SG10201910670RA - Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof - Google Patents

Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof

Info

Publication number
SG10201910670RA
SG10201910670RA SG10201910670RA SG10201910670RA SG10201910670RA SG 10201910670R A SG10201910670R A SG 10201910670RA SG 10201910670R A SG10201910670R A SG 10201910670RA SG 10201910670R A SG10201910670R A SG 10201910670RA SG 10201910670R A SG10201910670R A SG 10201910670RA
Authority
SG
Singapore
Prior art keywords
fxr
methods
acid derivatives
bile acid
tgr5 agonists
Prior art date
Application number
SG10201910670RA
Inventor
Guoqiang Wang
Yat Sun Or
Ruichao Shen
Xuechao Xing
Jiang Long
Peng Dai
Brett Granger
Jing He
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 SG10201910670RA publication Critical patent/SG10201910670RA/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/58Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • 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
    • A61P3/06Antihyperlipidemics
    • 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
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • 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
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • 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
    • C07J41/005Normal 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 only two carbon atoms, e.g. pregnane derivatives
    • 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
    • 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
    • C07J41/0088Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring not covered by C07J41/0005 containing unsubstituted amino radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J51/00Normal steroids with unmodified cyclopenta(a)hydrophenanthrene skeleton not provided for in groups C07J1/00 - C07J43/00
    • 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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
SG10201910670RA 2015-03-31 2016-03-30 Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof SG10201910670RA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562140927P 2015-03-31 2015-03-31
US201662287267P 2016-01-26 2016-01-26

Publications (1)

Publication Number Publication Date
SG10201910670RA true SG10201910670RA (en) 2020-01-30

Family

ID=57007583

Family Applications (2)

Application Number Title Priority Date Filing Date
SG11201707263XA SG11201707263XA (en) 2015-03-31 2016-03-30 Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
SG10201910670RA SG10201910670RA (en) 2015-03-31 2016-03-30 Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof

Family Applications Before (1)

Application Number Title Priority Date Filing Date
SG11201707263XA SG11201707263XA (en) 2015-03-31 2016-03-30 Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof

Country Status (27)

Country Link
US (3) US10457703B2 (en)
EP (1) EP3277286B1 (en)
JP (1) JP6785788B2 (en)
KR (1) KR20170131558A (en)
CN (1) CN107427527B (en)
AU (1) AU2016242861B2 (en)
CA (1) CA2981503C (en)
CY (1) CY1124404T1 (en)
DK (1) DK3277286T3 (en)
ES (1) ES2886766T3 (en)
HK (1) HK1250622A1 (en)
HR (1) HRP20211066T1 (en)
HU (1) HUE054960T2 (en)
IL (1) IL254288B (en)
LT (1) LT3277286T (en)
MX (1) MX2017012558A (en)
MY (1) MY192135A (en)
NZ (1) NZ735126A (en)
PH (1) PH12017501586B1 (en)
PL (1) PL3277286T3 (en)
PT (1) PT3277286T (en)
RS (1) RS62110B1 (en)
RU (1) RU2712099C2 (en)
SG (2) SG11201707263XA (en)
SI (1) SI3277286T1 (en)
WO (1) WO2016161003A1 (en)
ZA (2) ZA201707212B (en)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1948236B1 (en) 2005-09-27 2021-03-03 Special Water Patents B.V. Methods and compositions for treatment of skin
MX2017005935A (en) 2014-11-06 2018-01-11 Enanta Pharm Inc Bile acid analogs an 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
CA2968404A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs 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
MY196292A (en) * 2016-01-28 2023-03-24 Chia Tai Tianqing Pharmaceutical Group Co Ltd Steroid Derivative Fxr Agonist
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
US10364267B2 (en) 2016-02-23 2019-07-30 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
EA038580B9 (en) * 2016-05-18 2021-10-05 Чиа Тай Тяньцин Фармасьютикал Груп Ко., Лтд. Steroid derivative fxr agonist
ES2918698T3 (en) 2016-11-29 2022-07-19 Enanta Pharm Inc Process for the preparation of bile acid derivatives of sulfonylureas
CN108218946B (en) * 2016-12-15 2021-04-16 宁波百纳西药业有限公司 Deoxycholic acid compound, preparation method and application thereof
CN108218945B (en) * 2016-12-15 2021-05-28 宁波百纳西药业有限公司 Deoxycholic acid derivative, preparation method, pharmaceutical composition and application thereof
WO2018152171A1 (en) * 2017-02-14 2018-08-23 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr agonists and methods of use thereof
WO2018187804A1 (en) * 2017-04-07 2018-10-11 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
AU2018288883B2 (en) 2017-06-23 2022-06-02 Intercept Pharmaceuticals, Inc. Methods and intermediates for the preparation of bile acid derivatives
WO2019020067A1 (en) * 2017-07-26 2019-01-31 正大天晴药业集团股份有限公司 Method for preparing steroid derivative fxr agonist
GB201812382D0 (en) 2018-07-30 2018-09-12 Nzp Uk Ltd Compounds
AU2020312735A1 (en) 2019-07-18 2021-12-16 Enyo Pharma Method for decreasing adverse-effects of interferon
WO2021071837A1 (en) 2019-10-07 2021-04-15 Kallyope, Inc. Gpr119 agonists
AU2021207253A1 (en) 2020-01-15 2022-06-09 Centre National De La Recherche Scientifique Use of FXR agonists for treating an infection by hepatitis D virus
CA3178994A1 (en) 2020-05-19 2021-11-25 Iyassu Sebhat Ampk activators
CN116390925A (en) 2020-06-26 2023-07-04 卡尔优普公司 AMPK activator
WO2022152770A1 (en) 2021-01-14 2022-07-21 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
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 (144)

