JP2015511638A5 - - Google Patents
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- JP2015511638A5 JP2015511638A5 JP2015503165A JP2015503165A JP2015511638A5 JP 2015511638 A5 JP2015511638 A5 JP 2015511638A5 JP 2015503165 A JP2015503165 A JP 2015503165A JP 2015503165 A JP2015503165 A JP 2015503165A JP 2015511638 A5 JP2015511638 A5 JP 2015511638A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- pharmaceutical composition
- composition according
- kinase inhibitor
- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 25
- 238000000034 method Methods 0.000 claims 12
- 239000000203 mixture Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 9
- 229940043355 kinase inhibitor Drugs 0.000 claims 9
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 9
- 206010028980 Neoplasm Diseases 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- 239000003814 drug Substances 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 125000001072 heteroaryl group Chemical group 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- 102100026299 MAP kinase-interacting serine/threonine-protein kinase 1 Human genes 0.000 claims 4
- 101710139011 MAP kinase-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 4
- 102100033610 MAP kinase-interacting serine/threonine-protein kinase 2 Human genes 0.000 claims 4
- 101710138999 MAP kinase-interacting serine/threonine-protein kinase 2 Proteins 0.000 claims 4
- 125000001931 aliphatic group Chemical group 0.000 claims 4
- 125000004452 carbocyclyl group Chemical group 0.000 claims 4
- 150000002431 hydrogen Chemical group 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 239000012828 PI3K inhibitor Substances 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
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 239000008280 blood Substances 0.000 claims 2
- 210000004369 blood Anatomy 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 238000000338 in vitro Methods 0.000 claims 2
- 230000004968 inflammatory condition Effects 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 230000002503 metabolic effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015511638A JP2015511638A (ja) | 2015-04-20 |
| JP2015511638A5 true JP2015511638A5 (enExample) | 2016-06-09 |
| JP6475158B2 JP6475158B2 (ja) | 2019-02-27 |
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 After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US9908886B2 (enExample) |
| EP (2) | EP2831079B1 (enExample) |
| JP (2) | JP6475158B2 (enExample) |
| KR (1) | KR102153320B1 (enExample) |
| CN (1) | CN104350055B (enExample) |
| AU (2) | AU2013240612B2 (enExample) |
| BR (1) | BR112014024255B1 (enExample) |
| DK (1) | DK2831079T3 (enExample) |
| ES (2) | ES3034431T3 (enExample) |
| GB (1) | GB201205669D0 (enExample) |
| NO (1) | NO2831079T3 (enExample) |
| PL (2) | PL2831079T3 (enExample) |
| SG (2) | SG10201706594PA (enExample) |
| WO (1) | WO2013147711A1 (enExample) |
Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2013234955A1 (en) | 2012-03-23 | 2014-11-13 | 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 |
| KR102148681B1 (ko) | 2013-02-21 | 2020-08-27 | 칼리토르 사이언시즈, 엘엘씨 | Pi3 키나제 모듈레이터로서의 헤테로방향족 화합물 |
| 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 |
| 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 |
| WO2015086519A1 (en) * | 2013-12-09 | 2015-06-18 | Ucb Biopharma Sprl | Imidazopyridine derivatives as modulators of tnf activity |
| MY175865A (en) | 2013-12-19 | 2020-07-14 | Novartis Ag | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as protozoan proteasome inhibitors for the treatment of parasitic diseases such as leishmaniasis |
| BR112016016098A2 (pt) * | 2014-01-09 | 2017-08-08 | Intracellular Therapies Inc | Compostos orgânicos |
| AU2015209239C1 (en) | 2014-01-24 | 2026-05-07 | Turning Point Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
| KR102421235B1 (ko) | 2014-02-13 | 2022-07-15 | 인사이트 코포레이션 | Lsd1 저해제로서 사이클로프로필아민 |
| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | Incyte Corporation | Cyclopropylamines as LSD1 inhibitors |
| EP3392244A1 (en) | 2014-02-13 | 2018-10-24 | Incyte Corporation | Cyclopropylamines as lsd1 inhibitors |
| NZ723203A (en) | 2014-02-13 | 2020-08-28 | Incyte Corp | 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 |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | 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 |
| UA122688C2 (uk) | 2015-04-03 | 2020-12-28 | Інсайт Корпорейшн | Гетероциклічні сполуки як інгібітори lsd1 |
| KR20180004740A (ko) | 2015-04-20 | 2018-01-12 | 이펙터 테라퓨틱스, 인크. | 암 및 감염 치료에 사용하기 위한 면역 체크포인트 조절 인자의 억제제 |
