳医药科技有限公司 一种制备奥贝胆酸1型的方法
US10519193B2 (en) 2016-02-02 2019-12-31 Shenzhen Targetrx, Inc. Steroidal compound, composition containing the same and use thereof
WO2017136617A1 (en) * 2016-02-04 2017-08-10 Cinrx Pharma, Llc Deuterated domperidone compositions and methods for therapy of disorders
WO2017147137A1 (en) 2016-02-23 2017-08-31 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
US10323061B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as FXR/TGR5 agonists and methods of use thereof
EP3437659B1 (en) * 2016-03-28 2023-03-01 Intercept Pharmaceuticals, Inc. Combination of a fxr agonist and an angiotensin ii receptor blocker
WO2017167233A1 (zh) * 2016-03-31 2017-10-05 江苏恒瑞医药股份有限公司 一种奥贝胆酸的新结晶形式及其制备方法
EP3228306A1 (en) 2016-04-04 2017-10-11 ratiopharm GmbH Complex compound comprising obeticholic acid and cyclodextrin and pharmaceutical formulation comprising the complex compound
EP3440092A1 (en) 2016-04-04 2019-02-13 Dipharma Francis S.r.l. Method for preparing a farnesoid x receptor agonist
CN116790476A (zh) 2016-05-05 2023-09-22 儿童医院医疗中心 用于体外制造胃底组织的方法和与其相关的组合物
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
US10875887B2 (en) 2016-06-01 2020-12-29 Dr. Reddy's Laboratories Limited. Process for preparation of obeticholic acid
WO2017218337A1 (en) 2016-06-13 2017-12-21 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
CA3252823A1 (en) 2016-06-13 2025-02-25 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
CN106083971B (zh) * 2016-06-17 2017-11-14 苏州敬业医药化工有限公司 一种(E)‑3α‑羟基‑6‑亚乙基‑7‑酮‑5β‑胆烷‑24‑酸的制备方法
CZ2016385A3 (cs) 2016-06-28 2018-01-10 Zentiva, K.S. Způsoby přípravy intermediátů pro syntézu Obeticholové kyseliny
IL264129B2 (en) 2016-07-11 2024-05-01 Sage Therapeutics Inc C17, c20, and c21 substituted neuroactive steroids and their methods of use
NZ790187A (en) 2016-07-11 2025-08-29 Sage Therapeutics Inc C7, C12, and C16 substituted neuroactive steroids and their methods of use
EP3287467A1 (en) 2016-08-22 2018-02-28 ratiopharm GmbH Preparation of obeticholic acid comprising continuous flow process steps
EP3293196A1 (en) 2016-09-09 2018-03-14 Hexal AG Process for purifying obeticholic acid
BR112019006242A2 (pt) * 2016-09-30 2019-06-18 Intercept Pharmaceuticals Inc formas cristalinas de um derivado de ácido biliar
CN107976506B (zh) * 2016-10-25 2020-05-12 成都弘达药业有限公司 一种奥贝胆酸有关物质的检测方法
KR102546194B1 (ko) 2016-11-04 2023-06-21 칠드런즈 호스피탈 메디칼 센터 간 유사 장기 조성물 및 이를 제조 및 사용하는 방법
KR102499441B1 (ko) 2016-11-29 2023-02-13 이난타 파마슈티칼스, 인코포레이티드 술포닐우레아 담즙산 유도체의 제조 방법
KR102558606B1 (ko) 2016-12-05 2023-07-26 칠드런즈 호스피탈 메디칼 센터 결장 유사장기 및 이를 제조 및 사용하는 방법
EP3551180B1 (en) * 2016-12-09 2021-09-29 Cadila Healthcare Limited Treatment for primary biliary cholangitis
CN108614038B (zh) * 2016-12-13 2022-05-17 亚宝药业集团股份有限公司 一种测定奥贝胆酸原料药有关物质的方法
CN106645497A (zh) * 2017-01-03 2017-05-10 山东省药学科学院 一种奥贝胆酸及其制剂中有关物质的检测方法
KR20190103327A (ko) 2017-01-18 2019-09-04 트렘코 인코포레이티드 구조용 접합 복합재
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
JP2020514337A (ja) * 2017-03-08 2020-05-21 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 オベチコール酸の結晶形態