* 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
WO1987002367A2 (en) 1985-10-18 1987-04-23 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
US5571809A (en) 1989-04-20 1996-11-05 Boehringer Ingelheim Pharmaceuticals, Inc. The treatment of HIV-1 infection using certain pyridodiazepines
IT1255449B (en) 1992-06-30 1995-10-31 Fabio Berlati USE OF NOR- AND HOMO-DERIVATIVES OF BILE ACIDS AS DRUGS ABSORPTION PROMOTERS.
IT1255485B (en) 1992-08-04 1995-11-06 Erregierre Ind Chim PROCESS TO PREPARE GLYCINE CONJUGATED BILIARY ACIDS AND RELATED THERAPEUTIC COMPOSITIONS FOR THE TREATMENT OF HEPATIC INSUFFICIENCY
TW289757B (en) 1993-05-08 1996-11-01 Hoechst Ag
TW289020B (en) 1993-05-08 1996-10-21 Hoechst Sktiengesellschaft
US5541348A (en) * 1994-03-10 1996-07-30 National Research Council Of Canada Bile acids for biological and chemical applications and processes for the production thereof
DE69535592T2 (en) 1994-03-25 2008-06-12 Isotechnika, Inc., Edmonton IMPROVING THE EFFECTIVENESS OF MEDICINES BY DEUTERIZATION
US5646316A (en) 1994-04-08 1997-07-08 Osteoarthritis Sciences, Inc. Bile acid inhibitors of metalloproteinase enzymes
US7125866B1 (en) 1999-04-30 2006-10-24 Regents Of The University Of Michigan Therapeutic applications of pro-apoptotic benzodiazepines
JPH1160594A (en) 1997-08-25 1999-03-02 Sankyo Co Ltd Bile acid derivative
JP3865890B2 (en) 1997-09-30 2007-01-10 富士フイルムホールディングス株式会社 Positive photosensitive composition
DE69940958D1 (en) 1998-12-23 2009-07-16 Glaxo Group Ltd DETERMINATION METHOD FOR LIGANDS OF NUCLEAR RECEPTORS
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
AU2002211863A1 (en) * 2000-10-06 2002-04-15 Xenoport, Inc. Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration
DK1392714T3 (en) 2001-03-12 2006-01-09 Intercept Pharmaceuticals Inc Steroids as Agonists for FXR
EP1285914B1 (en) 2001-08-13 2007-12-19 PheneX Pharmaceuticals AG Nr1h4 nuclear receptor binding compounds
CA2482195A1 (en) 2002-04-12 2003-10-23 The University Of Chicago Farnesoid x-activated receptor agonists
ITMI20021080A1 (en) 2002-05-21 2003-11-21 Marcello Izzo PHARMACEUTICAL ASSOCIATIONS FOR TOPICAL USE BASED ON CHELATES OF THE METAL PROTEASIS FERROINHIBITORS AND FACTOR XIII FOR THE TREATMENT OF
WO2004046162A2 (en) 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
EP1562915A1 (en) 2002-11-22 2005-08-17 SmithKline Beecham Corporation Farnesoid x receptor agonists
JPWO2005054213A1 (en) 2003-12-02 2007-12-06 塩野義製薬株式会社 Isoxazole derivatives having peroxisome proliferator activated receptor agonist activity
EP1568706A1 (en) 2004-02-26 2005-08-31 Intercept Pharmaceuticals, Inc. Novel steroid agonist for FXR
EP2712617B2 (en) 2004-03-12 2020-11-18 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using Fxr ligands
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
EP1962838B1 (en) 2005-12-19 2011-09-28 GlaxoSmithKline LLC Farnesoid x receptor agonists
BRPI0706747A2 (en) 2006-01-30 2011-04-05 Exelixis Inc 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and pharmaceutical compositions containing them
EP1978968A2 (en) 2006-02-01 2008-10-15 Brigham Young University Cationic steroid antimicrobial compositions for treating or preventing hiv infections
