EA201490707A1 - Макроциклические ингибиторы flt3-киназы - Google Patents

Макроциклические ингибиторы flt3-киназы

Info

Publication number
EA201490707A1
EA201490707A1 EA201490707A EA201490707A EA201490707A1 EA 201490707 A1 EA201490707 A1 EA 201490707A1 EA 201490707 A EA201490707 A EA 201490707A EA 201490707 A EA201490707 A EA 201490707A EA 201490707 A1 EA201490707 A1 EA 201490707A1
Authority
EA
Eurasian Patent Office
Prior art keywords
flt3 kinase
macro cyclic
cyclic inhibitors
compounds
present
Prior art date
Application number
EA201490707A
Other languages
English (en)
Other versions
EA025881B1 (ru
Inventor
Петра Марселла Франсуаза Блом
Ян Мари Сирил Йозеф Хофлак
Original Assignee
Онкодизайн С.А.
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 Онкодизайн С.А. filed Critical Онкодизайн С.А.
Publication of EA201490707A1 publication Critical patent/EA201490707A1/ru
Publication of EA025881B1 publication Critical patent/EA025881B1/ru

Links

Classifications

    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K31/535—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
    • A61P35/00—Antineoplastic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
    • C07D487/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Настоящее изобретение относится к макроциклическим соединениям и композициям, содержащим указанные соединения, действующим в качестве ингибиторов киназ, в частности в качестве ингибиторов FLT3 (FMS-родственной тирозинкиназы 3). Более того, настоящее изобретение предусматривает способы получения раскрытых соединений, а также способы их применения, к примеру, в качестве медикамента, в частности, для лечения клеточных пролиферативных нарушений, таких как рак.
EA201490707A 2011-09-30 2012-09-28 Макроциклические ингибиторы flt3-киназы EA025881B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2011067084 2011-09-30
PCT/EP2012/069252 WO2013045653A1 (en) 2011-09-30 2012-09-28 Macrocyclic flt3 kinase inhibitors

Publications (2)

Publication Number Publication Date
EA201490707A1 true EA201490707A1 (ru) 2014-08-29
EA025881B1 EA025881B1 (ru) 2017-02-28

Family

ID=46980944

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201490707A EA025881B1 (ru) 2011-09-30 2012-09-28 Макроциклические ингибиторы flt3-киназы

Country Status (14)

Country Link
US (2) US9090630B2 (ru)
JP (1) JP6046728B2 (ru)
KR (1) KR20140078710A (ru)
CN (1) CN103930427B (ru)
AU (1) AU2012314376B2 (ru)
BR (1) BR112014007622A2 (ru)
CA (1) CA2849999A1 (ru)
DK (1) DK2760867T3 (ru)
EA (1) EA025881B1 (ru)
ES (1) ES2569048T3 (ru)
HK (1) HK1198764A1 (ru)
HU (1) HUE027318T2 (ru)
MX (1) MX347765B (ru)
WO (1) WO2013045653A1 (ru)

