EA201790445A1 - Производные индолинона и их применение - Google Patents
Производные индолинона и их применениеInfo
- Publication number
- EA201790445A1 EA201790445A1 EA201790445A EA201790445A EA201790445A1 EA 201790445 A1 EA201790445 A1 EA 201790445A1 EA 201790445 A EA201790445 A EA 201790445A EA 201790445 A EA201790445 A EA 201790445A EA 201790445 A1 EA201790445 A1 EA 201790445A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- derivatives
- indolinone
- indolinona
- application
- methods
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- 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
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- 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
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/38—Oxygen atoms in positions 2 and 3, e.g. isatin
-
- 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
- C07D401/06—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 only aliphatic carbon atoms
-
- 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
Abstract
Предложены соединения - производные индолинона, которые действуют как ингибиторы фактора транскрипции EWS-FLI1. Также предложены фармацевтические композиции, содержащие такие производные индолинона, способы синтеза производных индолинона, способы лечения с применением производных индолинона и способы анализа для идентификации ингибиторов онкобелка EWS-FLI.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201462062086P | 2014-10-09 | 2014-10-09 | |
PCT/US2015/054533 WO2016057698A1 (en) | 2014-10-09 | 2015-10-07 | Indolinone compounds and uses thereof |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201790445A1 true EA201790445A1 (ru) | 2017-09-29 |
EA032644B1 EA032644B1 (ru) | 2019-06-28 |
Family
ID=54337916
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201790445A EA032644B1 (ru) | 2014-10-09 | 2015-10-07 | Производные индолинона и их применение |
Country Status (14)
Country | Link |
---|---|
US (5) | US9604927B2 (ru) |
EP (1) | EP3204376B1 (ru) |
JP (2) | JP6654197B2 (ru) |
KR (1) | KR102482197B1 (ru) |
CN (2) | CN107108580B (ru) |
AR (1) | AR102222A1 (ru) |
AU (2) | AU2015328121B2 (ru) |
CA (1) | CA2961781C (ru) |
EA (1) | EA032644B1 (ru) |
IL (2) | IL251498B (ru) |
MX (1) | MX2017003589A (ru) |
NZ (1) | NZ730585A (ru) |
TW (2) | TWI750782B (ru) |
WO (1) | WO2016057698A1 (ru) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN107011242B (zh) | 2012-04-12 | 2020-08-07 | 乔治城大学 | 用于治疗尤文肉瘤家族肿瘤的方法和组合物 |
EP3204376B1 (en) | 2014-10-09 | 2023-04-19 | Oncternal Therapeutics, Inc. | Indolinone compounds and uses thereof |
KR102375929B1 (ko) * | 2016-03-31 | 2022-03-16 | 온크터널 테라퓨틱스, 인코포레이티드. | 인돌린 유사체 및 이의 용도 |
EP3490553A4 (en) | 2016-07-29 | 2020-03-25 | Oncternal Therapeutics, Inc. | USE OF INDOLINON COMPOUNDS |
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. |
AU1648600A (en) | 1998-12-04 | 2000-06-26 | Neurosearch A/S | Use of isatin derivatives as ion channel activating agents |
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 |
EP1750776A2 (en) | 2004-04-30 | 2007-02-14 | 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 |
WO2006117414A1 (es) | 2005-04-29 | 2006-11-09 | Proyecto De Biomedicina Cima, S.L. | Modelo animal no humano de sarcoma |
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 |
ES2434693T3 (es) | 2007-04-20 | 2013-12-17 | The Research Foundation For The State University Of New York | Bencimidazoles y composiciones farmacéuticas de los mismos |
US8377992B2 (en) | 2007-10-22 | 2013-02-19 | The Wistar Institute | TRBD-binding effectors and methods for using the same to modulate telomerase activity |
US20110218155A1 (en) * | 2008-10-10 | 2011-09-08 | 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 |
WO2010083505A1 (en) * | 2009-01-19 | 2010-07-22 | 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 |
WO2013151981A1 (en) | 2012-04-02 | 2013-10-10 | Gradalis, Inc. | Ewing's sarcoma bifunctional shrna design |
CN107011242B (zh) | 2012-04-12 | 2020-08-07 | 乔治城大学 | 用于治疗尤文肉瘤家族肿瘤的方法和组合物 |
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 |
WO2014160183A1 (en) * | 2013-03-13 | 2014-10-02 | 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 |
KR20160065986A (ko) | 2013-10-24 | 2016-06-09 | 조지타운 유니버시티 | 암 치료용 방법 및 조성물 |
EP3077384B1 (en) | 2013-12-05 | 2017-09-06 | F. Hoffmann-La Roche AG | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
US9737535B2 (en) | 2014-04-16 | 2017-08-22 | Signal Pharmaceuticals, Llc | Methods for treating cancer using TOR kinase inhibitor combination therapy comprising administering substituted pyrazino[2,3-b]pyrazines |
EP3204376B1 (en) | 2014-10-09 | 2023-04-19 | Oncternal Therapeutics, Inc. | Indolinone compounds and uses thereof |
KR102375929B1 (ko) | 2016-03-31 | 2022-03-16 | 온크터널 테라퓨틱스, 인코포레이티드. | 인돌린 유사체 및 이의 용도 |
EP3490553A4 (en) * | 2016-07-29 | 2020-03-25 | Oncternal Therapeutics, Inc. | USE OF INDOLINON COMPOUNDS |
-
2015
- 2015-10-07 EP EP15784237.8A patent/EP3204376B1/en active Active
- 2015-10-07 CN CN201580054973.6A patent/CN107108580B/zh active Active
- 2015-10-07 WO PCT/US2015/054533 patent/WO2016057698A1/en active Application Filing
- 2015-10-07 EA EA201790445A patent/EA032644B1/ru unknown
- 2015-10-07 JP JP2017538916A patent/JP6654197B2/ja active Active
- 2015-10-07 KR KR1020177012523A patent/KR102482197B1/ko active IP Right Grant
- 2015-10-07 US US14/877,708 patent/US9604927B2/en active Active
- 2015-10-07 NZ NZ730585A patent/NZ730585A/en unknown
- 2015-10-07 AU AU2015328121A patent/AU2015328121B2/en active Active
- 2015-10-07 MX MX2017003589A patent/MX2017003589A/es unknown
- 2015-10-07 CN CN202010495279.0A patent/CN111777596A/zh active Pending
- 2015-10-07 CA CA2961781A patent/CA2961781C/en active Active
- 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
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2016
- 2016-11-21 US US15/357,876 patent/US9987251B2/en active Active
- 2016-11-21 US US15/357,933 patent/US9895352B2/en active Active
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2017
- 2017-04-02 IL IL251498A patent/IL251498B/en unknown
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2018
- 2018-05-07 US US15/973,110 patent/US20180256546A1/en not_active Abandoned
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2019
- 2019-12-11 JP JP2019223835A patent/JP6795861B2/ja active Active
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2020
- 2020-01-29 AU AU2020200631A patent/AU2020200631B2/en active Active
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2021
- 2021-06-23 IL IL284322A patent/IL284322B2/en unknown
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2022
- 2022-06-02 US US17/830,668 patent/US20220288023A1/en active Pending
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