BE2017C018I2 - - Google Patents

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Publication number
BE2017C018I2
BE2017C018I2 BE2017C018C BE2017C018C BE2017C018I2 BE 2017C018 I2 BE2017C018 I2 BE 2017C018I2 BE 2017C018 C BE2017C018 C BE 2017C018C BE 2017C018 C BE2017C018 C BE 2017C018C BE 2017C018 I2 BE2017C018 I2 BE 2017C018I2
Authority
BE
Belgium
Prior art keywords
compounds
formula
solvates
allyl
propyl
Prior art date
Application number
BE2017C018C
Other languages
English (en)
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=BE2017C018(I2) "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
Publication of BE2017C018I2 publication Critical patent/BE2017C018I2/fr

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)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • External Artificial Organs (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
BE2017C018C 2001-03-12 2017-06-06 BE2017C018I2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US27495901P 2001-03-12 2001-03-12
PCT/EP2002/001832 WO2002072598A1 (fr) 2001-03-12 2002-02-21 Steroides comme agonistes de fxr

Publications (1)

Publication Number Publication Date
BE2017C018I2 true BE2017C018I2 (fr) 2021-02-04

Family

ID=23050302

Family Applications (1)

Application Number Title Priority Date Filing Date
BE2017C018C BE2017C018I2 (fr) 2001-03-12 2017-06-06

Country Status (16)

Country Link
US (9) USRE48286E1 (fr)
EP (1) EP1392714B1 (fr)
JP (2) JP4021327B2 (fr)
AT (1) ATE303399T1 (fr)
AU (1) AU2002308295B2 (fr)
BE (1) BE2017C018I2 (fr)
CA (1) CA2440680C (fr)
CY (1) CY2017020I2 (fr)
DE (1) DE60205891T2 (fr)
DK (1) DK1392714T3 (fr)
ES (1) ES2248581T3 (fr)
FR (1) FR17C0003I2 (fr)
IL (2) IL157816A0 (fr)
NL (1) NL300877I2 (fr)
NO (2) NO326134B1 (fr)
WO (1) WO2002072598A1 (fr)