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6082397B2 (ja) * 2011-09-30 2017-02-15 イプセン ファルマ ソシエテ パール アクシオン サンプリフィエＩｐｓｅｎ Ｐｈａｒｍａ Ｓ．Ａ．Ｓ． マクロ環状ｌｒｒｋ２キナーゼ阻害剤
GB201204384D0 (en) 2012-03-13 2012-04-25 Univ Dundee Anti-flammatory agents
KR20150133765A (ko) * 2013-03-15 2015-11-30 온코디자인 에스.에이. 거대고리 rip2 키나제 억제제
CN105209040A (zh) * 2013-03-15 2015-12-30 昂科迪塞恩股份有限公司 大环的盐可诱导的激酶抑制剂
AU2014230485A1 (en) * 2013-03-15 2015-09-24 Oncodesign S.A. Macrocyclic LRRK2 kinase inhibitors
US9861635B2 (en) * 2013-05-06 2018-01-09 Merck Patent Gmbh Macrocycles as kinase inhibitors
HRP20221518T1 (hr) 2014-01-24 2023-02-17 Turning Point Therapeutics, Inc. Diaril makrociklični spojevi kao modulatori protein kinaza
WO2015136073A1 (en) * 2014-03-14 2015-09-17 Oncodesign Sa Macrocyclic tgf-br2 kinase inhibitors
US10287268B2 (en) 2014-07-21 2019-05-14 Dana-Farber Cancer Institute, Inc. Imidazolyl kinase inhibitors and uses thereof
DK3172213T3 (da) * 2014-07-21 2021-12-13 Dana Farber Cancer Inst Inc Makrocykliske kinasehæmmere og anvendelser deraf
WO2016023014A2 (en) 2014-08-08 2016-02-11 Dana-Farber Cancer Institute, Inc. Uses of salt-inducible kinase (sik) inhibitors
JP6736545B2 (ja) * 2014-09-17 2020-08-05 オンコデザイン エス．ア． 大環状ｒｉｐ２キナーゼ阻害剤
BR112017005299A2 (pt) * 2014-09-17 2017-12-12 Ipsen Pharma Sas inibidores de lrrk2 cinase macrocíclicos
WO2016146651A1 (en) 2015-03-16 2016-09-22 Oncodesign Sa Macrocyclic activin-like receptor kinase inhibitors
MX2017017097A (es) 2015-07-02 2018-05-23 Tp Therapeutics Inc Macrociclos diarílicos quirales como moduladores de proteínas quinasas.
PT3319969T (pt) 2015-07-06 2024-06-17 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
RU2020123800A (ru) 2015-07-21 2020-10-02 Тёрнинг Поинт Терапьютикс, Инк. Хиральные диарильные макроциклы и их применение
RU2630958C2 (ru) * 2015-12-29 2017-09-15 федеральное государственное автономное образовательное учреждение высшего образования "Московский физико-технический институт (государственный университет)" (МФТИ) Новые макроциклические соединения, содержащие природное 3,7-диазабицикло[3.3.1]нонановое ядро и способ их получения
US10954242B2 (en) 2016-07-05 2021-03-23 The Broad Institute, Inc. Bicyclic urea kinase inhibitors and uses thereof
BR112019001607A2 (pt) 2016-07-28 2019-04-30 Tp Therapeutics, Inc. inibidores macrocíclicos de quinases
US11241435B2 (en) 2016-09-16 2022-02-08 The General Hospital Corporation Uses of salt-inducible kinase (SIK) inhibitors for treating osteoporosis
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
BR112019017741A2 (pt) 2017-02-28 2020-04-07 Dana Farber Cancer Inst Inc usos de pirimidopirimidinonas como inibidores de sik
PT3658148T (pt) 2017-07-28 2024-08-26 Turning Point Therapeutics Inc Compostos macrocíclicos e utilizações dos mesmos
MX2020006490A (es) 2017-12-19 2020-08-17 Turning Point Therapeutics Inc Compuestos macrociclicos para tratar enfermedades.
CN110950889B (zh) * 2018-09-27 2022-04-05 北京赛林泰医药技术有限公司 一种多靶点激酶抑制剂及其制备方法和用途
KR20220133869A (ko) 2019-12-03 2022-10-05 터닝 포인트 테라퓨틱스, 인크. 질환 치료에 사용하기 위한 거대고리

Family Cites Families (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IS2334B (is) 1992-09-08 2008-02-15 Vertex Pharmaceuticals Inc., (A Massachusetts Corporation) Aspartyl próteasi hemjari af nýjum flokki súlfonamíða
IL111080A (en) 1993-10-01 1999-08-17 Astra Ab Method for treating a finely divided powder medicament
US6043358A (en) 1995-11-01 2000-03-28 Merck & Co., Inc. Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
GB9718913D0 (en) 1997-09-05 1997-11-12 Glaxo Group Ltd Substituted oxindole derivatives
US6369087B1 (en) 1999-08-26 2002-04-09 Robert R. Whittle Alkoxy substituted benzimidazole compounds, pharmaceutical preparations containing the same, and methods of using the same
US7205308B2 (en) 2002-09-04 2007-04-17 Schering Corporation Trisubstituted 7-aminopyrazolopyrimidines as cyclin dependent kinase inhibitors
US20080207617A1 (en) 2002-10-29 2008-08-28 Kirin Beer Kabushiki Kaisha Quinoline Derivatives and Quinazoline Derivatives Inhibiting Autophosphrylation of Flt3 and Medicinal Compositions Containing the Same
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
DE102005042742A1 (de) * 2005-09-02 2007-03-08 Schering Ag Substituierte Imidazo[1,2b]pyridazine als Kinase-Inhibitoren, deren Herstellung und Verwendung als Arzneimittel
WO2007048088A2 (en) 2005-10-18 2007-04-26 Janssen Pharmaceutica N.V. Method of inhibiting flt3 kinase
WO2008016665A2 (en) 2006-08-02 2008-02-07 Xanthus Pharmaceuticals, Inc. Imidazoacridine compounds for treating flt3 -mediated disorders
US7517882B2 (en) * 2006-09-18 2009-04-14 Polaris Group Protein kinase inhibitors
ATE502943T1 (de) 2006-09-29 2011-04-15 Novartis Ag Pyrazolopyrimidine als pi3k-lipidkinasehemmer
SG176461A1 (en) * 2006-11-06 2011-12-29 Supergen Inc Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
WO2008060248A1 (en) * 2006-11-15 2008-05-22 S*Bio Pte Ltd. Indole sustituted pyrimidines and use thereof in the treatment of cancer
EP2183251A1 (en) 2007-08-02 2010-05-12 Antisoma Ventures Limited Indazole compounds for treating inflammatory disorders, demyelinating disorders and cancers
JP5608099B2 (ja) 2008-01-30 2014-10-15 ジェネンテック， インコーポレイテッド ピラゾロピリミジンｐｉ３ｋ阻害剤化合物および使用方法
CN101239978A (zh) 2008-03-05 2008-08-13 南方医科大学 一种咪唑并吡啶类化合物
MX2010012457A (es) * 2008-05-13 2010-12-07 Irm Llc Heterociclos que contienen nitrogeno fusionado y composiciones de los mismos como inhibidores de cinasa.
JP5731978B2 (ja) 2008-09-26 2015-06-10 インテリカイン， エルエルシー 複素環キナーゼ阻害剤
GB0906472D0 (en) 2009-04-15 2009-05-20 Astex Therapeutics Ltd New compounds
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
WO2013001310A1 (en) * 2011-06-30 2013-01-03 Centro Nacional De Investigaciones Oncológicas (Cnio) Macrocyclic compounds and their use as cdk8 inhibitors
JP6082397B2 (ja) * 2011-09-30 2017-02-15 イプセン ファルマ ソシエテ パール アクシオン サンプリフィエＩｐｓｅｎ Ｐｈａｒｍａ Ｓ．Ａ．Ｓ． マクロ環状ｌｒｒｋ２キナーゼ阻害剤

