TWI879854B - 蛋白質酪胺酸磷酸酶降解劑及其使用方法 - Google Patents
蛋白質酪胺酸磷酸酶降解劑及其使用方法 Download PDFInfo
- Publication number
- TWI879854B TWI879854B TW109145346A TW109145346A TWI879854B TW I879854 B TWI879854 B TW I879854B TW 109145346 A TW109145346 A TW 109145346A TW 109145346 A TW109145346 A TW 109145346A TW I879854 B TWI879854 B TW I879854B
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- compound
- mmol
- pharmaceutically acceptable
- acceptable salt
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Classifications
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- 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)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Obesity (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 (8)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962952097P | 2019-12-20 | 2019-12-20 | |
| US201962952161P | 2019-12-20 | 2019-12-20 | |
| US62/952,097 | 2019-12-20 | ||
| US62/952,161 | 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| TW202136250A TW202136250A (zh) | 2021-10-01 |
| TWI879854B true TWI879854B (zh) | 2025-04-11 |
Family
ID=74206162
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW109145346A TWI879854B (zh) | 2019-12-20 | 2020-12-21 | 蛋白質酪胺酸磷酸酶降解劑及其使用方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20240383886A1 (cg-RX-API-DMAC10.html) |
| EP (1) | EP4077319A1 (cg-RX-API-DMAC10.html) |
| JP (1) | JP7828893B2 (cg-RX-API-DMAC10.html) |
| CN (1) | CN116194453A (cg-RX-API-DMAC10.html) |
| AU (1) | AU2020407244A1 (cg-RX-API-DMAC10.html) |
| CA (1) | CA3162364A1 (cg-RX-API-DMAC10.html) |
| TW (1) | TWI879854B (cg-RX-API-DMAC10.html) |
| UY (1) | UY38999A (cg-RX-API-DMAC10.html) |
| WO (1) | WO2021127586A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102947433B1 (ko) | 2019-04-12 | 2026-04-06 | 씨4 테라퓨틱스, 인코포레이티드 | 이카로스 및 아이올로스의 트리시클릭 분해제 |
| AU2020401376A1 (en) | 2019-12-12 | 2022-06-30 | Kumquat Biosciences Inc. | Compositions and methods for potentiating immune activity |
| US20230167081A1 (en) * | 2020-04-30 | 2023-06-01 | President And Fellows Of Harvard College | 5-amino-2-piperidinon-3-yl-1-oxoisoindoline derivatives for degradation of ikzf2 degraders |
| JP7863100B2 (ja) * | 2020-10-14 | 2026-05-20 | シーフォー セラピューティクス， インコーポレイテッド | Ｉｋｚｆ２又はｉｋｚｆ４を分解する三環式リガンド |
| CA3194351A1 (en) * | 2020-10-14 | 2022-04-21 | Christopher G. Nasveschuk | Tricyclic compounds to degrade neosubstrates for medical therapy |
| IL302037A (en) * | 2020-10-14 | 2023-06-01 | C4 Therapeutics Inc | Tricyclic heterobifunctional compounds for degradation of targeted proteins |
| 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 |
| US20240287076A1 (en) | 2021-05-05 | 2024-08-29 | Biogen Ma Inc. | Compounds for targeting degradation of bruton's tyrosine kinase |
| WO2022271727A1 (en) * | 2021-06-21 | 2022-12-29 | Calico Life Sciences Llc | Degrader compounds and uses thereof |
| CA3224732A1 (en) | 2021-07-07 | 2023-01-12 | Kevin M. Guckian | Compounds for targeting degradation of irak4 proteins |
| US20250302815A1 (en) * | 2021-08-10 | 2025-10-02 | Calico Life Sciences Llc | Protein tyrosine phosphatase targeting ligands |
| WO2023061478A1 (zh) * | 2021-10-15 | 2023-04-20 | 先声再明医药有限公司 | 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 |
| WO2023240038A1 (en) * | 2022-06-06 | 2023-12-14 | Treeline Biosciences, Inc. | Tricyclic quinolone bcl6 bifunctional degraders |
| WO2024243441A1 (en) | 2023-05-24 | 2024-11-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| TW202519514A (zh) | 2023-07-14 | 2025-05-16 | 天主教魯汶大學 | 新穎化合物(一) |
| WO2025083594A1 (en) | 2023-10-18 | 2025-04-24 | Northridge Health Group (Hong Kong) Co., Limited | Ptpn2/ptp1b degrader and therapeutic method thereof |
| 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 |
