EA201991894A1 - ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ - Google Patents

ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ

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Publication number
EA201991894A1
EA201991894A1 EA201991894A EA201991894A EA201991894A1 EA 201991894 A1 EA201991894 A1 EA 201991894A1 EA 201991894 A EA201991894 A EA 201991894A EA 201991894 A EA201991894 A EA 201991894A EA 201991894 A1 EA201991894 A1 EA 201991894A1
Authority
EA
Eurasian Patent Office
Prior art keywords
piperidine
substituted
compounds
formula
mnk inhibitors
Prior art date
Application number
EA201991894A
Other languages
English (en)
Inventor
Джастин Т. Эрнст
Пол А. Шпренгелер
Зигфрид Х Райх
Сэмьюэл Сперри
Original Assignee
Эффектор 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 Эффектор Терапьютикс, Инк. filed Critical Эффектор Терапьютикс, Инк.
Publication of EA201991894A1 publication Critical patent/EA201991894A1/ru

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Classifications

    • 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
    • C07D471/12—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 system contains three hetero rings
    • C07D471/20—Spiro-condensed systems
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Настоящее изобретение относится к соединениям в соответствии с формулой (I)или к стереоизомеру, таутомеру или фармацевтически приемлемой соли такого соединения, где X, X, R, R, Rи n имеют значения, определенные в настоящей заявке. Также описаны фармацевтически приемлемые композиции соединений формулы (I), a также способы применения соединений формулы (I) и фармацевтически приемлемых композиций соединений формулы (I) в качестве ингибиторов Mnk, а также терапевтических средств для лечения заболеваний, таких как рак.
EA201991894A 2017-02-14 2018-02-13 ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ EA201991894A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762458671P 2017-02-14 2017-02-14
PCT/US2018/018022 WO2018152117A1 (en) 2017-02-14 2018-02-13 Piperidine-substituted mnk inhibitors and methods related thereto

Publications (1)

Publication Number Publication Date
EA201991894A1 true EA201991894A1 (ru) 2020-02-05

Family

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EA201991894A EA201991894A1 (ru) 2017-02-14 2018-02-13 ПИПЕРИДИН-ЗАМЕЩЕННЫЕ ИНГИБИТОРЫ Mnk И СВЯЗАННЫЕ С НИМИ СПОСОБЫ

Country Status (21)

Country Link
US (3) US20180228803A1 (ru)
EP (1) EP3582776B1 (ru)
JP (2) JP2020507588A (ru)
KR (1) KR20190117013A (ru)
CN (1) CN110719781A (ru)
AU (2) AU2018220840A1 (ru)
BR (1) BR112019016707A2 (ru)
CA (1) CA3053493A1 (ru)
CL (1) CL2019002297A1 (ru)
CO (1) CO2019009423A2 (ru)
DK (1) DK3582776T3 (ru)
EA (1) EA201991894A1 (ru)
ES (1) ES2969988T3 (ru)
FI (1) FI3582776T3 (ru)
IL (1) IL268619B (ru)
MX (1) MX2019009653A (ru)
PE (1) PE20191349A1 (ru)
PH (1) PH12019550140A1 (ru)
SG (1) SG11201907356SA (ru)
TW (1) TWI762579B (ru)
WO (1) WO2018152117A1 (ru)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20191349A1 (es) 2017-02-14 2019-09-30 Effector Therapeutics Inc Inhibidores de mnk sustituidos con piperidina y metodos relacionados con los mismos
BR112021007745A2 (pt) 2018-10-24 2021-07-27 Effector Therapeutics, Inc. formas cristalinas de inibidores de mnk
CN111484494B (zh) * 2019-01-29 2022-09-13 诺沃斯达药业(上海)有限公司 抑制mnk1和mnk2的多环化合物
WO2021098691A1 (zh) 2019-11-18 2021-05-27 南京明德新药研发有限公司 作为mnk抑制剂的吡咯并三嗪类化合物
EP4200296A1 (en) * 2020-08-20 2023-06-28 Hepagene Therapeutics (HK) Limited Mnk inhibitors
JP2024516885A (ja) 2021-05-08 2024-04-17 成都嘉葆薬銀医薬科技有限公司 ピロロトリアジン系化合物の塩形、その結晶形及びその製造方法
CN114736205B (zh) * 2022-03-31 2023-03-03 武汉九州钰民医药科技有限公司 化合物Tomivosertib的制备方法
CN114853756B (zh) * 2022-03-31 2023-03-28 武汉九州钰民医药科技有限公司 化合物Tomivosertib的制备工艺
WO2024017229A1 (zh) * 2022-07-19 2024-01-25 成都嘉葆药银医药科技有限公司 一种吡咯并三嗪类化合物在制备抗肿瘤药物中的应用
CN116425750A (zh) * 2023-02-10 2023-07-14 诺沃斯达药业(上海)有限公司 一种mnk抑制剂化合物的盐、晶体及其制备方法

