NZ716568A - Inhibitors of the farnesoid x receptor and uses in medicine - Google Patents

Inhibitors of the farnesoid x receptor and uses in medicine Download PDF

Info

Publication number
NZ716568A
NZ716568A NZ716568A NZ71656814A NZ716568A NZ 716568 A NZ716568 A NZ 716568A NZ 716568 A NZ716568 A NZ 716568A NZ 71656814 A NZ71656814 A NZ 71656814A NZ 716568 A NZ716568 A NZ 716568A
Authority
NZ
New Zealand
Prior art keywords
mice
mca
weeks
gly
treated
Prior art date
Application number
NZ716568A
Other languages
English (en)
Inventor
Frank J Gonzalez
Changtao Jiang
cen Xie
Andrew D Patterson
Fei Li
James B Mitchell
Shantu Amin
Dhimant Desai
Original Assignee
Us Health
Penn State Res Found
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 Us Health, Penn State Res Found filed Critical Us Health
Publication of NZ716568A publication Critical patent/NZ716568A/en

Links

Classifications

    • 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
    • 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
    • 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
    • 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
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • C07J41/0066Normal 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 a carbon atom forming part of an amide group

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
NZ716568A 2013-08-01 2014-08-01 Inhibitors of the farnesoid x receptor and uses in medicine NZ716568A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361861109P 2013-08-01 2013-08-01
US201462004436P 2014-05-29 2014-05-29
PCT/US2014/049460 WO2015017813A2 (en) 2013-08-01 2014-08-01 Inhibitors of the farnesoid x receptor and uses in medicine

Publications (1)

Publication Number Publication Date
NZ716568A true NZ716568A (en) 2021-07-30

Family

ID=51358096

Family Applications (1)

Application Number Title Priority Date Filing Date
NZ716568A NZ716568A (en) 2013-08-01 2014-08-01 Inhibitors of the farnesoid x receptor and uses in medicine

Country Status (9)

Country Link
US (2) US9540415B2 (https=)
EP (1) EP3027637B1 (https=)
JP (1) JP6556129B2 (https=)
CN (2) CN105593237B (https=)
AU (1) AU2014296023B2 (https=)
BR (1) BR112016002268B1 (https=)
CA (1) CA2920017C (https=)
NZ (1) NZ716568A (https=)
WO (1) WO2015017813A2 (https=)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
SMT202000070T1 (it) * 2014-05-29 2020-03-13 Bar Pharmaceuticals S R L Derivati del colano per l'uso del trattamento e/o la prevenzione di malattie mediate da fxr e tgr5/gpbar1
SG11201703717SA (en) 2014-11-06 2017-06-29 Enanta Pharm Inc Bile acid analogs an fxr/tgr5 agonists and methods of use thereof
EP3223823A4 (en) 2014-11-26 2018-10-17 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
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
EP3256134A4 (en) 2015-02-11 2018-10-03 Enanta Pharmaceuticals, Inc. Bile acid analogs as fxr/tgr5 agonists and methods of use thereof
WO2016161003A1 (en) 2015-03-31 2016-10-06 Enanta Phamraceuticals, Inc. Bile acid derivatives as fxr/tgr5 agonists and methods of use thereof
JP2018519246A (ja) * 2015-04-28 2018-07-19 ジエンス ハンセン ファーマセウティカル グループ カンパニー リミテッド コール酸誘導体、及びその製造方法及び医薬用途
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
CA3252823A1 (en) 2016-06-13 2025-02-25 Gilead Sciences, Inc. Substituted tert-butyl-3-(2-chloro-phenyl)-3-hydroxyazetidine-1-carboxylate compounds
MX385718B (es) 2016-06-13 2025-03-18 Gilead Sciences Inc Compuestos moduladores de fxr (nr1h4).
IT201600068742A1 (it) * 2016-07-01 2018-01-01 Bar Pharmaceuticals Soc A Responsabilita Limitata Derivati dell'acido iodesossicolico e loro uso
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
CN110121347A (zh) 2016-11-29 2019-08-13 英安塔制药有限公司 制备磺酰脲胆汁酸衍生物的方法
US10472386B2 (en) 2017-02-14 2019-11-12 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR agonists and methods of use thereof
PT3600309T (pt) 2017-03-28 2022-10-03 Gilead Sciences Inc Combinações terapêuticas para o tratamento de doenças hepáticas
BR112019020780A2 (pt) 2017-04-07 2020-04-28 Enanta Pharm Inc processo para preparação de derivados de ácido biliar de carbamato de sulfonila
US11028111B2 (en) 2017-12-19 2021-06-08 Xi' An Biocare Pharma Ltd. Compound for treating metabolic diseases and preparation method and use thereof
IT201800005598A1 (it) 2018-05-22 2019-11-22 Ossadiazoli come antagonisti del recettore fxr
EP3911647B1 (en) 2019-01-15 2023-12-13 Gilead Sciences, Inc. Isoxazole compound as fxr agonist and pharmaceutical compositions comprising same
CA3233305A1 (en) 2019-02-19 2020-08-27 Gilead Sciences, Inc. Solid forms of fxr agonists
CN112409435B (zh) * 2019-08-23 2023-07-18 深圳云合医药科技合伙企业(有限合伙) 胆汁酸衍生物及其组合物和应用
US20220378766A1 (en) * 2021-05-25 2022-12-01 Louis Habash Modulating expression level of a gene encoding an uncoupling protein by treating a human subject with a nitroxide
US20230128120A1 (en) * 2021-10-21 2023-04-27 University Of Washington Omega muricholic acid as a pregnane x receptor ligand for treating hepato-intestinal diseases

