ES2927352T3 - Inhibidores selectivos de HDAC6, método de preparación de los mismos y aplicación de los mismos - Google Patents
Inhibidores selectivos de HDAC6, método de preparación de los mismos y aplicación de los mismos Download PDFInfo
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- ES2927352T3 ES2927352T3 ES18739134T ES18739134T ES2927352T3 ES 2927352 T3 ES2927352 T3 ES 2927352T3 ES 18739134 T ES18739134 T ES 18739134T ES 18739134 T ES18739134 T ES 18739134T ES 2927352 T3 ES2927352 T3 ES 2927352T3
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- 239000002356 single layer Substances 0.000 description 1
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- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
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- 125000006253 t-butylcarbonyl group Chemical group [H]C([H])([H])C(C(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
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- ISIJQEHRDSCQIU-UHFFFAOYSA-N tert-butyl 2,7-diazaspiro[4.5]decane-7-carboxylate Chemical compound C1N(C(=O)OC(C)(C)C)CCCC11CNCC1 ISIJQEHRDSCQIU-UHFFFAOYSA-N 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 description 1
- 125000004192 tetrahydrofuran-2-yl group Chemical group [H]C1([H])OC([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
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- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
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- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
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Classifications
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- 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
-
- 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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/16—Amides, e.g. hydroxamic acids
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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-
- 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
- C07D405/14—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
Landscapes
- 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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
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| ES2927352T3 true ES2927352T3 (es) | 2022-11-04 |
| ES2927352T8 ES2927352T8 (es) | 2022-11-18 |
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| EP (1) | EP3569592B8 (OSRAM) |
| JP (1) | JP7237010B2 (OSRAM) |
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| MX (1) | MX394624B (OSRAM) |
| SA (1) | SA519402090B1 (OSRAM) |
| SG (1) | SG11201906361YA (OSRAM) |
| WO (1) | WO2018130155A1 (OSRAM) |
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| 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 |
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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 |
| KR20110038159A (ko) * | 2008-07-28 | 2011-04-13 | 길리애드 사이언시즈, 인코포레이티드 | 사이클로알킬리덴 및 헤테로사이클로알킬리덴 히스톤 데아세틸라아제 억제제 화합물 |
| WO2011106632A1 (en) * | 2010-02-26 | 2011-09-01 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| JP6041808B2 (ja) * | 2010-11-16 | 2016-12-14 | 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Ａｃｅｔｙｌｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | 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 |
| 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 |
| 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 |
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- 2018-01-10 MX MX2019008181A patent/MX394624B/es unknown
- 2018-01-10 SG SG11201906361YA patent/SG11201906361YA/en unknown
- 2018-01-10 CA CA3049834A patent/CA3049834A1/en active Pending
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- 2018-01-10 ES ES18739134T patent/ES2927352T3/es active Active
- 2018-01-10 AU AU2018208160A patent/AU2018208160B2/en active Active
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2019
- 2019-07-09 SA SA519402090A patent/SA519402090B1/ar unknown
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Also Published As
| 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 |
| JP7237010B2 (ja) | 2023-03-10 |
| 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 (OSRAM) | 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 |
| EP3569592B8 (en) | 2022-11-30 |
| AU2018208160B2 (en) | 2021-03-04 |
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