JP6882289B2 - 二環式ｂｅｔブロモドメイン阻害剤及びその使用 - Google Patents
二環式ｂｅｔブロモドメイン阻害剤及びその使用 Download PDFInfo
- Publication number
- JP6882289B2 JP6882289B2 JP2018527799A JP2018527799A JP6882289B2 JP 6882289 B2 JP6882289 B2 JP 6882289B2 JP 2018527799 A JP2018527799 A JP 2018527799A JP 2018527799 A JP2018527799 A JP 2018527799A JP 6882289 B2 JP6882289 B2 JP 6882289B2
- Authority
- JP
- Japan
- Prior art keywords
- quinazoline
- dimethylisoxazole
- chlorobenzyl
- mmol
- alkyl
- 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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Links
- 0 CN1CC(*)N(C)CC1 Chemical compound CN1CC(*)N(C)CC1 0.000 description 13
- OIYANYVIFQBNMS-UHFFFAOYSA-N CN(CCOC1)C1c1ccccc1 Chemical compound CN(CCOC1)C1c1ccccc1 OIYANYVIFQBNMS-UHFFFAOYSA-N 0.000 description 2
- OFFDUUOWWOMBOT-UHFFFAOYSA-N CNC(C1CCN(C)CC1)=O Chemical compound CNC(C1CCN(C)CC1)=O OFFDUUOWWOMBOT-UHFFFAOYSA-N 0.000 description 2
- SLQKSHVEUFFIRR-UHFFFAOYSA-N CNCN(CC1)CCC1C(O)=O Chemical compound CNCN(CC1)CCC1C(O)=O SLQKSHVEUFFIRR-UHFFFAOYSA-N 0.000 description 2
- WNPSWENOMUBHOP-UHFFFAOYSA-N CS(N(CC1)CC(c2ccccc2)N1N=C)(=O)=O Chemical compound CS(N(CC1)CC(c2ccccc2)N1N=C)(=O)=O WNPSWENOMUBHOP-UHFFFAOYSA-N 0.000 description 2
Classifications
-
- 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
-
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- 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
-
- 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
-
- 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
-
- 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
-
- 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
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- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Toxicology (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Molecular Biology (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pyridine Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021078741A JP7112567B2 (ja) | 2015-11-25 | 2021-05-06 | 二環式ｂｅｔブロモドメイン阻害剤及びその使用 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562259894P | 2015-11-25 | 2015-11-25 | |
| US62/259,894 | 2015-11-25 | ||
| PCT/US2016/063485 WO2017091661A1 (en) | 2015-11-25 | 2016-11-23 | Bicyclic bet bromodomain inhibitors and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021078741A Division JP7112567B2 (ja) | 2015-11-25 | 2021-05-06 | 二環式ｂｅｔブロモドメイン阻害剤及びその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019501140A JP2019501140A (ja) | 2019-01-17 |
| JP2019501140A5 JP2019501140A5 (OSRAM) | 2020-01-09 |
| JP6882289B2 true JP6882289B2 (ja) | 2021-06-02 |
Family
ID=57543210
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018527799A Active JP6882289B2 (ja) | 2015-11-25 | 2016-11-23 | 二環式ｂｅｔブロモドメイン阻害剤及びその使用 |
| JP2021078741A Active JP7112567B2 (ja) | 2015-11-25 | 2021-05-06 | 二環式ｂｅｔブロモドメイン阻害剤及びその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021078741A Active JP7112567B2 (ja) | 2015-11-25 | 2021-05-06 | 二環式ｂｅｔブロモドメイン阻害剤及びその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US10508106B2 (OSRAM) |
| EP (2) | EP4050005B1 (OSRAM) |
| JP (2) | JP6882289B2 (OSRAM) |
| CN (2) | CN109641886B (OSRAM) |
| AU (3) | AU2016361441B2 (OSRAM) |
| CA (1) | CA3006300C (OSRAM) |
| ES (2) | ES2918589T3 (OSRAM) |
| WO (1) | WO2017091661A1 (OSRAM) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108314680A (zh) * | 2017-01-16 | 2018-07-24 | 凯惠科技发展(上海)有限公司 | 一种含芳环化合物、其制备方法、药物组合物及应用 |
| CN109111426B (zh) * | 2017-06-23 | 2021-12-14 | 中国科学院上海药物研究所 | 一类稠合双环杂芳基或芳基化合物，及其用途 |
| WO2019201296A1 (zh) * | 2018-04-18 | 2019-10-24 | 南京明德新药研发有限公司 | 作为rho激酶抑制剂的吡唑类化合物 |