Families Citing this family (112)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2002308295B2 (en) 2001-03-12 2007-08-23 Intercept Pharmaceuticals, Inc. Steroids as agonists for FXR
ES2367539T3 (es) 2001-12-21 2011-11-04 X-Ceptor Therapeutics, Inc. Moduladores heterocíclicos de receptores nucleares.
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
US10987362B2 (en) 2004-03-12 2021-04-27 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using FXR ligands
EP1734970B1 (fr) * 2004-03-12 2014-12-31 Intercept Pharmaceuticals, Inc. Traitement de la fibrose au moyen de ligands de fxr
WO2005092328A1 (fr) * 2004-03-29 2005-10-06 Japan Health Sciences Foundation Compose d'activation de fxr
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
PT2040713E (pt) * 2006-06-27 2014-10-13 Intercept Pharmaceuticals Inc Para a prevenção ou o tratamento de doenças ou estados clínicos mediados por fxr
EP1886685A1 (fr) 2006-08-11 2008-02-13 INSERM (Institut National de la Santé et de la Recherche Médicale) Méthodes, utilisations et compositions pour la modulation de la réplication du HCV par activation ou inhibition du récepteur farnesoid X
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
AU2008209566C1 (en) 2007-01-19 2013-02-14 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as 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
EA020310B1 (ru) 2008-07-30 2014-10-30 Интерсепт Фармасьютикалз, Инк. Модуляторы рецептора tgr5 и их применение
ES2663948T3 (es) * 2008-11-19 2018-04-17 Intercept Pharmaceuticals, Inc. Moduladores de TGR5 y método de uso de los mismos
US20110257139A1 (en) 2008-12-19 2011-10-20 Royal College Of Surgeons In Ireland Treatment of diarrhoea
NZ734451A (en) 2012-06-19 2018-12-21 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
AU2013334122B2 (en) 2012-10-26 2017-11-02 Intercept Pharmaceuticals, Inc. Process for preparing bile acid derivatives
SG11201503697TA (en) * 2012-11-28 2015-06-29 Intercept Pharmaceuticals Inc Treatment of pulmonary disease
CN105636984A (zh) 2013-06-13 2016-06-01 法斯特弗沃德制药有限公司 用于治疗慢性炎症和预防胃肠道癌或纤维化的cd40信号转导抑制剂和其他化合物，该其他化合物是胆汁酸、胆汁酸衍生物、tgr5受体激动剂、fxr激动剂或其组合
SI3043865T1 (sl) * 2013-09-11 2021-04-30 Institut National De La Sante Et De La Recherche Medicale (Inserm) Metode in farmacevtski sestavki za zdravljenje virusne okužbe s hepatitisom 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
US10407462B2 (en) 2014-05-29 2019-09-10 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases
EP3006557A1 (fr) 2014-10-07 2016-04-13 Heinrich-Heine-Universität Düsseldorf Acides biliaires pour induire la différenciation hépatique
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
WO2016073767A1 (fr) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Analogues d'acide biliaire d'agonistes de fxr/tgr5 et leurs procédés d'utilisation
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
TWI688571B (zh) 2014-11-19 2020-03-21 英商Ｎｚｐ英國有限公司 化合物（四）
US10538550B2 (en) 2014-11-19 2020-01-21 NZP UK Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal FXR modulators
US10131688B2 (en) 2014-11-19 2018-11-20 NZP UK Limited 5.beta.-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal FXR modulators
KR102526631B1 (ko) 2014-11-19 2023-04-27 엔제트피 유케이 리미티드 스테로이드 fxr 조절인자를 제조하기 위한 중간체로서의 6-알킬-7-하이드록시-4-엔-3-온 스테로이드
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
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
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
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.
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
CA2981503C (fr) 2015-03-31 2023-09-19 Enanta Pharmaceuticals, Inc. Derives d'acide biliaire utilises comme agonistes de fxr/tgr5 et leurs procedes d'utilisation
CR20170456A (es) 2015-04-07 2018-06-13 Intercept Pharmaceuticals Inc Composiciones farmacéuticas para terapias combinadas
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
KR20180054770A (ko) 2015-09-21 2018-05-24 인터셉트 파마슈티컬즈, 인크. 간 재생 촉진 방법
EP3353189A4 (fr) 2015-09-24 2019-06-19 Intercept Pharmaceuticals, Inc. Procédés et intermédiaires pour la préparation de dérivés de l'acide biliaire
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
MX2018005520A (es) * 2015-11-06 2018-08-01 Intercept Pharmaceuticals Inc Metodos para preparacion de acido obeticolico y derivados de los mismos.
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 (fr) 2016-01-01 2017-07-06 Lupin Limited Formes solides d'acide obéticholique et procédés associés
US10875888B2 (en) 2016-01-28 2020-12-29 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Steroid derivative FXR agonist
ES2909907T3 (es) * 2016-02-10 2022-05-10 Dr Reddys Laboratories Ltd Proceso de purificación que implica la sal de amina del ácido obeticólico
WO2017147159A1 (fr) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Dérivés d'acide biliaire utilisés deutérés utilisés comme agonistes de fxr/tgr5 et leurs méthodes d'utilisation
