JP2024543497A - ユビキチン特異的プロテアーゼ１（ｕｓｐ１）の小分子阻害剤及びその使用 - Google Patents
ユビキチン特異的プロテアーゼ１（ｕｓｐ１）の小分子阻害剤及びその使用 Download PDFInfo
- Publication number
- JP2024543497A JP2024543497A JP2024528586A JP2024528586A JP2024543497A JP 2024543497 A JP2024543497 A JP 2024543497A JP 2024528586 A JP2024528586 A JP 2024528586A JP 2024528586 A JP2024528586 A JP 2024528586A JP 2024543497 A JP2024543497 A JP 2024543497A
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- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- heterocycloalkyl
- cycloalkyl
- heteroalkyl
- Prior art date
- 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.)
- Pending
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Classifications
-
- 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
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not 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
- A61K31/495—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
- A61K31/495—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
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2021/130284 | 2021-11-12 | ||
| CN2021130284 | 2021-11-12 | ||
| CN2022123821 | 2022-10-08 | ||
| CNPCT/CN2022/123821 | 2022-10-08 | ||
| PCT/CN2022/131290 WO2023083285A1 (en) | 2021-11-12 | 2022-11-11 | Small molecule inhibitors of ubiquitin specific protease 1 (usp1) and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2024543497A true JP2024543497A (ja) | 2024-11-21 |
| JP2024543497A5 JP2024543497A5 (enExample) | 2025-11-19 |
Family
ID=86335132
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024528586A Pending JP2024543497A (ja) | 2021-11-12 | 2022-11-11 | ユビキチン特異的プロテアーゼ１（ｕｓｐ１）の小分子阻害剤及びその使用 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20250066348A1 (enExample) |
| EP (1) | EP4430049A4 (enExample) |
| JP (1) | JP2024543497A (enExample) |
| KR (1) | KR20240117555A (enExample) |
| CN (1) | CN119173515A (enExample) |
| AU (1) | AU2022387669A1 (enExample) |
| CA (1) | CA3235603A1 (enExample) |
| CL (1) | CL2024001398A1 (enExample) |
| CO (1) | CO2024006278A2 (enExample) |
| CR (1) | CR20240190A (enExample) |
| DO (1) | DOP2024000081A (enExample) |
| GE (1) | GEAP202416531A (enExample) |
| IL (1) | IL312640A (enExample) |
| JO (1) | JOP20240095A1 (enExample) |
| MX (1) | MX2024005756A (enExample) |
| PE (1) | PE20241350A1 (enExample) |
| WO (1) | WO2023083285A1 (enExample) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR127646A1 (es) | 2021-11-12 | 2024-02-14 | Insilico Medicine Ip Ltd | Inhibidores de molécula pequeña de proteasa 1 específica de ubiquitina (usp1) y usos de los mismos |
| EP4480479A4 (en) * | 2022-02-18 | 2026-02-11 | Xizang Haisco Pharmaceutical Co Ltd | PYRAZOLOPYRIDINE DERIVATIVE AND ITS APPLICATION IN MEDICINE |
| WO2024022266A1 (en) * | 2022-07-25 | 2024-02-01 | Guangdong Newopp Biopharmaceuticals Co., Ltd. | Heteroaryl compounds as inhibitors of usp1 |
| CN119522224A (zh) * | 2022-08-09 | 2025-02-25 | 上海济煜医药科技有限公司 | 含氮杂环化合物作为泛素-特异性蛋白酶1抑制剂的制备方法、应用及其用途 |
| KR20250069611A (ko) * | 2022-09-20 | 2025-05-19 | 치아타이 티안큉 파마수티컬 그룹 주식회사 | 유비키틴 특이적 프로테아제 저해제로서의 카르보닐 축합 복소환 유도체 |
| CN120603835A (zh) * | 2023-01-20 | 2025-09-05 | 杭州英创医药科技有限公司 | 作为usp1抑制剂的化合物 |
| EP4741386A1 (en) * | 2023-07-05 | 2026-05-13 | Jiangsu Yahong Meditech Co., Ltd. | Pyrimidine compound, preparation method therefor and medical use thereof |
| WO2025010245A1 (en) | 2023-07-06 | 2025-01-09 | Exelixis, Inc. | Fused pyrazole derivatives as usp1 inhibitors |
| CN121532384A (zh) * | 2023-07-14 | 2026-02-13 | 来凯制药(宁波)有限公司 | 嘧啶化合物及其作为usp1抑制剂的用途 |
| TW202530200A (zh) * | 2023-09-25 | 2025-08-01 | 大陸商上海濟煜醫藥科技有限公司 | 嗒𠯤酮類化合物作為泛素－特異性蛋白酶１抑制劑的製備方法、應用及其用途 |
| CN121909194A (zh) * | 2023-09-26 | 2026-04-21 | 上海济煜医药科技股份有限公司 | 一类氮杂环胺类化合物作为泛素-特异性蛋白酶1抑制剂的制备方法、应用及其用途 |
