MX2017010376A - Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos. - Google Patents

Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.

Info

Publication number
MX2017010376A
MX2017010376A MX2017010376A MX2017010376A MX2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A MX 2017010376 A MX2017010376 A MX 2017010376A
Authority
MX
Mexico
Prior art keywords
disease
fxr
methods
bile acid
acid analogs
Prior art date
Application number
MX2017010376A
Other languages
English (en)
Inventor
Sun Or Yat
Wang Guoqiang
Shen Ruichao
Original Assignee
Enanta Pharm 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
Application filed by Enanta Pharm Inc filed Critical Enanta Pharm Inc
Publication of MX2017010376A publication Critical patent/MX2017010376A/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J41/00Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
    • C07J41/0033Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005
    • C07J41/0055Normal 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
    • C07J41/0061Normal 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 one of the carbon atoms being part of an amide group
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J43/00Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J9/00Normal 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
    • C07J9/005Normal 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Immunology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La presente invención proporciona compuestos de Fórmula I, composiciones farmacéuticas que comprenden estos compuestos y métodos para usar estos compuestos para tratar o prevenir una enfermedad o trastorno mediadao por FXR y/o TGR5. En ciertas modalidades, una enfermedad que conlleva la modulación del receptor TGR5 es seleccionado de enfermedad metabólica, enfermedad inflamatoria, enfermedad hepática, enfermedad autoinmune, enfermedad cardíaca, enfermedad renal, cáncer, y enfermedad gastroinstestinal. (Ver Fórmula I).
MX2017010376A 2015-02-11 2016-02-11 Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos. MX2017010376A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562114773P 2015-02-11 2015-02-11
PCT/US2016/017554 WO2016130809A1 (en) 2015-02-11 2016-02-11 Bile acid analogs as fxr/tgr5 agonists and methods of use thereof

Publications (1)

Publication Number Publication Date
MX2017010376A true MX2017010376A (es) 2017-12-20

Family

ID=56565728

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2017010376A MX2017010376A (es) 2015-02-11 2016-02-11 Análogos de ácido biliar como agonistas de fxr/tgr5 y métodos para el uso de los mismos.

Country Status (14)

Country Link
US (1) US10246483B2 (es)
EP (1) EP3256134A4 (es)
JP (1) JP2018505190A (es)
KR (1) KR20170133339A (es)
CN (1) CN107249594A (es)
AU (1) AU2016219266A1 (es)
BR (1) BR112017017238A2 (es)
CA (1) CA2975257A1 (es)
HK (1) HK1245100A1 (es)
MX (1) MX2017010376A (es)
PH (1) PH12017501339A1 (es)
RU (1) RU2017130466A (es)
SG (1) SG11201706089RA (es)
WO (1) WO2016130809A1 (es)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2016073767A1 (en) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an 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
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
CA2981503C (en) 2015-03-31 2023-09-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10517321B2 (en) 2015-07-10 2019-12-31 Sweet Green Fields USA LLC Compositions of steviol multiglycosylated derivatives and stevia components
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
WO2017147159A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof
CN106237332A (zh) * 2016-08-11 2016-12-21 河南大学 核受体fxr在肝癌干细胞靶向治疗中的应用
CA3045023A1 (en) 2016-11-29 2018-06-07 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonylurea bile acid derivatives
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
CA3058754A1 (en) 2017-04-07 2018-10-11 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
JP7224307B2 (ja) 2017-06-23 2023-02-17 インターセプト ファーマシューティカルズ, インコーポレイテッド 胆汁酸誘導体の調製のための方法及び中間体
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
EP3999101A1 (en) 2019-07-18 2022-05-25 ENYO Pharma Method for decreasing adverse-effects of interferon
KR20220150270A (ko) 2019-10-07 2022-11-10 칼리오페, 인크. Gpr119 효능제
WO2021144330A1 (en) 2020-01-15 2021-07-22 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
TW202140440A (zh) 2020-02-28 2021-11-01 美商克力歐普股份有限公司 Gpr40激動劑
WO2021236617A1 (en) 2020-05-19 2021-11-25 Kallyope, Inc. Ampk activators
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂
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
WO2023288123A1 (en) 2021-07-16 2023-01-19 Interecept Pharmaceuticals, Inc. Methods and intermediates for the preparation of 3.alpha.,7.alpha.,11.beta.-trihydroxy-6.alpha.-ethyl-5.beta.-cholan-24-oic acid

