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
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)
  • 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)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • 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)

Abstract

The invention relates to compounds of formula (I): wherein R is ethyl, propyl or allyl, and pharmaceutically acceptable salts, solvates or amino acid conjugates thereof. The compounds of formula (I) are useful as FXR agonists.
BE2017C018C 2001-03-12 2017-06-06 BE2017C018I2 (en)

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 (en) 2021-02-04

Family

ID=23050302

Family Applications (1)

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

Country Status (16)

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

Families Citing this family (113)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE303399T1 (en) 2001-03-12 2005-09-15 Intercept Pharmaceuticals Inc STEROIDS AS AGONISTS FOR FXR
US6696473B2 (en) 2001-12-21 2004-02-24 X-Ceptor Therapeutics, Inc. Heterocyclic 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 (en) * 2002-07-12 2004-01-12 Roberto Pellicciari CHEMICAL COMPOUNDS
PL1734970T3 (en) 2004-03-12 2015-05-29 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 (en) * 2004-03-29 2005-10-06 Japan Health Sciences Foundation Fxr activation compound
ITMI20050912A1 (en) * 2005-05-19 2006-11-20 Erregierre Spa PROCESS OF PREPARATION OF ACIDS 3-A-YA (B) -DIDROSSI-6-A (B) -ALCHIL-5B-COLANICI
US7618956B2 (en) 2005-05-31 2009-11-17 The Gillette Company Reduction of hair growth
CN101522703B (en) 2006-06-27 2013-04-17 英特塞普特医药品公司 Bile acid derivatives and its uses in the prevention or treatment of fxr-mediated diseases 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 (en) * 2006-12-22 2008-07-16 재단법인서울대학교산학협력재단 Pharmaceutical Compositions, Health Food Compositions, Cosmetic Compositions, and Panasonic X Nuclear Receptor Inhibitor Compositions Containing Sterol Derivatives
JP5292310B2 (en) * 2007-01-19 2013-09-18 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 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 (en) 2008-07-30 2014-10-30 Интерсепт Фармасьютикалз, Инк. Tgr5 modulators and use thereof
ES2663948T3 (en) 2008-11-19 2018-04-17 Intercept Pharmaceuticals, Inc. TGR5 modulators and their method of use
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
PT3336097T (en) * 2012-06-19 2020-10-29 Intercept Pharmaceuticals Inc Preparation of the non-crystalline form of obeticholic acid
HUE036887T2 (en) 2012-10-26 2018-08-28 Intercept Pharmaceuticals Inc Process for the preparation of bile acid derivatives
SG11201503697TA (en) * 2012-11-28 2015-06-29 Intercept Pharmaceuticals Inc Treatment of pulmonary disease
WO2014200349A1 (en) 2013-06-13 2014-12-18 Fast Forward Pharmaceutical B.V. Cd40 signalling inhibitor and a further compound, wherein the further compound is a bile acid, a bile acid derivative, an tgr5-receptor agonist, an fxr agonist or a combination thereof, for the treatment of chronic inflammation, and the prevention of gastrointestinal cancer or fibrosis.
PL3043865T3 (en) * 2013-09-11 2021-07-05 Institut National De La Santé Et De La Recherche Médicale (Inserm) Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection
CA3236835A1 (en) 2013-11-22 2015-05-28 Mina Therapeutics Limited C/ebp alpha short activating rna compositions and methods of use
CN104876995B (en) * 2014-02-27 2016-09-07 人福医药集团股份公司 The preparation method of chenodeoxycholic acid derivatives
