KR20240124952A - Hdac6 억제제로서의 화합물 및 이의 용도 - Google Patents
Hdac6 억제제로서의 화합물 및 이의 용도 Download PDFInfo
- 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
- Prior art keywords
- alkylene
- alkyl
- compound
- heterocycloalkyl
- cycloalkyl
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- Legal status (The legal status 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 status listed.)
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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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- 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
- A61K31/495—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
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with 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
- A61K31/495—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
-
- 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
- A61K31/517—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
- 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
- A61K31/53—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
- 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
- A61K31/535—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
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- 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
- C07D409/02—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
- 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
- C07D471/04—Ortho-condensed 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
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP21217182.1 | 2021-12-22 | ||
| EP21217181.3 | 2021-12-22 | ||
| EP21217181 | 2021-12-22 | ||
| EP21217182 | 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 |
Family
ID=84981649
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020247023082A Pending KR20240124952A (ko) | 2021-12-22 | 2022-12-22 | Hdac6 억제제로서의 화합물 및 이의 용도 |
Country Status (9)
| Country | Link |
|---|---|
| US (2) | US20250051319A1 (https=) |
| EP (1) | EP4452265A2 (https=) |
| JP (1) | JP2025503502A (https=) |
| KR (1) | KR20240124952A (https=) |
| AU (1) | AU2022420827A1 (https=) |
| CA (1) | CA3239992A1 (https=) |
| IL (1) | IL313636A (https=) |
| MX (1) | MX2024007904A (https=) |
| WO (1) | WO2023118507A2 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
| AU2020321955A1 (en) | 2019-07-30 | 2022-03-17 | Eikonizo Therapapeutics, Inc. | HDAC6 inhibitors and uses thereof |
| MX2024007904A (es) * | 2021-12-22 | 2024-09-18 | Augustine Therapeutics | Compuestos y uso de estos como inhibidores de hdac6. |
| IL316201A (en) | 2022-04-08 | 2024-12-01 | Eikonizo Therapeutics Inc | Oxadiazole HDAC6 inhibitors and their uses |
| WO2024261327A1 (en) * | 2023-06-21 | 2024-12-26 | Augustine Therapeutics | 2-(heteroaryl-thio)-1-(heteroaryl)ethanone compounds and use thereof as hdac6 inhibitors |
| KR20260025099A (ko) * | 2023-06-21 | 2026-02-23 | 어거스틴 테라퓨틱스 | 헤테로아릴-아민 화합물 및 이의 hdac6 억제제로서의 용도 |
| 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 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US8546588B2 (en) | 2010-02-26 | 2013-10-01 | Millennium Pharmaceuticals, Inc. | Substituted hydroxamic acids and uses thereof |
| CA2800717A1 (en) * | 2010-05-27 | 2011-12-01 | Bayer Intellectual Property Gmbh | Heterocyclic thiosubstituted alkanol derivatives as fungicides |
| US20130227717A1 (en) | 2010-10-08 | 2013-08-29 | Life Sciences Research Partners Vzw | Hdac inhibitors to treat charcot-marie-tooth disease |
| JP6338601B2 (ja) | 2013-03-01 | 2018-06-06 | フンダシオン パラ ラ インベスティガシオン メディカ アプリカダ | ホスホジエステラーゼとヒストンデアセチラーゼの二重阻害剤としての新規な化合物 |
| 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 |
| WO2021133957A1 (en) * | 2019-12-27 | 2021-07-01 | 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 |
| MX2024007904A (es) * | 2021-12-22 | 2024-09-18 | Augustine Therapeutics | Compuestos y uso de estos como inhibidores de hdac6. |
| 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 |
-
2022
- 2022-12-22 MX MX2024007904A patent/MX2024007904A/es unknown
- 2022-12-22 KR KR1020247023082A patent/KR20240124952A/ko active Pending
- 2022-12-22 EP EP22844102.8A patent/EP4452265A2/en active Pending
- 2022-12-22 AU AU2022420827A patent/AU2022420827A1/en active Pending
- 2022-12-22 US US18/723,237 patent/US20250051319A1/en active Pending
- 2022-12-22 WO PCT/EP2022/087613 patent/WO2023118507A2/en not_active Ceased
- 2022-12-22 CA CA3239992A patent/CA3239992A1/en active Pending
- 2022-12-22 IL IL313636A patent/IL313636A/en unknown
- 2022-12-22 JP JP2024538291A patent/JP2025503502A/ja active Pending
-
2025
- 2025-01-10 US US19/016,827 patent/US12421222B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2025503502A (ja) | 2025-02-04 |
| US20250051319A1 (en) | 2025-02-13 |
| IL313636A (en) | 2024-08-01 |
| US12421222B2 (en) | 2025-09-23 |
| WO2023118507A2 (en) | 2023-06-29 |
| EP4452265A2 (en) | 2024-10-30 |
| AU2022420827A1 (en) | 2024-06-13 |
| US20250145604A1 (en) | 2025-05-08 |
| WO2023118507A3 (en) | 2023-08-03 |
| MX2024007904A (es) | 2024-09-18 |
| CA3239992A1 (en) | 2023-06-29 |
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