ATE303399T1 - Steroide als agonisten für fxr - Google Patents

Steroide als agonisten für fxr

Info

Publication number
ATE303399T1
ATE303399T1 AT02750526T AT02750526T ATE303399T1 AT E303399 T1 ATE303399 T1 AT E303399T1 AT 02750526 T AT02750526 T AT 02750526T AT 02750526 T AT02750526 T AT 02750526T AT E303399 T1 ATE303399 T1 AT E303399T1
Authority
AT
Austria
Prior art keywords
fxr
agonists
steroids
compounds
formula
Prior art date
Application number
AT02750526T
Other languages
English (en)
Inventor
Roberto Pellicciari
Original Assignee
Intercept Pharmaceuticals Inc
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=23050302&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ATE303399(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Intercept Pharmaceuticals Inc filed Critical Intercept Pharmaceuticals Inc
Application granted granted Critical
Publication of ATE303399T1 publication Critical patent/ATE303399T1/de

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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/08—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with only one hydroxy group and one amino group bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
    • C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
    • C07C215/12—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic the nitrogen atom of the amino group being further bound to hydrocarbon groups substituted by hydroxy groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055—Normal 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • External Artificial Organs (AREA)
AT02750526T 2001-03-12 2002-02-21 Steroide als agonisten für fxr ATE303399T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27495901P 2001-03-12 2001-03-12
PCT/EP2002/001832 WO2002072598A1 (en) 2001-03-12 2002-02-21 Steroids as agonists for fxr

Publications (1)

Publication Number Publication Date
ATE303399T1 true ATE303399T1 (de) 2005-09-15

Family

ID=23050302

Family Applications (1)

Application Number Title Priority Date Filing Date
AT02750526T ATE303399T1 (de) 2001-03-12 2002-02-21 Steroide als agonisten für fxr

Country Status (16)

Country Link
US (9) US7138390B2 (de)
EP (1) EP1392714B1 (de)
JP (2) JP4021327B2 (de)
AT (1) ATE303399T1 (de)
AU (1) AU2002308295B2 (de)
BE (1) BE2017C018I2 (de)
CA (1) CA2440680C (de)
CY (1) CY2017020I1 (de)
DE (1) DE60205891T2 (de)
DK (1) DK1392714T3 (de)
ES (1) ES2248581T3 (de)
FR (1) FR17C0003I2 (de)
IL (2) IL157816A0 (de)
NL (1) NL300877I2 (de)
NO (2) NO326134B1 (de)
WO (1) WO2002072598A1 (de)