Family Cites Families (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1592791A (en) 1977-01-07 1981-07-08 Radiochemical Centre Ltd Selenium- or tellurium-containing bile acids and derivatives thereof
US4917826A (en) 1985-10-18 1990-04-17 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
IT1255449B (it) 1992-06-30 1995-10-31 Fabio Berlati Uso di nor- e omo-derivati di acidi biliari come promotori di assorbimento di farmaci.
IT1255485B (it) 1992-08-04 1995-11-06 Erregierre Ind Chim Processo per preparare gli acidi biliari coniugati con la glicina e relative composizioni terapeutiche per il trattamento dell'insufficienza epatica
TW289020B (es) 1993-05-08 1996-10-21 Hoechst Sktiengesellschaft
TW289757B (es) * 1993-05-08 1996-11-01 Hoechst Ag
US5646316A (en) 1994-04-08 1997-07-08 Osteoarthritis Sciences, Inc. Bile acid inhibitors of metalloproteinase enzymes
JPH1160594A (ja) 1997-08-25 1999-03-02 Sankyo Co Ltd 胆汁酸誘導体
JP3865890B2 (ja) 1997-09-30 2007-01-10 富士フイルムホールディングス株式会社 ポジ型感光性組成物
US20020132223A1 (en) 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
US20020098999A1 (en) 2000-10-06 2002-07-25 Gallop Mark A. Compounds for sustained release of orally delivered drugs
AU2002308295B2 (en) 2001-03-12 2007-08-23 Intercept Pharmaceuticals, Inc. Steroids as agonists for FXR
ITMI20021080A1 (it) 2002-05-21 2003-11-21 Marcello Izzo Associazioni farmaceutiche per uso topico a base di chelati del ferroinibitori delle metalloproteasi e fattore xiii per il trattamento dell
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
EP1734970B1 (en) 2004-03-12 2014-12-31 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
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
AU2007230991A1 (en) 2006-03-22 2007-10-04 Syndexa Pharmaceuticals Corporation Compounds and methods for treatment of disorders associated with ER stress
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
AU2007276405A1 (en) 2006-07-17 2008-01-24 Novartis Ag Sulphonylaminocarbonyl derivatives of bile acid amides for use as immunomodulators
AU2008209566C1 (en) 2007-01-19 2013-02-14 Intercept Pharmaceuticals, Inc. 23-substituted bile acids as TGR5 modulators and methods of use thereof
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
WO2009032321A2 (en) 2007-09-06 2009-03-12 Genaera Corporation A method for treating diabetes
US20090163474A1 (en) 2007-10-19 2009-06-25 Wyeth FXR Agonists for the Treatment of Nonalcoholic Fatty Liver and Cholesterol Gallstone Diseases
EA020310B1 (ru) 2008-07-30 2014-10-30 Интерсепт Фармасьютикалз, Инк. Модуляторы рецептора tgr5 и их применение
EP2739286A4 (en) 2011-08-04 2015-06-03 Lumena Pharmaceuticals Inc GALLENIC ACID FLUID FOR THE TREATMENT OF PANCREATITIS
WO2013049595A1 (en) * 2011-09-29 2013-04-04 Ethicon Endo-Surgery, Inc. Methods and compositions of bile acids
US9084826B2 (en) 2012-05-01 2015-07-21 Catabasis Pharmaceuticals, Inc. Fatty acid conjugates of statin and FXR agonists; compositions and method of uses
NZ734451A (en) 2012-06-19 2018-12-21 Intercept Pharmaceuticals Inc Preparation, uses and solid forms of obeticholic acid
