EA201790445A1 - Производные индолинона и их применение - Google Patents

Производные индолинона и их применение

Info

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
Application number
EA201790445A
Other languages
English (en)
Other versions
EA032644B1 (ru
Inventor
Жан-Мишель Вернье
Original Assignee
Онктернал Терапьютикс, Инк.
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Онктернал Терапьютикс, Инк. filed Critical Онктернал Терапьютикс, Инк.
Publication of EA201790445A1 publication Critical patent/EA201790445A1/ru
Publication of EA032644B1 publication Critical patent/EA032644B1/ru

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic 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
    • A61K31/403Heterocyclic 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
    • A61K31/404Indoles, e.g. pindolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/32Oxygen atoms
    • C07D209/34Oxygen atoms in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/32Oxygen atoms
    • C07D209/38Oxygen atoms in positions 2 and 3, e.g. isatin
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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.
EA201790445A 2014-10-09 2015-10-07 Производные индолинона и их применение EA032644B1 (ru)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
AU2020200631B2 (en) 2022-03-24
EP3204376A1 (en) 2017-08-16
CN111777596A (zh) 2020-10-16
CN107108580B (zh) 2020-06-30
EA032644B1 (ru) 2019-06-28
US9604927B2 (en) 2017-03-28
AU2015328121B2 (en) 2019-11-21
IL284322B2 (en) 2023-08-01
IL284322A (en) 2021-07-29
IL284322B1 (en) 2023-04-01
CA2961781A1 (en) 2016-04-14
KR102482197B1 (ko) 2022-12-27
TWI750782B (zh) 2021-12-21
US20160102055A1 (en) 2016-04-14
CN107108580A (zh) 2017-08-29
EP3204376B1 (en) 2023-04-19
US9895352B2 (en) 2018-02-20
KR20170066609A (ko) 2017-06-14
AR102222A1 (es) 2017-02-15
MX2017003589A (es) 2018-08-15
NZ730585A (en) 2018-08-31
AU2015328121A1 (en) 2017-04-06
JP6654197B2 (ja) 2020-02-26
AU2020200631A1 (en) 2020-02-20
TW201629013A (zh) 2016-08-16
IL251498B (en) 2021-07-29
CA2961781C (en) 2023-10-03
IL251498A0 (en) 2017-05-29
US20220288023A1 (en) 2022-09-15
TW202114986A (zh) 2021-04-16
TWI705054B (zh) 2020-09-21
JP2020059736A (ja) 2020-04-16
US9987251B2 (en) 2018-06-05
JP2017532377A (ja) 2017-11-02
US20170066720A1 (en) 2017-03-09
WO2016057698A1 (en) 2016-04-14
US20180256546A1 (en) 2018-09-13
JP6795861B2 (ja) 2020-12-02
US20170065559A1 (en) 2017-03-09

Similar Documents

Publication Publication Date Title
CY1120969T1 (el) Παραγωγα κινοξαλινης χρησιμα ως τροποποιητες fgfr κινασης
EA201692079A1 (ru) Ингибиторы лизин-специфической деметилазы-1
PH12017500509A1 (en) Benzyl substituted indazoles as bub1 inhibitors
EA201891344A1 (ru) Новые агонисты рецептора апелина и способы применения
EA201790445A1 (ru) Производные индолинона и их применение
EA201890749A1 (ru) ИНГИБИТОРЫ АЦЕТИЛ-КоА-КАРБОКСИЛАЗЫ (ACC) И ИХ ПРИМЕНЕНИЕ
EA201792205A1 (ru) Гетероциклические соединения как ингибиторы lsd1
EA201792535A1 (ru) Гетероциклические амиды в качестве ингибиторов киназ
EA201691857A1 (ru) Соединения, применимые в качестве иммуномодуляторов
EA201791867A1 (ru) Бициклические гетероциклы как ингибиторы fgfr4
EA201790395A1 (ru) Производные аминотриазина, подходящие для применения в качестве соединений-ингибиторов tank-связывающей киназы
EA201692513A1 (ru) Ингибиторы лизин-специфической деметилазы-1
EA201790085A1 (ru) Ингибиторы лизин-специфической деметилазы-1
EA201692203A1 (ru) Соединения, ингибирующие tank-связывающую киназу
EA201691302A1 (ru) Новые гетероциклические соединения
EA201691134A1 (ru) Новые ингибиторы глутаминазы
MX2016015565A (es) Ciertos inhibidores de la proteina quinasa.
EA201591420A1 (ru) Гетероарильные соединения и их применение
EA201790376A1 (ru) Ингибиторы лизин-специфической деметилазы-1
EA201891251A1 (ru) Бициклические ингибиторы pad4
EA201790082A1 (ru) Ингибиторы лизин-специфической демитилазы-1
EA201591728A1 (ru) Гетероциклические соединения и способы их применения
CY1125150T1 (el) Ενωσεις φαινυλο-2-υδροξυ-ακετυλαμινο-2-μεθυλο-φαινυλιου
EA201691541A1 (ru) Новые анти-baff антитела
EA201791259A1 (ru) Производные пиперидина в качестве ингибиторов hdac1/2