CN101374834B (en) 2006-02-03 2011-12-14 伊莱利利公司 Compounds and methods for modulating FXR
BRPI0707794A2 (en) 2006-02-14 2011-05-10 Intercept Pharmaceuticals Inc bile acid derivatives, formulations and pharmaceutical compositions, as well as use of said compounds
CA2681639A1 (en) 2006-03-22 2007-10-04 Syndexa Pharmaceuticals Corporation Compounds and methods for treatment of disorders associated with er stress
PL2029547T3 (en) 2006-05-24 2010-09-30 Lilly Co Eli Fxr agonists
DK2040713T3 (en) 2006-06-27 2014-09-29 Intercept Pharmaceuticals Inc BILIC ACID DERIVATIVES AS FXR LIGANDS FOR THE PREVENTION OR TREATMENT OF FXR-MEDIATED DISEASES OR CONDITIONS
TW200811170A (en) 2006-06-27 2008-03-01 Sanofi Aventis Urea derivatives of tropane, their preparation and their therapeutic application
RU2009105179A (en) 2006-07-17 2010-08-27 Новартис АГ (CH) SULFONILAMINOCARBONYL DERIVATIVES OF CHOLIC ACID AMIDES FOR APPLICATION AS IMMUNOMODULATORS
CN101535303B (en) 2006-08-15 2012-07-18 诺瓦提斯公司 Heterocyclic compounds suitable for the treatment of diseases related to elevated lipid level
EP1894928A1 (en) 2006-08-29 2008-03-05 PheneX Pharmaceuticals AG Heterocyclic fxr binding compounds
EP1894924A1 (en) 2006-08-29 2008-03-05 Phenex Pharmaceuticals AG Heterocyclic FXR binding compounds
EP2069177A4 (en) 2006-09-15 2012-12-05 Volvo Lastvagnar Ab Method for adapting an automatic mechanical transmission on a heavy vehicle
CL2007003035A1 (en) 2006-10-24 2008-05-16 Smithkline Beechman Corp COMPOUNDS DERIVED FROM ISOXAZOL REPLACED, FARNESOID X RECEIVER AGONISTS; PREPARATION PROCEDURE; PHARMACEUTICAL COMPOSITION THAT UNDERSTANDS IT; AND USE OF THE COMPOUND IN THE TREATMENT OF OBESITY, DIABETES MELLITUS, FIBROSIS IN ORGANS,
EP1918281A1 (en) 2006-11-02 2008-05-07 Laboratorios del Dr. Esteve S.A. Phenylamino-substituted piperidine compounds, their preparation and use as medicaments
WO2008075172A2 (en) 2006-12-19 2008-06-26 Pfizer Products Inc. Nicotinamide derivatives as inhibitors of h-pgds and their use for treating prostaglandin d2 mediated diseases
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
CN101668529A (en) 2007-03-15 2010-03-10 先灵公司 Piperazine-substituted pyridazinone derivatives useful as glucan synthase inhibitors
WO2008157270A1 (en) 2007-06-13 2008-12-24 Smithkline Beecham Corporation Farnesoid x receptor agonists
WO2009005998A1 (en) 2007-07-02 2009-01-08 Smithkline Beecham Corporation Farnesoid x receptor agonists
TW200906823A (en) 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
US8338628B2 (en) 2007-08-28 2012-12-25 City Of Hope Method of synthesizing alkylated bile acid derivatives
TW200927755A (en) 2007-09-06 2009-07-01 Genaera Corp 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
KR101239008B1 (en) 2008-03-31 2013-03-04 한양대학교 산학협력단 Bile acid derivatives and their applications
EP2110374A1 (en) 2008-04-18 2009-10-21 Merck Sante Benzofurane, benzothiophene, benzothiazol derivatives as FXR modulators
EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
CN105037476B (en) 2008-07-30 2018-06-12 英特塞普特医药品公司 TGR5 conditioning agents and its application method
