CN104350055B - 作为mnk1和mnk2调节剂的二环杂芳基衍生物及其用途 - Google Patents

作为mnk1和mnk2调节剂的二环杂芳基衍生物及其用途 Download PDF

Info

Publication number
CN104350055B
CN104350055B CN201380027654.7A CN201380027654A CN104350055B CN 104350055 B CN104350055 B CN 104350055B CN 201380027654 A CN201380027654 A CN 201380027654A CN 104350055 B CN104350055 B CN 104350055B
Authority
CN
China
Prior art keywords
alkyl
base
compound
optionally substituted
certain embodiments
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.)
Active
Application number
CN201380027654.7A
Other languages
English (en)
Chinese (zh)
Other versions
CN104350055A (zh
Inventor
卡索姆·纳克罗
阿什赛亚玛尼·泽亚拉·杜莱斯瓦米
洛希萨·劳·陈纳玛尼尼
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Agency for Science Technology and Research Singapore
Original Assignee
Agency for Science Technology and Research Singapore
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 Agency for Science Technology and Research Singapore filed Critical Agency for Science Technology and Research Singapore
Publication of CN104350055A publication Critical patent/CN104350055A/zh
Application granted granted Critical
Publication of CN104350055B publication Critical patent/CN104350055B/zh
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • C07D487/02—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 two hetero rings
    • C07D487/04—Ortho-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
    • A61K31/41—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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/519—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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • C07D471/02—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 two hetero rings
    • C07D471/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201380027654.7A 2012-03-30 2013-04-01 作为mnk1和mnk2调节剂的二环杂芳基衍生物及其用途 Active CN104350055B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1205669.3A GB201205669D0 (en) 2012-03-30 2012-03-30 Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
GB1205669.3 2012-03-30
PCT/SG2013/000126 WO2013147711A1 (en) 2012-03-30 2013-04-01 Bicyclic heterocyclic derivatives as mnk1 and mnk2 modulators and uses thereof

Publications (2)

Publication Number Publication Date
CN104350055A CN104350055A (zh) 2015-02-11
CN104350055B true CN104350055B (zh) 2019-05-31

Family

ID=46160013

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380027654.7A Active CN104350055B (zh) 2012-03-30 2013-04-01 作为mnk1和mnk2调节剂的二环杂芳基衍生物及其用途

Country Status (14)

Country Link
US (3) US9908886B2 (https=)
EP (2) EP3321268B1 (https=)
JP (2) JP6475158B2 (https=)
KR (1) KR102153320B1 (https=)
CN (1) CN104350055B (https=)
AU (2) AU2013240612B2 (https=)
BR (1) BR112014024255B1 (https=)
DK (1) DK2831079T3 (https=)
ES (2) ES2647959T3 (https=)
GB (1) GB201205669D0 (https=)
NO (1) NO2831079T3 (https=)
PL (2) PL2831079T3 (https=)
SG (2) SG11201406207PA (https=)
WO (1) WO2013147711A1 (https=)