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
WO2017147174A1 (fr) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Analogues de l'acide biliaire contenant de l'hétéroaryle utilisés comme agonistes de fxr/tgr5 et leurs méthodes d'utilisation
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
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
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
US11419878B2 (en) 2016-03-28 2022-08-23 Intercept Pharmaceuticals, Inc. Medicine obtained by combining FXR agonist and ARB
CA3019499A1 (fr) 2016-03-31 2017-10-05 Intercept Pharmaceuticals, Inc. Comprime enrobe d'un film et presentant une stabilite chimique elevee de son principe actif
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
US10752654B2 (en) 2016-04-04 2020-08-25 Dipharma Francis S.R.L. Method for preparing a farnesoid X receptor agonist
EP3228306A1 (fr) 2016-04-04 2017-10-11 ratiopharm GmbH Composé complexe comprenant un acide obéticholique et de la cyclodextrine et formulation pharmaceutique comprenant le composé complexe
ITUA20162272A1 (it) * 2016-04-04 2017-10-04 Dipharma Francis Srl Procedimento per la preparazione di un agonista del recettore farnesoide x
WO2017180577A1 (fr) 2016-04-13 2017-10-19 Intercept Pharmaceuticals, Inc. Procédés de traitement du cancer
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
GB201608777D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Compounds
EA038580B9 (ru) * 2016-05-18 2021-10-05 Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. Агонист fxr, представляющий собой производное стероидов
GB201608776D0 (en) 2016-05-18 2016-06-29 Dextra Lab Ltd Methods and compounds
WO2017207648A1 (fr) 2016-05-31 2017-12-07 Bionice, S.L.U Procédés et intermédiaires pour la préparation d'acide obéticholique et de dérivés de celui-ci
WO2017208165A1 (fr) 2016-06-01 2017-12-07 Dr. Reddy’S Laboratories Limited Procédé de préparation d'acide obéticholique
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 (fr) 2016-09-09 2018-03-14 Hexal AG Procédé de purification d'acide obéticholique
MX2019003790A (es) 2016-10-04 2019-09-26 Enanta Pharm Inc Analogos de isoxazol como agonistas de fxr y metodos de uso de los mismos.
EP3305799A3 (fr) 2016-10-07 2018-06-20 Lupin Limited Sels d'acide obéticholique
CA3045023A1 (fr) 2016-11-29 2018-06-07 Enanta Pharmaceuticals, Inc. Procede de preparation de derives de type acide biliaire de la famille des sulfonylurees
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
WO2018178260A1 (fr) 2017-03-30 2018-10-04 INSERM (Institut National de la Santé et de la Recherche Médicale) Méthodes et compositions pharmaceutiques pour réduire la persistance et l'expression des virus épisomiques
CA3058754A1 (fr) 2017-04-07 2018-10-11 Enanta Pharmaceuticals, Inc. Procede de preparation de derives sulfonylcarbamate d'acides biliaires
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 (fr) 2017-07-18 2019-01-23 Bionice, S.L.U. Procédé et intermédiaires de synthèse de l'acide obéticholique et leurs dérivés
WO2019048632A1 (fr) 2017-09-08 2019-03-14 Mina Therapeutics Limited Compositions stabilisées de petits arn activateurs (parna) de hnf4a et procédés d'utilisation
US10611793B1 (en) 2017-11-27 2020-04-07 Teva Czech Industries S.R.O. Solid state forms of obeticholic acid salts
WO2019106043A1 (fr) 2017-11-29 2019-06-06 Hexal Ag Composition pharmaceutique comprenant de l'acide obéticholique
US10689391B2 (en) * 2017-12-12 2020-06-23 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2019160813A1 (fr) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole en tant qu'agonistes de fxr et leurs procédés d'utilisation
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
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
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 (fr) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Dérivés d'isoxazole utilisés en tant qu'agonistes de fxr et leurs procédés d'utilisation
SG11202113155XA (en) 2019-05-30 2021-12-30 Intercept Pharmaceuticals Inc Pharmaceutical compositions comprising a fxr agonist and a fibrate for use in the treatment of cholestatic liver disease
EP3999101A1 (fr) 2019-07-18 2022-05-25 ENYO Pharma Procédé pour diminuer les effets secondaires de l'interféron
WO2021023100A1 (fr) * 2019-08-06 2021-02-11 杜心赟 Composés d'acide désoxycholique, compositions pharmaceutiques et leurs utilisations
WO2021144330A1 (fr) 2020-01-15 2021-07-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Utilisation d'agonistes de fxr pour traiter une infection par le virus de l'hépatite d
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
KR20230154806A (ko) 2021-01-14 2023-11-09 엔요 파마 Hbv 감염 치료를 위한 fxr 작용제 및 ifn의 상승작용효과
CN117320722A (zh) 2021-04-28 2023-12-29 埃尼奥制药公司 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用
WO2024104960A1 (fr) 2022-11-15 2024-05-23 Synthon B.V. Formulation stable comprenant de l'acide obéticholique