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4235871A (en) 1978-02-24 1980-11-25 Papahadjopoulos Demetrios P Method of encapsulating biologically active materials in lipid vesicles
US4501728A (en) 1983-01-06 1985-02-26 Technology Unlimited, Inc. Masking of liposomes from RES recognition
US5019369A (en) 1984-10-22 1991-05-28 Vestar, Inc. Method of targeting tumors in humans
WO1987002367A2 (en) 1985-10-18 1987-04-23 The Upjohn Company Cyclic hydrocarbons with an aminoalkyl sidechain
US4837028A (en) 1986-12-24 1989-06-06 Liposome Technology, Inc. Liposomes with enhanced circulation time
IT1222395B (it) * 1987-07-30 1990-09-05 Pierrel Spa Composizione farmaceutica per somministrazione intranasale comprendente l'ormone ghrh,un agonista colinergico e/o un sale biliare
IT1219733B (it) * 1988-06-28 1990-05-24 Istituto Chemioterapico Di Lod Derivato dell' acido ursodesossicolico
JPH0637392B2 (ja) * 1988-11-25 1994-05-18 健二 片桐 胆汁うっ滞改善剤
IT1229570B (it) 1989-04-17 1991-09-04 Giuliani Spa Derivati fluorurati di acidi biliari, loro preparazione e composizioni farmaceutiche che li contengono.
IT1264131B1 (it) * 1993-04-16 1996-09-16 D R Drug Research Srl Derivato dell'acido iodesossicolico
US6551623B1 (en) * 1993-09-09 2003-04-22 Lorus Therapeutics Inc. Immunomodulating compositions from bile
GB9320597D0 (en) * 1993-10-06 1993-11-24 Proteus Molecular Design Improvements in and realting to vaccines
IT1299270B1 (it) * 1998-05-15 2000-02-29 Moreno Paolini Acidi biliari come induttori del sistema citocromo p450-dipendente, in particolare ad attivita' anticolestatica
DE69940958D1 (de) 1998-12-23 2009-07-16 Glaxo Group Ltd Bestimmungsmethode fur liganden der nuklearen rezeptoren
US20020132223A1 (en) * 1999-03-26 2002-09-19 City Of Hope Methods for modulating activity of the FXR nuclear receptor
WO2002094865A1 (en) * 2001-05-24 2002-11-28 Smithkline Beecham Corporation Nonhuman pregnane x receptor sequences for use in comparative pharmacology
US7595311B2 (en) 2002-05-24 2009-09-29 Exelixis, Inc. Azepinoindole derivatives as pharmaceutical agents
JP2008509912A (ja) 2004-08-10 2008-04-03 エグゼリクシス, インコーポレイテッド 医薬品としての複素環化合物
CN101395170A (zh) * 2006-02-14 2009-03-25 英特塞普特药品公司 用于预防或治疗fxr介导的疾病或状态的作为fxr配体的胆汁酸衍生物
US7932244B2 (en) * 2006-06-27 2011-04-26 Intercept Pharmaceuticals, Inc. Bile acid derivatives as FXR ligands for the prevention or treatment of FXR-mediated diseases or conditions
WO2011022838A1 (en) 2009-08-25 2011-03-03 British Columbia Cancer Agency Branch Polyhydroxylated bile acids for treatment of biliary disorders
US20110071100A1 (en) * 2008-05-05 2011-03-24 Tiltan Pharma Ltd. Sulfobetaines for cancer, obesity, macular degeneration, neurodegenerative diseases
WO2010014836A2 (en) 2008-07-30 2010-02-04 Intercept Pharmaceuticals, Inc. Tgr5 modulators and methods of use thereof
CN101891791B (zh) * 2009-05-22 2012-10-03 中国科学院上海应用物理研究所 一种标记胆汁酸衍生物及其参照化合物、制备方法和应用

