JP2017512186A5 - - Google Patents
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- Publication number
- JP2017512186A5 JP2017512186A5 JP2016549433A JP2016549433A JP2017512186A5 JP 2017512186 A5 JP2017512186 A5 JP 2017512186A5 JP 2016549433 A JP2016549433 A JP 2016549433A JP 2016549433 A JP2016549433 A JP 2016549433A JP 2017512186 A5 JP2017512186 A5 JP 2017512186A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- protecting group
- attached
- nitrogen
- 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.)
- Pending
Links
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- 125000001072 heteroaryl group Chemical group 0.000 claims 27
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 18
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 18
- 125000003342 alkenyl group Chemical group 0.000 claims 17
- 125000000304 alkynyl group Chemical group 0.000 claims 17
- 125000004452 carbocyclyl group Chemical group 0.000 claims 17
- 102000001805 Bromodomains Human genes 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 13
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 11
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 11
- 229910052717 sulfur Inorganic materials 0.000 claims 11
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 10
- 108091005575 Bromodomain-containing proteins Proteins 0.000 claims 8
- 238000000034 method Methods 0.000 claims 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 8
- 229910052760 oxygen Inorganic materials 0.000 claims 8
- 239000001301 oxygen Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 125000002252 acyl group Chemical group 0.000 claims 7
- 125000004429 atom Chemical group 0.000 claims 7
- 125000004434 sulfur atom Chemical group 0.000 claims 7
- 108050009021 Bromodomains Proteins 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000004430 oxygen atom Chemical group O* 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000000694 effects Effects 0.000 claims 4
- 208000015181 infectious disease Diseases 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- -1 n- propyl Chemical group 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 208000030507 AIDS Diseases 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 102100033641 Bromodomain-containing protein 2 Human genes 0.000 claims 2
- 101710126816 Bromodomain-containing protein 2 Proteins 0.000 claims 2
- 102100033642 Bromodomain-containing protein 3 Human genes 0.000 claims 2
- 101710126814 Bromodomain-containing protein 3 Proteins 0.000 claims 2
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims 2
- 101710126815 Bromodomain-containing protein 4 Proteins 0.000 claims 2
- 108010040163 CREB-Binding Protein Proteins 0.000 claims 2
- 102100021975 CREB-binding protein Human genes 0.000 claims 2
- 208000009329 Graft vs Host Disease Diseases 0.000 claims 2
- 241000711549 Hepacivirus C Species 0.000 claims 2
- 102100038885 Histone acetyltransferase p300 Human genes 0.000 claims 2
- 101000882390 Homo sapiens Histone acetyltransferase p300 Proteins 0.000 claims 2
- 241000725303 Human immunodeficiency virus Species 0.000 claims 2
- 241000701806 Human papillomavirus Species 0.000 claims 2
- 201000003176 Severe Acute Respiratory Syndrome Diseases 0.000 claims 2
- 241000700584 Simplexvirus Species 0.000 claims 2
- 102000006467 TATA-Box Binding Protein Human genes 0.000 claims 2
- 108010044281 TATA-Box Binding Protein Proteins 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 208000024908 graft versus host disease Diseases 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 201000011001 Ebola Hemorrhagic Fever Diseases 0.000 claims 1
- 108010033040 Histones Proteins 0.000 claims 1
- 101000596093 Homo sapiens Transcription initiation factor TFIID subunit 1 Proteins 0.000 claims 1
- 101000596092 Homo sapiens Transcription initiation factor TFIID subunit 1-like Proteins 0.000 claims 1
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims 1
- VEYYWZRYIYDQJM-ZETCQYMHSA-N N(2)-acetyl-L-lysine Chemical group CC(=O)N[C@H](C([O-])=O)CCCC[NH3+] VEYYWZRYIYDQJM-ZETCQYMHSA-N 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 206010040047 Sepsis Diseases 0.000 claims 1
- 102100035222 Transcription initiation factor TFIID subunit 1 Human genes 0.000 claims 1
- 102100035238 Transcription initiation factor TFIID subunit 1-like Human genes 0.000 claims 1