Families Citing this family (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1392714B1 (de) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroide als agonisten für fxr
EP1465882B1 (de) 2001-12-21 2011-08-24 X-Ceptor Therapeutics, Inc. Heterocyclische modulatoren von nukleären rezeptoren
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
SI2712617T1 (sl) * 2004-03-12 2017-01-31 Intercept Pharmaceuticals, Inc. Zdravljenje fibroze z uporabo Fxr ligandov
US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
WO2005092328A1 (ja) * 2004-03-29 2005-10-06 Japan Health Sciences Foundation Ｆｘｒ活性化化合物
ITMI20050912A1 (it) * 2005-05-19 2006-11-20 Erregierre Spa Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
US7618956B2 (en) 2005-05-31 2009-11-17 The Gillette Company Reduction of hair growth
CA2656320C (en) * 2006-06-27 2015-04-28 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
EP1886685A1 (de) 2006-08-11 2008-02-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Methoden, Verwendungen und Zusammensetzungen zur Modulation der Replikation von HCV durch Aktivierung oder Hemmung des Farnesoid X Rezeptors
KR100846441B1 (ko) * 2006-12-22 2008-07-16 재단법인서울대학교산학협력재단 스테롤 계 유도체를 함유하는 약제학적 조성물, 건강식품조성물, 화장품 조성물 및 파나소이드 엑스 핵 수용체 활성억제제 조성물
EA017714B1 (ru) 2007-01-19 2013-02-28 Интерсепт Фармасьютикалз, Инк. Модуляторы tgr5 и способы их применения
US8338628B2 (en) * 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
CA2732323C (en) 2008-07-30 2017-06-27 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
PL2698375T3 (pl) 2008-11-19 2018-08-31 Intercept Pharmaceuticals, Inc. Modulatory TGR5 i sposób ich zastosowania
US20110257139A1 (en) 2008-12-19 2011-10-20 Royal College Of Surgeons In Ireland Treatment of diarrhoea
SG10201607230SA (en) 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
US9777038B2 (en) * 2012-10-26 2017-10-03 Intercept Pharmaceuticals, Inc. Process for preparing bile acid derivatives
AU2013352288B2 (en) * 2012-11-28 2017-11-23 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
WO2014200349A1 (en) 2013-06-13 2014-12-18 Fast Forward Pharmaceutical B.V. Cd40 signalling inhibitor and a further compound, wherein the further compound is a bile acid, a bile acid derivative, an tgr5-receptor agonist, an fxr agonist or a combination thereof, for the treatment of chronic inflammation, and the prevention of gastrointestinal cancer or fibrosis.
MX377523B (es) * 2013-09-11 2025-03-10 Inst Nat Sante Rech Med Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b.
CN112220797B (zh) 2013-11-22 2023-11-03 米纳治疗有限公司 C/EBPα组合物和使用方法
CN104876995B (zh) * 2014-02-27 2016-09-07 人福医药集团股份公司 鹅去氧胆酸衍生物的制备方法
PT3149019T (pt) 2014-05-29 2020-02-19 Bar Pharmaceuticals S R L Derivados de colano para utilização no tratamento e/ou na prevenção de doenças mediadas por fxr e tgr5/gp-bar1
EP3006557A1 (de) 2014-10-07 2016-04-13 Heinrich-Heine-Universität Düsseldorf Gallensäuren zur Induzierung hepatischer Differenzierung
CN105585603B (zh) * 2014-10-21 2019-05-24 重庆医药工业研究院有限责任公司 一种制备奥贝胆酸中间体的方法
SG11201703717SA (en) 2014-11-06 2017-06-29 Enanta Pharm Inc Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
CN105669811B (zh) * 2014-11-17 2020-09-04 正大天晴药业集团股份有限公司 新的7-酮-6β-烷基胆烷酸衍生物在制备奥贝胆酸以及其在医药领域的用途
KR102527821B1 (ko) 2014-11-19 2023-05-02 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 6α-알킬-6,7-다이온 스테로이드
PL3221332T3 (pl) 2014-11-19 2019-10-31 Nzp Uk Ltd Steroidy, 5.beta.-6-alkilo-7-hydroksy-3-ony jako związki pośrednie do wytwarzania steroidowych modulatorów fxr
ES2748692T3 (es) * 2014-11-19 2020-03-17 Nzp Uk Ltd Esteroides 6.alfa.-alquil-3,7-diona como intermedios para la producción de moduladores FXR de esteroides
