JP2019031560A5 - - Google Patents
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- JP2019031560A5 JP2019031560A5 JP2018206109A JP2018206109A JP2019031560A5 JP 2019031560 A5 JP2019031560 A5 JP 2019031560A5 JP 2018206109 A JP2018206109 A JP 2018206109A JP 2018206109 A JP2018206109 A JP 2018206109A JP 2019031560 A5 JP2019031560 A5 JP 2019031560A5
- Authority
- JP
- Japan
- Prior art keywords
- kinase
- acceptable salt
- hydrate
- solvate
- related disorder
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 24
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 22
- 239000012453 solvate Substances 0.000 claims 22
- 108091000080 Phosphotransferase Proteins 0.000 claims 20
- 208000035475 disorder Diseases 0.000 claims 20
- 239000000203 mixture Substances 0.000 claims 20
- 102000020233 phosphotransferase Human genes 0.000 claims 20
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 4
- 201000011510 cancer Diseases 0.000 claims 4
- 208000030159 metabolic disease Diseases 0.000 claims 4
- 239000012828 PI3K inhibitor Substances 0.000 claims 3
- 229940043355 kinase inhibitor Drugs 0.000 claims 3
- 229940124302 mTOR inhibitor Drugs 0.000 claims 3
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 3
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 3
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 3
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 208000002339 Frontotemporal Lobar Degeneration Diseases 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- 208000009829 Lewy Body Disease Diseases 0.000 claims 2
- 201000002832 Lewy body dementia Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 210000004227 basal ganglia Anatomy 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 230000001054 cortical effect Effects 0.000 claims 2
- 230000007850 degeneration Effects 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 150000004677 hydrates Chemical class 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 102100026299 MAP kinase-interacting serine/threonine-protein kinase 1 Human genes 0.000 claims 1
- 101710139011 MAP kinase-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 1
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 claims 1
- 101710138999 MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 claims 1
- 230000036571 hydration Effects 0.000 claims 1
- 238000006703 hydration reaction Methods 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000003419 tautomerization reaction Methods 0.000 claims 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB1205669.3 | 2012-03-30 | ||
| GBGB1205669.3A GB201205669D0 (en) | 2012-03-30 | 2012-03-30 | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Division JP6475158B2 (ja) | 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019031560A JP2019031560A (ja) | 2019-02-28 |
| JP2019031560A5 true JP2019031560A5 (2) | 2019-04-11 |
| JP6662984B2 JP6662984B2 (ja) | 2020-03-11 |
Family
ID=46160013
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Active JP6475158B2 (ja) | 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 |
| 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 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015503165A Active JP6475158B2 (ja) | 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 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US9908886B2 (2) |
| EP (2) | EP3321268B1 (2) |
| JP (2) | JP6475158B2 (2) |
| KR (1) | KR102153320B1 (2) |
| CN (1) | CN104350055B (2) |
| AU (2) | AU2013240612B2 (2) |
| BR (1) | BR112014024255B1 (2) |
| DK (1) | DK2831079T3 (2) |
| ES (2) | ES3034431T3 (2) |
| GB (1) | GB201205669D0 (2) |
| NO (1) | NO2831079T3 (2) |
| PL (2) | PL2831079T3 (2) |
| SG (2) | SG11201406207PA (2) |
| WO (1) | WO2013147711A1 (2) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US20150087687A1 (en) | 2012-03-23 | 2015-03-26 | Dennis 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. |
| US9186361B2 (en) | 2013-03-15 | 2015-11-17 | Novartis Ag | 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 |
| US9233961B2 (en) | 2013-03-15 | 2016-01-12 | 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 |
| US9920052B2 (en) * | 2013-12-09 | 2018-03-20 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of TNF activity |
| 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 |
| RU2016132574A (ru) * | 2014-01-09 | 2018-02-12 | Интра-Селлулар Терапиз, Инк. | Органические соединения |
| PL3636649T3 (pl) | 2014-01-24 | 2024-05-06 | Turning Point Therapeutics, Inc. | Diaryle makrocykliczne jako modulatory kinaz białkowych |
| SI3105218T1 (sl) | 2014-02-13 | 2019-11-29 | Incyte Corp | Ciklopropilamini kot inhibitorji LSD1 |
| MX373103B (es) | 2014-02-13 | 2020-04-17 | Incyte Holdings Corp | Ciclopropilaminas como inhibidores de desmetilasa específica de lisina 1 (lsd1). |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| EP3105219B9 (en) | 2014-02-13 | 2018-10-03 | 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 |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TW201613925A (en) | 2014-07-10 | 2016-04-16 | Incyte Corp | Imidazopyrazines as LSD1 inhibitors |
