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 |
|---|---|---|---|
| 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 |
| 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) | PL3321268T3 (enExample) |
| SG (2) | SG10201706594PA (enExample) |
| WO (1) | WO2013147711A1 (enExample) |
Families Citing this family (74)
| 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 |
| GB201205669D0 (en) * | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 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 |
| US9186361B2 (en) | 2013-03-15 | 2015-11-17 | Novartis Ag | 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 |
| 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 |
| ES2809535T3 (es) * | 2013-12-09 | 2021-03-04 | UCB Biopharma SRL | Derivados de imidazopiridina como moduladores de la actividad de TNF |
| JP6392352B2 (ja) | 2013-12-19 | 2018-09-19 | ノバルティス アーゲー | リーシュマニア症などの寄生虫病を処置するための原生動物のプロテアソーム阻害剤としての［１，２，４］トリアゾロ［１，５−ａ］ピリミジン誘導体 |
| ES2728932T3 (es) * | 2014-01-09 | 2019-10-29 | Intra Cellular Therapies Inc | Compuestos orgánicos |
| WO2015112806A2 (en) | 2014-01-24 | 2015-07-30 | Tp Therapeutics, Inc. | Diaryl macrocycles as modulators of protein kinases |
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| LT3105218T (lt) | 2014-02-13 | 2019-12-10 | Incyte Corp | Ciklopropilaminai kaip lsd1 inhibitoriai |
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| US9527835B2 (en) | 2014-02-13 | 2016-12-27 | 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 |
| WO2016007736A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyrazines as lsd1 inhibitors |
| WO2016007731A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Imidazopyridines and imidazopyrazines as lsd1 inhibitors |
| WO2016007722A1 (en) | 2014-07-10 | 2016-01-14 | Incyte Corporation | Triazolopyridines and triazolopyrazines as lsd1 inhibitors |
| US9758523B2 (en) | 2014-07-10 | 2017-09-12 | Incyte Corporation | Triazolopyridines and triazolopyrazines as LSD1 inhibitors |
| EA201792205A1 (ru) | 2015-04-03 | 2018-02-28 | Инсайт Корпорейшн | Гетероциклические соединения как ингибиторы lsd1 |
| AU2016252038B2 (en) | 2015-04-20 | 2021-08-12 | Effector Therapeutics, Inc. | Inhibitors of immune checkpoint modulators for use in treating cancer and infections |
| BR122023023802A2 (pt) * | 2015-04-29 | 2023-12-26 | Janssen Pharmaceutica Nv | Compostos azabenzimidazóis, seu uso como moduladores do receptor de ampa e composições farmacêuticas que os compreendem |
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| RU2732405C2 (ru) | 2015-07-02 | 2020-09-16 | Тёрнинг Поинт Терапьютикс, Инк. | Хиральные диарильные макроциклы в качестве модуляторов протеинкиназ |
| BR112018000297A2 (pt) | 2015-07-06 | 2018-09-04 | Tp Therapeutics Inc | polimorfo de macrociclo de diarila |
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| 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 |
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| SG11201803242TA (en) | 2015-10-29 | 2018-05-30 | Effector Therapeutics Inc | Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of mnk1 and mnk2 |
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| DK3582776T3 (da) | 2017-02-14 | 2024-01-08 | Effector Therapeutics Inc | Piperidinsubstituerede mnk-hæmmere og dertil relaterede fremgangsmåder |
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| RS63787B1 (sr) | 2017-12-19 | 2022-12-30 | Turning Point Therapeutics Inc | Makrociklična jedinjenja za lečenje bolesti |
| US11498930B2 (en) | 2018-02-13 | 2022-11-15 | Blueray Therapeutics (Shanghai) Co., Ltd | Pyrimidine-fused cyclic compound, preparation method therefor and application thereof |
| 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 |