SI3600309T1 (sl) 2017-03-28 2022-10-28 Gilead Sciences, Inc. Terapevtske kombinacije za zdravljenje bolezni jeter
CN108659086A (zh) * 2017-03-29 2018-10-16 杭州源昶医药科技有限公司 一种奥贝胆酸的合成方法
US10676500B2 (en) 2017-04-07 2020-06-09 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
WO2018191673A1 (en) 2017-04-14 2018-10-18 Children's Hospital Medical Center Multi donor stem cell compositions and methods of making same
US11053275B2 (en) 2017-04-20 2021-07-06 Daewoong Bio Inc. Method for bile acid derivative by using continuous flow reaction
WO2018211413A1 (en) * 2017-05-15 2018-11-22 Dr. Reddy’S Laboratories Limited Solid forms of obeticholic acid and process for preparation
CZ2017298A3 (cs) 2017-05-26 2018-12-05 Zentiva, K.S. Amorfní formy obeticholové kyseliny
KR20240125702A (ko) 2017-06-30 2024-08-19 신돔 파마, 인크. 중수소화 돔페리돈 조성물, 방법, 및 제조
US12478612B2 (en) 2017-06-30 2025-11-25 Cindome Pharma, Inc. Deuterated domperidone compositions, methods, and preparation
AU2018307611A1 (en) 2017-07-24 2020-02-06 Intercept Pharmaceuticals, Inc. Isotopically labeled bile acid derivatives
JP6937893B2 (ja) 2017-08-03 2021-09-22 メディトックス インク． 胆汁酸類を製造するための方法
EP3694603A4 (en) 2017-10-10 2021-07-14 Children's Hospital Medical Center ESOPHAGUS TISSUE AND / OR ORGANOID COMPOSITIONS AND METHOD FOR MANUFACTURING THEREOF
US10611793B1 (en) 2017-11-27 2020-04-07 Teva Czech Industries S.R.O. Solid state forms of obeticholic acid salts
WO2019106043A1 (en) 2017-11-29 2019-06-06 Hexal Ag Pharmaceutical composition comprising obeticholic acid
WO2019113494A1 (en) * 2017-12-08 2019-06-13 Sage Therapeutics, Inc. Deuterated 21 -[4-cyano-pyrazol-1 -yl]-19-nor-pregan-3. alpha-ol-20-one derivatives for treating cns disorders
EP3727394A4 (en) 2017-12-21 2021-09-08 Children's Hospital Medical Center DIGITALIZED HUMAN ORGANOIDS AND METHOD OF USING THEREOF
US11434256B2 (en) 2018-01-25 2022-09-06 Msn Laboratories Private Limited, R&D Center Process for the preparation of 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-oic acid
WO2019197962A1 (en) * 2018-04-09 2019-10-17 Biophore India Pharmaceuticals Pvt. Ltd Crystalline forms of (3α, 5β, 6α, 7α)-6-ethyl-3, 7-dihydroxycholan-24-oic acid (obeticholic acid) and processes thereof
JP7506657B2 (ja) 2018-07-26 2024-06-26 チルドレンズ ホスピタル メディカル センター 肝胆膵組織およびその作製方法
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
US20210261599A1 (en) * 2018-08-24 2021-08-26 Solara Active Pharma Sciences Limited Process for the Preparation of Obeticholic Acid and Intermediates Used In the Process Thereof
US12428622B2 (en) 2018-09-12 2025-09-30 Children's Hospital Medical Center Organoid compositions for the production of hematopoietic stem cells and derivatives thereof
JP2022506782A (ja) * 2018-11-08 2022-01-17 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 オベチコール酸の使用方法
CN109535217B (zh) * 2018-11-13 2020-04-14 丽珠集团新北江制药股份有限公司 一种奥贝胆酸的精制方法
WO2020150136A1 (en) 2019-01-15 2020-07-23 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
US11524005B2 (en) 2019-02-19 2022-12-13 Gilead Sciences, Inc. Solid forms of FXR agonists