EA033427B1 (ru) 2014-11-19 2019-10-31 Nzp Uk Ltd 6-алкил-7-гидрокси-4-ен-3-оновые стероиды в качестве промежуточных соединений для получения стероидных модуляторов fxr
KR20170099909A (ko) 2014-11-26 2017-09-01 이난타 파마슈티칼스, 인코포레이티드 Fxr/tgr5 작용제로서의 담즙산 유사체 및 이의 이용 방법
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
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
CN104672290B (zh) * 2015-01-05 2017-06-06 北京普禄德医药科技有限公司 一种用于预防或治疗fxr‑介导的疾病的药物及其制备方法和用途
BR112017016766B1 (pt) 2015-02-06 2023-11-07 Intercept Pharmaceuticals, Inc Composição compreendendo um agonista fxr e fibrato, bem como uso para tratar doença hepática colestática
CN107249594A (zh) 2015-02-11 2017-10-13 英安塔制药有限公司 作为fxr/tgr5激动剂的胆汁酸类似物及其使用方法
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
SG10201910670RA (en) 2015-03-31 2020-01-30 Enanta Pharm Inc Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
MA41083A1 (fr) 2015-04-07 2018-05-31 Intercept Pharmaceuticals Inc Compositions pharmaceutiques pour thérapie combinée
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
CZ2015504A3 (cs) 2015-07-16 2017-01-25 Zentiva, K.S. Krystalické formy obeticholové kyseliny
CN105085597B (zh) * 2015-08-28 2017-03-29 成都百裕制药股份有限公司 一种无定型奥贝胆酸的制备方法
CN106478759A (zh) * 2015-08-31 2017-03-08 陕西合成药业股份有限公司 奥贝胆酸衍生物及其制备方法和用途
HK1254056A1 (zh) 2015-09-21 2019-07-12 英特塞普特医药品公司 促进肝再生的方法
CN108350020A (zh) 2015-09-24 2018-07-31 英特塞普特医药品公司 用于制备胆汁酸衍生物的方法和中间体
CN106589039B (zh) * 2015-10-15 2019-12-17 苏州朗科生物技术股份有限公司 一种奥贝胆酸的制备方法及相关化合物
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
EP3370728A4 (de) * 2015-11-06 2019-07-10 Intercept Pharmaceuticals, Inc. Verfahren und vorrichtung zur herstellung von obeticholsäure und derivaten davon
CN106749466B (zh) * 2015-11-23 2019-05-21 南京济群医药科技股份有限公司 一种高纯度奥贝胆酸的制备方法
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
WO2017115324A1 (en) 2016-01-01 2017-07-06 Lupin Limited Solid forms of obeticholic acid and processes thereof
JP6924765B2 (ja) 2016-01-28 2021-08-25 チア タイ ティエンチン ファーマシューティカル グループ カンパニー リミテッドChia Tai Tianqing Pharmaceutical Group Co., Ltd. ステロイド誘導体ｆｘｒ作動薬
US11168107B2 (en) * 2016-02-10 2021-11-09 Dr. Reddy's Laboratories Limited Amine salt of obeticholic acid
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
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
US10364267B2 (en) 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
CN106008639B (zh) * 2016-03-11 2019-01-08 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
CN105541953B (zh) * 2016-03-15 2017-11-21 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
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
MX2018011813A (es) 2016-03-28 2019-01-24 Intercept Pharmaceuticals Inc Medicina obtenida mediante la combinacion de agonista fxr y arb.
CA3019499A1 (en) 2016-03-31 2017-10-05 Intercept Pharmaceuticals, Inc. Film-coated tablet having high chemical stability of active ingredient
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
CN109311933A (zh) * 2016-04-04 2019-02-05 迪法玛弗朗西斯有限公司 制备法尼醇x受体激动剂的方法
EP3228306A1 (de) 2016-04-04 2017-10-11 ratiopharm GmbH Komplexverbindung mit obeticholsäure und cyclodextrin sowie pharmazeutische formulierung mit der komplexverbindung
ITUA20162272A1 (it) * 2016-04-04 2017-10-04 Dipharma Francis Srl Procedimento per la preparazione di un agonista del recettore farnesoide x
KR102377338B1 (ko) 2016-04-13 2022-03-21 인터셉트 파마슈티컬즈, 인크. 암의 치료 방법
TW201738254A (zh) 2016-04-19 2017-11-01 英特賽普醫藥品公司 奧貝膽酸及其衍生物之製備方法
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
EA038580B9 (ru) * 2016-05-18 2021-10-05 Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. Агонист fxr, представляющий собой производное стероидов
