BE2017C018I2 - - Google Patents

Download PDF

Info

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)
French (fr)
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

  • 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)
  • Public Health (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)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Cardiology (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • External Artificial Organs (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)
  • Immobilizing And Processing Of Enzymes And Microorganisms (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
BE2017C018C 2001-03-12 2017-06-06 BE2017C018I2 (th)

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
BE2017C018I2 true BE2017C018I2 (th) 2021-02-04

Family

ID=23050302

Family Applications (1)

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

Country Status (16)

Country Link
US (9) US7138390B2 (th)
EP (1) EP1392714B1 (th)
JP (2) JP4021327B2 (th)
AT (1) ATE303399T1 (th)
AU (1) AU2002308295B2 (th)
BE (1) BE2017C018I2 (th)
CA (1) CA2440680C (th)
CY (1) CY2017020I2 (th)
DE (1) DE60205891T2 (th)
DK (1) DK1392714T3 (th)
ES (1) ES2248581T3 (th)
FR (1) FR17C0003I2 (th)
IL (2) IL157816A0 (th)
NL (1) NL300877I2 (th)
NO (2) NO326134B1 (th)
WO (1) WO2002072598A1 (th)

Families Citing this family (110)

* 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
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
SI1734970T1 (sl) 2004-03-12 2015-04-30 Intercept Pharmaceuticals, Inc. Zdravljenje fibroze z uporabo FXR ligandov
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
WO2008002573A2 (en) * 2006-06-27 2008-01-03 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions
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
BRPI0808684B1 (pt) 2007-01-19 2021-08-10 Intercept Pharmaceuticals, Inc Compostos moduladores de tgr5, composição e seus usos
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
PT2698375T (pt) 2008-11-19 2018-05-25 Intercept Pharmaceuticals Inc Moduladores de tgr5 e método de utilização dos mesmos
US20110257139A1 (en) 2008-12-19 2011-10-20 Royal College Of Surgeons In Ireland Treatment of diarrhoea
US9982008B2 (en) 2012-06-19 2018-05-29 Intercept Pharmaceuticals, Inc. Preparation and uses of obeticholic acid
IN2014MN02561A (th) 2012-06-19 2015-09-04 Intercept Pharmaceuticals Inc
NZ707389A (en) 2012-10-26 2018-08-31 Intercept Pharmaceuticals Inc Process for preparing bile acid derivatives
CA2891348C (en) * 2012-11-28 2020-04-28 Intercept Pharmaceuticals, Inc. Treatment of pulmonary disease
AU2014278833A1 (en) 2013-06-13 2016-01-07 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.
LT3043865T (lt) 2013-09-11 2021-04-26 Institut National De La Santé Et De La Recherche Médicale (Inserm) Hepatito b viruso infekcijos gydymo būdai ir farmacinė kompozicija
EP3985118A1 (en) 2013-11-22 2022-04-20 MiNA Therapeutics Limited C/ebp alpha short activating rna compositions and methods of use
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
CA2948585C (en) 2014-05-29 2022-07-26 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
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
AU2015343025A1 (en) 2014-11-06 2017-06-08 Enanta Pharmaceuticals, 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
ES2759725T3 (es) 2014-11-19 2020-05-12 Nzp Uk Ltd Esteroides 6-alquil-7-hidroxi-4-en-3-ona como intermediarios para la producción de moduladores de FXR esteroideo
ES2733643T3 (es) 2014-11-19 2019-12-02 Nzp Uk Ltd Esteroides 5.beta.-6-alquil-7-hidroxi-3-ona como intermedios para la producción de moduladores FXR de esteroides
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
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
EP3223823A4 (en) 2014-11-26 2018-10-17 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
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
AR103624A1 (es) 2015-02-06 2017-05-24 Intercept Pharmaceuticals Inc Composiciones farmacéuticas para terapia de combinación
BR112017017238A2 (pt) 2015-02-11 2018-04-10 Enanta Pharm Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
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
RS62110B1 (sr) 2015-03-31 2021-08-31 Enanta Pharm Inc Derivati žučnih kiselina kao agonisti fxr/tgr5 i postupci njihove upotrebe
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
AU2016326428A1 (en) 2015-09-21 2018-04-12 Intercept Pharmaceuticals, Inc. Methods of promoting hepatic regeneration
US11072631B2 (en) 2015-09-24 2021-07-27 Intercept Pharmaceuticals, Inc. Methods and intermediates for the preparation bile acid derivatives
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
KR20180067699A (ko) * 2015-11-06 2018-06-20 인터셉트 파마슈티컬즈, 인크. 오베티콜산 및 이의 유도체의 제조 방법
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
SG11201806348PA (en) * 2016-01-28 2018-08-30 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
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
WO2017147159A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives 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
JPWO2017170434A1 (ja) 2016-03-28 2019-01-31 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アゴニストとａｒｂの組み合わせ医薬
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
CA3019499A1 (en) 2016-03-31 2017-10-05 Intercept Pharmaceuticals, Inc. Film-coated tablet having high chemical stability of active ingredient
ITUA20162272A1 (it) * 2016-04-04 2017-10-04 Dipharma Francis Srl Procedimento per la preparazione di un agonista del recettore farnesoide x
