CN108290835B - Alk和srpk的抑制剂和使用方法 - Google Patents
Alk和srpk的抑制剂和使用方法 Download PDFInfo
- Publication number
- CN108290835B CN108290835B CN201680068205.0A CN201680068205A CN108290835B CN 108290835 B CN108290835 B CN 108290835B CN 201680068205 A CN201680068205 A CN 201680068205A CN 108290835 B CN108290835 B CN 108290835B
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- Prior art keywords
- compound
- alk
- alkyl
- cancer
- formula
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/80—[b, c]- or [b, d]-condensed
-
- 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
- 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
- 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
-
- 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
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- C07D413/02—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
- 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.)
- C12N9/12—Transferases (2.) transferring phosphorus containing groups, e.g. kinases (2.7)
-
- 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
- C12N9/96—Stabilising an enzyme by forming an adduct or a composition; Forming enzyme conjugates
-
- C—CHEMISTRY; METALLURGY
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12Y—ENZYMES
- C12Y207/00—Transferases transferring phosphorus-containing groups (2.7)
- C12Y207/11—Protein-serine/threonine kinases (2.7.11)
- C12Y207/11001—Non-specific serine/threonine protein kinase (2.7.11.1), i.e. casein kinase or checkpoint kinase
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Genetics & Genomics (AREA)
- Zoology (AREA)
- Wood Science & Technology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Biochemistry (AREA)
- General Engineering & Computer Science (AREA)
- Molecular Biology (AREA)
- Microbiology (AREA)
- Biotechnology (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562222504P | 2015-09-23 | 2015-09-23 | |
| US62/222,504 | 2015-09-23 | ||
| US201662356066P | 2016-06-29 | 2016-06-29 | |
| US62/356,066 | 2016-06-29 | ||
| PCT/US2016/053245 WO2017053657A1 (en) | 2015-09-23 | 2016-09-23 | Inhibitors of alk and srpk and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN108290835A CN108290835A (zh) | 2018-07-17 |
| CN108290835B true CN108290835B (zh) | 2022-03-08 |
Family
ID=58387305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201680068205.0A Expired - Fee Related CN108290835B (zh) | 2015-09-23 | 2016-09-23 | Alk和srpk的抑制剂和使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US10508082B2 (https=) |
| EP (1) | EP3353150A4 (https=) |
| JP (1) | JP6797923B2 (https=) |
| CN (1) | CN108290835B (https=) |
| HK (1) | HK1257171A1 (https=) |
| WO (1) | WO2017053657A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017053657A1 (en) * | 2015-09-23 | 2017-03-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of alk and srpk and methods of use |
| US11179412B2 (en) * | 2017-12-04 | 2021-11-23 | University of Pittsburgh—of the Commonwealth System of Higher Education | Methods of treating conditions involving elevated inflammatory response |
| JP7054134B2 (ja) * | 2017-12-07 | 2022-04-13 | 国立大学法人京都大学 | ベンゾ[b]カルバゾール化合物及びそれを用いたイメージング |
| EP4192832A1 (de) * | 2020-08-06 | 2023-06-14 | Merck Patent GmbH | Materialien für organische elektrolumineszenzvorrichtungen |
| WO2022076409A1 (en) * | 2020-10-06 | 2022-04-14 | Dana-Farber Cancer Institute, Inc. | Potent and selective covalent inhibitors of serine-arginine protein kinase (srpk) 1 and srpk2 and uses thereof |