CA2738453C (en) 2008-10-23 2017-07-04 Boehringer Ingelheim International Gmbh Urea derivatives of substituted nortropanes, medicaments containing such compounds and their use
AR075255A1 (en) 2009-02-12 2011-03-16 Exelixis Inc DIAZOLIC AND / OR TRIAZOLIC DERIVATIVES OF AGGRISTS OF TGR5 RECEPTORS COUPLED TO PROTEIN G, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN THE TREATMENT OF OBESITY, DIABETES AND OTHER METABOLIC DISORDERS.
US8329904B2 (en) 2009-05-12 2012-12-11 Hoffmann-La Roche Inc. Azacyclic derivatives
WO2011021645A1 (en) 2009-08-19 2011-02-24 大日本住友製薬株式会社 Bicyclic urea derivative or pharmacologically permitted salt thereof
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
ME02356B (en) 2009-11-05 2016-06-20 Glaxosmithkline Llc Benzodiazepine bromodomain inhibitor
US20130261108A1 (en) 2010-12-20 2013-10-03 Irm Llc Compositions and methods for modulating farnesoid x receptors
CN103391937A (en) 2010-12-20 2013-11-13 Irm责任有限公司 Compositions and methods for modulating farnesoid x receptors
CU24152B1 (en) 2010-12-20 2016-02-29 Irm Llc 1,2 OXAZOL-8-AZABICICLO [3,2,1] OCTANO 8 IL AS FXR MODULATORS
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
EP2739286A4 (en) 2011-08-04 2015-06-03 Lumena Pharmaceuticals Inc Bile acid recycling inhibitors for treatment of pancreatitis
WO2013037482A1 (en) 2011-09-15 2013-03-21 Phenex Pharmaceuticals Ag Farnesoid x receptor agonists for cancer treatment and prevention
US11154559B2 (en) 2011-09-29 2021-10-26 Ethicon Endo-Surgery, Inc. Methods and compositions of bile acids
MX2014013150A (en) 2012-05-01 2015-05-11 Catabasis Pharmaceuticals Inc Fatty acid conjugates of statin and fxr agonists; compositions and method of uses.
CA3028207A1 (en) 2012-06-19 2013-12-27 Intercept Pharmaceuticals, Inc. Preparation, uses and solid forms of obeticholic acid
US9079935B2 (en) 2012-08-13 2015-07-14 The Board Of Regents Of The Nevada System Of Higher Education On Behalf Of The University Of Nevada, Las Vegas Reducing risk of contracting Clostridium-difficile associated disease
WO2014036379A2 (en) * 2012-08-31 2014-03-06 Metselex Bile acids prevent or abolish progression of parkinson's and related neurodegenerative diseases
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
UA118673C2 (en) * 2013-05-14 2019-02-25 Інтерсепт Фармасутікалз, Інк. 11-hydroxyl-derivatives of bile acids and amino acid conjugates thereof as farnesoid x receptor modulators
CN105593237B (en) 2013-08-01 2019-06-04 美国卫生和人力服务部 The inhibitor of farnesoid X receptor and purposes in medicine
BR112016005507B1 (en) 2013-09-11 2023-02-07 Centre National De La Recherche Scientifique (Cnrs) USE OF A FARNESOID X RECEPTOR AGONIST (FXR)
WO2015061421A1 (en) 2013-10-22 2015-04-30 Metselex, Inc. Deuterated bile acids
SI3626725T1 (en) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Cholane derivatives for use in the treatment and/or prevention of fxr and tgr5/gpbar1 mediated diseases
MX2017005935A (en) 2014-11-06 2018-01-11 Enanta Pharm Inc 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 New 7-keto-6 beta-alkyl cholanic acid derivative in preparation of obeticholic acid and application thereof in medical field
US20160176917A1 (en) 2014-11-26 2016-06-23 Enanta Pharmaceuticals, Inc. Bile Acid Derivatives 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
