TWI895412B - 具有kdm5抑制活性之化合物及其醫藥用途 - Google Patents
具有kdm5抑制活性之化合物及其醫藥用途Info
- Publication number
- TWI895412B TWI895412B TW110116409A TW110116409A TWI895412B TW I895412 B TWI895412 B TW I895412B TW 110116409 A TW110116409 A TW 110116409A TW 110116409 A TW110116409 A TW 110116409A TW I895412 B TWI895412 B TW I895412B
- Authority
- TW
- Taiwan
- Prior art keywords
- azabicyclo
- group
- mmol
- general formula
- compound
- Prior art date
Links
Classifications
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/42—Oxazoles
- A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
-
- 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
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D413/14—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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2020088925 | 2020-05-07 | ||
| WOPCT/CN2020/088925 | 2020-05-07 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202200571A TW202200571A (zh) | 2022-01-01 |
| TWI895412B true TWI895412B (zh) | 2025-09-01 |
Family
ID=76159223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110116409A TWI895412B (zh) | 2020-05-07 | 2021-05-06 | 具有kdm5抑制活性之化合物及其醫藥用途 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US11691968B2 (https=) |
| EP (2) | EP4471027A1 (https=) |
| JP (3) | JP7643466B2 (https=) |
| KR (2) | KR20260046494A (https=) |
| CN (1) | CN115461338B (https=) |
| AU (1) | AU2021268223B2 (https=) |
| BR (1) | BR112022022005A2 (https=) |
| CA (1) | CA3181604A1 (https=) |
| ES (1) | ES3037418T3 (https=) |
| IL (1) | IL297900B2 (https=) |
| MX (1) | MX2022013692A (https=) |
| NZ (1) | NZ793960A (https=) |
| TW (1) | TWI895412B (https=) |
| WO (1) | WO2021223699A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3999183A4 (en) * | 2019-07-17 | 2023-11-15 | Ono Pharmaceutical Co., Ltd. | COMPOUNDS HAVING KDM5 INHIBITANT ACTION AND THEIR PHARMACEUTICAL USES |
| ES3037418T3 (en) | 2020-05-07 | 2025-10-01 | Ono Pharmaceutical Co | 3-azabicyclo(3.1.0)hexane derivatives having kdm5 inhibitory activity and use thereof |
| JP7743829B2 (ja) * | 2021-11-05 | 2025-09-25 | 小野薬品工業株式会社 | Ｋｄｍ５阻害作用を有する化合物を含有する医薬組成物 |
| WO2025239445A1 (ja) * | 2024-05-17 | 2025-11-20 | 小野薬品工業株式会社 | 認知症の行動および心理症状の予防、進行抑制および／または治療剤 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1140828B1 (en) * | 1998-12-23 | 2006-08-09 | Pfizer Limited | 3-azabicyclo¬3.1.0|hexane derivatives as opiate receptors ligands |
| WO2016057924A1 (en) * | 2014-10-10 | 2016-04-14 | Genentech, Inc. | Pyrrolidine amide compounds as histone demethylase inhibitors |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0311859D0 (en) | 2003-05-22 | 2003-06-25 | Merck Sharp & Dohme | Therapeutic agents |
| JP5017103B2 (ja) | 2004-06-17 | 2012-09-05 | トランスフオーム・フアーマシユーチカルズ・インコーポレーテツド | 薬剤共結晶組成物および関連した使用方法 |
| JP2008524331A (ja) | 2004-12-21 | 2008-07-10 | 武田薬品工業株式会社 | ジペプチジルペプチダーゼ阻害剤 |
| RU2487127C2 (ru) | 2007-10-09 | 2013-07-10 | Ф.Хоффманн-Ля Рош Аг | Хиральные цис-имидазолины |
| CN108341819B (zh) | 2017-01-22 | 2021-06-15 | 南京药捷安康生物科技有限公司 | 磷酸二酯酶抑制剂及其用途 |
