JP2017532377A5 - - Google Patents
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- Publication number
- JP2017532377A5 JP2017532377A5 JP2017538916A JP2017538916A JP2017532377A5 JP 2017532377 A5 JP2017532377 A5 JP 2017532377A5 JP 2017538916 A JP2017538916 A JP 2017538916A JP 2017538916 A JP2017538916 A JP 2017538916A JP 2017532377 A5 JP2017532377 A5 JP 2017532377A5
- Authority
- JP
- Japan
- Prior art keywords
- hours
- dichloro
- hydroxyindoline
- oxoethyl
- formula
- 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 4
- 101150025421 ETS gene Proteins 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 9
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- MWAUGZLJRYZZBX-UHFFFAOYSA-N 3-[2-[4-(azetidin-1-yl)phenyl]-2-oxoethyl]-4,7-dichloro-3-hydroxy-1H-indol-2-one Chemical compound N1(CCC1)C1=CC=C(C=C1)C(CC1(C(NC2=C(C=CC(=C12)Cl)Cl)=O)O)=O MWAUGZLJRYZZBX-UHFFFAOYSA-N 0.000 description 2
- XOLOINUNYGPTGM-UHFFFAOYSA-N 3-[2-[4-(aziridin-1-yl)phenyl]-2-oxoethyl]-4,7-dichloro-3-hydroxy-1H-indol-2-one Chemical compound N1(CC1)C1=CC=C(C=C1)C(CC1(C(NC2=C(C=CC(=C12)Cl)Cl)=O)O)=O XOLOINUNYGPTGM-UHFFFAOYSA-N 0.000 description 2
- FDPMWMDIYFGVKV-UHFFFAOYSA-N 4,7-dichloro-3-[2-(4-cyclopropyl-2-fluorophenyl)-2-oxoethyl]-3-hydroxy-1H-indol-2-one Chemical compound ClC1=C2C(C(NC2=C(C=C1)Cl)=O)(O)CC(=O)C1=C(C=C(C=C1)C1CC1)F FDPMWMDIYFGVKV-UHFFFAOYSA-N 0.000 description 2
- GRWSVPKRYXCYOR-UHFFFAOYSA-N 4,7-dichloro-3-[2-(4-cyclopropyl-3-fluorophenyl)-2-oxoethyl]-3-hydroxy-1H-indol-2-one Chemical compound ClC1=C2C(C(NC2=C(C=C1)Cl)=O)(O)CC(=O)C1=CC(=C(C=C1)C1CC1)F GRWSVPKRYXCYOR-UHFFFAOYSA-N 0.000 description 2
- ZWHNLSHDLKIXOG-UHFFFAOYSA-N 4,7-dichloro-3-[2-(4-cyclopropylphenyl)-2-oxoethyl]-3-hydroxy-1H-indol-2-one Chemical compound ClC1=C2C(C(NC2=C(C=C1)Cl)=O)(O)CC(=O)C1=CC=C(C=C1)C1CC1 ZWHNLSHDLKIXOG-UHFFFAOYSA-N 0.000 description 2
- GPQBOHJABMHCFO-UHFFFAOYSA-N 4,7-dichloro-3-hydroxy-3-[2-oxo-2-(4-pyrrolidin-1-ylphenyl)ethyl]-1H-indol-2-one Chemical compound ClC1=C2C(C(NC2=C(C=C1)Cl)=O)(CC(C1=CC=C(C=C1)N1CCCC1)=O)O GPQBOHJABMHCFO-UHFFFAOYSA-N 0.000 description 2
- 238000002347 injection Methods 0.000 description 2
- 239000007924 injection Substances 0.000 description 2
- JXDYKVIHCLTXOP-UHFFFAOYSA-N isatin Chemical class C1=CC=C2C(=O)C(=O)NC2=C1 JXDYKVIHCLTXOP-UHFFFAOYSA-N 0.000 description 2
- 150000002576 ketones Chemical class 0.000 description 2
- 230000008878 coupling Effects 0.000 description 1
- 238000010168 coupling process Methods 0.000 description 1
- 238000005859 coupling reaction Methods 0.000 description 1
- HPNMFZURTQLUMO-UHFFFAOYSA-N diethylamine Chemical compound CCNCC HPNMFZURTQLUMO-UHFFFAOYSA-N 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 238000003818 flash chromatography Methods 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000000425 proton nuclear magnetic resonance spectrum Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000011541 reaction mixture Substances 0.000 description 1
- 238000001953 recrystallisation Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462062086P | 2014-10-09 | 2014-10-09 | |
| US62/062,086 | 2014-10-09 | ||
| PCT/US2015/054533 WO2016057698A1 (en) | 2014-10-09 | 2015-10-07 | Indolinone compounds and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019223835A Division JP6795861B2 (ja) | 2014-10-09 | 2019-12-11 | インドリノン化合物及びその使用 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017532377A JP2017532377A (ja) | 2017-11-02 |
| JP2017532377A5 true JP2017532377A5 (https=) | 2018-09-13 |
| JP6654197B2 JP6654197B2 (ja) | 2020-02-26 |
Family
ID=54337916
