DK1392714T3 - Steroider som agonister for FXR - Google Patents

Steroider som agonister for FXR

Info

Publication number
DK1392714T3
DK1392714T3 DK02750526T DK02750526T DK1392714T3 DK 1392714 T3 DK1392714 T3 DK 1392714T3 DK 02750526 T DK02750526 T DK 02750526T DK 02750526 T DK02750526 T DK 02750526T DK 1392714 T3 DK1392714 T3 DK 1392714T3
Authority
DK
Denmark
Prior art keywords
fxr
agonists
steroids
compounds
formula
Prior art date
Application number
DK02750526T
Other languages
Danish (da)
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=DK1392714(T3) "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 DK1392714T3 publication Critical patent/DK1392714T3/da

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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (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)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • External Artificial Organs (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
DK02750526T 2001-03-12 2002-02-21 Steroider som agonister for FXR DK1392714T3 (da)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US27495901P 2001-03-12 2001-03-12

Publications (1)

Publication Number Publication Date
DK1392714T3 true DK1392714T3 (da) 2006-01-09

Family

ID=23050302

Family Applications (1)

Application Number Title Priority Date Filing Date
DK02750526T DK1392714T3 (da) 2001-03-12 2002-02-21 Steroider som agonister for FXR

Country Status (16)

Country Link
US (9) USRE48286E1 (enExample)
EP (1) EP1392714B1 (enExample)
JP (2) JP4021327B2 (enExample)
AT (1) ATE303399T1 (enExample)
AU (1) AU2002308295B2 (enExample)
BE (1) BE2017C018I2 (enExample)
CA (1) CA2440680C (enExample)
CY (1) CY2017020I1 (enExample)
DE (1) DE60205891T2 (enExample)
DK (1) DK1392714T3 (enExample)
ES (1) ES2248581T3 (enExample)
FR (1) FR17C0003I2 (enExample)
IL (2) IL157816A0 (enExample)
NL (1) NL300877I2 (enExample)
NO (2) NO326134B1 (enExample)
WO (1) WO2002072598A1 (enExample)

