KR20240124952A - Hdac6 억제제로서의 화합물 및 이의 용도 - Google Patents

Hdac6 억제제로서의 화합물 및 이의 용도 Download PDF

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Publication number
KR20240124952A
KR20240124952A KR1020247023082A KR20247023082A KR20240124952A KR 20240124952 A KR20240124952 A KR 20240124952A KR 1020247023082 A KR1020247023082 A KR 1020247023082A KR 20247023082 A KR20247023082 A KR 20247023082A KR 20240124952 A KR20240124952 A KR 20240124952A
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South Korea
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alkylene
alkyl
compound
heterocycloalkyl
cycloalkyl
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Korean (ko)
Inventor
실뱅 셀라니르
산토스 카르발로 주앙 페르난도 도스
프레데릭 얀 리타 롬바우츠
피터 크리스티안 젠헨
미셸 쿠시오
페드로 조아나 카타리나 라이스
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어거스틴 테라퓨틱스
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Publication of KR20240124952A publication Critical patent/KR20240124952A/ko
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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
    • A61K31/395—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • 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
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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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
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    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
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    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
KR1020247023082A 2021-12-22 2022-12-22 Hdac6 억제제로서의 화합물 및 이의 용도 Pending KR20240124952A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP21217182 2021-12-22
EP21217181 2021-12-22
EP21217182.1 2021-12-22
EP21217181.3 2021-12-22
PCT/EP2022/087613 WO2023118507A2 (en) 2021-12-22 2022-12-22 Compounds and use thereof as hdac6 inhibitors

Publications (1)

Publication Number Publication Date
KR20240124952A true KR20240124952A (ko) 2024-08-19

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KR1020247023082A Pending KR20240124952A (ko) 2021-12-22 2022-12-22 Hdac6 억제제로서의 화합물 및 이의 용도

Country Status (9)

Country Link
US (2) US20250051319A1 (enExample)
EP (1) EP4452265A2 (enExample)
JP (1) JP2025503502A (enExample)
KR (1) KR20240124952A (enExample)
AU (1) AU2022420827A1 (enExample)
CA (1) CA3239992A1 (enExample)
IL (1) IL313636A (enExample)
MX (1) MX2024007904A (enExample)
WO (1) WO2023118507A2 (enExample)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10357493B2 (en) 2017-03-10 2019-07-23 Selenity Therapeutics (Bermuda), Ltd. Metalloenzyme inhibitor compounds
CN114727974A (zh) 2019-07-30 2022-07-08 艾科尼佐治疗股份有限公司 Hdac6抑制剂及其用途
WO2023118507A2 (en) * 2021-12-22 2023-06-29 Augustine Therapeutics Compounds and use thereof as hdac6 inhibitors
AU2023250964A1 (en) 2022-04-08 2024-11-07 Eikonizo Therapeutics, Inc. Oxadiazole hdac6 inhibitors and uses thereof
WO2024261327A1 (en) * 2023-06-21 2024-12-26 Augustine Therapeutics 2-(heteroaryl-thio)-1-(heteroaryl)ethanone compounds and use thereof as hdac6 inhibitors
AU2024314277A1 (en) * 2023-06-21 2025-11-13 Augustine Therapeutics Heteroaryl-amine compounds and use thereof as hdac6 inhibitors
WO2024261328A1 (en) * 2023-06-21 2024-12-26 Augustine Therapeutics Amide-amine compounds and use thereof as hdac6 inhibitors
WO2026027696A1 (en) * 2024-07-31 2026-02-05 Augustine Therapeutics Thiomethyl carbonyl compounds and use thereof as hdac6 inhibitors

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EP1217000A1 (en) 2000-12-23 2002-06-26 Aventis Pharma Deutschland GmbH Inhibitors of factor Xa and factor VIIa
WO2005014588A1 (en) 2003-08-01 2005-02-17 Argenta Discovery Limited Substituted thienyl-hydroxamic acids having histone deacetylase activity
US20090023798A1 (en) 2007-06-15 2009-01-22 Pharmacyclics, Inc. Thiohydroxamates as inhibitors of histone deacetylase
JP5640005B2 (ja) 2008-07-14 2014-12-10 ギリアード サイエンシーズ, インコーポレイテッド Hdacおよび/またはcdk阻害剤としてのイミダゾシルピリジン化合物
GB0813403D0 (en) 2008-07-22 2008-08-27 Lectus Therapeutics Ltd Potassium ion channel modulators & uses thereof
WO2011106627A1 (en) 2010-02-26 2011-09-01 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
EA201291320A1 (ru) * 2010-05-27 2013-05-30 Байер Интеллектуэль Проперти Гмбх Гетероциклические тиозамещенные производные алканолов в качестве фунгицидов
CA2812855C (en) 2010-10-08 2017-12-19 Vib Vzw Hdac inhibitors to treat charcot-marie-tooth disease
ES2635016T3 (es) 2013-03-01 2017-10-02 Fundación Para La Investigación Médica Aplicada Nuevos compuestos como inhibidores duales de fosfodiesterasas e histonas deacetilasas
WO2017053360A1 (en) 2015-09-22 2017-03-30 The Board Of Trustees Of The University Of Illinois Bicyclic and tricyclic cap bearing mercaptoacetamide derivatives as histone deacetylase inhibitors
US11584733B2 (en) * 2017-01-09 2023-02-21 Shuttle Pharmaceuticals, Inc. Selective histone deacetylase inhibitors for the treatment of human disease
US12310967B2 (en) 2017-12-21 2025-05-27 Gliapharm Sa Compositions and methods of treatment for neurological disorders comprising motor neuron diseases
ES2749743B2 (es) 2018-09-21 2020-12-14 Consejo Superior Investigacion Derivados de purina inhibidores de cdc7 y su uso para el tratamiento de patologias neurologicas
US11339150B2 (en) * 2019-12-27 2022-05-24 Onkure, Inc. Benzimidazole compounds as HDAC6 inhibitors
EP4111863A1 (en) 2021-07-02 2023-01-04 EuroChem Antwerpen Phosphorus use efficiency enhancers as plant growth promotors
WO2023118507A2 (en) * 2021-12-22 2023-06-29 Augustine Therapeutics Compounds and use thereof as hdac6 inhibitors
US20240139187A1 (en) 2022-10-12 2024-05-02 The Children's Medical Center Corporation Selective hypothalamus permeable hdac6 inhibitors for treatment of leptin-resistant obesity

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Publication number Publication date
US12421222B2 (en) 2025-09-23
CA3239992A1 (en) 2023-06-29
EP4452265A2 (en) 2024-10-30
JP2025503502A (ja) 2025-02-04
AU2022420827A1 (en) 2024-06-13
US20250145604A1 (en) 2025-05-08
WO2023118507A3 (en) 2023-08-03
US20250051319A1 (en) 2025-02-13
WO2023118507A2 (en) 2023-06-29
IL313636A (en) 2024-08-01
MX2024007904A (es) 2024-09-18

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