EP3626725B1 (en) * 2014-05-29 2022-11-30 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 (en) * 2014-10-21 2019-05-24 重庆医药工业研究院有限责任公司 A method of preparing shellfish cholic acid intermediate difficult to understand
HK1243930A1 (en) 2014-11-06 2018-07-27 英安塔制药有限公司 Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
CN105669811B (en) * 2014-11-17 2020-09-04 正大天晴药业集团股份有限公司 Novel 7-keto-6β-alkylcholanoic acid derivatives in the preparation of obeticholic acid and its use in the field of medicine
EP3221331B1 (en) 2014-11-19 2019-09-18 Nzp Uk Limited 6-alkyl-7-hydroxy-4-en-3-one steroids as intermediates for the production of steroidal fxr modulators
JP6698085B2 (en) 2014-11-19 2020-05-27 エヌゼットピー ユーケー リミテッド 6α-Alkyl-6,7-dione-steroids as intermediates for the production of steroid FXR modulators
EA033445B1 (en) 2014-11-19 2019-10-31 Nzp Uk Ltd 5-beta-6-alkyl-7-hydroxy-3-one steroids as intermediates for the production of steroidal fxr modulators
EP3221333B1 (en) * 2014-11-19 2019-07-24 NZP UK Limited 6.alpha.-alkyl-3,7-dione steroids as intermediates for the production of steroidal fxr modulators
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
HK1244708A1 (en) 2014-11-26 2018-08-17 英安塔制药有限公司 Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
CN105801653B (en) * 2014-12-30 2018-04-17 苏州晶云药物科技有限公司 Crystal form A of shellfish cholic acid difficult to understand and preparation method thereof
CN104672290B (en) * 2015-01-05 2017-06-06 北京普禄德医药科技有限公司 A kind of medicine of disease for preventing or treating FXR mediations and its production and use
TN2017000344A1 (en) 2015-02-06 2019-01-16 Intercept Pharmaceuticals Inc Pharmaceutical compositions for combination therapy
MX2017010376A (en) 2015-02-11 2017-12-20 Enanta Pharm Inc Bile acid analogs as fxr/tgr5 agonists and methods of use thereof.
CN105985396A (en) * 2015-02-16 2016-10-05 苏州泽璟生物制药有限公司 Deuterated chenodeoxycholic acid derivative and pharmaceutical composition containing same
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10894054B2 (en) 2015-04-07 2021-01-19 Intercept Pharmaceuticals, Inc. FXR agonist compositions for combination therapy
PE20180690A1 (en) * 2015-04-27 2018-04-23 Intercept Pharmaceuticals Inc OBETICOLIC ACID COMPOSITIONS AND METHODS OF USE
CN106290594B (en) * 2015-05-27 2020-07-17 中美华世通生物医药科技（武汉）有限公司 Method for measuring dissolution content of obeticholic acid tablets
CZ2015504A3 (en) 2015-07-16 2017-01-25 Zentiva, K.S. Crystalline forms of obeticholic acid
CN105085597B (en) * 2015-08-28 2017-03-29 成都百裕制药股份有限公司 A kind of preparation method of unformed shellfish cholic acid difficult to understand
CN106478759A (en) * 2015-08-31 2017-03-08 陕西合成药业股份有限公司 Shellfish chlolic acid derivatives difficult to understand and its production and use
WO2017053428A1 (en) 2015-09-21 2017-03-30 Intercept Pharmaceuticals, Inc. Methods of promoting hepatic regeneration
CN108350020A (en) 2015-09-24 2018-07-31 英特塞普特医药品公司 It is used to prepare the method and intermediate of bile acid derivative
CN106589039B (en) * 2015-10-15 2019-12-17 苏州朗科生物技术股份有限公司 preparation method of obeticholic acid and related compound
CN106632564B (en) * 2015-10-30 2021-04-13 苏州泽璟生物制药股份有限公司 Obeticholate and its amorphous form and pharmaceutical composition
KR20180067699A (en) 2015-11-06 2018-06-20 인터셉트 파마슈티컬즈, 인크. METHOD FOR PRODUCING OBETYCHOLICANE AND ITS DERIVATIVE
CN106749466B (en) * 2015-11-23 2019-05-21 南京济群医药科技股份有限公司 A kind of preparation method of high-purity obeticholic acid
CN106854229A (en) * 2015-12-08 2017-06-16 陈剑 One class soap, it is prepared and its in application pharmaceutically
WO2017115324A1 (en) 2016-01-01 2017-07-06 Lupin Limited Solid forms of obeticholic acid and processes thereof