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 (en) 2016-04-04 2017-10-11 ratiopharm GmbH Complex compound comprising obeticholic acid and cyclodextrin and pharmaceutical formulation comprising the complex compound
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
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
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
CN109415405A (zh) 2016-06-01 2019-03-01 雷迪博士实验室有限公司 制备奥贝胆酸的方法
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
WO2018067704A1 (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
WO2018102418A1 (en) 2016-11-29 2018-06-07 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
WO2018152171A1 (en) 2017-02-14 2018-08-23 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr agonists and methods of use thereof
KR20190117632A (ko) 2017-02-21 2019-10-16 장피트 Ppar 효현제와 fxr 효현제의 병용
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
US10676500B2 (en) 2017-04-07 2020-06-09 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
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
US11447773B2 (en) 2017-09-08 2022-09-20 Mina Therapeutics Limited Stabilized HNF4A saRNA 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
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
KR20220016146A (ko) 2019-05-30 2022-02-08 인터셉트 파마슈티컬즈, 인크. 담즙정체성 간 질환의 치료에서 사용하기 위한 fxr 효능제 및 피브레이트를 포함하는 제약 조성물
US20220241376A1 (en) 2019-07-18 2022-08-04 Enyo Pharma Method for decreasing adverse-effects of interferon
CN114945361A (zh) 2020-01-15 2022-08-26 法国国家卫生及研究医学协会 Fxr激动剂在治疗丁型肝炎病毒感染中的用途
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
EP4277622A1 (en) 2021-01-14 2023-11-22 ENYO Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
WO2022229302A1 (en) 2021-04-28 2022-11-03 Enyo Pharma Strong potentiation of tlr3 agonists effects using fxr agonists as a combined treatment
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 (th) 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
ES2074113T3 (es) * 1989-12-13 1995-09-01 Mitsubishi Chem Corp Nuevos derivados de acido pirazolil acrilico, utiles como fungicidas sistemicos para la proteccion de plantas y materiales.
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
PL331148A1 (en) 1996-07-12 1999-06-21 Smithkline Beecham Plc Novel method of treating the leptin immunity
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
DE69939864D1 (de) 1998-01-29 2008-12-18 Amgen Inc Ppar-gamma modulatoren
WO1999050407A1 (fr) * 1998-03-26 1999-10-07 Kyowa Hakko Kogyo Co., Ltd. Anticorps monoclonal contre une sous-unite catalytique de telomerase humaine
WO2000025134A1 (en) 1998-10-23 2000-05-04 Glaxo Group Limited Assays for ligands for nuclear receptors
CN1332849A (zh) 1998-11-09 2002-01-23 埃瑟若詹尼克斯公司 降低血浆胆固醇水平的方法和组合物
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)
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
EP1473042B1 (en) 1999-03-26 2006-06-21 City of Hope Screening for FXR receptor modulators
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
WO2000057915A1 (en) 1999-03-26 2000-10-05 City Of Hope Method of affecting cholesterol catabolism using nuclear bile acid receptor
US6906057B1 (en) 1999-06-11 2005-06-14 Allergan, Inc. Methods for modulating FXR receptor activity
CA2377320A1 (en) 1999-06-11 2000-12-21 Allergan Sales, Inc. Methods for modulating fxr receptor activity
US6559188B1 (en) 1999-09-17 2003-05-06 Novartis Ag Method of treating metabolic disorders especially diabetes, or a disease or condition associated with diabetes
WO2001030343A1 (en) 1999-10-22 2001-05-03 Merck & Co., Inc. Pharmaceuticals for treating obesity
US6627636B2 (en) 2000-06-15 2003-09-30 Bristol-Myers Squibb Company HMG-CoA reductase inhibitors and method
WO2002020463A2 (en) 2000-09-05 2002-03-14 Tularik Inc. Fxr modulators
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 (en) 2001-04-12 2005-05-11 Takeda Pharmaceutical SCREENING METHOD
WO2003016280A1 (en) 2001-08-13 2003-02-27 Lion Bioscience Ag 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
CA2482195A1 (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
US7319109B2 (en) 2002-11-22 2008-01-15 Smith Kline Beecham Corporation Farnesoid X receptor agonists
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 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
EP1758608A2 (en) 2004-03-11 2007-03-07 Fresenius Kabi Deutschland GmbH Conjugates of hydroxyethyl starch and erythropoietin
SI1734970T1 (sl) 2004-03-12 2015-04-30 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
BRPI0707794A2 (pt) 2006-02-14 2011-05-10 Intercept Pharmaceuticals Inc compostos derivados de Ácido biliar, formulaÇÕes e composiÇÕes farmacÊuticas, bem como uso de ditos compostos
WO2008002573A2 (en) 2006-06-27 2008-01-03 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated deseases or conditions
WO2008062475A2 (en) 2006-10-26 2008-05-29 Cadila Healthcare Limited Pharmaceutical compositions of ursodiol
BRPI0808684B1 (pt) 2007-01-19 2021-08-10 Intercept Pharmaceuticals, Inc Compostos moduladores de tgr5, composição e seus usos
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
US8338628B2 (en) 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
PT2698375T (pt) 2008-11-19 2018-05-25 Intercept Pharmaceuticals Inc Moduladores de tgr5 e método de utilização dos mesmos
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 (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
IN2014MN02561A (th) 2012-06-19 2015-09-04 Intercept Pharmaceuticals Inc
DK2997035T3 (en) 2013-05-14 2018-07-02 Intercept Pharmaceuticals Inc 11-HYDROXY-6-SUBSTITUTED BALIC ACID DERIVATIVES AND AMINO ACID CONJUGATES THEREOF AS FARNESOID X RECEPTOR MODULATORS

