AU2018208160B2 - HDAC6 selective inhibitors, preparation method therefor, and application thereof - Google Patents

HDAC6 selective inhibitors, preparation method therefor, and application thereof Download PDF

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Publication number
AU2018208160B2
AU2018208160B2 AU2018208160A AU2018208160A AU2018208160B2 AU 2018208160 B2 AU2018208160 B2 AU 2018208160B2 AU 2018208160 A AU2018208160 A AU 2018208160A AU 2018208160 A AU2018208160 A AU 2018208160A AU 2018208160 B2 AU2018208160 B2 AU 2018208160B2
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Australia
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compound
isomer
acceptable salt
pharmaceutically acceptable
group
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AU2018208160A1 (en
Inventor
Shuhui Chen
Qiang Guo
Yonggang LIAO
Bin Liu
Changqing WEI
Hao Wu
Yao XIAO
Guifen Zhang
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CStone Pharmaceuticals Shanghai Co Ltd
CStone Pharmaceuticals Suzhou Co Ltd
CStone Pharmaceuticals
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CStone Pharmaceuticals Shanghai Co Ltd
CStone Pharmaceuticals Suzhou Co Ltd
CStone Pharmaceuticals
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/10—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D307/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • 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
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/341—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide not condensed with another ring, e.g. ranitidine, furosemide, bufetolol, muscarine
    • 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/443—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
    • 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
    • A61K31/69—Boron compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/04—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D307/06—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/04—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Furan Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
AU2018208160A 2017-01-10 2018-01-10 HDAC6 selective inhibitors, preparation method therefor, and application thereof Active AU2018208160B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710017287 2017-01-10
CN201710017287.2 2017-01-10
PCT/CN2018/072088 WO2018130155A1 (zh) 2017-01-10 2018-01-10 Hdac6选择性抑制剂及其制备方法和应用

Publications (2)

Publication Number Publication Date
AU2018208160A1 AU2018208160A1 (en) 2019-08-15
AU2018208160B2 true AU2018208160B2 (en) 2021-03-04

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AU2018208160A Active AU2018208160B2 (en) 2017-01-10 2018-01-10 HDAC6 selective inhibitors, preparation method therefor, and application thereof

Country Status (13)

Country Link
US (1) US10745389B2 (enExample)
EP (1) EP3569592B8 (enExample)
JP (1) JP7237010B2 (enExample)
KR (1) KR102549606B1 (enExample)
CN (1) CN110382463B (enExample)
AU (1) AU2018208160B2 (enExample)
CA (1) CA3049834A1 (enExample)
ES (1) ES2927352T3 (enExample)
IL (1) IL267968B (enExample)
MX (1) MX394624B (enExample)
SA (1) SA519402090B1 (enExample)
SG (1) SG11201906361YA (enExample)
WO (1) WO2018130155A1 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP7348214B2 (ja) 2018-07-04 2023-09-20 シーストーン・ファーマスーティカルズ・（スージョウ）・カンパニー・リミテッド Ｈｄａｃ６選択的阻害剤の結晶形及びその使用
US12485174B2 (en) 2019-06-27 2025-12-02 The George Washington University, A Congressionally Chartered Not-For-Profit Corporation HDAC6-activated macrophages, compositions, and uses thereof
WO2021110121A1 (zh) * 2019-12-05 2021-06-10 基石药业（苏州）有限公司 Hdac6选择性抑制剂及其组合疗法
BR112022011917A2 (pt) 2019-12-20 2022-09-06 Tenaya Therapeutics Inc Fluoroalquil-oxadiazois e seus usos
EP4326263A1 (en) 2021-04-23 2024-02-28 Tenaya Therapeutics, Inc. Hdac6 inhibitors for use in the treatment of dilated cardiomyopathy
MX2023012875A (es) 2021-05-04 2024-01-12 Tenaya Therapeutics Inc Inhibidores 2-fluoro alquil-l,3,4-oxadiazol-5-il-tiazol de hdac6 para su uso en el tratamiento de enfermedades metabólicas y hfpef.
WO2024123700A1 (en) * 2022-12-05 2024-06-13 The General Hospital Corporation Histone deacetylase inhibitors
WO2025215092A1 (en) 2024-04-10 2025-10-16 Institut National de la Santé et de la Recherche Médicale Selective hdac6 inhibitors for use in the treatment of myotonic dystrophy type 1

Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2011106632A1 (en) * 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof

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US20040091951A1 (en) * 2002-02-07 2004-05-13 Axys Pharmaceuticals, Inc. Assay for measuring acetylation or deacetylation activity of an enzyme
CN101641338A (zh) * 2006-09-11 2010-02-03 柯瑞斯公司 作为抗增殖制剂的多功能小分子
MX2011001090A (es) * 2008-07-28 2011-03-15 Gilead Sciences Inc Compuestos de inhibidor de desacetilasa de histona de cicloalquilideno y heterocicloalquilideno.
EP3067346A1 (en) * 2010-11-16 2016-09-14 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as protein deacetylase inhibitors and methods of use thereof
US8404738B2 (en) * 2011-01-21 2013-03-26 Hoffmann-La Roche Inc. 4-amino-N-hydroxy-benzamides for the treatment of cancer
EP2826769A1 (en) * 2013-07-18 2015-01-21 Institut de Recherche pour le Développement ( IRD) Compounds for the treatment and/or prevention of parasitic diseases and method of production thereof
WO2015100363A1 (en) * 2013-12-23 2015-07-02 The Trustees Of Columbia University In The City Of New York Selective hdac6 inhibitors
US9464073B2 (en) * 2014-02-26 2016-10-11 Acetylon Pharmaceuticals, Inc. Pyrimidine hydroxy amide compounds as HDAC6 selective inhibitors

Patent Citations (1)

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Publication number Priority date Publication date Assignee Title
WO2011106632A1 (en) * 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof

Also Published As

Publication number Publication date
JP2020505440A (ja) 2020-02-20
AU2018208160A1 (en) 2019-08-15
JP7237010B2 (ja) 2023-03-10
KR102549606B1 (ko) 2023-06-29
SG11201906361YA (en) 2019-08-27
EP3569592B8 (en) 2022-11-30
CN110382463A (zh) 2019-10-25
RU2019124962A (ru) 2021-02-15
ES2927352T3 (es) 2022-11-04
US10745389B2 (en) 2020-08-18
CA3049834A1 (en) 2018-07-19
US20190375735A1 (en) 2019-12-12
KR20190103286A (ko) 2019-09-04
EP3569592B1 (en) 2022-08-24
MX2019008181A (es) 2019-12-09
CN110382463B (zh) 2022-11-04
RU2019124962A3 (enExample) 2021-05-11
EP3569592A1 (en) 2019-11-20
SA519402090B1 (ar) 2022-05-30
MX394624B (es) 2025-03-24
BR112019014152A2 (pt) 2020-03-31
IL267968A (en) 2019-10-31
WO2018130155A1 (zh) 2018-07-19
EP3569592A4 (en) 2020-08-12
IL267968B (en) 2022-06-01
ES2927352T8 (es) 2022-11-18

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