BR112021020681A2 - Agonista de molécula pequena de fxr e método de preparação para o mesmo e uso do mesmo - Google Patents

Agonista de molécula pequena de fxr e método de preparação para o mesmo e uso do mesmo

Info

Publication number
BR112021020681A2
BR112021020681A2 BR112021020681A BR112021020681A BR112021020681A2 BR 112021020681 A2 BR112021020681 A2 BR 112021020681A2 BR 112021020681 A BR112021020681 A BR 112021020681A BR 112021020681 A BR112021020681 A BR 112021020681A BR 112021020681 A2 BR112021020681 A2 BR 112021020681A2
Authority
BR
Brazil
Prior art keywords
small molecule
preparation therefor
fxr agonist
fxr
molecule fxr
Prior art date
Application number
BR112021020681A
Other languages
English (en)
Inventor
Dandan Sun
Erli You
Huaqiang Xu
Jia Li
Jingjing Shi
Lixin Gao
Mingliang Liu
Qian Tan
Rongrong Xie
Yi Zang
Original Assignee
Shanghai Inst Materia Medica Cas
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
Priority claimed from CN201910969552.6A external-priority patent/CN111825667B/zh
Application filed by Shanghai Inst Materia Medica Cas filed Critical Shanghai Inst Materia Medica Cas
Publication of BR112021020681A2 publication Critical patent/BR112021020681A2/pt

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Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/439—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 the ring forming part of a bridged ring system, e.g. quinuclidine
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • 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
    • 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
    • C07D451/04—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 with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

agonista de molécula pequena de fxr e método de preparação para o mesmo e uso do mesmo. um agonista de molécula pequena de fxr e um método de preparação para o mesmo e um uso do mesmo, tendo uma estrutura conforme mostrada na fórmula (i). o composto representado pela fórmula (i) tem atividade agonística de fxr e é capaz de preparar fármacos para tratamento de doenças relacionadas a fxr.
BR112021020681A 2019-04-19 2020-04-20 Agonista de molécula pequena de fxr e método de preparação para o mesmo e uso do mesmo BR112021020681A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201910319757 2019-04-19
CN201910969552.6A CN111825667B (zh) 2019-04-19 2019-10-12 Fxr小分子激动剂及其制备方法和用途
PCT/CN2020/085713 WO2020211872A1 (zh) 2019-04-19 2020-04-20 Fxr小分子激动剂及其制备方法和用途

Publications (1)

Publication Number Publication Date
BR112021020681A2 true BR112021020681A2 (pt) 2021-12-07

Family

ID=72837054

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112021020681A BR112021020681A2 (pt) 2019-04-19 2020-04-20 Agonista de molécula pequena de fxr e método de preparação para o mesmo e uso do mesmo

Country Status (9)

Country Link
US (1) US20220213083A1 (pt)
EP (1) EP3957640A4 (pt)
JP (1) JP7398605B2 (pt)
KR (1) KR20220003558A (pt)
BR (1) BR112021020681A2 (pt)
IL (1) IL287159A (pt)
MX (1) MX2021012750A (pt)
SG (1) SG11202111502XA (pt)
WO (1) WO2020211872A1 (pt)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA3159163A1 (en) 2020-01-15 2021-07-22 Raphael Darteil Use of fxr agonists for treating an infection by hepatitis d virus
CN114315830A (zh) * 2020-09-30 2022-04-12 中国科学院上海药物研究所 Fxr小分子激动剂及其制备方法和用途
CN116887827A (zh) * 2020-12-30 2023-10-13 拓臻制药公司 用于调节fxr的化合物和方法
MX2023008365A (es) 2021-01-14 2023-10-04 Enyo Pharma Efecto sinérgico de un agonista de fxr e ifn para el tratamiento de infección por hbv.
JP2024517181A (ja) 2021-04-28 2024-04-19 ウエヌイグレックオ・ファーマ 組合せ治療としてｆｘｒアゴニストを使用するｔｌｒ３アゴニストの効果の強い増強
JP7450951B2 (ja) * 2022-02-17 2024-03-18 カスケード ファーマシューティカルズ、インコーポレーテッド 新型ｆｘｒ小分子作動剤の製造およびその使用
EP4245365A1 (en) * 2022-03-16 2023-09-20 Cascade Pharmaceuticals, Inc. A fxr small molecule agonist, the preparation and use thereof
US20230295141A1 (en) * 2022-03-17 2023-09-21 Cascade Pharmaceuticals, Inc. Fxr small molecule agonist, the preparation and use thereof

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012087521A1 (en) 2010-12-20 2012-06-28 Irm Llc Compositions and methods for modulating farnesoid x receptors
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
JP2014500318A (ja) 2010-12-20 2014-01-09 アイアールエム・リミテッド・ライアビリティ・カンパニー ファルネソイドｘ受容体を調節するための組成物および方法
EP3034501A1 (en) 2014-12-17 2016-06-22 Gilead Sciences, Inc. Hydroxy containing FXR (NR1H4) modulating compounds
MA55632A (fr) * 2016-08-23 2022-02-16 Ardelyx Inc Procédé de preparation de modulateurs du récepteur hormonal pour le traitement d'états et de troubles métaboliques
CN107973790A (zh) * 2016-10-22 2018-05-01 合帕吉恩治疗公司 杂环fxr调节剂
CN108017636A (zh) * 2016-11-04 2018-05-11 合帕吉恩治疗公司 作为fxr调节剂的含氮杂环化合物

Also Published As

Publication number Publication date
EP3957640A4 (en) 2022-12-14
JP7398605B2 (ja) 2023-12-15
SG11202111502XA (en) 2021-11-29
WO2020211872A1 (zh) 2020-10-22
KR20220003558A (ko) 2022-01-10
IL287159A (en) 2021-12-01
US20220213083A1 (en) 2022-07-07
EP3957640A1 (en) 2022-02-23
JP2022529296A (ja) 2022-06-20
MX2021012750A (es) 2021-11-18

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Owner name: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES (CN) ; VAN ANDEL RESEARCH INSTITUTE. (US)

B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]