Families Citing this family (73)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2868302A1 (en) 2012-03-23 2013-09-26 Dennis M. Brown Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
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
TWI574962B (zh) 2012-11-14 2017-03-21 加拓科學公司 作爲ｐｉ３激酶調節劑的芳雜環化合物及其使用方法和用途
MX2015010700A (es) 2013-02-21 2017-01-23 Calitor Sciences Llc Compuestos heteroaromaticos como moduladores de la p13 cinasa.
WO2014151630A2 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
WO2014151729A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
US9296754B2 (en) 2013-03-15 2016-03-29 Novartis Ag Compounds and compositions for the treatment of parasitic diseases
US9227969B2 (en) 2013-08-14 2016-01-05 Novartis Ag Compounds and compositions as inhibitors of MEK
TW201542550A (zh) * 2013-09-06 2015-11-16 Lexicon Pharmaceuticals Inc 吡唑并［１，５－ａ］嘧啶基化合物、包含彼之組合物以及使用彼之方法
AR097543A1 (es) * 2013-09-06 2016-03-23 Lexicon Pharmaceuticals Inc COMPUESTOS BASADOS EN IMIDAZO[1,2-b]PIRIDAZINA, COMPOSICIONES QUE LOS COMPRENDEN Y SUS MÉTODOS DE USO
GB2518873A (en) * 2013-10-03 2015-04-08 Agency Science Tech & Res Bicyclic alkyne derivatives and uses thereof
BR112016012243A2 (pt) * 2013-12-09 2017-08-08 Ucb Biopharma Sprl Derivados de imidazopiridina como moduladores de atividade de tnf
BR112016014004B1 (pt) 2013-12-19 2022-11-01 Novartis Ag Compostos para tratamento de doenças parasíticas, seus usos, e composições farmacêuticas
ES2728932T3 (es) * 2014-01-09 2019-10-29 Intra Cellular Therapies Inc Compuestos orgánicos
ES2933350T3 (es) 2014-01-24 2023-02-06 Turning Point Therapeutics Inc Macrociclos de diarilo como moduladores de proteína quinasas
EP3105219B9 (en) 2014-02-13 2018-10-03 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
JP6602779B2 (ja) 2014-02-13 2019-11-06 インサイト・コーポレイション Ｌｓｄ１阻害剤としてのシクロプロピルアミン類
US9527835B2 (en) 2014-02-13 2016-12-27 Incyte Corporation Cyclopropylamines as LSD1 inhibitors
EP3105218B1 (en) 2014-02-13 2019-09-25 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
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
US9758523B2 (en) 2014-07-10 2017-09-12 Incyte Corporation Triazolopyridines and triazolopyrazines as LSD1 inhibitors
US9695180B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted imidazo[1,2-a]pyrazines as LSD1 inhibitors
US9695167B2 (en) 2014-07-10 2017-07-04 Incyte Corporation Substituted triazolo[1,5-a]pyridines and triazolo[1,5-a]pyrazines as LSD1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
EP3277689B1 (en) 2015-04-03 2019-09-04 Incyte Corporation Heterocyclic compounds as lsd1 inhibitors
EP3285809B1 (en) 2015-04-20 2019-09-11 eFFECTOR Therapeutics, Inc. Inhibitors of immune checkpoint modulators for use in treating cancer and infections
ES2865330T3 (es) 2015-04-29 2021-10-15 Janssen Pharmaceutica Nv Azabenzimidazoles y su uso como moduladores del receptor AMPA
WO2016205590A1 (en) * 2015-06-18 2016-12-22 Cephalon, Inc. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
KR20180026459A (ko) 2015-06-18 2018-03-12 세파론, 인코포레이티드 1,4-치환된 피페리딘 유도체
AU2016287568B2 (en) 2015-07-02 2020-08-20 Turning Point Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
RU2765181C2 (ru) 2015-07-06 2022-01-26 Тёрнинг Поинт Терапьютикс, Инк. Полиморфная форма диарильного макроцикла
PT3733187T (pt) 2015-07-21 2024-11-08 Turning Point Therapeutics Inc Macrociclo de diarilo quiral e utilização do mesmo no tratamento do cancro
MY189367A (en) 2015-08-12 2022-02-08 Incyte Corp Salts of an lsd1 inhibitor
US10730842B2 (en) 2015-09-03 2020-08-04 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK1A and uses thereof
WO2017068064A1 (en) * 2015-10-22 2017-04-27 Selvita S.A. Pyridone derivatives and their use as kinase inhibitors
US10851082B2 (en) 2015-10-28 2020-12-01 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (MNK1) and 2 (MNK2)
BR112018008711A2 (pt) * 2015-10-29 2018-10-30 Effector Therapeutics Inc compostos de pirrolo-, pirazolo-, imidazo-pirimidina e piridina que inibem mnk1 e mnk2
US10112955B2 (en) 2015-10-29 2018-10-30 Effector Therapeutics, Inc. Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
WO2017087808A1 (en) 2015-11-20 2017-05-26 Effector Therapeutics, Inc. Heterocyclic compounds that inhibit the kinase activity of mnk useful for treating various cancers
WO2017117052A1 (en) 2015-12-31 2017-07-06 Effector Therapeutics, Inc. Mnk biomarkers and uses thereof
TWI833686B (zh) 2016-04-22 2024-03-01 美商英塞特公司 Lsd1 抑制劑之調配物
US11352328B2 (en) 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
US10689400B2 (en) 2016-07-28 2020-06-23 Turning Point Therapeutics, Inc. Macrocycle kinase inhibitors
GB201700692D0 (en) * 2017-01-16 2017-03-01 Salvensis Novel compounds and their use in the treatment of schistosomiasis
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
CA3053493A1 (en) 2017-02-14 2018-08-23 Effector Therapeutics, Inc. Piperidine-substituted mnk inhibitors and methods related thereto
CN111182903A (zh) 2017-07-28 2020-05-19 特普医药公司 巨环化合物及其用途
LT3728271T (lt) 2017-12-19 2022-12-12 Turning Point Therapeutics, Inc. Makrocikliniai junginiai, skirti ligų gydymui
JP7335882B2 (ja) 2018-02-13 2023-08-30 ブルーレイ セラピューティクス （シャンハイ） カンパニー，リミティド ピリミジン縮合環式化合物及びその製造方法、並びに使用
CN110156786B (zh) * 2018-02-13 2022-06-03 青煜医药研发(上海)有限公司 嘧啶并环化合物及其制备方法和应用
US12528810B2 (en) 2018-03-01 2026-01-20 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK/CLK and uses thereof
EP3564235A1 (en) * 2018-05-03 2019-11-06 Northwestern University Substituted aromatic n-heterocyclic compounds as inhibitors of mitogen-activated protein kinase interacting kinase 1 (mnk1) and 2 (mnk2)
US10968200B2 (en) 2018-08-31 2021-04-06 Incyte Corporation Salts of an LSD1 inhibitor and processes for preparing the same
CA3118093A1 (en) 2018-09-28 2020-04-02 Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of dyrk1/clk and uses thereof
CN113286592A (zh) 2018-10-24 2021-08-20 效应治疗股份有限公司 Mnk抑制剂的结晶形式
US12419865B2 (en) 2018-12-06 2025-09-23 Arisan Therapeutics Inc. Compounds for the treatment of arenavirus infection
CN111978317A (zh) * 2019-05-22 2020-11-24 上海道熵生物科技有限公司 咪唑并吡啶类mnk1/mnk2激酶抑制剂及其制备方法和应用
CN111978325B (zh) * 2019-05-22 2023-11-17 中国药科大学 咪唑并哒嗪类mnk1/mnk2激酶抑制剂及其制备方法和应用
TWI759829B (zh) * 2019-08-23 2022-04-01 財團法人生物技術開發中心 作為第iii型受體酪胺酸激酶抑制劑之雜環吡唑衍生物
KR102459614B1 (ko) * 2019-08-30 2022-10-31 주식회사 티에스디라이프사이언스 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물
US12558363B2 (en) * 2019-12-30 2026-02-24 Devicare SL Compositions for clinical complications associated to devices implanted in the urinary tract
JP2023533616A (ja) * 2020-06-30 2023-08-03 ４イー セラピューティクス， インコーポレイテッド Ｍｎｋ阻害を示すピリジン－１，５－ジオン及びそれらの使用方法
WO2022053838A1 (en) * 2020-09-14 2022-03-17 The University Of Sussex Small molecule inhibitors of lemur tyrosine kinase 3
CN112047950B (zh) * 2020-09-14 2023-07-25 华东师范大学 咪唑并吡嗪类衍生物及其合成方法和应用
US20230000986A1 (en) * 2021-07-01 2023-01-05 Board Of Regents, The University Of Texas System Mnk inhibitors and eif4e phosphorylation modulation to treat inflammatory pain in the aged
WO2023093700A1 (zh) * 2021-11-29 2023-06-01 中国海洋大学 咪唑并噻唑衍生物及其制备方法与应用
CN114113639B (zh) * 2022-01-29 2022-04-19 北京大有天弘科技有限公司 一种血型抗体检测方法及其应用
CN118908959B (zh) * 2023-05-08 2025-11-14 广西大学 咪唑并[1,2-b]哒嗪类化合物及其制备方法和PI3K抑制剂应用
ES2993583B2 (es) 2023-06-27 2025-09-22 Univ Valencia Derivados de imidazo[1,2-a]piridina con actividad antiinflamatoria
WO2025165301A1 (en) * 2024-01-31 2025-08-07 National University Of Singapore Targeting metabolic pathways with mnk inhibitors
CN121646587A (zh) * 2024-05-30 2026-03-10 深圳微芯生物科技股份有限公司 一种苯并咪唑类化合物、其制备方法及应用
CN119614691B (zh) * 2024-12-09 2026-03-13 武汉大学 干扰nlk基因靶点在制备改善巨噬细胞炎性激活的药物中的应用

