AU2014296023B2 - Inhibitors of the farnesoid X receptor and uses in medicine - Google Patents

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

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Publication number
AU2014296023B2
AU2014296023B2 AU2014296023A AU2014296023A AU2014296023B2 AU 2014296023 B2 AU2014296023 B2 AU 2014296023B2 AU 2014296023 A AU2014296023 A AU 2014296023A AU 2014296023 A AU2014296023 A AU 2014296023A AU 2014296023 B2 AU2014296023 B2 AU 2014296023B2
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Australia
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mice
fxr
mca
weeks
gly
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AU2014296023A
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AU2014296023A1 (en
Inventor
Shantu Amin
Dhimant Desai
Frank J. Gonzalez
Changtao Jiang
Fei Li
James B. Mitchell
Andrew D. PATTERSON
Cen XIE
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Penn State Research Foundation
United States Department of Health and Human Services
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Penn State Research Foundation
Government of the United States of America
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    • 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
    • C07J41/0061—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 one of the carbon atoms being part of an amide group
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/48—Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50—Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J31/00—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006—Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003
    • 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
    • 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
    • C07J41/0066—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 a carbon atom forming part of an amide group
    • 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

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Hematology (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)
AU2014296023A 2013-08-01 2014-08-01 Inhibitors of the farnesoid X receptor and uses in medicine Ceased AU2014296023B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361861109P 2013-08-01 2013-08-01
US61/861,109 2013-08-01
US201462004436P 2014-05-29 2014-05-29
US62/004,436 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 (2)

Publication Number Publication Date
AU2014296023A1 AU2014296023A1 (en) 2016-02-25
AU2014296023B2 true AU2014296023B2 (en) 2020-02-06

Family

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AU2014296023A Ceased AU2014296023B2 (en) 2013-08-01 2014-08-01 Inhibitors of the farnesoid X receptor and uses in medicine

Country Status (9)

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

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SI3626725T1 (sl) 2014-05-29 2023-04-28 Bar Pharmaceuticals S.R.L. Derivati holana za uporabo pri zdravljenju in/ali preprečevanju bolezni, posredovanih s FXR in TGR5/GPBAR1
BR112017009657A2 (pt) 2014-11-06 2018-01-23 Enanta Pharmaceuticals, Inc análogos de ácidos biliares como agonistas de fxr/tgr5 e métodos de uso dos mesmos
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
RU2017121457A (ru) 2014-11-26 2018-12-26 Энанта Фармасьютикалс, Инк. Аналоги желчной кислоты в качестве агонистов fxr/tgr5 и способы их применения
AU2016219266A1 (en) 2015-02-11 2017-08-10 Enanta Pharmaceuticals, Inc. Bile acid analogs as FXR/TGR5 agonists and methods of use thereof
RU2712099C2 (ru) 2015-03-31 2020-01-24 Энанта Фармасьютикалс, Инк. Производные желчных кислот в качестве агонистов fxr/tgr5 и способы их применения
WO2016173397A1 (zh) * 2015-04-28 2016-11-03 上海翰森生物医药科技有限公司 胆酸衍生物及其制备方法和医药用途
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
NZ748641A (en) 2016-06-13 2020-04-24 Gilead Sciences Inc Fxr (nr1h4) modulating compounds
CA2968836C (en) 2016-06-13 2025-09-02 Gilead Sciences, Inc. FXR MODULATING COMPOUNDS (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
AU2017368069B2 (en) 2016-11-29 2021-07-08 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
ES2982801T3 (es) 2017-03-28 2024-10-17 Gilead Sciences Inc Combinaciones terapéuticas para el tratamiento de las enfermedades hepáticas
MX388300B (es) 2017-04-07 2025-03-19 Enanta Pharm Inc Proceso para la preparación de derivados de ácidos biliares de sulfonil carbamato
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
KR102692309B1 (ko) 2019-01-15 2024-08-07 길리애드 사이언시즈, 인코포레이티드 Fxr (nr1h4) 조정 화합물
WO2020172075A1 (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

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Also Published As

Publication number Publication date
CN110437297B (zh) 2021-12-21
CA2920017C (en) 2021-11-23
WO2015017813A2 (en) 2015-02-05
CN110437297A (zh) 2019-11-12
WO2015017813A3 (en) 2015-04-02
JP2016527277A (ja) 2016-09-08
CN110437297B9 (zh) 2022-01-11
NZ716568A (en) 2021-07-30
US10233209B2 (en) 2019-03-19
US9540415B2 (en) 2017-01-10
US20160159851A1 (en) 2016-06-09
CN105593237B (zh) 2019-06-04
US20170152283A1 (en) 2017-06-01
JP6556129B2 (ja) 2019-08-07
BR112016002268B1 (pt) 2022-11-01
EP3027637A2 (en) 2016-06-08
EP3027637B1 (en) 2019-10-09
AU2014296023A1 (en) 2016-02-25
CN105593237A (zh) 2016-05-18
CA2920017A1 (en) 2015-02-05
BR112016002268A2 (pt) 2017-08-01

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