CA3142358A1 (en) 2019-05-30 2020-12-03 Intercept Pharmaceuticals, Inc. Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease
JP7610533B2 (ja) 2019-05-31 2025-01-08 チルドレンズ ホスピタル メディカル センター 造血幹細胞の生成および拡大方法
SG11202112391UA (en) 2019-05-31 2021-12-30 Sage Therapeutics Inc Neuroactive steroids and compositions thereof
WO2021029656A1 (ko) * 2019-08-14 2021-02-18 주식회사 바이오톡스텍 하이드로퀴논 유도체, 및 오베티콜릭산을 포함하는 비알콜성 지방간염의 예방 또는 치료용 약학조성물
CN112824425B (zh) * 2019-11-21 2023-10-03 成都西岭源药业有限公司 一种6-位烯基取代胆酸化合物及其制备方法和应用
US20230201222A1 (en) * 2020-05-13 2023-06-29 Children's Hospital Medical Center Alleviation of liver injury by activating the signaling pathway mediated by farnesoid x receptor
WO2022051321A1 (en) 2020-09-03 2022-03-10 Coherus Biosciences, Inc. Fixed dose combinations of chs-131 and a fxr agonist
KR102526452B1 (ko) * 2020-10-28 2023-04-27 (주)델로 관절 구조를 포함하는 토이 로봇
CN114644670A (zh) * 2020-12-17 2022-06-21 四川弘远药业有限公司 奥贝胆酸和对氨基苯甲酸的共晶及其制备方法
CN114236027B (zh) * 2021-12-22 2024-01-12 中山百灵生物技术股份有限公司 一种(E)-6-亚乙基-3α-羟基-7-酮基-5β-胆甾烷-24-酸的检测方法
US12343351B2 (en) 2022-03-25 2025-07-01 Rutgers, The State University Of New Jersey Pulmonary function treatment

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002072598A1 (en) * 2001-03-12 2002-09-19 Roberto Pellicciari Steroids as agonists for fxr
WO2005082925A2 (en) * 2004-02-26 2005-09-09 Intercept Pharmaceuticals Inc. Novel steroid agonist for fxr
CN101203526A (zh) * 2005-05-19 2008-06-18 伊莱吉尔瑞公司 制备3α(β)-7α(β)-二羟基-6α(β)-烷基-5β-胆烷酸的方法

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4072695A (en) * 1972-09-21 1978-02-07 Intellectual Property Development Corporation 3α,7α-Dihydroxy-cholanic acid derivatives
IT1137459B (it) * 1981-04-14 1986-09-10 Erregierre Spa Prodesso per la preparazione di acido ursodeossicolico ad alta purezza
DE3366932D1 (en) 1982-07-29 1986-11-20 Lehner Ag New derivatives of biliary acids, process for the production thereof and pharmaceutical compositions containing the same
IT1206112B (it) 1983-04-29 1989-04-14 Lehner Ag Nuovi derivati di acidi biliari, procedimento per la loro preparazione e relative composizioni farmaceutiche.
IT1212835B (it) 1983-08-18 1989-11-30 Lehner Ag Derivati di acidi biliari, procedimento per la loro preparazione e relative composizioni farmaceutiche.
US4892868A (en) 1984-08-17 1990-01-09 Gipharmex, S.P.A. Derivatives of biliary acids, process for the production thereof and corresponding pharmaceutical compositions
IT1196377B (it) 1984-12-21 1988-11-16 Lehner Ag Derivati di acidi biliari,procedimento per la loro preparazione e relative composizioni farmaceutiche
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
IT1223313B (it) 1987-10-20 1990-09-19 Gipharmex Spa Derivati di acidi biliari loro preparazione e composizioni farmaceutiche che li contengono
JPH0320265A (ja) * 1989-02-10 1991-01-29 Meiji Seika Kaisha Ltd アミノチアゾール酢酸誘導体並びにその製造法
IT1229570B (it) 1989-04-17 1991-09-04 Giuliani Spa Derivati fluorurati di acidi biliari, loro preparazione e composizioni farmaceutiche che li contengono.