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1746099A1 (en) * 2004-12-23 2007-01-24 DeveloGen Aktiengesellschaft Mnk1 or Mnk2 inhibitors
WO2008078091A1 (en) * 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
CN101454325A (zh) * 2006-03-09 2009-06-10 法马科皮亚公司 用于治疗代谢性疾病的8-杂芳基嘌呤mnk2抑制剂
CN101472912A (zh) * 2006-06-22 2009-07-01 比奥维特罗姆上市公司 作为mnk激酶抑制剂的吡啶和吡嗪衍生物
CN101600718A (zh) * 2006-11-06 2009-12-09 休普基因公司 咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途
CN101678026A (zh) * 2007-05-11 2010-03-24 诺瓦提斯公司 作为磷脂酰肌醇-3-激酶抑制剂的3,6-二取代的-咪唑并[1,2-b]哒嗪和3,5-二取代的-吡唑并[1,5-a]嘧啶
WO2010055072A2 (en) * 2008-11-12 2010-05-20 Novartis Forschungsstiftung, Zweigniederlassung, Friedrich Miescher Institute For Biomedical Research Treating cancer by modulating a mnk
WO2011104337A1 (en) * 2010-02-26 2011-09-01 Boehringer Ingelheim International Gmbh Heterocycloalkyl-containing thienopyrimidines for pharmaceutical compositions