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
WO2017207648A1 (en) 2016-05-31 2017-12-07 Bionice, S.L.U Process and intermediates for the preparation of obeticholic acid and derivatives thereof
US10875887B2 (en) 2016-06-01 2020-12-29 Dr. Reddy's Laboratories Limited. Process for preparation of obeticholic acid
CZ2016385A3 (cs) 2016-06-28 2018-01-10 Zentiva, K.S. Způsoby přípravy intermediátů pro syntézu Obeticholové kyseliny
TWI606565B (zh) * 2016-08-31 2017-11-21 金寶電子工業股份有限公司 封裝結構及其製作方法
EP3293196A1 (de) 2016-09-09 2018-03-14 Hexal AG Verfahren zur reinigung von obeticholsäure
AU2017338853A1 (en) 2016-10-04 2019-04-18 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
EP3305799A3 (de) 2016-10-07 2018-06-20 Lupin Limited Salze von obeticholsäure
JP7057783B2 (ja) 2016-11-29 2022-04-20 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 スルホニル尿素胆汁酸誘導体の調製方法
CN108264532B (zh) * 2016-12-30 2021-02-26 上海现代制药股份有限公司 一种奥贝胆酸的制备方法及其中间体
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
EP3585374B1 (de) 2017-02-21 2023-07-19 Genfit Kombination aus einem ppar agonisten und einem fxr agonisten
CN110944635A (zh) 2017-03-30 2020-03-31 国家医疗保健研究所 用于减少附加体病毒的持久性和表达的方法和药物组合物
BR112019020780A2 (pt) 2017-04-07 2020-04-28 Enanta Pharm Inc processo para preparação de derivados de ácido biliar de carbamato de sulfonila
CZ2017298A3 (cs) 2017-05-26 2018-12-05 Zentiva, K.S. Amorfní formy obeticholové kyseliny
CN109134572A (zh) * 2017-06-19 2019-01-04 中国科学院上海药物研究所 胆酸衍生物及其制备方法和用途
US11189472B2 (en) * 2017-07-17 2021-11-30 Applied Materials, Inc. Cathode assembly having a dual position magnetron and centrally fed coolant
EP3431486A1 (de) 2017-07-18 2019-01-23 Bionice, S.L.U. Verfahren und zwischenprodukte zur synthese von obeticholsäure und derivaten davon
WO2019048631A1 (en) 2017-09-08 2019-03-14 Mina Therapeutics Limited SMALL HNF4A ACTIVATOR RNA COMPOSITIONS AND METHODS OF USE
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
US10689391B2 (en) * 2017-12-12 2020-06-23 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
ES2779985B2 (es) 2019-02-20 2021-03-04 Moehs Iberica Sl Sal de dietilamina del ácido 3alfa-tetrahidropiraniloxi-6alfa-etil-7alfa-hidroxi-5ß-colánico
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
WO2020039449A1 (en) 2018-08-24 2020-02-27 Solara Active Pharma Sciences Limited An improved process for the preparation of obeticholic acid and intermediates used in the process thereof
CN111718388A (zh) 2019-03-19 2020-09-29 苏州泽璟生物制药股份有限公司 鹅去氧胆酸衍生物的制备方法
CN110025591A (zh) * 2019-04-29 2019-07-19 郑州泰丰制药有限公司 一种奥贝胆酸自乳化制剂及其软胶囊
US11555032B2 (en) 2019-05-13 2023-01-17 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
JP2022536060A (ja) 2019-05-30 2022-08-12 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 胆汁鬱滞性肝疾患の処置で使用するためのｆｘｒアゴニストおよびフィブラートを含む医薬組成物
US20220241376A1 (en) 2019-07-18 2022-08-04 Enyo Pharma Method for decreasing adverse-effects of interferon
EP4011899A4 (de) * 2019-08-06 2022-09-28 Huang, Qiang Deoxycholsäureverbindungen, pharmazeutische zusammensetzungen und verwendungen davon
IL293892A (en) 2020-01-15 2022-08-01 Inserm Institut National De La Sant? Et De La Rech M?Dicale Use of fxr agonists for treating an infection by hepatitis d virus
CN112341516B (zh) * 2020-11-14 2022-07-15 湖南科瑞生物制药股份有限公司 5,6-环氧类固醇类化合物及其制备方法和应用
CN117202905A (zh) 2021-01-14 2023-12-08 埃尼奥制药公司 Fxr激动剂和ifn用于治疗hbv感染的协同效果
JP2024517181A (ja) 2021-04-28 2024-04-19 ウエヌイグレックオ・ファーマ 組合せ治療としてｆｘｒアゴニストを使用するｔｌｒ３アゴニストの効果の強い増強
WO2024104960A1 (en) 2022-11-15 2024-05-23 Synthon B.V. Stable formulation comprising obeticholic acid