CA2968404A1 (en) 2014-11-26 2016-06-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
EP3034501A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy containing FXR (NR1H4) modulating compounds
EP3034499A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Novel FXR (NR1H4) modulating compounds
WO2016097933A1 (en) 2014-12-18 2016-06-23 Novartis Ag Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases
US10246483B2 (en) 2015-02-11 2019-04-02 Enanta Pharmaceuticals, Inc. Bile acid analogs as FXR/TGR5 agonists and methods of use thereof
TWI698430B (en) 2015-02-13 2020-07-11 南北兄弟藥業投資有限公司 Tricyclic compounds and uses thereof in medicine
CA2981503C (en) 2015-03-31 2023-09-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
CN106083978A (en) 2015-04-28 2016-11-09 上海迪诺医药科技有限公司 Sulfonyl amino carbonyl derivant, its pharmaceutical composition and application
US20180148470A1 (en) 2015-04-28 2018-05-31 Jiangsu Hansoh Pharmaceutical Group Co., Ltd. Cholic acid derivative, and preparation method and medical use thereof
CN111574577A (en) 2015-04-29 2020-08-25 正大天晴药业集团股份有限公司 Chenodeoxycholic acid derivatives
CA2989167A1 (en) 2015-06-19 2016-12-22 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
JP2018522054A (en) 2015-08-07 2018-08-09 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 Process for the preparation of bile acids and their derivatives
CN105175473B (en) 2015-08-19 2018-12-21 丽珠医药集团股份有限公司 A kind of Austria shellfish cholic acid crystal form I and preparation method thereof, pharmaceutical composition and purposes
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
CN106518946A (en) 2015-09-10 2017-03-22 上海迪诺医药科技有限公司 Sulfonylurea derivative and pharmaceutical composition and application thereof
MX2018003649A (en) 2015-09-24 2018-05-11 Intercept Pharmaceuticals Inc Methods and intermediates for the preparation bile acid derivatives.
IL258359B2 (en) 2015-10-07 2023-11-01 Intercept Pharmaceuticals Inc Farnesoid x receptor modulators
CN106946867B (en) 2016-01-06 2019-11-12 广州市恒诺康医药科技有限公司 FXR receptor modulators and its preparation method and application
CN106995416A (en) 2016-01-26 2017-08-01 上海翰森生物医药科技有限公司 FXR activators and its preparation method and application
WO2017128896A1 (en) 2016-01-26 2017-08-03 江苏豪森药业集团有限公司 Fxr agonist and preparation method and use thereof
MY196292A (en) 2016-01-28 2023-03-24 Chia Tai Tianqing Pharmaceutical Group Co Ltd Steroid Derivative Fxr Agonist
CN107021957A (en) 2016-02-01 2017-08-08 山东轩竹医药科技有限公司 FXR receptor stimulating agents
CN108602811B (en) 2016-02-01 2021-11-16 轩竹生物科技有限公司 FXR receptor agonists
SI3419625T1 (en) 2016-02-22 2021-08-31 Novartis Ag Methods for using fxr agonists
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
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
US10364267B2 (en) 2016-02-23 2019-07-30 Enanta Pharmaceuticals, Inc. Deuterated bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
ES2874682T3 (en) 2016-03-11 2021-11-05 Intercept Pharmaceuticals Inc 3-deoxy derivatives and pharmaceutical compositions thereof
US10080742B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
