JP2018531993A5 - - Google Patents
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- Publication number
- JP2018531993A5 JP2018531993A5 JP2018534509A JP2018534509A JP2018531993A5 JP 2018531993 A5 JP2018531993 A5 JP 2018531993A5 JP 2018534509 A JP2018534509 A JP 2018534509A JP 2018534509 A JP2018534509 A JP 2018534509A JP 2018531993 A5 JP2018531993 A5 JP 2018531993A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutical composition
- compound
- substituted
- membered ring
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims description 60
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 56
- 125000005842 heteroatom Chemical group 0.000 claims description 40
- 125000001072 heteroaryl group Chemical group 0.000 claims description 32
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 239000008194 pharmaceutical composition Substances 0.000 claims description 30
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 28
- 125000003118 aryl group Chemical group 0.000 claims description 22
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 20
- 101000615178 Saccharomyces cerevisiae (strain ATCC 204508 / S288c) Serine/threonine-protein kinase SKY1 Proteins 0.000 claims description 16
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 15
- 206010028980 Neoplasm Diseases 0.000 claims description 15
- 201000011510 cancer Diseases 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 208000035475 disorder Diseases 0.000 claims description 14
- 239000000651 prodrug Substances 0.000 claims description 14
- 229940002612 prodrug Drugs 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 14
- 239000012453 solvate Substances 0.000 claims description 14
- 230000033115 angiogenesis Effects 0.000 claims description 13
- 230000002401 inhibitory effect Effects 0.000 claims description 12
- 206010064930 age-related macular degeneration Diseases 0.000 claims description 11
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 10
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims description 10
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims description 10
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 claims description 10
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 claims description 10
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 claims description 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 10
- 229910052736 halogen Inorganic materials 0.000 claims description 10
- 150000002367 halogens Chemical class 0.000 claims description 10
- 230000001404 mediated effect Effects 0.000 claims description 10
- 108091000080 Phosphotransferase Proteins 0.000 claims description 8
- 208000002780 macular degeneration Diseases 0.000 claims description 8
- 102000020233 phosphotransferase Human genes 0.000 claims description 8
- 230000002265 prevention Effects 0.000 claims description 7
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 5
- -1 amino, aminocarbonyl Chemical group 0.000 claims description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
- 125000002541 furyl group Chemical group 0.000 claims description 5
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 5
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 5
- 238000002626 targeted therapy Methods 0.000 claims description 5
- 125000001544 thienyl group Chemical group 0.000 claims description 5
- 125000001425 triazolyl group Chemical group 0.000 claims description 5
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims description 5
- 101000826081 Homo sapiens SRSF protein kinase 1 Proteins 0.000 claims description 4
- 102100023010 SRSF protein kinase 1 Human genes 0.000 claims description 4
- 230000001419 dependent effect Effects 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 101000826077 Homo sapiens SRSF protein kinase 2 Proteins 0.000 claims description 2
- 102100023015 SRSF protein kinase 2 Human genes 0.000 claims description 2
- 125000000539 amino acid group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000002372 labelling Methods 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 31
- 0 CC(N)=CC(*N)=C* Chemical compound CC(N)=CC(*N)=C* 0.000 description 1
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 (3)
| Publication Number | Publication Date |
|---|---|
| JP2018531993A JP2018531993A (ja) | 2018-11-01 |
| JP2018531993A5 true JP2018531993A5 (OSRAM) | 2019-09-12 |
| JP6797923B2 JP6797923B2 (ja) | 2020-12-09 |
Family
ID=58387305
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018534509A Active JP6797923B2 (ja) | 2015-09-23 | 2016-09-23 | Ａｌｋおよびｓｒｐｋ阻害剤ならびに使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US10508082B2 (OSRAM) |
| EP (1) | EP3353150A4 (OSRAM) |
| JP (1) | JP6797923B2 (OSRAM) |
| CN (1) | CN108290835B (OSRAM) |
| HK (1) | HK1257171A1 (OSRAM) |
| WO (1) | WO2017053657A1 (OSRAM) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6797923B2 (ja) | 2015-09-23 | 2020-12-09 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ａｌｋおよびｓｒｐｋ阻害剤ならびに使用方法 |
| 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 |
| KR20230049107A (ko) * | 2020-08-06 | 2023-04-12 | 메르크 파텐트 게엠베하 | 유기 전계 발광 디바이스용 재료 |
| 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 |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201001687A1 (ru) * | 2008-04-29 | 2011-06-30 | Новартис Аг | Производные имидазопиридина в качестве ингибиторов активиноподобной рецепторной киназы ( alk-4 или alk-5 ) |
| TWI624457B (zh) * | 2009-06-10 | 2018-05-21 | 中外製藥股份有限公司 | 四環性化合物 |
| 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 |
| CN104177342B (zh) * | 2013-05-21 | 2018-01-05 | 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 |
| JP6797923B2 (ja) * | 2015-09-23 | 2020-12-09 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Ａｌｋおよびｓｒｐｋ阻害剤ならびに使用方法 |
-
2016
- 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
- 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
-
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
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