| WO2026035999A1 (en) | 2024-08-09 | 2026-02-12 | Triana Biomedicines, Inc. | Anaplastic lymphoma kinase (alk) degraders and uses thereof |
| WO2026096574A1 (en) * | 2024-10-30 | 2026-05-07 | Synnovation Therapeutics, Inc. | Nrf2 degrader for the treatment of cancer |
| WO2026112350A1 (en) * | 2024-11-22 | 2026-05-28 | Kumquat Biosciences Inc. | Heterocyclic compounds and uses thereof |
| CN122103122A (zh) * | 2024-11-29 | 2026-05-29 | 中科中山药物创新研究院 | 一种蛋白酪氨酸磷酸酶降解剂及其用途与制备方法 |
| WO2026119184A2 (en) | 2024-12-04 | 2026-06-11 | Northridge Health Group (Hong Kong) Co., Limited | Ptpn2/ptp1b degraders and therapeutic method thereof |
| WO2026132150A1 (en) | 2024-12-19 | 2026-06-25 | Katholieke Universiteit Leuven | Inhibitors of ptpn 2/ ptpn1 tyrosine phosphatase |
| WO2026132146A1 (en) | 2024-12-19 | 2026-06-25 | Katholieke Universiteit Leuven | Inhibitors of ptpn 2/ ptpn1 tyrosine phosphatase |
| WO2026132149A1 (en) | 2024-12-19 | 2026-06-25 | Katholieke Universiteit Leuven | Inhibitors of ptpn2 and/or ptpn1 |
| WO2026132148A1 (en) | 2024-12-19 | 2026-06-25 | Katholieke Universiteit Leuven | Inhibitors of ptpn2/ptpn1 tyrosine phosphatase |
| WO2026136866A1 (en) | 2024-12-20 | 2026-06-25 | Prelude Therapeutics Incorporated | Kat6 targeting compounds |
| WO2026139448A1 (en) | 2024-12-23 | 2026-07-02 | Merck Patent Gmbh | Heterobifunctional compounds for the degradation of kras protein |
| WO2026156134A1 (en) | 2025-01-17 | 2026-07-23 | F. Hoffmann-La Roche Ag | Tyk2 degraders |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007067612A1 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
| WO2007067615A2 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | Thiadiazole derivatives as antidiabetic agents |
| TW200911769A (en) * | 2007-06-04 | 2009-03-16 | Novartis Ag | Organic compounds |
| WO2017197046A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10689366B2 (en) * | 2016-11-01 | 2020-06-23 | Cornell University | Compounds for MALT1 degredation |
| EP4717317A3 (en) * | 2017-06-20 | 2026-06-03 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| MX2020003190A (es) * | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| IL315310A (en) * | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
-
2020
- 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 AU AU2020407244A patent/AU2020407244A1/en active Pending
- 2020-12-18 US US17/787,828 patent/US20240383886A1/en active Pending
- 2020-12-18 JP JP2022538068A patent/JP7828893B2/ja active Active
- 2020-12-18 CA CA3162364A patent/CA3162364A1/en active Pending
- 2020-12-18 WO PCT/US2020/066243 patent/WO2021127586A1/en not_active Ceased
- 2020-12-21 UY UY0001038999A patent/UY38999A/es unknown
- 2020-12-21 TW TW109145346A patent/TWI879854B/zh active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007067612A1 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | 1-orthofluorophenyl substituted 1, 2, 5-thiazolidinedione derivatives as ptp-as inhibitors |
| WO2007067615A2 (en) * | 2005-12-08 | 2007-06-14 | Novartis Ag | Thiadiazole derivatives as antidiabetic agents |
| TW200911769A (en) * | 2007-06-04 | 2009-03-16 | Novartis Ag | Organic compounds |
| WO2017197046A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
Also Published As
| Publication number | Publication date |
|---|---|
| TW202136250A (zh) | 2021-10-01 |
| AU2020407244A1 (en) | 2022-07-28 |
| JP2023508914A (ja) | 2023-03-06 |
| US20240383886A1 (en) | 2024-11-21 |
| JP7828893B2 (ja) | 2026-03-12 |
| WO2021127586A1 (en) | 2021-06-24 |
| UY38999A (es) | 2021-07-30 |
| EP4077319A1 (en) | 2022-10-26 |
| CA3162364A1 (en) | 2021-06-24 |
| CN116194453A (zh) | 2023-05-30 |
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