US10080741B2 (en) 2016-04-26 2018-09-25 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as FXR agonists and methods of use thereof
WO2017189663A1 (en) 2016-04-26 2017-11-02 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
US10144729B2 (en) 2016-05-18 2018-12-04 Enanta Pharmaceuticals, Inc. Isoxazole analogs as FXR agonists and methods of use thereof
WO2017201155A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. lSOXAZOLE DERIVATIVES AS FXR AGONISTS AND METHODS OF USE THEREOF
WO2017201152A1 (en) 2016-05-18 2017-11-23 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
AR108711A1 (en) 2016-06-13 2018-09-19 Gilead Sciences Inc FXR MODULATING COMPOUNDS (NR1H4)
CA2968836A1 (en) 2016-06-13 2017-12-13 Gilead Sciences, Inc. Fxr (nr1h4) modulating compounds
JP6678779B2 (en) 2016-06-13 2020-04-08 ギリアード サイエンシーズ, インコーポレイテッド FXR (NR1H4) modulating compound
TW201808283A (en) 2016-08-05 2018-03-16 廣東東陽光藥業有限公司 Nitrogen-containing tricyclic compounds and uses thereof in medicine
EP3954684A1 (en) 2016-08-23 2022-02-16 Ardelyx, Inc. Process for the preparation of hormone receptor modulators for treating metabolic conditions and disorders
KR20190056436A (en) 2016-10-04 2019-05-24 이난타 파마슈티칼스, 인코포레이티드 Isoxazole analogs as FXR agonists and methods for their use
CN107973790A (en) 2016-10-22 2018-05-01 合帕吉恩治疗公司 Heterocyclic FXR conditioning agent
US10597391B2 (en) 2016-10-26 2020-03-24 Enanta Pharmaceuticals, Inc. Urea-containing isoxazole derivatives as FXR agonists and methods of use thereof
CN108017636A (en) 2016-11-04 2018-05-11 合帕吉恩治疗公司 Nitrogen-containing heterocycle compound as FXR conditioning agents
WO2018091540A1 (en) 2016-11-17 2018-05-24 Glaxosmithkline Biologicals Sa Zika viral antigen constructs
ES2918698T3 (en) 2016-11-29 2022-07-19 Enanta Pharm Inc Process for the preparation of bile acid derivatives of sulfonylureas
CN106588804B (en) 2016-12-09 2018-11-09 都创(上海)医药科技有限公司 A kind of preparation method of compound as Farnesoid X receptor (FXR)
CN106632294A (en) 2016-12-15 2017-05-10 宁波百纳西药业有限公司 Spiro compound and medicinal use thereof
WO2018133730A1 (en) 2017-01-20 2018-07-26 四川科伦博泰生物医药股份有限公司 Heterocyclic compound, preparation method and use therefor
CN108341822B (en) 2017-01-23 2021-04-16 广州市恒诺康医药科技有限公司 FXR receptor modulator and preparation method and application thereof
WO2018152171A1 (en) 2017-02-14 2018-08-23 Enanta Pharmaceuticals, Inc. Bile acid derivatives as fxr agonists and methods of use thereof
WO2018170173A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2018187804A1 (en) 2017-04-07 2018-10-11 Enanta Pharmaceuticals, Inc. Process for preparation of sulfonyl carbamate bile acid derivatives
WO2018190643A1 (en) 2017-04-12 2018-10-18 Il Dong Pharmaceutical Co., Ltd. An isoxazole derivatives as nuclear receptor agonists and used thereof
CA3064794A1 (en) 2017-05-26 2018-11-29 Medshine Discovery Inc. Lactam compound as fxr receptor agonist
MX2020000268A (en) 2017-07-06 2020-07-22 Xuanzhu Biopharmaceutical Co Ltd Fxr receptor agonist.
WO2019160813A1 (en) 2018-02-14 2019-08-22 Enanta Pharmaceuticals, Inc. Isoxazole derivatives as fxr agonists and methods of use thereof
CN109053751A (en) 2018-08-30 2018-12-21 成都海博锐药业有限公司 FXR regulator with spirane structure