Family Cites Families (54)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5491144A (en) 1991-05-30 1996-02-13 Ciba-Geigy Corporation Substituted diaminophthalimides and analogues
WO2002098428A1 (en) 2001-06-05 2002-12-12 Lilly Icos Llc Tetracyclic compounds as pde5-inhibitors
ES2359233T3 (es) 2001-10-29 2011-05-19 Boehringer Ingelheim International Gmbh Proteínas homólogas de la quinasa mnk implicadas en la regulación de la homeostasis energética y en el metabolismo organular.
US20050012622A1 (en) 2003-05-19 2005-01-20 Sutton William R. Monitoring and control of sleep cycles
TWI301760B (en) 2004-02-27 2008-10-11 Merz Pharma Gmbh & Co Kgaa Tetrahydroquinolinones and their use as antagonists of metabotropic glutamate receptors
US7488745B2 (en) 2004-07-16 2009-02-10 Schering Corporation Compounds for the treatment of inflammatory disorders
TW200613272A (en) 2004-08-13 2006-05-01 Astrazeneca Ab Isoindolone compounds and their use as metabotropic glutamate receptor potentiators
US20060281670A1 (en) 2005-06-10 2006-12-14 Wisconsin Alumni Research Foundation (Warf) Compositions and methods for modulating angiogenesis
WO2007021308A1 (en) 2005-08-12 2007-02-22 Astrazeneca Ab Metabotropic glutamate-receptor-potentiating isoindolones
BRPI0713328A2 (pt) 2006-06-22 2012-10-30 Biovitrum Ab derivados de piridina e pirazina como inibidores de cinase mnk
EP1889847A1 (en) 2006-07-10 2008-02-20 DeveloGen Aktiengesellschaft Pyrrolopyrimidines for pharmaceutical compositions
DK2134689T3 (da) 2007-03-16 2014-06-30 Scripps Research Inst Inhibitorer af fokal adhæsionskinase
GB0706072D0 (en) 2007-03-28 2007-05-09 Sterix Ltd Compound
JP2011504474A (ja) 2007-11-22 2011-02-10 ベーリンガー インゲルハイム インテルナツィオナール ゲゼルシャフト ミット ベシュレンクテル ハフツング アルツハイマー氏病を治療するためのＭｎｋインヒビターの使用
JP2009173629A (ja) 2007-12-21 2009-08-06 Banyu Pharmaceut Co Ltd Ｒｓｋ１阻害作用を有する新規スピロインダン誘導体
WO2009112445A1 (en) 2008-03-10 2009-09-17 Novartis Ag Method of increasing cellular phosphatidyl choline by dgat1 inhibition
UY32072A (es) * 2008-08-26 2010-03-26 Boehringer Ingelheim Int Tienopirimidinas para composiciones farmacéuticas
WO2010055072A2 (en) 2008-11-12 2010-05-20 Novartis Forschungsstiftung, Zweigniederlassung, Friedrich Miescher Institute For Biomedical Research Treating cancer by modulating a mnk
US8637525B2 (en) 2009-07-31 2014-01-28 Bristol-Myers Squibb Company Compounds for the reduction of beta-amyloid production
TWI468402B (zh) 2009-07-31 2015-01-11 必治妥美雅史谷比公司 降低β－類澱粉生成之化合物
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
US8604217B2 (en) 2009-11-12 2013-12-10 Selvita S.A. Compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine kinases and a serine/threonine kinases modulating agent
WO2011106168A1 (en) 2010-02-24 2011-09-01 Dcam Pharma Inc Purine compounds for treating autoimmune and demyelinating diseases
EA201300420A1 (ru) 2010-10-01 2013-09-30 Байер Интеллектчуал Проперти Гмбх Комбинации, которые содержат замещенный n-(2-ариламино) арилсульфонамид
CA2818853A1 (en) 2010-11-30 2012-06-07 Gilead Pharmasset Llc 2'-spirocyclo-nucleosides for use in therapy of hcv or dengue virus
US9938269B2 (en) 2011-06-30 2018-04-10 Abbvie Inc. Inhibitor compounds of phosphodiesterase type 10A
WO2013043192A1 (en) 2011-09-23 2013-03-28 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Galactokinase inhibitors for the treatment and prevention of associated diseases and disorders
KR101490761B1 (ko) 2011-12-30 2015-02-09 한미약품 주식회사 단백질 키나아제 저해활성을 갖는 티에노[3,2-d]피리미딘 유도체
CA2868966C (en) 2012-03-29 2021-01-26 Francis Xavier Tavares Lactam kinase inhibitors
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
US10280168B2 (en) 2012-03-30 2019-05-07 Agency For Science, Technology And Research Bicyclic heteroaryl derivatives as MNK1 and MNK2 modulators and uses thereof
WO2013151975A1 (en) 2012-04-02 2013-10-10 Northeastern University Compositions and methods for the inhibition of methyltransferases
CN104470926A (zh) 2012-05-21 2015-03-25 拜耳医药股份有限公司 取代的吡咯并嘧啶
TW201412740A (zh) 2012-09-20 2014-04-01 Bayer Pharma AG 經取代之吡咯并嘧啶胺基苯并噻唑酮
WO2014072244A1 (en) 2012-11-09 2014-05-15 Boehringer Ingelheim International Gmbh Sulfoximine substituted quinazolines for pharmaceutical compositions
GB2508652A (en) 2012-12-07 2014-06-11 Agency Science Tech & Res Heterocyclic piperazine derivatives
US9211300B2 (en) 2012-12-19 2015-12-15 Idenix Pharmaceuticals Llc 4′-fluoro nucleosides for the treatment of HCV
CN105143227A (zh) 2013-02-20 2015-12-09 拜耳医药股份公司 作为mknk1抑制剂的取代的咪唑并[1,2-b]哒嗪类化合物
TW201605867A (zh) 2013-11-20 2016-02-16 拜耳製藥公司 噻吩并嘧啶
TWI713455B (zh) 2014-06-25 2020-12-21 美商伊凡克特治療公司 ＭｎＫ抑制劑及其相關方法
EA201791363A1 (ru) 2014-12-19 2018-01-31 Байер Фарма Акциенгезельшафт Пиразолопиридинамины в качестве ингибиторов mknk1 и mknk2
KR20240038145A (ko) * 2015-04-20 2024-03-22 이펙터 테라퓨틱스, 인크. 암 및 감염 치료에 사용하기 위한 면역 체크포인트 조절 인자의 억제제
JP6888006B2 (ja) 2015-10-29 2021-06-16 イーフェクター セラピューティクス， インコーポレイテッド Ｍｎｋ１およびｍｎｋ２を阻害するピロロ−、ピラゾロ−、イミダゾ−ピリミジンおよびピリジン化合物
KR20180070695A (ko) 2015-10-29 2018-06-26 이펙터 테라퓨틱스, 인크. Mnk1 및 mnk2의 이소인돌린, 아자이소인돌린, 디히드로인데논 및 디히드로아자인데논 억제제
US10000487B2 (en) 2015-11-20 2018-06-19 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of Mnk useful for treating various cancers
GB201520499D0 (en) 2015-11-20 2016-01-06 Medical Res Council Technology Compounds
GB201520500D0 (en) 2015-11-20 2016-01-06 Medical Res Council Technology Compounds
US20170191136A1 (en) 2015-12-31 2017-07-06 Effector Therapeutics, Inc. Mnk biomarkers and uses thereof
SG10201913464TA (en) * 2016-12-19 2020-03-30 Epizyme Inc Amine-substituted heterocyclic compounds as ehmt2 inhibitors and methods of use thereof
PE20191349A1 (es) 2017-02-14 2019-09-30 Effector Therapeutics Inc Inhibidores de mnk sustituidos con piperidina y metodos relacionados con los mismos
WO2018218038A1 (en) 2017-05-24 2018-11-29 Effector Therapeutics, Inc. Methods and compositions for cellular immunotherapy
CA3081602A1 (en) 2017-11-16 2019-05-23 Novartis Ag Combination therapies
WO2019103926A1 (en) 2017-11-21 2019-05-31 Saint Louis University P38 inhibitors for the treatment of fshd
BR112021007745A2 (pt) 2018-10-24 2021-07-27 Effector Therapeutics, Inc. formas cristalinas de inibidores de mnk