Family Cites Families (76)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2615902A (en) 1950-10-24 1952-10-28 Merck & Co Inc Chemical compounds and processes for preparing the same
US3859437A (en) 1972-06-02 1975-01-07 Intellectual Property Dev Corp Reducing cholesterol levels
US4072695A (en) 1972-09-21 1978-02-07 Intellectual Property Development Corporation 3α,7α-Dihydroxy-cholanic acid derivatives
FR2444048B1 (de) 1978-12-15 1981-08-14 Roussel Uclaf
FR2457302A1 (fr) 1979-05-23 1980-12-19 Roussel Uclaf Nouveau procede de purification de l'acide ursodesoxycholique
IT1165252B (it) 1979-07-12 1987-04-22 Blasinachim Spa Procedimento di purificazione dell'acido ursodesossicolico attraverso nuovi derivati
DE3003607C2 (de) 1980-02-01 1984-01-05 Dr.-Ing. Rudolf Hell Gmbh, 2300 Kiel Schaltungsanordnung zur partiellen Nachkorrektur von Farberkennungsräumen bei der Farberkennung
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.
US4721709A (en) 1984-07-26 1988-01-26 Pyare Seth Novel pharmaceutical compositions containing hydrophobic practically water-insoluble drugs adsorbed on pharmaceutical excipients as carrier; process for their preparation and the use of said compositions
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
IT1223313B (it) 1987-10-20 1990-09-19 Gipharmex Spa Derivati di acidi biliari loro preparazione e composizioni farmaceutiche che li contengono
FR2627696B1 (fr) 1988-02-26 1991-09-13 Fournier Innovation Synergie Nouvelle forme galenique du fenofibrate
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
IT1229570B (it) * 1989-04-17 1991-09-04 Giuliani Spa Derivati fluorurati di acidi biliari, loro preparazione e composizioni farmaceutiche che li contengono.
US4982868A (en) * 1989-11-07 1991-01-08 Robbins Edward S Iii Bail type pitcher for thin walled container
ATE121080T1 (de) * 1989-12-13 1995-04-15 Mitsubishi Chem Corp Pyrazolylacrylsäure-derivate, verwendbar als systemische fungiziden in pflanzen- und materialschutz.
JPH04250093A (ja) 1991-01-18 1992-09-04 Kanzaki Paper Mfg Co Ltd 感熱記録体
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
US6060465A (en) 1997-02-06 2000-05-09 Miljkovic; Dusan Bile acids and their derivatives as glycoregulatory agents
US6008237A (en) 1997-12-19 1999-12-28 Merck & Co., Inc. Arylthiazolidinedione derivatives
AU759255B2 (en) 1998-01-29 2003-04-10 Amgen, Inc. PPAR-gamma modulators
US6639057B1 (en) * 1998-03-26 2003-10-28 Kyowa Hakko Kogyo Co., Ltd. Monoclonal antibody against human telomerase catalytic subunit
EP1137940A4 (de) 1998-10-23 2004-06-02 Glaxo Group Ltd Verfahren zur identifizierung von liganden von nukleären rezeptoren
MXPA01004683A (es) 1998-11-09 2002-09-18 Atherogenics Inc Metodos y composiciones para disminuir los niveles de colesterol en el plasma.
UA74141C2 (uk) 1998-12-09 2005-11-15 Дж.Д. Сірл Енд Ко. Фармацевтична композиція на основі тонкоподрібненого еплеренону (варіанти), спосіб її одержання та спосіб лікування розладів, опосередкованих альдостероном (варіанти)
ES2326850T3 (es) 1998-12-23 2009-10-20 Glaxo Group Limited Ensayos para ligandos de receptores nucleares.
AU2409600A (en) 1999-01-07 2000-07-24 Tularik Inc. Fxr receptor-mediated modulation of cholesterol metabolism
WO2000057915A1 (en) 1999-03-26 2000-10-05 City Of Hope Method of affecting cholesterol catabolism using nuclear bile acid receptor
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
EP1473042B1 (de) 1999-03-26 2006-06-21 City of Hope Selektion von FXR-Rezeptormodulatoren