EP3409684B1 (en) 2016-01-28 2024-01-03 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Steroid derivative fxr agonist
ES2909907T3 (en) 2016-02-10 2022-05-10 Dr Reddys Laboratories Ltd Purification process involving the amine salt of obeticholic acid
WO2017147137A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as fxr/tgr5 agonists and methods of use thereof
WO2017147159A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10323061B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Heteroaryl containing bile acid analogs as FXR/TGR5 agonists and methods of use thereof
CN109467585A (en) * 2016-03-11 2019-03-15 深圳市塔吉瑞生物医药有限公司 Cholanic acid compounds for preventing or treating FXR-mediated diseases
CN107188917A (en) * 2016-03-15 2017-09-22 正大天晴药业集团股份有限公司 Shellfish cholate difficult to understand and its pharmaceutical composition
CN105541953B (en) * 2016-03-15 2017-11-21 成都市新功生物科技有限公司 A kind of recrystallization purifying method of high-purity Austria shellfish cholic acid
TW201733582A (en) 2016-03-28 2017-10-01 大日本住友製藥股份有限公司 Pharmaceutical combination comprising FXR agonist and ARB
EP3437646A4 (en) * 2016-03-31 2019-11-27 Intercept Pharmaceuticals, Inc. ORAL PREPARATION HAVING EXCEPTIONAL ABILITY TO ELUTE
KR20180125573A (en) * 2016-03-31 2018-11-23 인터셉트 파마슈티컬즈, 인크. A film-coated tablet with excellent chemical stability
EP3228306A1 (en) 2016-04-04 2017-10-11 ratiopharm GmbH Complex compound comprising obeticholic acid and cyclodextrin and pharmaceutical formulation comprising the complex compound
CN109311933A (en) * 2016-04-04 2019-02-05 迪法玛弗朗西斯有限公司 Method for preparing farnesoid X receptor agonists
ITUA20162272A1 (en) * 2016-04-04 2017-10-04 Dipharma Francis Srl PROCEDURE FOR THE PREPARATION OF AN AGONIST OF THE FARNESOID RECEPTOR X
WO2017180577A1 (en) 2016-04-13 2017-10-19 Intercept Pharmaceuticals, Inc. Methods of treating cancer
TW201738254A (en) 2016-04-19 2017-11-01 英特賽普醫藥品公司 Preparation method of oleic acid and its derivative
EA038580B9 (en) * 2016-05-18 2021-10-05 Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. Steroid derivative fxr agonist
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 (en) 2016-06-01 2019-03-01 雷迪博士实验室有限公司 The method for preparing shellfish cholic acid difficult to understand
CZ2016385A3 (en) 2016-06-28 2018-01-10 Zentiva, K.S. A method of preparing intermediates for synthesis of obeticholic acid
TWI606565B (en) * 2016-08-31 2017-11-21 金寶電子工業股份有限公司 Package structure and manufacturing method thereof
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
CN110121347A (en) 2016-11-29 2019-08-13 英安塔制药有限公司 The method for preparing sulfonylureas bile acid derivative
CN108264532B (en) * 2016-12-30 2021-02-26 上海现代制药股份有限公司 A kind of preparation method of obeticholic acid and intermediate thereof
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
AU2018223146B2 (en) 2017-02-21 2023-12-21 Genfit Combination of a PPAR agonist with a FXR agonist
US20210085662A1 (en) 2017-03-30 2021-03-25 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses
BR112019020780A2 (en) 2017-04-07 2020-04-28 Enanta Pharm Inc process for preparing sulfonyl carbamate bile acid derivatives
CZ2017298A3 (en) 2017-05-26 2018-12-05 Zentiva, K.S. Amorphous forms of obeticholic acid
CN109134572A (en) * 2017-06-19 2019-01-04 中国科学院上海药物研究所 Chlolic acid derivatives and its preparation method and application
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
CA3075205A1 (en) 2017-09-08 2019-03-14 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
US10829486B2 (en) 2018-02-14 2020-11-10 Enanta Pharmacueticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