WO2014036377A1 (en) 2012-08-31 2014-03-06 Metselex Methods of promoting cell viability
US20140187633A1 (en) 2012-12-31 2014-07-03 Amarin Pharmaceuticals Ireland Limited Methods of treating or preventing nonalcoholic steatohepatitis and/or primary biliary cirrhosis
US9814733B2 (en) 2012-12-31 2017-11-14 A,arin Pharmaceuticals Ireland Limited Compositions comprising EPA and obeticholic acid and methods of use thereof
US20140206657A1 (en) 2013-01-18 2014-07-24 City Of Hope Bile acid analog tgr5 agonists
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
JP6556129B2 (ja) 2013-08-01 2019-08-07 アメリカ合衆国 ファルネソイドx受容体の阻害剤及び医薬としての使用
US20150112089A1 (en) 2013-10-22 2015-04-23 Metselex, Inc. Deuterated bile acids
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
WO2016073767A1 (en) 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Bile acid analogs an 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
CN111116699B (zh) 2015-04-28 2023-02-28 江苏豪森药业集团有限公司 胆酸衍生物及其制备方法和医药用途
WO2016173493A1 (en) 2015-04-28 2016-11-03 Shanghai De Novo Pharmatech Co. Ltd. Sulfonylaminocarbonyl derivative, pharmaceutical composition and uses thereof
TW201704251A (zh) 2015-04-29 2017-02-01 正大天晴藥業集團股份有限公司 鵝去氧膽酸衍生物
EP3310801B1 (en) 2015-06-19 2021-04-07 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
CN108137643A (zh) 2015-08-07 2018-06-08 英特塞普特医药品公司 制备胆汁酸及其衍生物的方法
CN105175473B (zh) 2015-08-19 2018-12-21 丽珠医药集团股份有限公司 一种奥贝胆酸晶型i及其制备方法、药物组合物和用途
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
CN106518946A (zh) 2015-09-10 2017-03-22 上海迪诺医药科技有限公司 磺酰脲衍生物、其药物组合物及应用
EP3353189A4 (en) 2015-09-24 2019-06-19 Intercept Pharmaceuticals, Inc. METHOD AND INTERMEDIATE PRODUCTS FOR THE PREPARATION OF GALLENIC ACID DERIVATIVES
EP3981779A1 (en) 2015-10-07 2022-04-13 Intercept Pharmaceuticals, Inc. Farnesoid x receptor modulators
US10875888B2 (en) 2016-01-28 2020-12-29 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Steroid derivative FXR agonist
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
WO2017147159A1 (en) 2016-02-23 2017-08-31 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
US10323060B2 (en) 2016-02-23 2019-06-18 Enanta Pharmaceuticals, Inc. Benzoic acid derivatives of bile acid as FXR/TGR5 agonists and methods of use thereof
EP3426348B1 (en) 2016-03-11 2021-05-05 Intercept Pharmaceuticals, Inc. 3-desoxy derivative and pharmaceutical compositions thereof
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof

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CA2975257A1 (en) 2016-08-18
AU2016219266A1 (en) 2017-08-10
BR112017017238A2 (pt) 2018-04-10
RU2017130466A (ru) 2019-03-12
JP2018505190A (ja) 2018-02-22
SG11201706089RA (en) 2017-09-28
US20160229886A1 (en) 2016-08-11
KR20170133339A (ko) 2017-12-05
EP3256134A1 (en) 2017-12-20
PH12017501339A1 (en) 2017-12-18
CN107249594A (zh) 2017-10-13
WO2016130809A1 (en) 2016-08-18
US10246483B2 (en) 2019-04-02
HK1245100A1 (zh) 2018-08-24
EP3256134A4 (en) 2018-10-03

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