CN111356458A - 用于治疗肝疾病的fxr激动剂 - Google Patents

用于治疗肝疾病的fxr激动剂 Download PDF

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Publication number
CN111356458A
CN111356458A CN201880074342.4A CN201880074342A CN111356458A CN 111356458 A CN111356458 A CN 111356458A CN 201880074342 A CN201880074342 A CN 201880074342A CN 111356458 A CN111356458 A CN 111356458A
Authority
CN
China
Prior art keywords
tropinfexol
nash
dose
liver
treatment
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201880074342.4A
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English (en)
Chinese (zh)
Inventor
M·巴德曼
C·布拉斯
B·拉菲特
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CN111356458A publication Critical patent/CN111356458A/zh
Pending legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
    • A61K47/549—Sugars, nucleosides, nucleotides or nucleic acids
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Emergency Medicine (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201880074342.4A 2017-11-30 2018-11-28 用于治疗肝疾病的fxr激动剂 Pending CN111356458A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762593084P 2017-11-30 2017-11-30
US62/593,084 2017-11-30
PCT/IB2018/059383 WO2019106550A1 (en) 2017-11-30 2018-11-28 Fxr agonists for the treatment of liver diseases

Publications (1)

Publication Number Publication Date
CN111356458A true CN111356458A (zh) 2020-06-30

Family

ID=64959384

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201880074342.4A Pending CN111356458A (zh) 2017-11-30 2018-11-28 用于治疗肝疾病的fxr激动剂

Country Status (12)

Country Link
US (2) US20210361638A1 (https=)
EP (1) EP3716977A1 (https=)
JP (1) JP2021504370A (https=)
KR (1) KR20200094175A (https=)
CN (1) CN111356458A (https=)
AU (1) AU2018376904B2 (https=)
CA (1) CA3081656A1 (https=)
IL (1) IL274747A (https=)
MX (1) MX2020005557A (https=)
RU (1) RU2020121222A (https=)
TW (1) TW201936189A (https=)
WO (1) WO2019106550A1 (https=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2021014349A1 (en) * 2019-07-23 2021-01-28 Novartis Ag Treatment comprising fxr agonists
WO2021064575A1 (en) * 2019-09-30 2021-04-08 Novartis Ag Treatment comprising the use of fxr agonists

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005089316A2 (en) * 2004-03-12 2005-09-29 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
WO2017145041A1 (en) * 2016-02-22 2017-08-31 Novartis Ag Methods for using fxr agonists

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
ES2902404T3 (es) * 2016-02-22 2022-03-28 Novartis Ag Métodos para utilizar agonistas de fxr.
ES2862194T3 (es) * 2016-02-22 2021-10-07 Novartis Ag Métodos para usar agonistas del FXR
AR114930A1 (es) * 2017-09-12 2020-11-11 Novartis Ag Composición farmacéutica

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005089316A2 (en) * 2004-03-12 2005-09-29 Intercept Pharmaceuticals, Inc. Treatment of fibrosis using fxr ligands
WO2017145041A1 (en) * 2016-02-22 2017-08-31 Novartis Ag Methods for using fxr agonists

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
B. LAFFITTE1 等: "LJN452 (tropifexor) attenuates steatohepatitis, inflammation, and fibrosis in dietary mouse models of nonalcoholic steatohepatitis", 《JOURNAL OF HEPATOLOGY》 *
DR. ARUN J. SANYAL 等: "Tropifexor (TXR), an FXR Agonist for the Treatment of Nash - Interim Results from First Two Parts of Phase 2b Study Flight-FXR", 《WILEY INTERSCIENCE》 *
WIEST REINER 等: "Targeting the gut-liver axis in liver disease", 《JOURNAL OF HEPATOLOGY》 *

Also Published As

Publication number Publication date
US20190161483A1 (en) 2019-05-30
AU2018376904A1 (en) 2020-05-21
RU2020121222A3 (https=) 2022-04-19
TW201936189A (zh) 2019-09-16
JP2021504370A (ja) 2021-02-15
RU2020121222A (ru) 2021-12-30
WO2019106550A1 (en) 2019-06-06
EP3716977A1 (en) 2020-10-07
MX2020005557A (es) 2020-08-20
KR20200094175A (ko) 2020-08-06
CA3081656A1 (en) 2019-06-06
US20210361638A1 (en) 2021-11-25
AU2018376904B2 (en) 2021-07-22
IL274747A (en) 2020-07-30

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