ES2779985B2 (en) 2019-02-20 2021-03-04 Moehs Iberica Sl 3alpha-tetrahydropyranyloxy-6alpha-ethyl-7alpha-hydroxy-5ß-cholanic acid diethylamine salt
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 (en) 2019-03-19 2020-09-29 苏州泽璟生物制药股份有限公司 Preparation method of chenodeoxycholic acid derivative
CN110025591A (en) * 2019-04-29 2019-07-19 郑州泰丰制药有限公司 A kind of Austria's shellfish cholic acid self-emulsifiable preparation and its soft capsule
WO2020231917A1 (en) 2019-05-13 2020-11-19 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
EA202193334A1 (en) 2019-05-30 2022-03-14 Интерсепт Фармасьютикалз, Инк. PHARMACEUTICAL COMPOSITIONS CONTAINING FXR AGONIST AND FIBRATE FOR USE IN THE TREATMENT OF CHOLESTATIC LIVER DISEASE
AU2020312735A1 (en) 2019-07-18 2021-12-16 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
US20230060715A1 (en) 2020-01-15 2023-03-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
CN112341516B (en) * 2020-11-14 2022-07-15 湖南科瑞生物制药股份有限公司 5, 6-epoxy steroid compound and preparation method and application thereof
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CN117320722A (en) 2021-04-28 2023-12-29 埃尼奥制药公司 Use of FXR agonists as combination therapy strongly potentiates the effects of TLR3 agonists
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 (en) 1978-12-15 1981-08-14 Roussel Uclaf
FR2457302A1 (en) 1979-05-23 1980-12-19 Roussel Uclaf NEW PROCESS FOR THE PURIFICATION OF URSODESOXYCHOLIC ACID
IT1165252B (en) 1979-07-12 1987-04-22 Blasinachim Spa PURIFICATION PROCEDURE FOR URSODESOXICOLIC ACID THROUGH NEW DERIVATIVES
DE3003607C2 (en) 1980-02-01 1984-01-05 Dr.-Ing. Rudolf Hell Gmbh, 2300 Kiel Circuit arrangement for partial post-correction of color recognition spaces during color recognition
IT1137459B (en) 1981-04-14 1986-09-10 Erregierre Spa PRODUCTION FOR THE PREPARATION OF HIGH PURITY URSODEOXICOLIC ACID
EP0101554B1 (en) 1982-07-29 1986-10-15 Lehner A.G. New derivatives of biliary acids, process for the production thereof and pharmaceutical compositions containing the same
IT1206112B (en) 1983-04-29 1989-04-14 Lehner Ag NEW DERIVATIVES OF BILE ACIDS, PROCEDURE FOR THEIR PREPARATION AND RELATED PHARMACEUTICAL COMPOSITIONS.
IT1212835B (en) 1983-08-18 1989-11-30 Lehner Ag BILIARY ACID DERIVATIVES, PROCEDURE FOR THEIR PREPARATION AND RELATED PHARMACEUTICAL COMPOSITIONS.
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 (en) 1984-12-21 1988-11-16 Lehner Ag BILIARY ACID DERIVATIVES, PROCEDURE FOR THEIR PREPARATION AND RELATED PHARMACEUTICAL COMPOSITIONS
IT1223313B (en) 1987-10-20 1990-09-19 Gipharmex Spa BILIARY ACID DERIVATIVES THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
FR2627696B1 (en) 1988-02-26 1991-09-13 Fournier Innovation Synergie NEW GALENIC FORM OF 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 (en) * 1989-04-17 1991-09-04 Giuliani Spa FLUORATED DERIVATIVES OF BILIARY ACIDS, THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM.
US4982868A (en) * 1989-11-07 1991-01-08 Robbins Edward S Iii Bail type pitcher for thin walled container
ATE121080T1 (en) * 1989-12-13 1995-04-15 Mitsubishi Chem Corp PYRAZOLYLACRYLIC ACID DERIVATIVES, USABLE AS SYSTEMIC FUNGICIDES IN PLANT AND MATERIAL PROTECTION.
JPH04250093A (en) 1991-01-18 1992-09-04 Kanzaki Paper Mfg Co Ltd Thermal recording body
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
WO1999038845A1 (en) 1998-01-29 1999-08-05 Tularik Inc. Ppar-gamma modulators
WO1999050407A1 (en) * 1998-03-26 1999-10-07 Kyowa Hakko Kogyo Co., Ltd. Monoclonal antibody against human telomerase catalytic subunit