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| US10968200B2 (en) | 2018-08-31 | 2021-04-06 | Incyte Corporation | Salts of an LSD1 inhibitor and processes for preparing the same |
| EP3856186A4 (en) | 2018-09-28 | 2022-07-06 | Arizona Board of Regents on behalf of the University of Arizona | SMALL MOLECULAR DYRK1/CLK INHIBITORS 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 |
| JP7345220B2 (ja) * | 2019-08-30 | 2023-09-15 | ティーエスディー ライフ サイエンス カンパニー リミテッド | イミダゾピリジン誘導体及びこれを有効成分として含有する薬学的組成物 |
| EP4084836B1 (en) * | 2019-12-30 | 2024-10-09 | Devicare, S.L. | Compositions for clinical complications associated to devices implanted in the urinary tract |
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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 |
| WO2022053838A1 (en) * | 2020-09-14 | 2022-03-17 | The University Of Sussex | Small molecule inhibitors of lemur tyrosine kinase 3 |
| 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 |
| 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 |
| 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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| 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 |
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| EP1991547A2 (en) | 2006-03-09 | 2008-11-19 | Pharmacopeia, Inc. | 8-heteroarylpurine mnk2 inhibitors for treating metabolic disorders |
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| AR067326A1 (es) * | 2007-05-11 | 2009-10-07 | Novartis Ag | Imidazopiridinas y pirrolo -pirimidinas sustituidas como inhibidores de cinasa de lipido |
| EA201000615A1 (ru) * | 2007-10-17 | 2010-12-30 | Новартис Аг | Производные имидазо[1,2-а]пиридина, применимые в качестве ингибиторов апк (активиноподобной киназы) |
| US20110280886A1 (en) * | 2008-11-12 | 2011-11-17 | University Hospital Basel | Treating cancer by modulating mnk |
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| UA111579C2 (uk) * | 2009-08-17 | 2016-05-25 | Інтеллікіне Ллк | ГЕТЕРОЦИКЛІЧНІ ПОХІДНІ 2-АМІНОБЕНЗО[d]ОКСАЗОЛУ, ФАРМАЦЕВТИЧНА КОМПОЗИЦІЯ НА ЇХ ОСНОВІ ТА ЇХ ЗАСТОСУВАННЯ ДЛЯ ЛІКУВАННЯ ЗАХВОРЮВАННЯ, ПОВ'АНОГО З РІ3-КІНАЗОЮ |
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| JPWO2011136264A1 (ja) * | 2010-04-28 | 2013-07-22 | 第一三共株式会社 | ［５，６］複素環化合物 |
| JP5926727B2 (ja) * | 2010-07-28 | 2016-05-25 | バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ | 置換イミダゾ［１，２−ｂ］ピリダジン |
| 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 |
| CN105431148A (zh) * | 2013-03-07 | 2016-03-23 | 加利菲亚生物公司 | 混合谱系激酶抑制剂及治疗方法 |
-
2012
- 2012-03-30 GB GBGB1205669.3A patent/GB201205669D0/en not_active Ceased
-
2013
- 2013-04-01 AU AU2013240612A patent/AU2013240612B2/en active Active
- 2013-04-01 JP JP2015503165A patent/JP6475158B2/ja active Active
- 2013-04-01 ES ES17179630T patent/ES3034431T3/es active Active
- 2013-04-01 BR BR112014024255-0A patent/BR112014024255B1/pt active IP Right Grant
- 2013-04-01 KR KR1020147027686A patent/KR102153320B1/ko active Active
- 2013-04-01 SG SG10201706594PA patent/SG10201706594PA/en unknown
- 2013-04-01 SG SG11201406207PA patent/SG11201406207PA/en unknown
- 2013-04-01 US US14/363,718 patent/US9908886B2/en active Active
- 2013-04-01 WO PCT/SG2013/000126 patent/WO2013147711A1/en not_active Ceased
- 2013-04-01 NO NO13768800A patent/NO2831079T3/no unknown
- 2013-04-01 PL PL17179630.3T patent/PL3321268T3/pl unknown
- 2013-04-01 CN CN201380027654.7A patent/CN104350055B/zh active Active
- 2013-04-01 DK DK13768800.8T patent/DK2831079T3/da active
- 2013-04-01 PL PL13768800T patent/PL2831079T3/pl unknown
- 2013-04-01 EP EP13768800.8A patent/EP2831079B1/en active Active
- 2013-04-01 EP EP17179630.3A patent/EP3321268B1/en active Active
- 2013-04-01 ES ES13768800.8T patent/ES2647959T3/es active Active
-
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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