JP7789662B2 - Mta協働prmt5阻害剤 - Google Patents
Mta協働prmt5阻害剤Info
- Publication number
- JP7789662B2 JP7789662B2 JP2022516295A JP2022516295A JP7789662B2 JP 7789662 B2 JP7789662 B2 JP 7789662B2 JP 2022516295 A JP2022516295 A JP 2022516295A JP 2022516295 A JP2022516295 A JP 2022516295A JP 7789662 B2 JP7789662 B2 JP 7789662B2
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- JP
- Japan
- Prior art keywords
- mmol
- equiv
- alkyl
- mixture
- bromo
- 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
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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
- A61K31/495—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
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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
- A61K31/535—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
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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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
- C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
- C07D237/30—Phthalazines
- C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- C07D403/10—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 carbon chain containing aromatic rings
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- 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
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- 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
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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
- C07D413/02—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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
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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
- C07D413/02—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
- C07D413/10—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 carbon chain containing aromatic rings
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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
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- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
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- 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
- C07D417/10—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 carbon chain containing aromatic rings
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- 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
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- 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
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- 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
- C07D471/12—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 three hetero rings
- C07D471/14—Ortho-condensed systems
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- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—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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- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
- C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
- C12N9/10—Transferases (2.)
- C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
- C12N9/1007—Methyltransferases (general) (2.1.1.)