Also Published As

Publication number Publication date
RU2712099C2 (en) 2020-01-24
LT3277286T (en) 2021-07-26
BR112017020917A2 (en) 2018-07-10
EP3277286B1 (en) 2021-04-21
HK1250622A1 (en) 2019-01-11
WO2016161003A1 (en) 2016-10-06
HUE054960T2 (en) 2021-10-28
US11958879B2 (en) 2024-04-16
IL254288B (en) 2021-04-29
MY192135A (en) 2022-07-29
AU2016242861A1 (en) 2017-09-21
JP6785788B2 (en) 2020-11-18
MX2017012558A (en) 2018-04-20
ES2886766T3 (en) 2021-12-20
EP3277286A4 (en) 2018-10-24
EP3277286A1 (en) 2018-02-07
IL254288A0 (en) 2017-10-31
US20200109164A1 (en) 2020-04-09
PL3277286T3 (en) 2021-11-08
RS62110B1 (en) 2021-08-31
CN107427527A (en) 2017-12-01
KR20170131558A (en) 2017-11-29
CN107427527B (en) 2021-01-26
RU2017134013A3 (en) 2019-08-08
PH12017501586A1 (en) 2018-02-05
US10457703B2 (en) 2019-10-29
CA2981503A1 (en) 2016-10-06
HRP20211066T1 (en) 2021-10-29
US11040998B2 (en) 2021-06-22
CA2981503C (en) 2023-09-19
ZA202102769B (en) 2022-04-28
NZ735126A (en) 2022-10-28
DK3277286T3 (en) 2021-07-05
JP2018510176A (en) 2018-04-12
CY1124404T1 (en) 2022-07-22
ZA201707212B (en) 2021-08-25
PH12017501586B1 (en) 2018-02-05
US20220402966A1 (en) 2022-12-22
RU2017134013A (en) 2019-04-30
PT3277286T (en) 2021-07-01
SG11201707263XA (en) 2017-10-30
US20160289262A1 (en) 2016-10-06
SI3277286T1 (en) 2021-09-30
AU2016242861B2 (en) 2020-08-20

Similar Documents

Publication Publication Date Title
ZA202102769B (en) Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
ZA201908293B (en) Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
HK1244708A1 (en) Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
HK1245100A1 (en) Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
HK1243930A1 (en) Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
ZA201707981B (en) Compositions of obeticholic acid and methods of use
IL252596A0 (en) Azabicyclooctane derivatives as fxr agonists for use in the treatment of liver and gastrointestinal diseases
IL247529A0 (en) Lipoic acid choline ester compositions and methods of use
SG11201509738RA (en) Methods of treatment and compositions with xanthine oxidase inhibitors
GB201810520D0 (en) Branched acid emulsifer compositions and methods of use
HK1232209A1 (en) Method for the preparation of (s)-2-acetyloxypropionic acid and derivatives thereof (s)-2-