WO2000025134A1 (en) 1998-10-23 2000-05-04 Glaxo Group Limited Assays for ligands for nuclear receptors
AU1911200A (en) 1998-11-09 2000-05-29 Atherogenics, Inc. Methods and compositions to lower plasma cholesterol levels
UA74141C2 (en) 1998-12-09 2005-11-15 Дж.Д. Сірл Енд Ко. Oral pharmaceutical compositions comprising micronized eplerenone (variants), method for its production and method for treating aldosterone-mediated states (variants)
ES2326850T3 (en) 1998-12-23 2009-10-20 Glaxo Group Limited TESTS FOR NUCLEAR RECEPTORS LIGANDOS.
AU2409600A (en) 1999-01-07 2000-07-24 Tularik Inc. Fxr receptor-mediated modulation of cholesterol metabolism
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
EP1473042B1 (en) 1999-03-26 2006-06-21 City of Hope Screening for FXR receptor modulators
WO2000057915A1 (en) 1999-03-26 2000-10-05 City Of Hope Method of affecting cholesterol catabolism using nuclear bile acid receptor
CN1368884A (en) 1999-06-11 2002-09-11 阿勒根销售公司 Method 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
ATE303399T1 (en) 2001-03-12 2005-09-15 Intercept Pharmaceuticals Inc STEROIDS AS AGONISTS FOR FXR
WO2002084286A1 (en) 2001-04-12 2002-10-24 Takeda Chemical Industries, Ltd. Screening method
EP1285914B1 (en) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4 nuclear receptor binding compounds
EP1423113A4 (en) 2001-08-13 2007-04-18 Phenex Pharmaceuticals Ag Nr1h4 nuclear receptor binding compounds
US20070010562A1 (en) 2001-08-13 2007-01-11 Ulrike Bauer 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
US20050107475A1 (en) 2002-03-21 2005-05-19 Jones Stacey A. Methods of using farnesoid x receptor (frx) 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 (en) 2002-07-12 2004-01-12 Roberto Pellicciari CHEMICAL COMPOUNDS
JP2006515838A (en) 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 Farnesoid X receptor agonist
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
WO2005092369A2 (en) 2004-03-11 2005-10-06 Fresenius Kabi Deutschland Gmbh Conjugates of hydroxyethyl starch and erythropoietin
PL1734970T3 (en) 2004-03-12 2015-05-29 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 (en) 2005-05-19 2006-11-20 Erregierre Spa PROCESS OF PREPARATION OF ACIDS 3-A-YA (B) -DIDROSSI-6-A (B) -ALCHIL-5B-COLANICI
WO2007095174A2 (en) 2006-02-14 2007-08-23 Intercept Pharmaceuticals, Inc. Bile acid derivatives as fxr ligands for the prevention or treatment of fxr-mediated diseases or conditions
CN101522703B (en) 2006-06-27 2013-04-17 英特塞普特医药品公司 Bile acid derivatives and its uses in the prevention or treatment of fxr-mediated diseases or conditions
US20100239661A1 (en) 2006-10-26 2010-09-23 Sunilendu Bhushan Roy Pharmaceutical compositions of ursodiol
EP1947108A1 (en) 2007-01-19 2008-07-23 Intercept Pharmaceuticals, Inc. TGR5 modulators and methods of use thereof
JP5292310B2 (en) 2007-01-19 2013-09-18 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 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 (en) 2008-11-19 2018-04-17 Intercept Pharmaceuticals, Inc. TGR5 modulators and their method of use
NZ595902A (en) 2009-04-24 2014-10-31 Iceutica Pty Ltd Method for the production of commercial nanoparticle and microparticle powders
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 (en) 2011-10-21 2018-01-19 Inopharm Limited PHARMACEUTICAL COMPOSITIONS OF URSODESOXYCHOLIC ACID
PT3336097T (en) 2012-06-19 2020-10-29 Intercept Pharmaceuticals Inc Preparation of the non-crystalline form of obeticholic acid
CA2912139C (en) 2013-05-14 2021-04-20 Roberto Pellicciari 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators