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Wood Science & Technology (AREA)
- Zoology (AREA)
- Genetics & Genomics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- General Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (11)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962899575P | 2019-09-12 | 2019-09-12 | |
| US62/899,575 | 2019-09-12 | ||
| US201962942833P | 2019-12-03 | 2019-12-03 | |
| US62/942,833 | 2019-12-03 | ||
| US202062961371P | 2020-01-15 | 2020-01-15 | |
| US62/961,371 | 2020-01-15 | ||
| US202062994927P | 2020-03-26 | 2020-03-26 | |
| US62/994,927 | 2020-03-26 | ||
| US202063060261P | 2020-08-03 | 2020-08-03 | |
| US63/060,261 | 2020-08-03 | ||
| PCT/US2020/050457 WO2021050915A1 (en) | 2019-09-12 | 2020-09-11 | Mta-cooperative prmt5 inhibitors |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022548255A JP2022548255A (ja) | 2022-11-17 |
| JPWO2021050915A5 JPWO2021050915A5 (https=) | 2023-09-13 |
| JP2022548255A5 JP2022548255A5 (https=) | 2023-09-13 |
| JP7789662B2 true JP7789662B2 (ja) | 2025-12-22 |
Family
ID=72659905
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022516295A Active JP7789662B2 (ja) | 2019-09-12 | 2020-09-11 | Mta協働prmt5阻害剤 |
Country Status (17)
| Country | Link |
|---|---|
| US (3) | US11492351B2 (https=) |
| EP (1) | EP4028388A1 (https=) |
| JP (1) | JP7789662B2 (https=) |
| KR (1) | KR20220083691A (https=) |
| CN (2) | CN114728912A (https=) |
| AU (1) | AU2020345899B2 (https=) |
| BR (1) | BR112022004248A2 (https=) |
| CA (1) | CA3150515A1 (https=) |
| CL (1) | CL2022000603A1 (https=) |
| CO (1) | CO2022004513A2 (https=) |
| IL (2) | IL290341B2 (https=) |
| MX (1) | MX2022002938A (https=) |
| NO (1) | NO20220309A1 (https=) |
| PH (1) | PH12022550399A1 (https=) |
| SA (1) | SA522431915B1 (https=) |
| TW (1) | TW202122387A (https=) |
| WO (1) | WO2021050915A1 (https=) |
Families Citing this family (46)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW202122387A (zh) * | 2019-09-12 | 2021-06-16 | 美商米瑞替療法公司 | Mta協同性之prmt5抑制劑 |
| US20240208912A1 (en) * | 2021-03-11 | 2024-06-27 | Mirati Therapeutics, Inc. | MTA-Cooperative PRMT5 Inhibitors |
| IL307393A (en) * | 2021-04-08 | 2023-12-01 | Mirati Therapeutics Inc | Combination therapies used in PRMT5 inhibitors to treat cancer |
| IL307392A (en) * | 2021-04-08 | 2023-12-01 | Mirati Therapeutics Inc | Combination therapies with PRMT5 inhibitors for cancer treatment |
| EP4347569A4 (en) * | 2021-06-02 | 2025-03-26 | Ideaya Biosciences, Inc. | Combination therapy comprising a mat2a inhibitor and a type ii prmt inhibitor |
| EP4412607A1 (en) | 2021-10-06 | 2024-08-14 | Mirati Therapeutics, Inc. | Combination therapies using prmt5 inhibitors for the treatment of cancer |
| IL311707A (en) | 2021-10-06 | 2024-05-01 | Mirati Therapeutics Inc | Methods for the separation of enantiomers |
| US20260109709A1 (en) | 2021-11-05 | 2026-04-23 | Mirati Therapeutics, Inc. | 2-amino imidazole derivatives as prmt5 inhibitors |
| WO2023098439A1 (zh) * | 2021-11-30 | 2023-06-08 | 上海和誉生物医药科技有限公司 | 一种吡唑衍生物,其制备方法和在药学上的应用 |
| EP4458812A1 (en) * | 2021-12-27 | 2024-11-06 | Medshine Discovery Inc. | Pyrazole-1(2h)-phthalazinone compound and application thereof |
| CN114315735B (zh) * | 2021-12-29 | 2023-08-01 | 广州中医药大学(广州中医药研究院) | 一种鲁米诺酯化衍生物及其制备方法与应用 |
| CN116903611A (zh) * | 2022-01-26 | 2023-10-20 | 上海优理惠生医药有限公司 | 一种酞嗪酮类化合物、其制备方法、包含其药物组合物及其应用 |
