JP6475158B2 - Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 - Google Patents

Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 Download PDF

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JP6475158B2
JP6475158B2 JP2015503165A JP2015503165A JP6475158B2 JP 6475158 B2 JP6475158 B2 JP 6475158B2 JP 2015503165 A JP2015503165 A JP 2015503165A JP 2015503165 A JP2015503165 A JP 2015503165A JP 6475158 B2 JP6475158 B2 JP 6475158B2
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certain embodiments
compound
pyrazin
optionally substituted
alkyl
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JP2015511638A5 (OSRAM
JP2015511638A (ja
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ナクロ，カッソウム
デュライスワミー，アシサヤマニ，ジェヤラージ
チェンナマネニ，ロヒタ，ラオ
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    • 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
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    • 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
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    • 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
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  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)
JP2015503165A 2012-03-30 2013-04-01 Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用 Active JP6475158B2 (ja)

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

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JP2018206109A Division JP6662984B2 (ja) 2012-03-30 2018-10-31 Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用

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JP2015511638A JP2015511638A (ja) 2015-04-20
JP2015511638A5 JP2015511638A5 (OSRAM) 2016-06-09
JP6475158B2 true JP6475158B2 (ja) 2019-02-27

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JP2018206109A Active JP6662984B2 (ja) 2012-03-30 2018-10-31 Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用

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US (3) US9908886B2 (OSRAM)
EP (2) EP3321268B1 (OSRAM)
JP (2) JP6475158B2 (OSRAM)
KR (1) KR102153320B1 (OSRAM)
CN (1) CN104350055B (OSRAM)
AU (2) AU2013240612B2 (OSRAM)
BR (1) BR112014024255B1 (OSRAM)
DK (1) DK2831079T3 (OSRAM)
ES (2) ES3034431T3 (OSRAM)
GB (1) GB201205669D0 (OSRAM)
NO (1) NO2831079T3 (OSRAM)
PL (2) PL2831079T3 (OSRAM)
SG (2) SG11201406207PA (OSRAM)
WO (1) WO2013147711A1 (OSRAM)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019031560A (ja) * 2012-03-30 2019-02-28 エージェンシー フォー サイエンス，テクノロジー アンド リサーチ Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013142817A2 (en) 2012-03-23 2013-09-26 Dennis Brown Compositions and methods to improve the therapeutic benefit of indirubin and analogs thereof, including meisoindigo
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
MY182036A (en) 2013-02-21 2021-01-18 Sunshine Lake Pharma Co Ltd Heteroaromatic compounds as pi3 kinase modulators
WO2014151729A1 (en) 2013-03-15 2014-09-25 Irm Llc Compounds and compositions for the treatment of parasitic diseases
WO2014151630A2 (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
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
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
GB2518873A (en) * 2013-10-03 2015-04-08 Agency Science Tech & Res Bicyclic alkyne derivatives and uses thereof
RU2695664C1 (ru) * 2013-12-09 2019-07-25 Юсб Байофарма Спрл Производные имидазопиридина в качестве модуляторов активности tnf
TWI674263B (zh) 2013-12-19 2019-10-11 瑞士商諾華公司 用於治療寄生蟲疾病之化合物及組合物
CN106029075A (zh) * 2014-01-09 2016-10-12 细胞内治疗公司 有机化合物
WO2015112806A2 (en) 2014-01-24 2015-07-30 Tp Therapeutics, Inc. Diaryl macrocycles as modulators of protein kinases
WO2015123437A1 (en) 2014-02-13 2015-08-20 Incyte Corporation Cyclopropylamines as lsd1 inhibitors
TW201613860A (en) 2014-02-13 2016-04-16 Incyte Corp Cyclopropylamines as LSD1 inhibitors
ME03654B (me) 2014-02-13 2020-07-20 Incyte Corp Ciklopropilamini kao lsd1 inhibitori
PT3105226T (pt) 2014-02-13 2019-11-06 Incyte Corp Ciclopropilaminas como inibidores de lsd1
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
TW201613925A (en) 2014-07-10 2016-04-16 Incyte Corp Imidazopyrazines as LSD1 inhibitors
WO2016007722A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
WO2016007731A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Imidazopyridines and imidazopyrazines as lsd1 inhibitors
WO2016007727A1 (en) 2014-07-10 2016-01-14 Incyte Corporation Triazolopyridines and triazolopyrazines as lsd1 inhibitors
AU2016243939B2 (en) 2015-04-03 2020-09-03 Incyte Holdings Corporation Heterocyclic compounds as LSD1 inhibitors
KR102891799B1 (ko) 2015-04-20 2025-11-26 이펙터 테라퓨틱스, 인크. 암 및 감염 치료에 사용하기 위한 면역 체크포인트 조절 인자의 억제제
DK3288940T5 (da) * 2015-04-29 2021-09-20 Janssen Pharmaceutica Nv Azabenzimidazoler og deres anvendelse som ampa-receptormodulatorer
ES2821049T3 (es) 2015-06-18 2021-04-23 89Bio Ltd Derivados de piperidina 1,4 sustituidos
US10919875B2 (en) 2015-06-18 2021-02-16 89Bio Ltd Substituted 4-benzyl and 4-benzoyl piperidine derivatives
ES2864839T3 (es) 2015-07-02 2021-10-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales como moduladores de proteína quinasas
ES2979111T3 (es) 2015-07-06 2024-09-24 Turning Point Therapeutics Inc Polimorfo de macrociclo de diarilo
MX383823B (es) 2015-07-21 2025-03-14 Turning Point Therapeutics Inc Macrociclos de diarilo quirales y usos de los mismo.
KR102710120B1 (ko) 2015-08-12 2024-09-27 인사이트 홀딩스 코포레이션 Lsd1 저해제의 염
AU2016315881B2 (en) * 2015-09-03 2019-09-19 The Arizona Board Of Regents On Behalf Of The University Of Arizona Small molecule inhibitors of DYRK1A and uses thereof
JP2018531266A (ja) * 2015-10-22 2018-10-25 セルビタ エス．エー． ピリドン誘導体およびキナーゼ阻害剤としてのその使用
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)
CA3002877A1 (en) 2015-10-29 2017-05-04 Effector Therapeutics, Inc. Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2
EA034440B1 (ru) 2015-10-29 2020-02-07 Эффектор Терапьютикс, Инк. СОЕДИНЕНИЯ ПИРРОЛО-, ПИРАЗОЛО-, ИМИДАЗОПИРИМИДИНА И ПИРИДИНА, КОТОРЫЕ ИНГИБИРУЮТ Mnk1 И Mnk2
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
WO2017117052A1 (en) 2015-12-31 2017-07-06 Effector Therapeutics, Inc. Mnk biomarkers and uses thereof
AR109452A1 (es) 2016-04-22 2018-12-12 Incyte Corp Formulación farmacéutica de un inhibidor de lsd1 y método de tratamiento
US11352328B2 (en) * 2016-07-12 2022-06-07 Arisan Therapeutics Inc. Heterocyclic compounds for the treatment of arenavirus
CN109715165A (zh) 2016-07-28 2019-05-03 Tp生物医药公司 巨环激酶抑制剂
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
EP3582776B1 (en) 2017-02-14 2023-11-08 Effector Therapeutics, Inc. Piperidine-substituted mnk inhibitors and methods related thereto
MY201925A (en) 2017-07-28 2024-03-23 Turning Point Therapeutics Inc Macrocyclic compounds and uses thereof
JP7194188B2 (ja) 2017-12-19 2022-12-21 ターニング・ポイント・セラピューティクス・インコーポレイテッド 疾患を治療するための大環状化合物
EP3753941B1 (en) * 2018-02-13 2024-05-01 Shanghai Blueray Biopharma Co., Ltd. Pyrimidine-fused cyclic compound, preparation method therefor and application thereof
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
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)
WO2020047198A1 (en) 2018-08-31 2020-03-05 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
KR20210102211A (ko) 2018-10-24 2021-08-19 이펙터 테라퓨틱스, 인크. Mnk 억제제의 결정질 형태
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
EP4023647B1 (en) * 2019-08-30 2025-04-09 TSD Life Sciences Co., Ltd. Imidazopyridine derivative and pharmaceutical composition comprising same as active ingredient
CN115038471B (zh) * 2019-12-30 2024-05-14 德维护理有限公司 用于与植入泌尿道的装置相关的临床并发症的组合物
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
JP2023541262A (ja) * 2020-09-14 2023-09-29 ザ ユニバーシティー オブ サセックス Ｌｅｍｕｒチロシンキナーゼ３の小分子阻害剤
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
CN117203211B (zh) * 2021-11-29 2025-08-19 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