Also Published As

Publication number Publication date
CN103930427A (zh) 2014-07-16
MX347765B (es) 2017-05-12
EA025881B1 (ru) 2017-02-28
JP2014528398A (ja) 2014-10-27
JP6046728B2 (ja) 2016-12-21
US9370519B2 (en) 2016-06-21
KR20140078710A (ko) 2014-06-25
US20140303159A1 (en) 2014-10-09
US20150283141A1 (en) 2015-10-08
MX2014003807A (es) 2015-01-12
BR112014007622A2 (pt) 2017-04-04
HK1198764A1 (zh) 2015-06-05
WO2013045653A1 (en) 2013-04-04
US9090630B2 (en) 2015-07-28
DK2760867T3 (en) 2016-04-11
HUE027318T2 (en) 2016-10-28
AU2012314376B2 (en) 2017-04-06
AU2012314376A1 (en) 2014-05-15
CA2849999A1 (en) 2013-04-04
CN103930427B (zh) 2016-03-09
ES2569048T3 (es) 2016-05-06

Similar Documents

Publication Publication Date Title
EA201490707A1 (ru) Макроциклические ингибиторы flt3-киназы
EA201490891A1 (ru) Пиридопиразины, обладающие противораковой активностью через ингибирование fgfr киназ
PH12013502565A1 (en) Substituted imidazopyridinyl-aminopyridine compounds
EA201492216A1 (ru) Ингибиторы бромодомена и их применение
EA201492092A1 (ru) Соединения и композиции для ингибирования активности abl1, abl2 и bcr-abl1
EA201491824A1 (ru) Производные бензамида для ингибирования активности abl1, abl2 и bcr-abl1
EA201992270A2 (ru) 4-имидазопиридазин-1-ил-бензамиды и 4-имидазотриазин-1-ил-бензамиды в качестве btk-ингибиторов
EA201291143A1 (ru) Пиразолилхиназолиновые ингибиторы киназы
EA201692166A1 (ru) Гетероциклические ингибиторы глютаминазы
EA201301209A1 (ru) Производные пирролотриазинона в качестве ингибиторов p13k
EA201890333A1 (ru) Противовирусные соединения
EA201591166A1 (ru) Ингибиторы аутотаксина
EA201490357A1 (ru) Индазолы
EA201591591A1 (ru) Соединения карбазола, применяемые в качестве ингибиторов бромодомена
EA201400412A1 (ru) ЗАМЕЩЕННЫЕ БЕНЗИЛИНДАЗОЛЫ ДЛЯ ПРИМЕНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ Bub1 КИНАЗЫ ДЛЯ ЛЕЧЕНИЯ ГИПЕРПРОЛИФЕРАТИВНЫХ ЗАБОЛЕВАНИЙ
EA201391416A1 (ru) Новые соединения в качестве модуляторов протеинкиназ
EA201491579A1 (ru) Соединения оксазолидин-2-она и их применения в качестве ингибиторов pi3k
EA201491672A1 (ru) Гетероциклильные соединения как ингибиторы mek
IN2014KN02601A (ru)
EA201500426A1 (ru) Производные пирролотриазинона в качестве ингибиторов pi3k
EA201390766A1 (ru) БЕНЗОКСАЗЕПИНЫ КАК ИНГИБИТОРЫ PI3K/mTOR И СПОСОБЫ ИХ ИСПОЛЬЗОВАНИЯ И ПОЛУЧЕНИЯ
EA201492002A1 (ru) Противовирусные соединения
EA201391106A1 (ru) Новые гетероциклические производные
EA201370166A1 (ru) Содержащие диарилацетиленгидразид ингибиторы тирозинкиназы
EA201301181A1 (ru) Триазолопиридины

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG TJ TM RU