| WO2025102016A1 (en) | 2023-11-10 | 2025-05-15 | Vrise Therapeutics, Inc. | Novel molecules as inhibitors of dna damage repair pathway |
| WO2025151705A1 (en) | 2024-01-10 | 2025-07-17 | Vrise Therapeutics, Inc. | Novel inhibitors of dna damage repair pathway |
| WO2025227060A1 (en) * | 2024-04-26 | 2025-10-30 | Insilico Medicine Ip Limited | Heterocyclic inhibitors of ubiquitin specific protease 1 (usp1) in combination with additional agents for use in the treatment of cancer |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3377493B1 (en) * | 2015-11-20 | 2020-04-08 | Forma Therapeutics, Inc. | Purinones as ubiquitin-specific protease 1 inhibitors |
| AU2019405925B2 (en) * | 2018-12-20 | 2025-07-03 | KSQ Therapeutics, Inc. | Substituted pyrazolopyrimidines and substituted purines and their use as ubiquitin-specific-processing protease 1 (USP1) inhibitors |
| US20230277533A1 (en) * | 2020-02-14 | 2023-09-07 | KSQ Therapeutics, Inc. | Therapeutic combinations comprising ubiquitin-specific-processing protease 1 (usp1) inhibitors and poly (adp-ribose) polymerase (parp) inhibitors |
| AU2021371305A1 (en) * | 2020-10-30 | 2023-06-15 | KSQ Therapeutics, Inc. | Solid state forms of substituted pyrazolopyrimidines and uses thereof |
| EP4291559A1 (en) * | 2021-02-15 | 2023-12-20 | Tango Therapeutics, Inc. | Pyrrolo[3,2-d]pyrimidine compounds and methods of use in the treatment of cancer |
| JP2024511996A (ja) * | 2021-03-17 | 2024-03-18 | タンゴ セラピューティクス， インコーポレイテッド | 抗がん剤としてのプリン誘導体 |
| WO2022199652A1 (en) * | 2021-03-24 | 2022-09-29 | Impact Therapeutics (Shanghai) , Inc | Five-membered heteroaryl-pyrimidine compounds as usp1 inhibitors and the use thereof |
| IL307157A (en) * | 2021-04-07 | 2023-11-01 | Forma Therapeutics Inc | Ubiquitin-specific protease 1 (USP1) inhibition |
-
2022
- 2022-11-11 CN CN202280087722.8A patent/CN119173515A/zh active Pending
- 2022-11-11 CR CR20240190A patent/CR20240190A/es unknown
- 2022-11-11 AU AU2022387669A patent/AU2022387669A1/en active Pending
- 2022-11-11 IL IL312640A patent/IL312640A/en unknown
- 2022-11-11 EP EP22892078.1A patent/EP4430049A4/en active Pending
- 2022-11-11 JP JP2024528586A patent/JP2024543497A/ja active Pending
- 2022-11-11 CA CA3235603A patent/CA3235603A1/en active Pending
- 2022-11-11 US US18/708,686 patent/US20250066348A1/en active Pending
- 2022-11-11 MX MX2024005756A patent/MX2024005756A/es unknown
- 2022-11-11 GE GEAP202416531A patent/GEAP202416531A/en unknown
- 2022-11-11 WO PCT/CN2022/131290 patent/WO2023083285A1/en not_active Ceased
- 2022-11-11 PE PE2024001034A patent/PE20241350A1/es unknown
- 2022-11-11 KR KR1020247018880A patent/KR20240117555A/ko active Pending
-
2024
- 2024-04-24 JO JOJO/P/2024/0095A patent/JOP20240095A1/ar unknown
- 2024-05-09 CL CL2024001398A patent/CL2024001398A1/es unknown
- 2024-05-10 DO DO2024000081A patent/DOP2024000081A/es unknown
- 2024-05-17 CO CONC2024/0006278A patent/CO2024006278A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JOP20240095A1 (ar) | 2024-04-24 |
| CL2024001398A1 (es) | 2024-11-08 |
| CA3235603A1 (en) | 2023-05-19 |
| KR20240117555A (ko) | 2024-08-01 |
| PE20241350A1 (es) | 2024-07-03 |
| EP4430049A4 (en) | 2025-12-17 |
| CO2024006278A2 (es) | 2024-05-30 |
| GEAP202416531A (en) | 2024-10-28 |
| US20250066348A1 (en) | 2025-02-27 |
| DOP2024000081A (es) | 2024-11-29 |
| WO2023083285A1 (en) | 2023-05-19 |
| EP4430049A1 (en) | 2024-09-18 |
| MX2024005756A (es) | 2024-09-06 |
| AU2022387669A1 (en) | 2024-05-16 |
| CR20240190A (es) | 2024-09-13 |
| IL312640A (en) | 2024-07-01 |
| CN119173515A (zh) | 2024-12-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20251111 |
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| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20251111 |