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1910369A1 (en) * 2005-07-29 2008-04-16 Astellas Pharma Inc. Fused heterocycles as lck inhibitors
US20070049591A1 (en) * 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
US20120058997A1 (en) * 2006-11-06 2012-03-08 Supergen, Inc. Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors
AR068877A1 (es) * 2007-10-17 2009-12-09 Novartis Ag Derivados heterociclicos de imidazol
TW201107329A (en) * 2009-07-30 2011-03-01 Oncotherapy Science Inc Fused imidazole derivative having ttk inhibitory action
NZ598220A (en) * 2009-08-17 2014-02-28 Intellikine Llc Heterocyclic compounds and uses thereof
KR20130065632A (ko) * 2010-04-28 2013-06-19 다이이찌 산쿄 가부시키가이샤 ［５，６］복소 고리 화합물
CA2806655A1 (en) * 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Substituted imidazo[1,2-b]pyridazines
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
GB201205669D0 (en) 2012-03-30 2012-05-16 Agency Science Tech & Res Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof
JP2016510764A (ja) * 2013-03-07 2016-04-11 カリフィア バイオ, インク.Califia Bio, Inc. 混合系キナーゼ阻害剤および治療法

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1746099A1 (en) * 2004-12-23 2007-01-24 DeveloGen Aktiengesellschaft Mnk1 or Mnk2 inhibitors
CN101454325A (zh) * 2006-03-09 2009-06-10 法马科皮亚公司 用于治疗代谢性疾病的8-杂芳基嘌呤mnk2抑制剂
CN101472912A (zh) * 2006-06-22 2009-07-01 比奥维特罗姆上市公司 作为mnk激酶抑制剂的吡啶和吡嗪衍生物
CN101600718A (zh) * 2006-11-06 2009-12-09 休普基因公司 咪唑并[1,2-b]哒嗪和吡唑并[1,5-a]嘧啶衍生物及其作为蛋白激酶抑制剂的用途
WO2008078091A1 (en) * 2006-12-22 2008-07-03 Astex Therapeutics Limited Bicyclic heterocyclic compounds as fgfr inhibitors
CN101679408A (zh) * 2006-12-22 2010-03-24 Astex治疗学有限公司 作为fgfr抑制剂的双环杂环化合物
CN101678026A (zh) * 2007-05-11 2010-03-24 诺瓦提斯公司 作为磷脂酰肌醇-3-激酶抑制剂的3,6-二取代的-咪唑并[1,2-b]哒嗪和3,5-二取代的-吡唑并[1,5-a]嘧啶
WO2010055072A2 (en) * 2008-11-12 2010-05-20 Novartis Forschungsstiftung, Zweigniederlassung, Friedrich Miescher Institute For Biomedical Research Treating cancer by modulating a mnk
WO2011104337A1 (en) * 2010-02-26 2011-09-01 Boehringer Ingelheim International Gmbh Heterocycloalkyl-containing thienopyrimidines for pharmaceutical compositions

Non-Patent Citations (6)