Families Citing this family (113)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1392714T3 (da) 2001-03-12 2006-01-09 Intercept Pharmaceuticals Inc Steroider som agonister for FXR
EP1465882B1 (en) 2001-12-21 2011-08-24 X-Ceptor Therapeutics, Inc. Hetrocyclic modulators of nuclear receptors
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
WO2005089316A2 (en) * 2004-03-12 2005-09-29 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
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
DK2040713T3 (da) * 2006-06-27 2014-09-29 Intercept Pharmaceuticals Inc Galdesyrederivater som fxr-ligander til forebyggelsen eller behandlingen af fxr-medierede sygdomme eller tilstande
EP1886685A1 (en) 2006-08-11 2008-02-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods, uses and compositions for modulating replication of hcv through the farnesoid x receptor (fxr) activation or inhibition
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
CA2928178C (en) 2007-01-19 2019-09-10 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
US8796249B2 (en) 2008-07-30 2014-08-05 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
HUE039171T2 (hu) 2008-11-19 2018-12-28 Intercept Pharmaceuticals Inc TGR5 modulátorok és azok alkalmazási eljárása
WO2010069604A1 (en) 2008-12-19 2010-06-24 Royal College Of Surgeons In Ireland Treatment of diarrhoea
ES2822375T3 (es) 2012-06-19 2021-04-30 Intercept Pharmaceuticals Inc Preparación de la forma no cristalina del ácido obeticólico
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
NZ707389A (en) 2012-10-26 2018-08-31 Intercept Pharmaceuticals Inc Process for preparing bile acid derivatives
WO2014085474A1 (en) * 2012-11-28 2014-06-05 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
CA2914924A1 (en) 2013-06-13 2014-12-18 Fast Forward Pharmaceuticals 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.
SI3071696T1 (sl) 2013-11-22 2019-11-29 Mina Therapeutics Ltd C/EBP alfa kratko delujoči RNA sestavki in postopki uporabe
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
SI3626725T1 (sl) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1
EP3006557A1 (en) 2014-10-07 2016-04-13 Heinrich-Heine-Universität Düsseldorf Bile acids for inducing hepatic differentiation
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
BR112017009657A2 (pt) 2014-11-06 2018-01-23 Enanta Pharmaceuticals, Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
CN111944006B (zh) * 2014-11-17 2021-12-17 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
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
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
KR102526632B1 (ko) 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 FXR 조절인자를 제조하기 위한 중간체로서의 5β-6-알킬-7-하이드록시-3-온 스테로이드
JP6698085B2 (ja) 2014-11-19 2020-05-27 エヌゼットピー ユーケー リミテッド ステロイドFXRモジュレーター製造のための中間体としての6α−アルキル−6,7−ジオン−ステロイド
RU2017121457A (ru) 2014-11-26 2018-12-26 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2016086115A1 (en) 2014-11-26 2016-06-02 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
ES2905872T3 (es) 2015-02-06 2022-04-12 Intercept Pharmaceuticals Inc Composiciones farmacéuticas para terapia combinada
AU2016219266A1 (en) 2015-02-11 2017-08-10 Enanta Pharmaceuticals, Inc. Bile acid analogs as FXR/TGR5 agonists and methods of use thereof
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
RU2712099C2 (ru) 2015-03-31 2020-01-24 Энанта Фармасьютикалс, Инк. Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения
CN107613986A (zh) 2015-04-07 2018-01-19 英特塞普特医药品公司 用于组合疗法的药物组合物
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
AU2016326428A1 (en) 2015-09-21 2018-04-12 Intercept Pharmaceuticals, Inc. Methods of promoting hepatic regeneration
KR20180052756A (ko) 2015-09-24 2018-05-18 인터셉트 파마슈티컬즈, 인크. 담즙산 유도체 제조를 위한 방법 및 중간체
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
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
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
MY196292A (en) 2016-01-28 2023-03-24 Chia Tai Tianqing Pharmaceutical Group Co Ltd Steroid Derivative Fxr Agonist
WO2017137931A1 (en) * 2016-02-10 2017-08-17 Dr. Reddy’S Laboratories Limited Amine salt of obeticholic acid
US10364267B2 (en) 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
WO2017147174A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof
CN109467585A (zh) * 2016-03-11 2019-03-15 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.
JPWO2017170858A1 (ja) * 2016-03-31 2019-02-14 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 溶出性に優れた経口製剤
EP3437645B1 (en) 2016-03-31 2021-09-22 Intercept Pharmaceuticals, Inc. Film-coated tablet having high chemical stability of active ingredient
EP3228306A1 (en) 2016-04-04 2017-10-11 ratiopharm GmbH Complex compound comprising obeticholic acid and cyclodextrin and pharmaceutical formulation comprising the complex compound
WO2017174515A1 (en) 2016-04-04 2017-10-12 Dipharma Francis S.R.L. Method for preparing a farnesoid x receptor agonist
ITUA20162272A1 (it) * 2016-04-04 2017-10-04 Dipharma Francis Srl Procedimento per la preparazione di un agonista del recettore farnesoide x
CA3020698A1 (en) 2016-04-13 2017-10-19 Intercept Pharmaceuticals, Inc. Methods of treating or preventing hepatocellular carcinoma
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
EP3464316A4 (en) 2016-06-01 2020-02-19 Dr. Reddy's Laboratories Ltd. PROCESS FOR THE 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 (en) 2016-09-09 2018-03-14 Hexal AG Process for purifying obeticholic acid
CA3039124A1 (en) 2016-10-04 2018-04-12 Enanta Pharmaceuticals, Inc. Isoxazole analogs as fxr agonists and methods of use thereof
EP3305799A3 (en) 2016-10-07 2018-06-20 Lupin Limited Salts of obeticholic acid
AU2017368069B2 (en) 2016-11-29 2021-07-08 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
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
JP7618384B2 (ja) 2017-02-21 2025-01-21 ジェンフィ Pparアゴニストとfxrアゴニストとの組合せ
JP2020515564A (ja) 2017-03-30 2020-05-28 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物
MX388300B (es) 2017-04-07 2025-03-19 Enanta Pharm Inc Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato
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 (en) 2017-07-18 2019-01-23 Bionice, S.L.U. Process and intermediates for the synthesis of obeticholic acid and derivatives thereof
WO2019048632A1 (en) 2017-09-08 2019-03-14 Mina Therapeutics Limited STABILIZED COMPOSITIONS OF SMALL ACTIVATORY RNA (PARNA) OF HNF4A 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
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US20220226350A1 (en) 2019-05-30 2022-07-21 Intercept Pharmaceuticals, Inc. Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease
WO2021009332A1 (en) 2019-07-18 2021-01-21 Enyo Pharma Method for decreasing adverse-effects of interferon
US20230146782A1 (en) * 2019-08-06 2023-05-11 Du Jessica Xinyun Deoxycholic acid compounds, pharmaceutical compositions and uses thereof
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
MX2023008365A (es) 2021-01-14 2023-10-04 Enyo Pharma Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv.
TW202308629A (zh) 2021-04-28 2023-03-01 法商Enyo製藥公司 使用fxr激動劑作為組合治療以增強tlr3激動劑之療效
WO2024104960A1 (en) 2022-11-15 2024-05-23 Synthon B.V. Stable formulation comprising obeticholic acid
GB202416085D0 (en) 2024-10-31 2024-12-18 Nzp Uk Ltd Reduction process