| CN113135907B (zh) * | 2021-04-28 | 2022-02-22 | 山东大学 | 一种提高α-微管蛋白乙酰化水平的化合物及其制备方法与应用 |
| CN115340523B (zh) * | 2021-05-12 | 2023-12-15 | 盛世泰科生物医药技术(苏州)股份有限公司 | 一种具有alk抑制活性的化合物及其制备方法和用途 |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010143664A1 (ja) * | 2009-06-10 | 2010-12-16 | 中外製薬株式会社 | 4環性化合物 |
| CN102015691A (zh) * | 2008-04-29 | 2011-04-13 | 诺瓦提斯公司 | 作为活化素样受体激酶(alk4或alk5)抑制剂的咪唑并吡啶衍生物 |
| CN104177342A (zh) * | 2013-05-21 | 2014-12-03 | 中国科学院上海药物研究所 | 杂环基取代的吲哚并萘酮衍生物及其医药用途 |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP5006987B2 (ja) * | 2010-11-22 | 2012-08-22 | 中外製薬株式会社 | 4環性化合物を含む医薬 |
| WO2017053657A1 (en) * | 2015-09-23 | 2017-03-30 | Dana-Farber Cancer Institute, Inc. | Inhibitors of alk and srpk and methods of use |
-
2016
- 2016-09-23 WO PCT/US2016/053245 patent/WO2017053657A1/en not_active Ceased
- 2016-09-23 US US15/761,939 patent/US10508082B2/en not_active Expired - Fee Related
- 2016-09-23 JP JP2018534509A patent/JP6797923B2/ja active Active
- 2016-09-23 CN CN201680068205.0A patent/CN108290835B/zh not_active Expired - Fee Related
- 2016-09-23 EP EP16849655.2A patent/EP3353150A4/en not_active Withdrawn
- 2016-09-23 HK HK18116064.7A patent/HK1257171A1/zh unknown
-
2019
- 2019-10-30 US US16/668,484 patent/US11066363B2/en active Active
-
2021
- 2021-06-15 US US17/348,394 patent/US11858897B2/en active Active
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102015691A (zh) * | 2008-04-29 | 2011-04-13 | 诺瓦提斯公司 | 作为活化素样受体激酶(alk4或alk5)抑制剂的咪唑并吡啶衍生物 |
| WO2010143664A1 (ja) * | 2009-06-10 | 2010-12-16 | 中外製薬株式会社 | 4環性化合物 |
| CN104177342A (zh) * | 2013-05-21 | 2014-12-03 | 中国科学院上海药物研究所 | 杂环基取代的吲哚并萘酮衍生物及其医药用途 |
Non-Patent Citations (3)
| Title |
|---|
| "CH5424802, a Selective ALK Inhibitor Capable of Blocking the Resistant Gatekeeper Mutant";Hiroshi Sakamoto等;《Cancer Cell》;20110517;第19卷(第5期);第679-690页 * |
| "Design and synthesis of a highly selective,orally active and potent anaplastic lymphoma kinase inhibitor (CH5424802)";Kazutomo Kinoshita等;《Bioorganic & Medicinal Chemistry》;20111222;第20卷(第3期);第1271-1280页 * |
| "Targeting SRPK1 to control VEGF-mediated tumour angiogenesis in metastatic melanoma";M V Gammons等;《British Journal of Cancer》;20140710;第111卷;第477-485页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3353150A1 (en) | 2018-08-01 |
| CN108290835A (zh) | 2018-07-17 |
| WO2017053657A1 (en) | 2017-03-30 |
| US20180258040A1 (en) | 2018-09-13 |
| EP3353150A4 (en) | 2019-06-19 |
| HK1257171A1 (zh) | 2019-10-18 |
| JP2018531993A (ja) | 2018-11-01 |
| US11066363B2 (en) | 2021-07-20 |
| US11858897B2 (en) | 2024-01-02 |
| US10508082B2 (en) | 2019-12-17 |
| US20200223798A1 (en) | 2020-07-16 |
| JP6797923B2 (ja) | 2020-12-09 |
| US20210340102A1 (en) | 2021-11-04 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PB01 | Publication | ||
| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| CB03 | Change of inventor or designer information | ||
| CB03 | Change of inventor or designer information |
Inventor after: J. Hatcher Inventor after: N.S. Grey Inventor after: Cui Huangen Inventor after: P. Jenny Inventor after: T.Zhang Inventor before: J. Hatcher Inventor before: N.S. Grey Inventor before: H.G.Cui Inventor before: P. Jenny Inventor before: T.Zhang |
|
| GR01 | Patent grant | ||
| GR01 | Patent grant | ||
| CF01 | Termination of patent right due to non-payment of annual fee | ||
| CF01 | Termination of patent right due to non-payment of annual fee |
Granted publication date: 20220308 |