| EP3999183A4 (en) | 2019-07-17 | 2023-11-15 | Ono Pharmaceutical Co., Ltd. | COMPOUNDS HAVING KDM5 INHIBITANT ACTION AND THEIR PHARMACEUTICAL USES |
| ES3037418T3 (en) | 2020-05-07 | 2025-10-01 | Ono Pharmaceutical Co | 3-azabicyclo(3.1.0)hexane derivatives having kdm5 inhibitory activity and use thereof |
-
2021
- 2021-05-06 ES ES21728166T patent/ES3037418T3/es active Active
- 2021-05-06 MX MX2022013692A patent/MX2022013692A/es unknown
- 2021-05-06 KR KR1020267006670A patent/KR20260046494A/ko active Pending
- 2021-05-06 CA CA3181604A patent/CA3181604A1/en active Pending
- 2021-05-06 AU AU2021268223A patent/AU2021268223B2/en active Active
- 2021-05-06 CN CN202180032139.2A patent/CN115461338B/zh active Active
- 2021-05-06 NZ NZ793960A patent/NZ793960A/en unknown
- 2021-05-06 EP EP24182835.9A patent/EP4471027A1/en active Pending
- 2021-05-06 KR KR1020227037880A patent/KR102937044B1/ko active Active
- 2021-05-06 BR BR112022022005A patent/BR112022022005A2/pt unknown
- 2021-05-06 TW TW110116409A patent/TWI895412B/zh active
- 2021-05-06 WO PCT/CN2021/091843 patent/WO2021223699A1/en not_active Ceased
- 2021-05-06 EP EP21728166.6A patent/EP4146645B1/en active Active
- 2021-05-06 JP JP2022567355A patent/JP7643466B2/ja active Active
- 2021-05-06 IL IL297900A patent/IL297900B2/en unknown
-
2022
- 2022-10-24 US US17/971,844 patent/US11691968B2/en active Active
-
2023
- 2023-05-05 US US18/144,030 patent/US12269817B2/en active Active
-
2024
- 2024-10-02 JP JP2024173464A patent/JP7643632B2/ja active Active
-
2025
- 2025-02-26 JP JP2025029239A patent/JP2025081677A/ja not_active Withdrawn
- 2025-02-28 US US19/067,084 patent/US20250214984A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1140828B1 (en) * | 1998-12-23 | 2006-08-09 | Pfizer Limited | 3-azabicyclo¬3.1.0|hexane derivatives as opiate receptors ligands |
| WO2016057924A1 (en) * | 2014-10-10 | 2016-04-14 | Genentech, Inc. | Pyrrolidine amide compounds as histone demethylase inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| IL297900B2 (en) | 2026-04-01 |
| JP7643466B2 (ja) | 2025-03-11 |
| WO2021223699A1 (en) | 2021-11-11 |
| JP2023524547A (ja) | 2023-06-12 |
| IL297900B1 (en) | 2025-12-01 |
| CN115461338A (zh) | 2022-12-09 |
| IL297900A (en) | 2023-01-01 |
| US12269817B2 (en) | 2025-04-08 |
| EP4146645A1 (en) | 2023-03-15 |
| US20230271952A1 (en) | 2023-08-31 |
| CA3181604A1 (en) | 2021-11-11 |
| KR20260046494A (ko) | 2026-04-07 |
| TW202200571A (zh) | 2022-01-01 |
| JP7643632B2 (ja) | 2025-03-11 |
| JP2025081677A (ja) | 2025-05-27 |
| KR20230007352A (ko) | 2023-01-12 |
| AU2021268223B2 (en) | 2025-10-09 |
| AU2021268223A1 (en) | 2022-12-08 |
| CN115461338B (zh) | 2024-02-20 |
| US20250214984A1 (en) | 2025-07-03 |
| EP4471027A1 (en) | 2024-12-04 |
| BR112022022005A2 (pt) | 2022-12-13 |
| US20230109293A1 (en) | 2023-04-06 |
| JP2024177345A (ja) | 2024-12-19 |
| KR102937044B1 (ko) | 2026-03-09 |
| ES3037418T3 (en) | 2025-10-01 |
| EP4146645B1 (en) | 2025-06-25 |
| US11691968B2 (en) | 2023-07-04 |
| NZ793960A (en) | 2025-12-19 |
| MX2022013692A (es) | 2022-11-30 |
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