JP7237010B2 - Ｈｄａｃ６選択的阻害剤およびその製造方法と使用 - Google Patents

Ｈｄａｃ６選択的阻害剤およびその製造方法と使用 Download PDF

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JP7237010B2
JP7237010B2 JP2019557669A JP2019557669A JP7237010B2 JP 7237010 B2 JP7237010 B2 JP 7237010B2 JP 2019557669 A JP2019557669 A JP 2019557669A JP 2019557669 A JP2019557669 A JP 2019557669A JP 7237010 B2 JP7237010 B2 JP 7237010B2
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group
compound
mmol
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pharmaceutically acceptable
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JP2020505440A (ja
JP2020505440A5 (enExample
Inventor
▲ハオ▼ ▲呉▼
昌青 ▲韋▼
▲強▼ 郭
▲貴▼芬 ▲張▼
斌 ▲劉▼
勇▲剛▼ 廖
瑶 肖
曙▲輝▼ ▲陳▼
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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
    • 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
    • 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

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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)
JP2019557669A 2017-01-10 2018-01-10 Ｈｄａｃ６選択的阻害剤およびその製造方法と使用 Active JP7237010B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CN201710017287.2 2017-01-10
CN201710017287 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 (3)

Publication Number Publication Date
JP2020505440A JP2020505440A (ja) 2020-02-20
JP2020505440A5 JP2020505440A5 (enExample) 2021-02-18
JP7237010B2 true JP7237010B2 (ja) 2023-03-10

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JP2019557669A Active JP7237010B2 (ja) 2017-01-10 2018-01-10 Ｈｄａｃ６選択的阻害剤およびその製造方法と使用

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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
EP3822267B1 (en) * 2018-07-04 2023-08-30 Cstone Pharmaceuticals (Suzhou) Co., Ltd. Polymorph of hdac6-selective inhibitor and application thereof
CA3144985A1 (en) 2019-06-27 2020-12-30 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
CA3165424A1 (en) 2019-12-20 2021-06-24 Tenaya Therapeutics, Inc. Fluoroalkyl-oxadiazoles and uses thereof
EP4326263A1 (en) 2021-04-23 2024-02-28 Tenaya Therapeutics, Inc. Hdac6 inhibitors for use in the treatment of dilated cardiomyopathy
TW202308619A (zh) 2021-05-04 2023-03-01 美商特納亞治療股份有限公司 用於治療代謝疾病和hfpef的hdac6抑制劑
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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011529504A (ja) 2008-07-28 2011-12-08 ギリアード サイエンシーズ， インコーポレイテッド シクロアルキリデンヒストン脱アセチル化酵素阻害剤化合物およびヘテロシクロアルキリデンヒストン脱アセチル化酵素阻害剤化合物
JP2013542994A (ja) 2010-11-16 2013-11-28 アセチロン ファーマシューティカルズ インコーポレイテッド 蛋白質脱アセチル化酵素抑制剤としてのピリミジン水酸基アミド化合物およびその利用方法
JP2014502983A (ja) 2011-01-21 2014-02-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 癌治療用のｈｄａｃ阻害剤としての新規４−アミノ−ｎ−ヒドロキシ−ベンズアミド
WO2015007870A1 (en) 2013-07-18 2015-01-22 Institut De Recherche Pour Le Developpement (I.R.D.) New compounds for the treatment and/or prevention of parasitic diseases and method of production of thereof

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US20060058553A1 (en) * 2002-02-07 2006-03-16 Axys Pharmaceuticals, Inc. Novel bicyclic hydroxamates as inhibitors of histone deacetylase
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
WO2011106632A1 (en) * 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
CA2933907A1 (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 (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2011529504A (ja) 2008-07-28 2011-12-08 ギリアード サイエンシーズ， インコーポレイテッド シクロアルキリデンヒストン脱アセチル化酵素阻害剤化合物およびヘテロシクロアルキリデンヒストン脱アセチル化酵素阻害剤化合物
JP2013542994A (ja) 2010-11-16 2013-11-28 アセチロン ファーマシューティカルズ インコーポレイテッド 蛋白質脱アセチル化酵素抑制剤としてのピリミジン水酸基アミド化合物およびその利用方法
JP2014502983A (ja) 2011-01-21 2014-02-06 エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト 癌治療用のｈｄａｃ阻害剤としての新規４−アミノ−ｎ−ヒドロキシ−ベンズアミド
WO2015007870A1 (en) 2013-07-18 2015-01-22 Institut De Recherche Pour Le Developpement (I.R.D.) New compounds for the treatment and/or prevention of parasitic diseases and method of production of thereof

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Publication number Publication date
US10745389B2 (en) 2020-08-18
IL267968B (en) 2022-06-01
EP3569592A4 (en) 2020-08-12
JP2020505440A (ja) 2020-02-20
EP3569592A1 (en) 2019-11-20
CN110382463B (zh) 2022-11-04
AU2018208160A1 (en) 2019-08-15
SG11201906361YA (en) 2019-08-27
CA3049834A1 (en) 2018-07-19
MX394624B (es) 2025-03-24
BR112019014152A2 (pt) 2020-03-31
US20190375735A1 (en) 2019-12-12
KR102549606B1 (ko) 2023-06-29
SA519402090B1 (ar) 2022-05-30
EP3569592B1 (en) 2022-08-24
RU2019124962A3 (enExample) 2021-05-11
WO2018130155A1 (zh) 2018-07-19
MX2019008181A (es) 2019-12-09
RU2019124962A (ru) 2021-02-15
KR20190103286A (ko) 2019-09-04
IL267968A (en) 2019-10-31
ES2927352T8 (es) 2022-11-18
CN110382463A (zh) 2019-10-25
ES2927352T3 (es) 2022-11-04
EP3569592B8 (en) 2022-11-30
AU2018208160B2 (en) 2021-03-04

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