* Cited by examiner, † Cited by third party
Title
Design and evaluation of 3,6-di(hetero)aryl imidazo[1,2-a]pyrazines as inhibitors of checkpoint and other kinases;Thomas P. Matthews，等;《Bioorganic & Medicinal Chemistry Letters》;20100527;第20卷(第14期);4045-4049 *
Design and Synthesis of Imidazopyridine Analogues as Inhibitors of Phosphoinositide 3-Kinase Signaling and Angiogenesis;Okseon Kim，等;《Journal of Medicinal Chemistry》;20110309;第54卷(第7期);2455-2466 *
Direct Arylation of Imidazo[1,2-b]pyridazines: Microwave-Assisted One-PotSuzuki Coupling/Pd-Catalysed Arylation;Ahmed El Akkaoui, 等;《Eur. J. Org. Chem.》;20100105;第2010卷(第5期);表5，化合物29 *
Docking and quantitative structure-activity relationship studies for imidazo[1,2-a]pyrazines as inhibitors of checkpoint kinase-1;Julio Caballero，等;《Med Chem Res》;20110706;第21卷(第8期);1912-1920 *
Inhibition of Mammalian Target of Rapamycin Induces Phosphatidylinositol 3-Kinase-Dependent and Mnk-Mediated Eukaryotic Translation Initiation Factor 4E Phosphorylation;Xuerong Wang，等;《MOLECULAR AND CELLULAR BIOLOGY》;20071130;第27卷(第21期);7405-7413 *
The synthesis of imidazo[4,5-d]pyridines from a substituted imidazole and acyl or sulfonyl acetonitrile;Magdi E. A. Zaki，等;《Tetrahedron》;20070223;第63卷(第18期);3745-3753 *

Also Published As

Publication number Publication date
EP3321268C0 (en) 2025-06-04
PL2831079T3 (pl) 2018-01-31
KR20150002639A (ko) 2015-01-07
US11040978B2 (en) 2021-06-22
DK2831079T3 (da) 2017-11-27
JP6662984B2 (ja) 2020-03-11
CN104350055A (zh) 2015-02-11
JP2015511638A (ja) 2015-04-20
EP2831079A1 (en) 2015-02-04
ES3034431T3 (en) 2025-08-18
US20140371199A1 (en) 2014-12-18
EP2831079A4 (en) 2015-11-18
ES2647959T3 (es) 2017-12-27
BR112014024255A2 (pt) 2017-06-20
JP2019031560A (ja) 2019-02-28
AU2017219039A1 (en) 2017-09-14
NO2831079T3 (https=) 2018-01-13
US9908886B2 (en) 2018-03-06
US20190315755A1 (en) 2019-10-17
AU2013240612B2 (en) 2017-05-25
EP3321268A1 (en) 2018-05-16
JP6475158B2 (ja) 2019-02-27
SG10201706594PA (en) 2017-09-28
PL3321268T3 (pl) 2025-11-17
US20180208600A1 (en) 2018-07-26
WO2013147711A1 (en) 2013-10-03
KR102153320B1 (ko) 2020-09-08
GB201205669D0 (en) 2012-05-16
BR112014024255B1 (pt) 2021-12-28
EP2831079B1 (en) 2017-08-16
AU2013240612A1 (en) 2014-10-16
EP3321268B1 (en) 2025-06-04
SG11201406207PA (en) 2014-11-27

Similar Documents

Publication Publication Date Title
CN104350055B (zh) 作为mnk1和mnk2调节剂的二环杂芳基衍生物及其用途
JP6947651B2 (ja) ４，６−ピリミジニレン誘導体およびこれらの使用
US20190211020A1 (en) Bicyclic heteroaryl derivatives as mnk1 and mnk2 modulators and uses thereof
CN105026398B (zh) 用于治疗疾病诸如癌症的三唑并[4,5-d]嘧啶衍生物
CN105793262B (zh) 二环炔衍生物及其用途
JP2018522867A (ja) 縮合二環式ピリミジン誘導体およびこれらの使用
KR20160111520A (ko) 디히드로프테리디논 유도체 및 그의 용도
AU2012367141B2 (en) Triazolo[4,5-d]pyrimidine derivatives
CN104812756A (zh) 多激酶通路抑制剂

Legal Events

Date Code Title Description
C06 Publication
PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
GR01 Patent grant
GR01 Patent grant