JP7828893B2 - プロテインチロシンホスファターゼ分解剤及びその使用方法 - Google Patents
プロテインチロシンホスファターゼ分解剤及びその使用方法Info
- Publication number
- JP7828893B2 JP7828893B2 JP2022538068A JP2022538068A JP7828893B2 JP 7828893 B2 JP7828893 B2 JP 7828893B2 JP 2022538068 A JP2022538068 A JP 2022538068A JP 2022538068 A JP2022538068 A JP 2022538068A JP 7828893 B2 JP7828893 B2 JP 7828893B2
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- compound
- hydrogen
- formula
- alkylene
- 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.)
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Classifications
-
- 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
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
-
- 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
- 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
- C07D471/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical 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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Enzymes And Modification Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Micro-Organisms Or Cultivation Processes Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962952161P | 2019-12-20 | 2019-12-20 | |
| US201962952097P | 2019-12-20 | 2019-12-20 | |
| US62/952,161 | 2019-12-20 | ||
| US62/952,097 | 2019-12-20 | ||
| US202063121721P | 2020-12-04 | 2020-12-04 | |
| US63/121,721 | 2020-12-04 | ||
| US202063125937P | 2020-12-15 | 2020-12-15 | |
| US63/125,937 | 2020-12-15 | ||
| PCT/US2020/066243 WO2021127586A1 (en) | 2019-12-20 | 2020-12-18 | Protein tyrosine phosphatase degraders and methods of use thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2023508914A JP2023508914A (ja) | 2023-03-06 |
| JP2023508914A5 JP2023508914A5 (https=) | 2023-12-25 |
| JPWO2021127586A5 JPWO2021127586A5 (https=) | 2023-12-25 |
| JP7828893B2 true JP7828893B2 (ja) | 2026-03-12 |
Family
ID=74206162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022538068A Active JP7828893B2 (ja) | 2019-12-20 | 2020-12-18 | プロテインチロシンホスファターゼ分解剤及びその使用方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20240383886A1 (https=) |
| EP (1) | EP4077319A1 (https=) |
| JP (1) | JP7828893B2 (https=) |
| CN (1) | CN116194453A (https=) |
| AU (1) | AU2020407244A1 (https=) |
| CA (1) | CA3162364A1 (https=) |
| TW (1) | TWI879854B (https=) |
| UY (1) | UY38999A (https=) |
| WO (1) | WO2021127586A1 (https=) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN120172958A (zh) | 2019-04-12 | 2025-06-20 | C4医药公司 | Ikaros和aiolos的三环降解物 |
| JP2023506227A (ja) | 2019-12-12 | 2023-02-15 | カムクワット バイオサイエンシーズ インコーポレイテッド | 免疫活性を強化するための組成物および方法 |
| WO2021222542A1 (en) * | 2020-04-30 | 2021-11-04 | President And Fellows Of Harvard College | 5-amino-2-piperidinon-3-yl-1-oxoisoindoline derivatives for degradation of ikzf2 degraders |
| IL302038A (en) * | 2020-10-14 | 2023-06-01 | C4 Therapeutics Inc | Tricyclic ligands for degradation of ikzf2 or ikzf4 |
| EP4228625A4 (en) * | 2020-10-14 | 2026-01-14 | C4 Therapeutics Inc | TRICYCLIC HETEROBFUNCTIONAL COMPOUNDS FOR TARGETED PROTEIN DEGRADATION |
| CN116457339A (zh) * | 2020-10-14 | 2023-07-18 | C4医药公司 | 用于医学治疗的降解新底物的三环化合物 |
| WO2022161414A1 (zh) * | 2021-01-26 | 2022-08-04 | 成都茵创园医药科技有限公司 | 芳香化合物、含其的药物组合物及其应用 |
| KR20240017814A (ko) | 2021-05-05 | 2024-02-08 | 바이오젠 엠에이 인코포레이티드 | 브루톤 티로신 키나제의 분해를 표적으로 하는 화합물 |
| WO2022271727A1 (en) * | 2021-06-21 | 2022-12-29 | Calico Life Sciences Llc | Degrader compounds and uses thereof |
| KR20240035526A (ko) | 2021-07-07 | 2024-03-15 | 바이오젠 엠에이 인코포레이티드 | Irak4 단백질의 분해를 표적하는 화합물 |
| AU2022326553A1 (en) * | 2021-08-10 | 2024-03-28 | Abbvie Inc. | Protein tyrosine phosphatase targeting ligands |