US5175320A (en) 1989-04-17 1992-12-29 Giuliani S.P.A. Fluorinated bile acid derivatives, processes for the preparation thereof and pharmaceutical compositions containing them
ES2074113T3 (es) 1989-12-13 1995-09-01 Mitsubishi Chem Corp Nuevos derivados de acido pirazolil acrilico, utiles como fungicidas sistemicos para la proteccion de plantas y materiales.
WO1997028149A1 (en) 1996-02-02 1997-08-07 Merck & Co., Inc. Method for raising hdl cholesterol levels
GB9604242D0 (en) 1996-02-28 1996-05-01 Glaxo Wellcome Inc Chemical compounds
GB9606805D0 (en) 1996-03-30 1996-06-05 Glaxo Wellcome Inc Medicaments
JP2000514807A (ja) 1996-07-12 2000-11-07 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー レプチン耐性の新規な治療
JP3600713B2 (ja) * 1997-08-06 2004-12-15 東京応化工業株式会社 ポジ型ホトレジスト組成物
US6008237A (en) 1997-12-19 1999-12-28 Merck & Co., Inc. Arylthiazolidinedione derivatives
JP4253126B2 (ja) 1998-01-29 2009-04-08 アムジェン インコーポレイテッド Ｐｐａｒ−ガンマ調節剤
JP3146187B2 (ja) * 1998-06-26 2001-03-12 高砂香料工業株式会社 ジホスフィンオキシドの新規な製造方法
AU1229000A (en) 1998-10-23 2000-05-15 Glaxo Group Limited Assays for ligands for nuclear receptors
AU2389100A (en) 1998-12-23 2000-07-12 Glaxo Group Limited Assays for ligands for nuclear receptors
AU2409600A (en) 1999-01-07 2000-07-24 Tularik Inc. Fxr receptor-mediated modulation of cholesterol metabolism
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
EP1473042B1 (en) 1999-03-26 2006-06-21 City of Hope Screening for FXR receptor modulators
CA2368234A1 (en) 1999-03-26 2000-10-05 City Of Hope Method of affecting cholesterol catabolism using nuclear bile acid receptor
BR0011743A (pt) 1999-06-11 2002-03-05 Allergan Sales Inc Método para modular a atividade de receptor de fxr
US6906057B1 (en) 1999-06-11 2005-06-14 Allergan, Inc. Methods for modulating FXR receptor activity
US6559188B1 (en) 1999-09-17 2003-05-06 Novartis Ag Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes
WO2001030343A1 (en) 1999-10-22 2001-05-03 Merck & Co., Inc. Pharmaceuticals for treating obesity
US6627636B2 (en) 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
AU2001288623A1 (en) 2000-09-05 2002-03-22 Tularik, Inc. Fxr modulators
US20020119958A1 (en) 2001-02-13 2002-08-29 Shinichiro Tojo Therapeutic agent for hyperlipidemia
US7354726B2 (en) 2001-04-12 2008-04-08 Takeda Pharmaceutical Company Limited Screening method
EP1423113A4 (en) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag NR1H4 NUCLEAR RECEPTOR BINDING COMPOUNDS
DE60131967D1 (de) 2001-08-13 2008-01-31 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
WO2003016280A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
US7112340B2 (en) * 2001-10-19 2006-09-26 Baxter International Inc. Compositions of and method for preparing stable particles in a frozen aqueous matrix
KR20050044450A (ko) 2001-11-14 2005-05-12 테바 파마슈티컬 인더스트리즈 리미티드 로사르탄 칼륨의 무정형 및 결정형 형태 및 이의 제조 방법
US20030144360A1 (en) 2001-11-19 2003-07-31 Allergan Sales, Inc. Composition and method for modulating BAR/FXR receptor activity
WO2003080803A2 (en) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Methods of using farnesoid x receptor (fxr) agonists
WO2003086303A2 (en) 2002-04-12 2003-10-23 The University Of Chicago Farnesoid x-activated receptor agonists