EP1185277B1 (de) 1999-06-11 2005-10-26 Allergan, Inc. Verwendung von synthetischen FXR Liganden zur Behandlung von Krankheiten die mit einem gestörten Gleichgewicht des Cholesterin-Spiegels verbunden sind und von Kolonkrebs
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
JP2003525217A (ja) 1999-10-22 2003-08-26 メルク エンド カムパニー インコーポレーテッド 肥満治療用薬剤
US6627636B2 (en) 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
US6777446B2 (en) * 2000-09-05 2004-08-17 Tularik, Inc. FXR modulators
US20020119958A1 (en) 2001-02-13 2002-08-29 Shinichiro Tojo Therapeutic agent for hyperlipidemia
EP1392714B1 (de) 2001-03-12 2005-08-31 Intercept Pharmaceuticals, Inc. Steroide als agonisten für fxr
WO2002084286A1 (en) 2001-04-12 2002-10-24 Takeda Chemical Industries, Ltd. Screening method
WO2003015777A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
WO2003016280A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag Nr1h4 nuclear receptor binding compounds
EP1285914B1 (de) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4-kern-rezeptor-bindende verbindungen
US7112340B2 (en) 2001-10-19 2006-09-26 Baxter International Inc. Compositions of and method for preparing stable particles in a frozen aqueous matrix
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
EP1562915A1 (de) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x rezeptor agonisten
US6993380B1 (en) 2003-06-04 2006-01-31 Cleveland Medical Devices, Inc. Quantitative sleep analysis method and system
EP1696910A4 (de) 2003-09-26 2009-12-09 Smithkline Beecham Corp Zusammensetzungen und verfahren zur behandlung von fibrose
EP1568706A1 (de) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Neuer Steroid-Agonist für FXR
AR048918A1 (es) 2004-03-11 2006-06-14 Fresenius Kabi De Gmbh Conjugados de almidon de hidroxietilo y eritropoyetina
SI2712617T1 (sl) 2004-03-12 2017-01-31 Intercept Pharmaceuticals, Inc. Zdravljenje fibroze z uporabo Fxr ligandov
US20060252670A1 (en) 2004-10-14 2006-11-09 Intercept Pharmaceuticals Inc. Method of reducing drug-induced adverse side effects in a patient
ITMI20050912A1 (it) 2005-05-19 2006-11-20 Erregierre Spa Processo di preparazione di acidi 3-a-ya(b)-diidrossi-6-a(b)-alchil-5b-colanici
WO2007095174A2 (en) 2006-02-14 2007-08-23 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
CA2656320C (en) 2006-06-27 2015-04-28 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
US20100239661A1 (en) 2006-10-26 2010-09-23 Sunilendu Bhushan Roy Pharmaceutical compositions of ursodiol
EP1947108A1 (de) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5-Modulatoren und Anwendungsverfahren dafür
EA017714B1 (ru) 2007-01-19 2013-02-28 Интерсепт Фармасьютикалз, Инк. Модуляторы tgr5 и способы их применения
US8338628B2 (en) 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
PL2698375T3 (pl) 2008-11-19 2018-08-31 Intercept Pharmaceuticals, Inc. Modulatory TGR5 i sposób ich zastosowania
MA33294B1 (fr) 2009-04-24 2012-05-02 Iceutica Pty Ltd Procédé destiné à la production de poudres de nanoparticules et de microparticules à usage commercial
EP2468762A1 (de) 2010-11-30 2012-06-27 Dr. Falk Pharma Gmbh Optimierte Synthese von reinen, nichtpolymorphen, kristallinen Gallensäuren mit definierter Partikelgröße
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
FR2981572B1 (fr) 2011-10-21 2018-01-19 Inopharm Limited Compositions pharmaceutiques d'acide ursodesoxycholique
SG10201607230SA (en) 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
PL2997035T3 (pl) 2013-05-14 2018-10-31 Intercept Pharmaceuticals, Inc. 11-hydroksy-6-podstawione pochodne kwasów żółciowych i ich koniugaty aminokwasowe jako modulatory receptorów farnezoidu x