Also Published As

Publication number Publication date
CN110437297B (zh) 2021-12-21
JP2016527277A (ja) 2016-09-08
JP6556129B2 (ja) 2019-08-07
US20170152283A1 (en) 2017-06-01
CN105593237B (zh) 2019-06-04
CN105593237A (zh) 2016-05-18
WO2015017813A3 (en) 2015-04-02
US20160159851A1 (en) 2016-06-09
WO2015017813A2 (en) 2015-02-05
BR112016002268B1 (pt) 2022-11-01
US9540415B2 (en) 2017-01-10
CN110437297A (zh) 2019-11-12
EP3027637A2 (en) 2016-06-08
US10233209B2 (en) 2019-03-19
BR112016002268A2 (pt) 2017-08-01
EP3027637B1 (en) 2019-10-09
CN110437297B9 (zh) 2022-01-11
CA2920017A1 (en) 2015-02-05
CA2920017C (en) 2021-11-23
AU2014296023A1 (en) 2016-02-25
AU2014296023B2 (en) 2020-02-06

Similar Documents

Publication Publication Date Title
NZ716568A (en) Inhibitors of the farnesoid x receptor and uses in medicine
Ushiroda et al. Green tea polyphenol (epigallocatechin-3-gallate) improves gut dysbiosis and serum bile acids dysregulation in high-fat diet-fed mice
US10844089B2 (en) Nuclear sulfated oxysterol, potent regulator of lipid homeostasis, for therapy of hypercholesterolemia, hypertriglycerides, fatty liver diseases, and atherosclerosis
Hui et al. Capsaicin improves glucose homeostasis by enhancing glucagon‐like peptide‐1 secretion through the regulation of bile acid metabolism via the remodeling of the gut microbiota in male mice
Qi et al. Bile acid signaling in lipid metabolism: metabolomic and lipidomic analysis of lipid and bile acid markers linked to anti-obesity and anti-diabetes in mice
Marschall et al. Fxr−/− mice adapt to biliary obstruction by enhanced phase I detoxification and renal elimination of bile acids
Jiang et al. Intestinal farnesoid X receptor signaling promotes nonalcoholic fatty liver disease
Jiang et al. Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction
CN108883305B (zh) 3-脱氧衍生物及其药物组合物
US8399441B2 (en) Nuclear sulfated oxysterol, potent regulator of lipid homeostasis, for therapy of hypercholesterolemia, hypertriglycerides, fatty liver diseases, and atherosclerosis
EA020140B1 (ru) Модуляторы tgr5 и способы их применения
Xin et al. Stigmasterol protects against steatohepatitis induced by high-fat and high-cholesterol diet in mice by enhancing the alternative bile acid synthesis pathway
Chung et al. A synthesis of a rationally designed inhibitor of cytochrome P450 8B1, a therapeutic target to treat obesity
Stefela et al. The farnesoid X receptor (FXR) antagonist 7β-isopropylchenodeoxycholic acid improves glucose metabolism in mice on a Western diet
Li et al. Increase in bile acids after sleeve gastrectomy improves metabolism by activating GPBAR1 to increase cAMP in mice with nonalcoholic fatty liver disease
EP2603096A1 (en) Method for treating fatty liver diseases, in particular non-alcoholic steatohepatitis.
Chen et al. Farnesoid X receptor is inhibited after ileum transposition in diabetic rats: its hypoglycemic effect
Dohnalová et al. Pregnane X receptor antagonist MI-891 reduces hepatic triglycerides in PXR-CAR-CYP3A4/3A7-humanized mice
LA SALUTE DOTTORATO IN SCIENZA DEL FARMACO XXXIII CICLO 2018/2020
Auclair Mechanisms of Individual Variation in Glucuronidation, Sulfonation, and Amidation: Bisphenol A and Bile Acids
Jiang et al. BissonWilliamEnvironMoleToxIntestineSelectiveFarnesoid. pdf

Legal Events

Date Code Title Description
PSEA Patent sealed
RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 01 AUG 2023 BY COMPUTER PACKAGES INC

Effective date: 20220717

RENW Renewal (renewal fees accepted)

Free format text: PATENT RENEWED FOR 1 YEAR UNTIL 01 AUG 2024 BY COMPUTER PACKAGES INC

Effective date: 20230717

LAPS Patent lapsed