Also Published As

Publication number Publication date
ES2248581T3 (es) 2006-03-16
JP2007269815A (ja) 2007-10-18
NO2017022I2 (no) 2018-08-20
WO2002072598A1 (en) 2002-09-19
EP1392714B1 (en) 2005-08-31
AU2002308295B2 (en) 2007-08-23
NL300877I2 (nl) 2017-06-22
NO2017022I1 (no) 2017-05-26
US20140024631A1 (en) 2014-01-23
DE60205891T2 (de) 2006-06-22
US20190300564A9 (en) 2019-10-03
NO20034011D0 (no) 2003-09-11
ATE303399T1 (de) 2005-09-15
DE60205891D1 (de) 2005-10-06
USRE48286E1 (en) 2020-10-27
IL157816A0 (en) 2004-03-28
US8058267B2 (en) 2011-11-15
US20120053163A1 (en) 2012-03-01
JP2004519492A (ja) 2004-07-02
US20160152657A1 (en) 2016-06-02
CA2440680C (en) 2010-06-01
US20150166598A1 (en) 2015-06-18
US10421772B2 (en) 2019-09-24
EP1392714A1 (en) 2004-03-03
US20050080064A1 (en) 2005-04-14
FR17C0003I1 (fr) 2017-07-21
IL157816A (en) 2009-05-04
US7786102B2 (en) 2010-08-31
CY2017020I1 (el) 2017-11-14
FR17C0003I2 (fr) 2018-05-25
NO326134B1 (no) 2008-10-06
NO20034011L (no) 2003-11-12
US20100022498A1 (en) 2010-01-28
US8377916B2 (en) 2013-02-19
US8969330B2 (en) 2015-03-03
US9732117B2 (en) 2017-08-15
US7138390B2 (en) 2006-11-21
US20070142340A1 (en) 2007-06-21
JP4021327B2 (ja) 2007-12-12
DK1392714T3 (da) 2006-01-09
CY2017020I2 (el) 2017-11-14
US20170305961A1 (en) 2017-10-26
CA2440680A1 (en) 2002-09-19

Similar Documents

Publication Publication Date Title
BE2017C018I2 (th)
MXPA02012033A (es) Derivados de 2-aminocarbonil-9h-purina.
TNSN03144A1 (en) Pyrrolopyrimidines as protein kinase inhibitors
WO2003006425A3 (en) Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
MXPA02003977A (es) Inhibidores de adhesion de celula mediada por al°2.
WO2004007521A3 (en) Bile acid derivatives as agonists of the farnesoid x receptor
AP2003002929A0 (en) Pyrrolopyrimidines as protein kinase inhibitors
NO20043016L (no) 6-aminomorfinan-derivater, fremgangsmate for fremstilling og anvendelse derav
HK1045990A1 (en) Novel derivatives and analogues of galanthamin.
MXPA04006041A (es) Antivirales de piridoquinoxalina.
IL150061A0 (en) Purine derivatives
AU2001263278A1 (en) Cyclic gmp-specific phosphodiesterase inhibitors
DK1204658T3 (da) Benzofurylpiperazin-serotoninagonister
MXPA04005809A (es) Inhibidores de proteinas quinasas.
DE60201074D1 (en) Pyrazolopyridinderivate
AU2001296699A1 (en) Condensed pyrazindione derivatives as pde inhibitors
AU2002357740A1 (en) Pyrazolo-pyridine derivatives as antiherpes agents
MXPA03008248A (es) Agentes colorantes para fibras de queratina que contienen derivados de n-heteroarilmetil-m-fenilendiamina, asi como nuevos derivados de n-heteroarilmetil-m-fenilendiamina.
SI1651596T1 (sl) Novi derivati ditiobis aminobutan sulfonatov in sestavki ki jih vsebujejo
MXPA03006057A (es) Proceso para preparar (+) trans-4-p-fluorofenil -3 hidroximetil.
ATE282608T1 (de) Chinoxalindionen
EP1057829A4 (en) Condensed pyrimidine derivatives and pharmaceutical compositions containing them
IL159493A0 (en) Pharmaceutical formulation containing an ltb4 antagonist
AP2001002179A0 (en) 2-Aminocarbonyl-9h-purine derivatives.