| EP4493555A4 (en) * | 2022-03-15 | 2026-03-25 | Beone Medicines I Gmbh | 4-(AMINOMETHYL)-6-(1-METHYL-1H-PYRAZOL-4-YL)ISOQUINOLIN-1(2H)-ONE DERIVATIVES USED AS PRMT5 INHIBITORS COOPERATE WITH MTA |
| WO2023202626A1 (zh) * | 2022-04-22 | 2023-10-26 | 北京望实智慧科技有限公司 | 稠和哒嗪酮化合物作为prmt5抑制剂 |
| CN117843634A (zh) * | 2022-05-24 | 2024-04-09 | 上海美悦生物科技发展有限公司 | Sik抑制剂及其组合物、制备方法和用途 |
| CN116178347B (zh) * | 2022-06-29 | 2025-07-04 | 苏州浦合医药科技有限公司 | Prmt5-mta抑制剂 |
| EP4574816A4 (en) | 2022-07-07 | 2026-01-14 | Xizang Haisco Pharmaceutical Co Ltd | HETEROCYCLIC COMPOUND CAPABLE OF INHIBITING PRMT5 - MTA AND ITS USE |
| CN117430596A (zh) * | 2022-07-13 | 2024-01-23 | 上海海和药物研究开发股份有限公司 | 二并环类mat2a抑制剂及其用途 |
| CN119301101A (zh) * | 2022-07-29 | 2025-01-10 | 四川科伦博泰生物医药股份有限公司 | 甲基吡唑化合物、包含其的药物组合物及其制备方法和用途 |
| CN119585261A (zh) * | 2022-08-02 | 2025-03-07 | 上海艾力斯医药科技股份有限公司 | 一种prmt5抑制剂、其制备方法及应用 |
| CN119730853A (zh) | 2022-08-15 | 2025-03-28 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的mta协同prmt5抑制剂 |
| CN119836290A (zh) | 2022-09-01 | 2025-04-15 | 米拉蒂治疗公司 | 使用prmt5抑制剂和bcl-2家族抑制剂治疗癌症的组合疗法 |
| WO2024091551A1 (en) * | 2022-10-25 | 2024-05-02 | Tango Therapeutics, Inc. | Crystalline forms, pharmaceutical compositions and methods of use thereof |
| EP4628483A1 (en) * | 2022-11-29 | 2025-10-08 | Chia Tai Tianqing Pharmaceutical Group Co., Ltd. | Dihydrophthalazine-containing compound |
| WO2024173215A1 (en) | 2023-02-13 | 2024-08-22 | Mirati Therapeutics, Inc. | Crystalline forms of 2-(4-(4-(aminomethyl)-1-oxo-1,2- dihydrophthalazin-6-yl)-1-methyl-1h- pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile |
| US20240270719A1 (en) | 2023-02-13 | 2024-08-15 | Mirati Therapeutics, Inc. | Crystalline forms of 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile |
| WO2024170488A1 (en) | 2023-02-13 | 2024-08-22 | Astrazeneca Ab | Prmt5 inhibitor for use in cancer therapy |
| EP4665722A1 (en) | 2023-02-13 | 2025-12-24 | Mirati Therapeutics, Inc. | Crystalline forms of 2-(4-(4-(aminomethyl)-1-oxo-1,2-dihydrophthalazin-6-yl)-1-methyl-1h-pyrazol-5-yl)-4-chloro-6-cyclopropoxy-3-fluorobenzonitrile |
| KR102818470B1 (ko) * | 2023-02-23 | 2025-06-10 | 한양대학교 산학협력단 | 신규한 아미노락톤 유도체 및 이의 신규한 제조방법 |
| WO2024220917A1 (en) | 2023-04-21 | 2024-10-24 | Gilead Sciences, Inc. | Prmt5 inhibitors and uses thereof |
| CN121752566A (zh) * | 2023-06-16 | 2026-03-27 | 中山优理生物医药有限公司 | 一种氨基吡啶类化合物、其制备方法、包含其药物组合物及其应用 |
| WO2025016323A1 (zh) | 2023-07-14 | 2025-01-23 | 江苏亚虹医药科技股份有限公司 | 蛋白质精氨酸酶甲基转移酶-5抑制剂及其医药用途 |
| AU2024320474A1 (en) | 2023-08-08 | 2026-03-26 | Mirati Therapeutics, Inc. | Methods and compositions for treating malignant peripheral nerve sheath tumors |
| AU2024319888A1 (en) * | 2023-08-09 | 2026-02-26 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Heteroaryl compound, preparation method therefor, and use thereof in medicine |
| WO2025059579A1 (en) | 2023-09-15 | 2025-03-20 | Ideaya Biosciences, Inc. | Methods of treating mat2a related diseases |
| WO2025064286A1 (en) * | 2023-09-19 | 2025-03-27 | Mirati Therapeutics, Inc. | Stable 4-(aminomethyl)-6-(phenylpyrazolyl)phthalazinone compositions and processes for preparation thereof |
| AU2024344078A1 (en) | 2023-09-20 | 2026-04-02 | Ideaya Biosciences, Inc. | Combination therapy with a parg inhibitor |
| WO2025061102A1 (zh) * | 2023-09-20 | 2025-03-27 | 西藏海思科制药有限公司 | 一种含氰基的杂环化合物及其用途 |