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017538916A Active JP6654197B2 (ja) | 2014-10-09 | 2015-10-07 | インドリノン化合物及びその使用 |
| JP2019223835A Active JP6795861B2 (ja) | 2014-10-09 | 2019-12-11 | インドリノン化合物及びその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019223835A Active JP6795861B2 (ja) | 2014-10-09 | 2019-12-11 | インドリノン化合物及びその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (6) | US9604927B2 (https=) |
| EP (1) | EP3204376B1 (https=) |
| JP (2) | JP6654197B2 (https=) |
| KR (1) | KR102482197B1 (https=) |
| CN (2) | CN107108580B (https=) |
| AR (1) | AR102222A1 (https=) |
| AU (2) | AU2015328121B2 (https=) |
| CA (1) | CA2961781C (https=) |
| EA (1) | EA032644B1 (https=) |
| IL (2) | IL251498B (https=) |
| MX (1) | MX388564B (https=) |
| NZ (1) | NZ730585A (https=) |
| TW (2) | TWI750782B (https=) |
| WO (1) | WO2016057698A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2869513C (en) | 2012-04-12 | 2020-07-07 | Georgetown University | Methods and compositions for treating ewings sarcoma family of tumors |
| EP3204376B1 (en) * | 2014-10-09 | 2023-04-19 | Oncternal Therapeutics, Inc. | Indolinone compounds and uses thereof |
| EP3795563B1 (en) * | 2016-03-31 | 2024-07-17 | Oncternal Therapeutics, Inc. | Indoline analogs and uses thereof |
| CA3029851A1 (en) * | 2016-07-29 | 2018-02-01 | Oncternal Therapeutics, Inc. | Uses of indoline compounds such as tk216 for the treatment of cancer |
| CN110818611B (zh) * | 2018-08-13 | 2023-01-24 | 中国科学院上海药物研究所 | 一类吲哚酮类化合物、其制备方法、药物组合物和用途 |
| US20240139153A1 (en) * | 2020-09-17 | 2024-05-02 | Oklahoma Medical Research Foundation | Inhibition of Endothelial ETS Family Transcription Factors Promotes Flow-Dependent Ocular Vessel Regression |
| CN113456631B (zh) * | 2021-08-06 | 2022-06-21 | 徐州医科大学 | 一种靶向acsl1的小分子药物及其在治疗子宫内膜癌中的应用 |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE3483704D1 (de) | 1983-07-22 | 1991-01-17 | Du Pont | Phenylchinolinsaeure und derivate als antitumormittel. |
| DE69922997T2 (de) | 1998-12-04 | 2005-12-15 | Neurosearch A/S | Verwendung von isatinderivaten als ionenkanalaktivierende mittel |
| CN1155572C (zh) | 2001-01-19 | 2004-06-30 | 中国人民解放军军事医学科学院毒物药物研究所 | 吲哚类衍生物及其抗肿瘤用途 |
| US20030157486A1 (en) | 2001-06-21 | 2003-08-21 | Graff Jonathan M. | Methods to identify signal sequences |
| AU2005323437B2 (en) | 2004-04-30 | 2011-10-06 | Alnylam Pharmaceuticals, Inc. | Oligonucleotides comprising a C5-modified pyrimidine |
| AR056317A1 (es) * | 2005-04-20 | 2007-10-03 | Xenon Pharmaceuticals Inc | Compuestos de oxindol y composicion farmaceutica |
| US20090217390A1 (en) | 2005-04-29 | 2009-08-27 | Fernando Lecanda Cordero | Non-human animal sarcoma model |
| WO2008046083A2 (en) | 2006-10-12 | 2008-04-17 | Xenon Pharmaceuticals Inc. | Use of oxindole compounds as therapeutic agents |
| CA2953987A1 (en) | 2006-12-29 | 2008-07-10 | Georgetown University | Targeting of ews-fli1 as anti-tumor therapy |
| US8232310B2 (en) | 2006-12-29 | 2012-07-31 | Georgetown University | Targeting of EWS-FLI1 as anti-tumor therapy |
| HRP20131103T1 (hr) | 2007-04-20 | 2013-12-20 | The Research Foundation Of State University Of New York | Benzimidazoli i njihovi farmaceutski pripravci |
| US8377992B2 (en) | 2007-10-22 | 2013-02-19 | The Wistar Institute | TRBD-binding effectors and methods for using the same to modulate telomerase activity |
| EP3401684B1 (en) * | 2008-10-10 | 2022-03-16 | Dana Farber Cancer Institute, Inc. | Chemical modulators of pro-apoptotic bax and bcl-2 polypeptides |
| EP3090737A1 (en) | 2008-10-21 | 2016-11-09 | Onyx Therapeutics, Inc. | Combination therapy with peptide epoxyketones |