Also Published As

Publication number Publication date
FR17C0003I2 (en) 2018-05-25
FR17C0003I1 (en) 2017-07-21
IL157816A (en) 2009-05-04
NO20034011L (en) 2003-11-12
NO326134B1 (en) 2008-10-06
US20150166598A1 (en) 2015-06-18
WO2002072598A1 (en) 2002-09-19
US20120053163A1 (en) 2012-03-01
US8969330B2 (en) 2015-03-03
US20190300564A9 (en) 2019-10-03
US20170305961A1 (en) 2017-10-26
JP2004519492A (en) 2004-07-02
JP4021327B2 (en) 2007-12-12
US20160152657A1 (en) 2016-06-02
US20050080064A1 (en) 2005-04-14
DE60205891T2 (en) 2006-06-22
NO2017022I1 (en) 2017-05-26
CY2017020I1 (en) 2017-11-14
USRE48286E1 (en) 2020-10-27
ES2248581T3 (en) 2006-03-16
JP2007269815A (en) 2007-10-18
ATE303399T1 (en) 2005-09-15
US20100022498A1 (en) 2010-01-28
US7786102B2 (en) 2010-08-31
CA2440680C (en) 2010-06-01
US7138390B2 (en) 2006-11-21
US10421772B2 (en) 2019-09-24
US20140024631A1 (en) 2014-01-23
NO2017022I2 (en) 2018-08-20
US8058267B2 (en) 2011-11-15
EP1392714B1 (en) 2005-08-31
AU2002308295B2 (en) 2007-08-23
DE60205891D1 (en) 2005-10-06
CA2440680A1 (en) 2002-09-19
CY2017020I2 (en) 2017-11-14
US9732117B2 (en) 2017-08-15
EP1392714A1 (en) 2004-03-03
NL300877I2 (en) 2017-06-22
US20070142340A1 (en) 2007-06-21
DK1392714T3 (en) 2006-01-09
IL157816A0 (en) 2004-03-28
US8377916B2 (en) 2013-02-19
NO20034011D0 (en) 2003-09-11

Similar Documents

Publication Publication Date Title
NL300877I2 (en) obeticholic acid
MXPA02012033A (en) 2-aminocarbonyl-9h-purine derivatives.
TNSN03144A1 (en) Pyrrolopyrimidines as protein kinase inhibitors
WO2003006425A3 (en) Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
MXPA02003977A (en) INHIBITORS OF agr;L.
YU83602A (en) Phenylglycine derivatives
WO2004007521A3 (en) Bile acid derivatives as agonists of the farnesoid x receptor
AP2003002929A0 (en) Pyrrolopyrimidines as protein kinase inhibitors
NO20043016L (en) 6-aminomorphinan derivatives, process for preparation and use thereof
IL150061A0 (en) Purine derivatives
MXPA04006041A (en) Pyridoquinoxaline antivirals.
AU2001263278A1 (en) Cyclic gmp-specific phosphodiesterase inhibitors
MXPA04005809A (en) Protein kinase inhibitors.
DK1204658T3 (en) Benzofurylpiperazine-serotonin agonists
AU2002357740A1 (en) Pyrazolo-pyridine derivatives as antiherpes agents
DE60201074D1 (en) Pyrazolopyridinderivate
AU2001296699A1 (en) Condensed pyrazindione derivatives as pde inhibitors
MXPA03008248A (en) N-heteroarylmethyl-m-phenylenediamine derivative-containing dyes for keratin fibers and novel n-heteroarylmethyl-m-phenylenediamine derivatives.
SI1651596T1 (en) Novel derivatives of 4,4'-dithiobis-(3-aminobutane-1-sulfonates) and compositions comprising the same
MXPA03006057A (en) Process for preparing (plusmn;) trans-4 -p-fluorophenyl -3-hydroxymethyl -1-methylpiperidine.
ATE282608T1 (en) QUINOXALINDIONES
EP1057829A4 (en) Novel compounds and pharmaceutical compositions containing the same
IL159493A0 (en) Pharmaceutical formulation containing an ltb4 antagonist
AP2001002179A0 (en) 2-Aminocarbonyl-9h-purine derivatives.