| WO2025072544A1 (en) | 2023-09-27 | 2025-04-03 | Ideaya Biosciences, Inc. | Sulfonamino indazole compounds as inhibitors of parg |
| WO2025068985A1 (en) * | 2023-09-28 | 2025-04-03 | Beigene Switzerland Gmbh | 1-(1-oxo-1,2-dihydrophthalazin-6-yl)cycloalkyl-1-carboxamide derivatives as mta-cooperative inhibitors of prmt5 |
| TW202532064A (zh) * | 2023-11-28 | 2025-08-16 | 大陸商正大天晴藥業集團股份有限公司 | 含有雜環二氫酞嗪的化合物 |
| WO2025180390A1 (zh) * | 2024-02-27 | 2025-09-04 | 烨辉医药科技(上海)有限公司 | 具有四环并环结构的mta协同性prmt5抑制剂化合物 |
| WO2025212574A1 (en) | 2024-04-02 | 2025-10-09 | Mirati Therapeutics, Inc. | Processes for preparation of prmt5 inhibitors and intermediates for making the same |
| WO2025217008A1 (en) | 2024-04-08 | 2025-10-16 | Mirati Therapeutics, Inc. | Combination therapies using prmt5 inhibitors and sos1 inhibitors for the treatment of cancer |
| US20250312343A1 (en) | 2024-04-08 | 2025-10-09 | Mirati Therapeutics, Inc. | Combination therapies using prmt5 inhibitors and kras g12d inhibitors for the treatment of cancer |
| WO2025217007A1 (en) | 2024-04-08 | 2025-10-16 | Mirati Therapeutics, Inc. | Combination therapies using prmt5 inhibitors and immune checkpoint inhibitors for the treatment of cancer |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002006285A1 (en) | 2000-07-17 | 2002-01-24 | Merck Sharp & Dohme Limited | Imidazolophthalazine derivatives as ligands for gabaa receptors |
| JP2005501085A (ja) | 2001-08-07 | 2005-01-13 | フアルマシア・イタリア・エツセ・ピー・アー | キナーゼ阻害剤として活性なアミノフタラジノン誘導体、それらを調製する方法およびそれらを含有する薬剤組成物 |
| WO2017153518A1 (en) | 2016-03-09 | 2017-09-14 | Ctxt Pty Limited | Prmt5 inhibitors |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6919351B2 (en) * | 2000-10-12 | 2005-07-19 | Merck & Co., Inc. | Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors |
| TW202122387A (zh) * | 2019-09-12 | 2021-06-16 | 美商米瑞替療法公司 | Mta協同性之prmt5抑制劑 |
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Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002006285A1 (en) | 2000-07-17 | 2002-01-24 | Merck Sharp & Dohme Limited | Imidazolophthalazine derivatives as ligands for gabaa receptors |
| JP2005501085A (ja) | 2001-08-07 | 2005-01-13 | フアルマシア・イタリア・エツセ・ピー・アー | キナーゼ阻害剤として活性なアミノフタラジノン誘導体、それらを調製する方法およびそれらを含有する薬剤組成物 |
| WO2017153518A1 (en) | 2016-03-09 | 2017-09-14 | Ctxt Pty Limited | Prmt5 inhibitors |
Non-Patent Citations (3)
| Title |
|---|
| Mackanova, M.; Vanags, G.,1-Aminomethyl-4-phthalazone,Zhurnal Obshchei Khimii,1958年,28,2798-2801 |
| Mahmoud, Mahmoud R. et al.,Synthesis and spectral characterisation of some phthalazinone derivatives,Journal of Chemical Research,2012年,36(2),75-82 |
| Puodzhyunas, A. S. et al.,Phthalazine and heterocycles related to it XI. Derivatives of 4-(aminomethyl)-1-phthalazone,Pharmaceutical Chemistry Journal,1973年,7,566-570 |
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| IL313281A (en) | 2024-08-01 |
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| IL290341A (en) | 2022-04-01 |
| AU2020345899A1 (en) | 2022-03-03 |
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| US20230054883A1 (en) | 2023-02-23 |
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| CN120208880A (zh) | 2025-06-27 |
| SA522431915B1 (ar) | 2025-06-12 |
| EP4028388A1 (en) | 2022-07-20 |
| KR20220083691A (ko) | 2022-06-20 |
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