| US8710068B2 (en) * | 2009-01-19 | 2014-04-29 | The Trustees Of The University Of Pennsylvania | Method of treating cancer using a survivin inhibitor |
| WO2012078519A2 (en) | 2010-12-06 | 2012-06-14 | Numerate, Inc. | 3-acylidene-2-oxoindole derivatives for inhibition of transglutaminase 2 |
| CN102516152B (zh) | 2011-12-12 | 2014-12-10 | 华东师范大学 | 一种α-二氟羰基取代的手性叔醇类化合物及其合成方法和应用 |
| US20130259927A1 (en) | 2012-04-02 | 2013-10-03 | Gradalis, Inc. | Ewing's Sarcoma Bifunctional shRNA Design |
| CA2869513C (en) * | 2012-04-12 | 2020-07-07 | Georgetown University | Methods and compositions for treating ewings sarcoma family of tumors |
| WO2014015153A2 (en) | 2012-07-20 | 2014-01-23 | Star Biotechnology, Llc | Compositions and methods for treating ewing's sarcoma and other disorders related to ews-fli1 |
| AU2014244083B2 (en) * | 2013-03-13 | 2018-09-27 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Methods for modulating chemotherapeutic cytotoxicity |
| CN103435606A (zh) * | 2013-08-22 | 2013-12-11 | 中国药科大学 | CDK2与GSK3β双重抑制剂及用途 |
| CN103613580B (zh) * | 2013-09-03 | 2016-02-10 | 遵义医学院 | 用于抗肿瘤药物的3-羟基吲哚-2-酮类化合物或其药学上能够接受的盐 |
| CN105848654B (zh) | 2013-10-24 | 2018-10-02 | 乔治城大学 | 用于治疗癌症的方法和组合物 |
| WO2015082583A1 (en) | 2013-12-05 | 2015-06-11 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
| ES2823756T3 (es) | 2014-04-16 | 2021-05-10 | Signal Pharm Llc | Métodos para tratar el cáncer usando terapia de combinación de inhibidores de quinasa TOR |
| EP3204376B1 (en) | 2014-10-09 | 2023-04-19 | Oncternal Therapeutics, Inc. | Indolinone compounds and uses thereof |
| EP3795563B1 (en) | 2016-03-31 | 2024-07-17 | Oncternal Therapeutics, Inc. | Indoline analogs and uses thereof |
| CA3029851A1 (en) * | 2016-07-29 | 2018-02-01 | Oncternal Therapeutics, Inc. | Uses of indoline compounds such as tk216 for the treatment of cancer |
-
2015
- 2015-10-07 EP EP15784237.8A patent/EP3204376B1/en active Active
- 2015-10-07 KR KR1020177012523A patent/KR102482197B1/ko active Active
- 2015-10-07 NZ NZ730585A patent/NZ730585A/en unknown
- 2015-10-07 MX MX2017003589A patent/MX388564B/es unknown
- 2015-10-07 EA EA201790445A patent/EA032644B1/ru unknown
- 2015-10-07 JP JP2017538916A patent/JP6654197B2/ja active Active
- 2015-10-07 AU AU2015328121A patent/AU2015328121B2/en active Active
- 2015-10-07 CN CN201580054973.6A patent/CN107108580B/zh active Active
- 2015-10-07 WO PCT/US2015/054533 patent/WO2016057698A1/en not_active Ceased
- 2015-10-07 CN CN202010495279.0A patent/CN111777596A/zh active Pending
- 2015-10-07 CA CA2961781A patent/CA2961781C/en active Active
- 2015-10-07 US US14/877,708 patent/US9604927B2/en active Active - Reinstated
- 2015-10-08 TW TW109129160A patent/TWI750782B/zh active
- 2015-10-08 TW TW104133287A patent/TWI705054B/zh active
- 2015-10-09 AR ARP150103264A patent/AR102222A1/es unknown
-
2016
- 2016-11-21 US US15/357,933 patent/US9895352B2/en active Active
- 2016-11-21 US US15/357,876 patent/US9987251B2/en active Active
-
2017
- 2017-04-02 IL IL251498A patent/IL251498B/en unknown
-
2018
- 2018-05-07 US US15/973,110 patent/US20180256546A1/en not_active Abandoned
-
2019
- 2019-12-11 JP JP2019223835A patent/JP6795861B2/ja active Active
-
2020
- 2020-01-29 AU AU2020200631A patent/AU2020200631B2/en active Active
-
2021
- 2021-06-23 IL IL284322A patent/IL284322B2/en unknown
-
2022
- 2022-06-02 US US17/830,668 patent/US20220288023A1/en not_active Abandoned
-
2025
- 2025-09-22 US US19/335,663 patent/US20260076941A1/en active Pending
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