| CN118201923A (zh) * | 2021-10-15 | 2024-06-14 | 海南先声再明医药股份有限公司 | 三环类化合物 |
| TW202333670A (zh) * | 2022-01-04 | 2023-09-01 | 大陸商海思科醫藥集團股份有限公司 | 抑制並降解irak4的化合物及其藥物组合物和藥學上的應用 |
| MA69177B1 (fr) * | 2022-06-06 | 2026-03-31 | Treeline Biosciences, Inc. | Agents de dégradation bifonctionnels de quinolone-bcl6 tricycliques |
| CN120981456A (zh) | 2023-05-24 | 2025-11-18 | 金橘生物科技公司 | 杂环化合物及其用途 |
| KR20260040037A (ko) | 2023-07-14 | 2026-03-23 | 카톨리에케 유니버시테이트 루벤 | 암 및 대사 질병의 치료를 위한 신규 화합물 |
| TW202535389A (zh) | 2023-10-18 | 2025-09-16 | 香港商北嶺健康集團(香港)有限公司 | Ｐｔｐｎ２／ｐｔｐ１ｂ降解劑及其治療方法 |
| CN117343052B (zh) * | 2023-12-04 | 2024-02-06 | 英矽智能科技(上海)有限公司 | 蛋白酪氨酸磷酸酶抑制剂及其应用 |
| US12565492B2 (en) | 2024-08-09 | 2026-03-03 | Triana Biomedicines, Inc. | Anaplastic Lymphoma Kinase (ALK) degraders and uses thereof |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009518419A (ja) | 2005-12-08 | 2009-05-07 | ノバルティス アクチエンゲゼルシャフト | ＰＴＰａｓｅ阻害剤としての１−オルトフルオロフェニル置換１，２，５−チアゾリジンジオン誘導体 |
| JP2009519248A (ja) | 2005-12-08 | 2009-05-14 | ノバルティス アクチエンゲゼルシャフト | 抗糖尿病剤としてのチアジアゾール誘導体 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| WO2018085247A1 (en) | 2016-11-01 | 2018-05-11 | Cornell University | Compounds for malt1 degradation |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS |
| WO2019060742A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc | AGENTS FOR DEGRADING PROTEINS AND USES THEREOF |
| WO2019133531A1 (en) | 2017-12-26 | 2019-07-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR066820A1 (es) * | 2007-06-04 | 2009-09-16 | Novartis Ag | Compuestos de tiadiazolidin-3 ona |
-
2020
- 2020-12-18 US US17/787,828 patent/US20240383886A1/en active Pending
- 2020-12-18 WO PCT/US2020/066243 patent/WO2021127586A1/en not_active Ceased
- 2020-12-18 CN CN202080097241.6A patent/CN116194453A/zh active Pending
- 2020-12-18 EP EP20845470.2A patent/EP4077319A1/en active Pending
- 2020-12-18 CA CA3162364A patent/CA3162364A1/en active Pending
- 2020-12-18 AU AU2020407244A patent/AU2020407244A1/en active Pending
- 2020-12-18 JP JP2022538068A patent/JP7828893B2/ja active Active
- 2020-12-21 UY UY0001038999A patent/UY38999A/es unknown
- 2020-12-21 TW TW109145346A patent/TWI879854B/zh active
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009518419A (ja) | 2005-12-08 | 2009-05-07 | ノバルティス アクチエンゲゼルシャフト | ＰＴＰａｓｅ阻害剤としての１−オルトフルオロフェニル置換１，２，５−チアゾリジンジオン誘導体 |
| JP2009519248A (ja) | 2005-12-08 | 2009-05-14 | ノバルティス アクチエンゲゼルシャフト | 抗糖尿病剤としてのチアジアゾール誘導体 |
| WO2017197046A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| WO2018085247A1 (en) | 2016-11-01 | 2018-05-11 | Cornell University | Compounds for malt1 degradation |
| WO2018237026A1 (en) | 2017-06-20 | 2018-12-27 | C4 Therapeutics, Inc. | N / O-LINKED DEGRONS AND DEGRONIMERS FOR DEGRADATION OF PROTEINS |
| WO2019060742A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc | AGENTS FOR DEGRADING PROTEINS AND USES THEREOF |
| WO2019133531A1 (en) | 2017-12-26 | 2019-07-04 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
Non-Patent Citations (1)
| Title |
|---|
| Christian STEINEBACH et al.，"A MedChem toolbox for cereblon-directed PROTACs"，MedChemComm，2019年，Vol. 10, No. 6，p.1037-1041，DOI: 10.1039/c9md00185a |
Also Published As
| Publication number | Publication date |
|---|---|
| UY38999A (es) | 2021-07-30 |
| EP4077319A1 (en) | 2022-10-26 |
| WO2021127586A1 (en) | 2021-06-24 |
| JP2023508914A (ja) | 2023-03-06 |
| CA3162364A1 (en) | 2021-06-24 |
| TW202136250A (zh) | 2021-10-01 |
| TWI879854B (zh) | 2025-04-11 |
| CN116194453A (zh) | 2023-05-30 |
| US20240383886A1 (en) | 2024-11-21 |
| AU2020407244A1 (en) | 2022-07-28 |
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