Also Published As

Publication number Publication date
TWI762579B (zh) 2022-05-01
TW201835076A (zh) 2018-10-01
IL268619B (en) 2022-05-01
PH12019550140A1 (en) 2020-06-01
SG11201907356SA (en) 2019-09-27
AU2022202864A1 (en) 2022-05-19
KR20190117013A (ko) 2019-10-15
CN110719781A (zh) 2020-01-21
JP2022185050A (ja) 2022-12-13
US20180228803A1 (en) 2018-08-16
JP2020507588A (ja) 2020-03-12
EP3582776A4 (en) 2020-09-02
EP3582776B1 (en) 2023-11-08
EP3582776A1 (en) 2019-12-25
US20220096472A1 (en) 2022-03-31
US11878015B2 (en) 2024-01-23
US11083727B2 (en) 2021-08-10
MX2019009653A (es) 2019-12-19
AU2022202864B2 (en) 2024-06-06
US20190275039A1 (en) 2019-09-12
FI3582776T3 (fi) 2024-01-03
IL268619A (en) 2019-10-31
CA3053493A1 (en) 2018-08-23
AU2018220840A1 (en) 2019-09-19
DK3582776T3 (da) 2024-01-08
PE20191349A1 (es) 2019-09-30
WO2018152117A1 (en) 2018-08-23
BR112019016707A2 (pt) 2020-04-07
CO2019009423A2 (es) 2019-09-09
ES2969988T3 (es) 2024-05-23
CL2019002297A1 (es) 2019-11-08

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