US6987121B2 (en) 2002-04-25 2006-01-17 Smithkline Beecham Corporation Compositions and methods for hepatoprotection and treatment of cholestasis
ITMI20021532A1 (it) 2002-07-12 2004-01-12 Roberto Pellicciari Composti chimici
AU2003290700A1 (en) 2002-11-22 2004-06-18 Smithkline Beecham Corporation Farnesoid x receptor agonists
US20070015796A1 (en) 2003-09-26 2007-01-18 Smithkline Beecham Corporation Compositions and methods for treatment of fibrosis
TW200603818A (en) * 2004-03-11 2006-02-01 Fresenius Kabi De Gmbh Conjugates of hydroxyethyl starch and erythropoietin
EP3175855B1 (en) 2004-03-12 2020-07-15 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
CA2574279A1 (en) * 2004-08-10 2006-02-23 Exelixis, Inc. Heterocyclic compounds as pharmaceutical agents
US20060252670A1 (en) * 2004-10-14 2006-11-09 Intercept Pharmaceuticals Inc. Method of reducing drug-induced adverse side effects in a patient
ES2732251T3 (es) 2005-04-25 2019-11-21 Enterin Inc Dilactato de escualamina cristalino
JP2007077123A (ja) 2005-09-16 2007-03-29 Shiono Chemical Co Ltd 非晶質セフジニル、その製造方法およびこれを含有する経口投与用医薬組成物
PL2040713T3 (pl) 2006-06-27 2014-11-28 Intercept Pharmaceuticals Inc Pochodne kwasów żółciowych jako ligandy FXR do zapobiegania lub leczenia chorób lub stanów, w których pośredniczy FXR
EP1894924A1 (en) * 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
CL2007003035A1 (es) * 2006-10-24 2008-05-16 Smithkline Beechman Corp Compuestos derivados de isoxazol sustituidos, agonistas de receptores farnesoid x; procedimiento de preparacion; composicion farmaceutica que lo comprende; y uso del compuesto en el tratamiento de la obesidad, diabetes mellitus, fibrosis en organos,
BRPI0808684B1 (pt) 2007-01-19 2021-08-10 Intercept Pharmaceuticals, Inc Compostos moduladores de tgr5, composição e seus usos
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
US8338628B2 (en) 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
AU2008323017B2 (en) * 2007-11-15 2012-12-20 F. Hoffmann-La Roche Ag Methyl-benzimidazole derivatives
WO2011022838A1 (en) 2009-08-25 2011-03-03 British Columbia Cancer Agency Branch Polyhydroxylated bile acids for treatment of biliary disorders
US8796249B2 (en) 2008-07-30 2014-08-05 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
US20110190242A1 (en) * 2008-09-23 2011-08-04 Resolvyx Pharmaceuticals, Inc. Compositions and methods for the treatment of inflammatory disease
PL2698375T3 (pl) 2008-11-19 2018-08-31 Intercept Pharmaceuticals, Inc. Modulatory TGR5 i sposób ich zastosowania
CN102121547B (zh) * 2010-12-23 2013-01-16 拉卡萨安吉拉股份有限公司 用于管道接头的衬套和采用该衬套的管道接头
CN102372757B (zh) 2011-10-31 2013-01-16 安徽科宝生物工程有限公司 酯化法制备猪胆汁中鹅去氧胆酸的方法
PT3336097T (pt) 2012-06-19 2020-10-29 Intercept Pharmaceuticals Inc Preparação da forma não cristalina de ácido obeticólico

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002072598A1 (en) * 2001-03-12 2002-09-19 Roberto Pellicciari Steroids as agonists for fxr
WO2005082925A2 (en) * 2004-02-26 2005-09-09 Intercept Pharmaceuticals Inc. Novel steroid agonist for fxr
CN101203526A (zh) * 2005-05-19 2008-06-18 伊莱吉尔瑞公司 制备3α(β)-7α(β)-二羟基-6α(β)-烷基-5β-胆烷酸的方法

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
贾薇等: "法呢醇X受体激动剂研究进展", 《中国药物化学杂志》 *

Cited By (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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