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 (enExample) 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
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
US4982868A (en) * 1989-11-07 1991-01-08 Robbins Edward S Iii Bail type pitcher for thin walled container
US5055477A (en) * 1989-12-13 1991-10-08 Mitsubishi Kasei Corporation Pyrazolyl acrylic acid derivatives, useful as systemic fungicides for plant and material protection
JPH04250093A (ja) 1991-01-18 1992-09-04 Kanzaki Paper Mfg Co Ltd 感熱記録体
AU1856997A (en) 1996-02-02 1997-08-22 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
AU3552697A (en) 1996-07-12 1998-02-09 Smithkline Beecham Plc Novel treatment of leptine resistance
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
JP2002528721A (ja) 1998-10-23 2002-09-03 グラクソ グループ リミテッド 核内受容体のリガンド用のアッセイ
CA2350316A1 (en) 1998-11-09 2000-05-18 Atherogenics, Inc. Methods and compositions to lower plasma cholesterol levels
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.
US6465258B1 (en) 1999-01-07 2002-10-15 Tularik, Inc. FXR receptor-mediated modulation cholesterol metabolism
ATE274921T1 (de) 1999-03-26 2004-09-15 Hope City Verfahren zur selektion von fxr- rezeptormodulatoren
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
CA2377320A1 (en) 1999-06-11 2000-12-21 Allergan Sales, Inc. Methods for modulating fxr receptor activity
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
CA2386750A1 (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
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
DK1392714T3 (da) 2001-03-12 2006-01-09 Intercept Pharmaceuticals Inc Steroider som agonister for FXR
WO2002084286A1 (en) 2001-04-12 2002-10-24 Takeda Chemical Industries, Ltd. Screening method
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer Nr1h4 nuclear receptor binding compounds
DE60131967D1 (de) 2001-08-13 2008-01-31 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
WO2003015777A1 (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
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
AU2003228485A1 (en) 2002-04-12 2003-10-27 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
JP2006515838A (ja) 2002-11-22 2006-06-08 スミスクライン ビーチャム コーポレーション ファルネソイドx受容体アゴニスト
US6993380B1 (en) 2003-06-04 2006-01-31 Cleveland Medical Devices, Inc. Quantitative sleep analysis method and system
EP1696910A4 (en) 2003-09-26 2009-12-09 Smithkline Beecham Corp COMPOSITIONS AND METHOD FOR THE TREATMENT OF FIBROSIS
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
TW200603818A (en) 2004-03-11 2006-02-01 Fresenius Kabi De Gmbh Conjugates of hydroxyethyl starch and erythropoietin
WO2005089316A2 (en) 2004-03-12 2005-09-29 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
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
CN101395170A (zh) 2006-02-14 2009-03-25 英特塞普特药品公司 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物
DK2040713T3 (da) 2006-06-27 2014-09-29 Intercept Pharmaceuticals Inc Galdesyrederivater som fxr-ligander til forebyggelsen eller behandlingen af fxr-medierede sygdomme eller tilstande
US20100239661A1 (en) 2006-10-26 2010-09-23 Sunilendu Bhushan Roy Pharmaceutical compositions of ursodiol
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
CA2928178C (en) 2007-01-19 2019-09-10 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
HUE039171T2 (hu) 2008-11-19 2018-12-28 Intercept Pharmaceuticals Inc TGR5 modulátorok és azok alkalmazási eljárása
CA2759109A1 (en) 2009-04-24 2010-10-28 Iceutica Pty Ltd A solid dosage form of ciprofloxacin having small particle size and improved powder handling characteristics
EP2468762A1 (en) 2010-11-30 2012-06-27 Dr. Falk Pharma Gmbh Optimized synthesis of pure, non-polymorphic, crystalline bile acids with defined particle size
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
ES2822375T3 (es) 2012-06-19 2021-04-30 Intercept Pharmaceuticals Inc Preparación de la forma no cristalina del ácido obeticólico
CN105377870B (zh) 2013-05-14 2018-04-03 英特塞普特医药品公司 作为法尼醇x受体调节剂的胆汁酸的11‑羟基衍生物及其氨基酸共轭物

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