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 (fr) 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
EP0433899B1 (fr) * 1989-12-13 1995-04-12 Mitsubishi Chemical Corporation Dérivés d'acide pyrazolyl acrylique, utilisable comme fongicides systémique dans la protection des plantes et matériaux
JPH04250093A (ja) 1991-01-18 1992-09-04 Kanzaki Paper Mfg Co Ltd 感熱記録体
WO1997028149A1 (fr) 1996-02-02 1997-08-07 Merck & Co., Inc. Procede pour augmenter les niveaux de cholesterol hdl
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
CA2260044A1 (fr) 1996-07-12 1998-01-22 Stephen Alistair Smith Nouveau traitement contre la resistance a la leptine
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
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
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
JP2002529740A (ja) 1998-11-09 2002-09-10 アセロジエニクス・インコーポレイテツド 血漿コレステロールレベルを低下させるための方法及び組成物
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)
JP2002532729A (ja) 1998-12-23 2002-10-02 グラクソ グループ リミテッド 核内受容体のリガンドのアッセイ
WO2000040965A1 (fr) 1999-01-07 2000-07-13 Tularik, Inc. Modulation du metabolisme du cholesterol induite par le recepteur fxr
EP1165135B1 (fr) 1999-03-26 2004-09-01 City of Hope Procedes de criblage de composes modulant l'activite des recepteurs fxr
EP1473042B1 (fr) 1999-03-26 2006-06-21 City of Hope Criblage de composés modulant l'activité des récepteurs FXR
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
US6906057B1 (en) 1999-06-11 2005-06-14 Allergan, Inc. Methods for modulating FXR receptor activity
BR0011743A (pt) 1999-06-11 2002-03-05 Allergan Sales Inc Método para modular a atividade de receptor de fxr
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
AU1215701A (en) 1999-10-22 2001-05-08 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
WO2002020463A2 (fr) 2000-09-05 2002-03-14 Tularik Inc. Modulateurs fxr
US20020119958A1 (en) 2001-02-13 2002-08-29 Shinichiro Tojo Therapeutic agent for hyperlipidemia
AU2002308295B2 (en) 2001-03-12 2007-08-23 Intercept Pharmaceuticals, Inc. Steroids as agonists for FXR
EP1378749A4 (fr) 2001-04-12 2005-05-11 Takeda Pharmaceutical Procede de criblage
ATE381542T1 (de) 2001-08-13 2008-01-15 Phenex Pharmaceuticals Ag Nr1h4-kern-rezeptor-bindende verbindungen
WO2003016280A1 (fr) 2001-08-13 2003-02-27 Lion Bioscience Ag Composes liant le recepteur nucleaire nr1h4
EP1423113A4 (fr) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag Composes de liaison au recepteur nucleaire nr1h4
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 (fr) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Procedes d'utilisation d'agonistes du recepteur farnesoide x (fxr)
WO2003086303A2 (fr) 2002-04-12 2003-10-23 The University Of Chicago Agonistes de recepteur active frx (farnesoid x receptor)
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
US20070015796A1 (en) 2003-09-26 2007-01-18 Smithkline Beecham Corporation Compositions and methods for treatment of fibrosis
EP1568706A1 (fr) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Nouveau agonist steroidal pour FXR
WO2005092369A2 (fr) 2004-03-11 2005-10-06 Fresenius Kabi Deutschland Gmbh Conjugues d'hydroxy-ethyl-amidon et d'erythropoietine
EP1734970B1 (fr) 2004-03-12 2014-12-31 Intercept Pharmaceuticals, Inc. Traitement de la fibrose au moyen de ligands de fxr
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
JP2010517931A (ja) 2006-02-14 2010-05-27 インターセプト ファーマシューティカルズ， インコーポレイテッド Ｆｘｒ媒介性の疾患または状態の予防または治療用のｆｘｒリガンドとしての胆汁酸誘導体
PT2040713E (pt) 2006-06-27 2014-10-13 Intercept Pharmaceuticals Inc Para a prevenção ou o tratamento de doenças ou estados clínicos mediados por fxr
US20100239661A1 (en) 2006-10-26 2010-09-23 Sunilendu Bhushan Roy Pharmaceutical compositions of ursodiol
EP1947108A1 (fr) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. Modulateurs TGR5 et procédés d'utilisation correspondants
AU2008209566C1 (en) 2007-01-19 2013-02-14 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as 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
ES2663948T3 (es) 2008-11-19 2018-04-17 Intercept Pharmaceuticals, Inc. Moduladores de TGR5 y método de uso de los mismos
US20120160944A1 (en) 2009-04-24 2012-06-28 Aaron Dodd Method for the production of commercial nanoparticle and micro particle powders
EP2468762A1 (fr) 2010-11-30 2012-06-27 Dr. Falk Pharma Gmbh Synthèse optimisée d'acides biliaires purs, cristallins et non polymorphes avec une taille de particules définie
WO2013037482A1 (fr) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Agonistes du récepteur du farnésoïde x pour le traitement et la prévention du cancer
FR2981572B1 (fr) 2011-10-21 2018-01-19 Inopharm Limited Compositions pharmaceutiques d'acide ursodesoxycholique
NZ734451A (en) 2012-06-19 2018-12-21 Intercept Pharmaceuticals Inc Preparation, uses and solid forms of obeticholic acid
CA2912139C (fr) 2013-05-14 2021-04-20 Roberto Pellicciari Derives 11-hydroxyle d'acides biliaires et leurs conjugues d'acides amines en tant que modulateurs du recepteur de farnesoide x

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US20140024631A1 (en) 2014-01-23
CY2017020I1 (el) 2017-11-14
EP1392714A1 (fr) 2004-03-03
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