| EP3620164A1 (en) * | 2018-09-05 | 2020-03-11 | Genoscience Pharma SAS | Substituted 2,4 diamino-quinoline as new medicament for fibrosis, autophagy and cathepsins b (ctsb), l (ctsl) and d (ctsd) related diseases |
| US12497395B2 (en) * | 2019-04-24 | 2025-12-16 | Convergene, Llc | Small molecule bromodomain inhibitors and uses therof |
| US20230212169A9 (en) * | 2019-05-31 | 2023-07-06 | Chiesi Farmaceutici S.P.A. | Pyridopyrimidines derivatives as p2x3 inhibitors |
| JP7644029B2 (ja) * | 2019-05-31 | 2025-03-11 | キエシ・フアルマチエウテイチ・ソチエタ・ペル・アチオニ | Ｐ２ｘ３阻害剤としてのアミノキナゾリン誘導体 |
| US20240336606A1 (en) * | 2020-10-20 | 2024-10-10 | Suzhou Zelgen Biopharmaceuticals Co., Ltd. | Substituted benzo or pyridopyrimidine amine inhibitor, preparation method therefor, and application thereof |
| CN117279914A (zh) * | 2021-01-29 | 2023-12-22 | 南京再明医药有限公司 | Sos1抑制剂及其制备方法和应用 |
| WO2022171018A1 (zh) * | 2021-02-09 | 2022-08-18 | 苏州泽璟生物制药股份有限公司 | 取代苯并或吡啶并嘧啶胺类抑制剂及其制备方法和应用 |
| CA3211053A1 (en) * | 2021-02-11 | 2022-08-18 | The Medical College Of Wisconsin, Inc. | Small molecule inhibitors of pbrm1-bd2 |
| JP2024511507A (ja) * | 2021-03-26 | 2024-03-13 | メッドシャイン ディスカバリー インコーポレイテッド | ６－カルバメート置換複素芳香環誘導体 |
| TW202416953A (zh) * | 2022-08-26 | 2024-05-01 | 日商衛材R&D企管股份有限公司 | 抗體藥物複合物 |
| WO2024235225A1 (zh) * | 2023-05-15 | 2024-11-21 | 苏州泽璟生物制药股份有限公司 | 取代嘧啶并环类抑制剂及其制备方法和应用 |
| WO2025209570A1 (zh) * | 2024-04-03 | 2025-10-09 | 北京大学 | Bet抑制剂及其应用 |
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2016
- 2016-11-23 EP EP22162126.1A patent/EP4050005B1/en active Active
- 2016-11-23 EP EP16810193.9A patent/EP3380469B1/en active Active
- 2016-11-23 ES ES16810193T patent/ES2918589T3/es active Active
- 2016-11-23 CN CN201680079771.1A patent/CN109641886B/zh active Active
- 2016-11-23 US US15/779,353 patent/US10508106B2/en active Active
- 2016-11-23 WO PCT/US2016/063485 patent/WO2017091661A1/en not_active Ceased
- 2016-11-23 ES ES22162126T patent/ES3011058T3/es active Active
- 2016-11-23 CA CA3006300A patent/CA3006300C/en active Active
- 2016-11-23 JP JP2018527799A patent/JP6882289B2/ja active Active
- 2016-11-23 CN CN202211334125.9A patent/CN115806550B/zh active Active
- 2016-11-23 AU AU2016361441A patent/AU2016361441B2/en active Active
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2019
- 2019-11-15 US US16/685,128 patent/US11028079B2/en active Active
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2021
- 2021-05-06 JP JP2021078741A patent/JP7112567B2/ja active Active
- 2021-07-28 AU AU2021209257A patent/AU2021209257B2/en active Active
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| AU2016361441B2 (en) | 2021-08-12 |
| CN115806550B (zh) | 2025-11-28 |
| CA3006300A1 (en) | 2017-06-01 |
| ES2918589T3 (es) | 2022-07-19 |
| US20200223836A1 (en) | 2020-07-16 |
| AU2016361441A1 (en) | 2018-06-21 |
| CN109641886A (zh) | 2019-04-16 |
| JP7112567B2 (ja) | 2022-08-03 |
| US11028079B2 (en) | 2021-06-08 |
| CN109641886B (zh) | 2022-11-18 |
| JP2019501140A (ja) | 2019-01-17 |
| AU2021209257A1 (en) | 2021-08-19 |
| WO2017091661A1 (en) | 2017-06-01 |
| CA3006300C (en) | 2024-02-27 |
| EP4050005B1 (en) | 2024-12-25 |
| AU2024201890A1 (en) | 2024-05-16 |
| AU2021209257B2 (en) | 2023-12-21 |
| ES3011058T3 (en) | 2025-04-07 |
| CN115806550A (zh) | 2023-03-17 |
| US10508106B2 (en) | 2019-12-17 |
| EP3380469A1 (en) | 2018-10-03 |
| JP2021119188A (ja) | 2021-08-12 |
| US20180305344A1 (en) | 2018-10-25 |
| EP3380469B1 (en) | 2022-03-16 |
| EP4050005A1 (en) | 2022-08-31 |
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