| WO2016007727A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| TWI687419B (zh) | 2014-07-10 | 2020-03-11 | 美商英塞特公司 | 作為lsd1抑制劑之咪唑并吡啶及咪唑并吡嗪 |
| EP3277689B1 (en) | 2015-04-03 | 2019-09-04 | Incyte Corporation | Heterocyclic compounds as lsd1 inhibitors |
| US10702526B2 (en) | 2015-04-20 | 2020-07-07 | Effector Therapeutics Inc. | Inhibitors of immune checkpoint modulators and related methods |
| RS61688B1 (sr) * | 2015-04-29 | 2021-05-31 | Janssen Pharmaceutica Nv | Azabenzimidazoli i njihiova upotreba kao modulatori ampa receptora |
| EA201890086A1 (ru) | 2015-06-18 | 2018-06-29 | Сефалон, Инк. | 1,4-замещенные производные пиперидина |
| ES2849951T3 (es) | 2015-06-18 | 2021-08-24 | 89Bio Ltd | Derivados de piperidina 4-bencil y 4-benzoil sustituidos |
| ES2864839T3 (es) | 2015-07-02 | 2021-10-14 | Turning Point Therapeutics Inc | Macrociclos de diarilo quirales como moduladores de proteína quinasas |
| JP6917974B2 (ja) | 2015-07-06 | 2021-08-11 | 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Turning Point Therapeutics,Inc. | ジアリール大環状多形 |
| FI3733187T3 (fi) | 2015-07-21 | 2024-12-18 | Turning Point Therapeutics Inc | Kiraalinen diaryylimakrosykli ja sen käyttö syövän hoidossa |
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| EP3344039A4 (en) * | 2015-09-03 | 2019-08-28 | Arizona Board of Regents on behalf of the University of Arizona | LOW MOLECULAR DYRK1A INHIBITORS AND USES THEREOF |
| AU2016341259B2 (en) * | 2015-10-22 | 2019-09-12 | 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) |
| SG11201803242TA (en) | 2015-10-29 | 2018-05-30 | Effector Therapeutics Inc | Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2 |
| KR20180070696A (ko) * | 2015-10-29 | 2018-06-26 | 이펙터 테라퓨틱스, 인크. | Mnk1 및 mnk2를 억제하는 피롤로-, 피라졸로-, 이미다조-피리미딘 및 피리딘 화합물 |
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| 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 |
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| TWI857981B (zh) | 2018-10-24 | 2024-10-11 | 美商伊凡克特治療公司 | Mnk抑制劑的結晶形式 |
| US12419865B2 (en) | 2018-12-06 | 2025-09-23 | Arisan Therapeutics Inc. | Compounds for the treatment of arenavirus infection |
| 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 |
| 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 |
| 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 |
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| 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 |
| US20250042920A1 (en) * | 2021-11-29 | 2025-02-06 | Ocean University Of China | Imidazothiazole derivative, preparation method therefor, and application thereof |
| 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 |
| WO2025247379A1 (zh) * | 2024-05-30 | 2025-12-04 | 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 |
| CN121085942A (zh) * | 2025-08-28 | 2025-12-09 | 中国海洋大学 | 3,5-位取代的咪唑并噻二唑杂环衍生物及其制备方法与应用 |
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| EP1746099A1 (en) * | 2004-12-23 | 2007-01-24 | DeveloGen Aktiengesellschaft | Mnk1 or Mnk2 inhibitors |
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| 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 |
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-
2012
- 2012-03-30 GB GBGB1205669.3A patent/GB201205669D0/en not_active Ceased
-
2013
- 2013-04-01 SG SG11201406207PA patent/SG11201406207PA/en unknown
- 2013-04-01 PL PL13768800T patent/PL2831079T3/pl unknown
- 2013-04-01 US US14/363,718 patent/US9908886B2/en active Active
- 2013-04-01 PL PL17179630.3T patent/PL3321268T3/pl unknown
- 2013-04-01 EP EP17179630.3A patent/EP3321268B1/en active Active
- 2013-04-01 ES ES17179630T patent/ES3034431T3/es active Active
- 2013-04-01 WO PCT/SG2013/000126 patent/WO2013147711A1/en not_active Ceased
- 2013-04-01 KR KR1020147027686A patent/KR102153320B1/ko active Active
- 2013-04-01 CN CN201380027654.7A patent/CN104350055B/zh active Active
- 2013-04-01 AU AU2013240612A patent/AU2013240612B2/en active Active
- 2013-04-01 BR BR112014024255-0A patent/BR112014024255B1/pt active IP Right Grant
- 2013-04-01 NO NO13768800A patent/NO2831079T3/no unknown
- 2013-04-01 SG SG10201706594PA patent/SG10201706594PA/en unknown
- 2013-04-01 ES ES13768800.8T patent/ES2647959T3/es active Active
- 2013-04-01 JP JP2015503165A patent/JP6475158B2/ja active Active
- 2013-04-01 DK DK13768800.8T patent/DK2831079T3/da active
- 2013-04-01 EP EP13768800.8A patent/EP2831079B1/en active Active
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2017
- 2017-08-24 AU AU2017219039A patent/AU2017219039A1/en not_active Abandoned
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2018
- 2018-01-16 US US15/872,571 patent/US20180208600A1/en not_active Abandoned
- 2018-10-31 JP JP2018206109A patent/JP6662984B2/ja active Active
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2019
- 2019-06-05 US US16/432,469 patent/US11040978B2/en active Active
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