Family Cites Families (19)

* 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
US20100216798A1 (en) * 2005-07-29 2010-08-26 Astellas Pharma Inc Fused heterocycles as lck inhibitors
US20070049591A1 (en) * 2005-08-25 2007-03-01 Kalypsys, Inc. Inhibitors of MAPK/Erk Kinase
BRPI0709007A2 (pt) * 2006-03-09 2011-06-21 Pharmacopeia Inc inibidores de 8-heteroarilpurina mnk2 para tratamento de distúrbios metabólicos
BRPI0713328A2 (pt) * 2006-06-22 2012-10-30 Biovitrum Ab derivados de piridina e pirazina como inibidores de cinase mnk
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
MX2009004700A (es) * 2006-11-06 2009-05-15 Supergen Inc Derivados de imidazo[1,2-b]piridazin y pirazolo[1,5-a] pirimidina y su uso como inhibidores de proteina cinasa.
HRP20150642T1 (hr) * 2006-12-22 2015-08-14 Astex Therapeutics Limited BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a
AR067326A1 (es) * 2007-05-11 2009-10-07 Novartis Ag Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido
JP5456681B2 (ja) * 2007-10-17 2014-04-02 ノバルティス アーゲー ＡＬＫ阻害剤として有用なイミダゾ［１，２−ａ］ピリジン誘導体
US20110280886A1 (en) * 2008-11-12 2011-11-17 University Hospital Basel Treating cancer by modulating mnk
TW201107329A (en) * 2009-07-30 2011-03-01 Oncotherapy Science Inc Fused imidazole derivative having ttk inhibitory action
CN102573846B (zh) * 2009-08-17 2015-10-07 因特利凯公司 杂环化合物及其用途
UY33241A (es) * 2010-02-26 2011-09-30 Boehringer Ingelheim Int ?Tienopirimidinas que contienen heterocicloalquilo para composiciones farmacéuticas?.
SG183426A1 (en) * 2010-04-28 2012-09-27 Daiichi Sankyo Co Ltd [5,6] heterocyclic compound
CA2806655A1 (en) * 2010-07-28 2012-02-02 Bayer Intellectual Property Gmbh Substituted imidazo[1,2-b]pyridazines
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
US9370515B2 (en) * 2013-03-07 2016-06-21 Califia Bio, Inc. Mixed lineage kinase inhibitors and method of treatments

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2019031560A (ja) * 2012-03-30 2019-02-28 エージェンシー フォー サイエンス，テクノロジー アンド リサーチ Ｍｎｋ１およびｍｎｋ２調節剤としての二環式ヘテロアリール誘導体、およびその使用

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