| HRP20210403T1 (hr) * | 2015-04-29 | 2021-10-29 | Janssen Pharmaceutica Nv | Azabenzimidazoli i njihova uporaba kao modulatora ampa receptora |
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| PL3319969T3 (pl) | 2015-07-06 | 2024-06-24 | Turning Point Therapeutics, Inc. | Diarylowe polimorfy makrocykliczne |
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| JP2018526452A (ja) * | 2015-09-03 | 2018-09-13 | アリゾナ ボード オブ リージェンツ オン ビハーフ オブ ザ ユニバーシティー オブ アリゾナ | Ｄｙｒｋ１ａの小分子抑制剤およびその使用 |
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| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
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| 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 |
| MX394700B (es) | 2017-02-14 | 2025-03-24 | Effector Therapeutics Inc | Inhibidores de mnk sustituidos con piperidina y métodos relacionados con los mismos. |
| CA3069232A1 (en) | 2017-07-28 | 2019-01-31 | Turning Point Therapeutics, Inc. | Macrocyclic compounds and uses thereof |
| HUE060711T2 (hu) | 2017-12-19 | 2023-04-28 | Turning Point Therapeutics Inc | Makrociklusos vegyületek betegségek kezelésére |
| MA51845A (fr) * | 2018-02-13 | 2020-12-23 | Shanghai Blueray Biopharma Co Ltd | Composé cyclique fusionné à une pyrimidine, son procédé de préparation et son application |
| CN115448923B (zh) * | 2018-02-13 | 2024-03-22 | 上海青煜医药科技有限公司 | 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) |
| WO2020047198A1 (en) | 2018-08-31 | 2020-03-05 | Incyte Corporation | Salts of an lsd1 inhibitor and processes for preparing the same |
| US12054483B2 (en) | 2018-09-28 | 2024-08-06 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Small molecule inhibitors of DYRK/CLK and uses thereof |
| EP3870178A4 (en) | 2018-10-24 | 2022-08-03 | Effector Therapeutics Inc. | Crystalline forms of mnk inhibitors |
| 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 |
| WO2021040502A1 (ko) * | 2019-08-30 | 2021-03-04 | 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 |
| BR112022026275A2 (pt) * | 2020-06-30 | 2023-03-14 | 4E Therapeutics Inc | Piridina-1,5-dionas que exibem inibição de mnk e seus métodos de uso |
| US20230355617A1 (en) * | 2020-09-14 | 2023-11-09 | 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 |
| JP7814782B2 (ja) * | 2021-11-29 | 2026-02-17 | オーシャン ユニバーシティ オブ チャイナ | イミダゾチアゾール誘導体およびその製造方法と使用 |
| 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 |
| CN121085942B (zh) * | 2025-08-28 | 2026-05-08 | 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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| JP2009502734A (ja) * | 2005-07-29 | 2009-01-29 | アステラス製薬株式会社 | Ｌｃｋ阻害剤としての縮合複素環 |
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| CA2791020A1 (en) * | 2010-04-28 | 2011-11-03 | Daiichi Sankyo Company, Limited | [5,6] heterocyclic compound |
| ES2539257T3 (es) * | 2010-07-28 | 2015-06-29 | Bayer Intellectual Property Gmbh | Imidazo[1,2-b]piridazinas sustituidas |
| 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 |
-
2012
- 2012-03-30 GB GBGB1205669.3A patent/GB201205669D0/en not_active Ceased
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2013
- 2013-04-01 NO NO13768800A patent/NO2831079T3/no unknown
- 2013-04-01 BR BR112014024255-0A patent/BR112014024255B1/pt active IP Right Grant
- 2013-04-01 ES ES17179630T patent/ES3034431T3/es active Active
- 2013-04-01 CN CN201380027654.7A patent/CN104350055B/zh active Active
- 2013-04-01 JP JP2015503165A patent/JP6475158B2/ja active Active
- 2013-04-01 SG SG10201706594PA patent/SG10201706594PA/en unknown
- 2013-04-01 PL PL13768800T patent/PL2831079T3/pl unknown
- 2013-04-01 DK DK13768800.8T patent/DK2831079T3/da active
- 2013-04-01 ES ES13768800.8T patent/ES2647959T3/es active Active
- 2013-04-01 AU AU2013240612A patent/AU2013240612B2/en active Active
- 2013-04-01 EP EP13768800.8A patent/EP2831079B1/en active Active
- 2013-04-01 WO PCT/SG2013/000126 patent/WO2013147711A1/en not_active Ceased
- 2013-04-01 US US14/363,718 patent/US9908886B2/en active Active
- 2013-04-01 SG SG11201406207PA patent/SG11201406207PA/en unknown
- 2013-04-01 PL PL17179630.3T patent/PL3321268T3/pl unknown
- 2013-04-01 EP EP17179630.3A patent/EP3321268B1/en active Active
- 2013-04-01 KR KR1020147027686A patent/KR102153320B1/ko active Active
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2017
- 2017-08-24 AU AU2017219039A patent/AU2017219039A1/en not_active Abandoned
-
2018
- 2018-01-16 US US15/872,571 patent/US20180208600A1/en not_active Abandoned
- 2018-10-31 JP JP2018206109A patent/JP6662984B2/ja active Active
-
2019
- 2019-06-05 US US16/432,469 patent/US11040978B2/en active Active
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