Also Published As

Publication number Publication date
IL157816A0 (en) 2004-03-28
CA2440680A1 (en) 2002-09-19
DK1392714T3 (da) 2006-01-09
FR17C0003I1 (fr) 2017-07-21
NO20034011L (no) 2003-11-12
US20120053163A1 (en) 2012-03-01
FR17C0003I2 (fr) 2018-05-25
AU2002308295B2 (en) 2007-08-23
JP2007269815A (ja) 2007-10-18
US8058267B2 (en) 2011-11-15
EP1392714B1 (de) 2005-08-31
CA2440680C (en) 2010-06-01
USRE48286E1 (en) 2020-10-27
IL157816A (en) 2009-05-04
EP1392714A1 (de) 2004-03-03
NL300877I2 (nl) 2017-06-22
NO2017022I1 (no) 2017-05-26
WO2002072598A1 (en) 2002-09-19
DE60205891D1 (de) 2005-10-06
CY2017020I2 (el) 2017-11-14
ES2248581T3 (es) 2006-03-16
NO20034011D0 (no) 2003-09-11
US8969330B2 (en) 2015-03-03
US20100022498A1 (en) 2010-01-28
US20150166598A1 (en) 2015-06-18
US9732117B2 (en) 2017-08-15
BE2017C018I2 (de) 2021-02-04
NO2017022I2 (no) 2018-08-20
JP2004519492A (ja) 2004-07-02
US7786102B2 (en) 2010-08-31
US10421772B2 (en) 2019-09-24
DE60205891T2 (de) 2006-06-22
US20070142340A1 (en) 2007-06-21
NO326134B1 (no) 2008-10-06
US20140024631A1 (en) 2014-01-23
US8377916B2 (en) 2013-02-19
US20170305961A1 (en) 2017-10-26
US20050080064A1 (en) 2005-04-14
CY2017020I1 (el) 2017-11-14
US7138390B2 (en) 2006-11-21
US20160152657A1 (en) 2016-06-02
US20190300564A9 (en) 2019-10-03
JP4021327B2 (ja) 2007-12-12

Similar Documents

Publication Publication Date Title
ATE303399T1 (de) Steroide als agonisten für fxr
CY1110243T1 (el) Ανταγωνιστες npyy5
PL1776377T3 (pl) Nowy steroid, agonista FXR
ATE256681T1 (de) N-heterozyklische derivate als nos inhibitoren
TR200201506T2 (tr) Terapötik maddeler olarak kinaz inhibitörleri
NO20044731L (no) Kinolin- og isokinolinderivater fremgangsmate for fremstilling derav og anvendelse derav som betennelseshemmere
MXPA02012033A (es) Derivados de 2-aminocarbonil-9h-purina.
SE0202465D0 (sv) New compounds
MXPA02004415A (es) Pirazolonas sustituidas con heterociclicas.
DE69821985D1 (de) Ortho-anthranilamide derivate als antikoagulantien
MY129796A (en) Novel anti-inflammatory androstane derivatives
DE60107449D1 (de) Substituierte aminopropoxyarylderivate als lxr agonisten
WO2004007521A3 (en) Bile acid derivatives as agonists of the farnesoid x receptor
CY1106247T1 (el) Θειοφαινο- και θειαζολοσουλφοναμιδες ως αντινεοπλαστικοι παραγοντες
DE60121461D1 (de) Kondensierte pyridoindolderivate
NO20043016L (no) 6-aminomorfinan-derivater, fremgangsmate for fremstilling og anvendelse derav
ATE300543T1 (de) Kondensierte pyrazindionderivate als pde5 inhibitore
BR0313969A (pt) Inibidores de oxitocina
ATE505462T1 (de) Neue biologischaktive molekü le
ATE333457T1 (de) Zyklische gmp-spezifische phosphodiesteraseinhibitoren
ATE419242T1 (de) Pyrrolidinylharnstoffderivate als angiogeneseinhibitoren
ATE308540T1 (de) Antithrombosemittel
DE60041001D1 (de) Substituierte homopiperidylbenzimidazolanaloga als fundusrelaxantien
DE60222465D1 (de) Pyrazolopyridin-derivate als antiherpesmittel
DE60110124D1 (de) Kondensierte pyrazindionderivate als pde inhibitoren

Legal Events

Date Code Title Description
UEP Publication of translation of european patent specification

Ref document number: 1392714

Country of ref document: EP