- 208000036142 Viral infection Diseases 0.000 claims 1
- 230000036523 atherogenesis Effects 0.000 claims 1
- 125000001246 bromo group Chemical group Br* 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 208000016097 disease of metabolism Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 206010022000 influenza Diseases 0.000 claims 1
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 230000005855 radiation Effects 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 231100000419 toxicity Toxicity 0.000 claims 1
- 230000001988 toxicity Effects 0.000 claims 1
- 238000013518 transcription Methods 0.000 claims 1
- 230000035897 transcription Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
- 230000009385 viral infection Effects 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461934624P | 2014-01-31 | 2014-01-31 | |
| US61/934,624 | 2014-01-31 | ||
| PCT/US2015/014044 WO2015117055A1 (en) | 2014-01-31 | 2015-02-02 | Dihydropteridinone derivatives and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2017512186A JP2017512186A (ja) | 2017-05-18 |
| JP2017512186A5 true JP2017512186A5 (https=) | 2018-03-15 |
Family
ID=53757802
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016549433A Pending JP2017512186A (ja) | 2014-01-31 | 2015-02-02 | ジヒドロプテリジノン誘導体およびその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20160347750A1 (https=) |
| EP (1) | EP3099171A4 (https=) |
| JP (1) | JP2017512186A (https=) |
| KR (1) | KR20160111520A (https=) |
| CN (1) | CN105939607A (https=) |
| CA (1) | CA2936871A1 (https=) |
| MX (1) | MX2016009975A (https=) |
| RU (1) | RU2673944C2 (https=) |
| WO (1) | WO2015117055A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9180127B2 (en) | 2009-12-29 | 2015-11-10 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
| CA2856291C (en) | 2011-11-17 | 2020-08-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US9758522B2 (en) | 2012-10-19 | 2017-09-12 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| EP3057955B1 (en) | 2013-10-18 | 2018-04-11 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| US10047070B2 (en) | 2013-10-18 | 2018-08-14 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2015117087A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Uses of diazepane derivatives |
| CA2936865A1 (en) | 2014-01-31 | 2015-08-06 | Dana-Farber Cancer Institute, Inc. | Diaminopyrimidine benzenesulfone derivatives and uses thereof |
| US9862688B2 (en) | 2014-04-23 | 2018-01-09 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| US10017477B2 (en) | 2014-04-23 | 2018-07-10 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| CN106715437A (zh) | 2014-08-08 | 2017-05-24 | 达纳-法伯癌症研究所股份有限公司 | 二氮杂环庚烷衍生物及其用途 |
| AU2015371251B2 (en) | 2014-12-23 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| EP3347018B1 (en) | 2015-09-09 | 2021-09-01 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| RU2018112953A (ru) | 2015-09-11 | 2019-10-14 | Дана-Фарбер Кэнсер Инститьют, Инк. | Ацетамидтиенотриазолодиазепины и пути их применения |
| HK1256417A1 (zh) | 2015-09-11 | 2019-09-20 | 达纳-法伯癌症研究所股份有限公司 | 氰基噻吩并三唑并二氮杂环庚三烯及其用途 |
| MX2018006499A (es) | 2015-11-25 | 2018-08-01 | Dana Farber Cancer Inst Inc | Inhibidores de bromodominio bivalentes y usos de los mismos. |
| CN105597100B (zh) * | 2016-01-07 | 2018-08-21 | 国家卫生计生委科学技术研究所 | 一种brdt蛋白抑制剂在雄性抗生育中的应用 |
| CN105640962B (zh) * | 2016-01-07 | 2017-07-07 | 国家卫生计生委科学技术研究所 | 一种蛋白抑制剂在抗生育中的应用 |
| CN105412107B (zh) * | 2016-01-07 | 2017-05-03 | 国家卫生计生委科学技术研究所 | 蛋白抑制剂t323在抗生育中的应用 |
| CN105412931B (zh) * | 2016-01-07 | 2017-05-10 | 国家卫生计生委科学技术研究所 | 一种小分子抑制剂在抗生育中的用途 |
| CN105801582A (zh) * | 2016-04-12 | 2016-07-27 | 合肥工业大学 | 一类新型二氢蝶啶酮类衍生物及其制备方法和在医药上的用途 |
| DE102017005091A1 (de) | 2016-05-30 | 2017-11-30 | Bayer Pharma Aktiengesellschaft | Substituierte 3,4-Dihydropyrido[2,3-b]pyrazin-2(1H)-one |
| CN107586315B (zh) * | 2016-07-08 | 2020-03-31 | 成都海创药业有限公司 | 一种嵌合分子 |
| US20210261539A1 (en) * | 2018-02-06 | 2021-08-26 | Shanghai Haihe Pharmaceutical Co., Ltd. | Compound having bet inhibitory activity and preparation method and use therefor |
| ES2969982T3 (es) * | 2018-04-24 | 2024-05-23 | Vertex Pharma | Compuestos de pteridinona y usos de los mismos |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| EP3833353A4 (en) * | 2018-08-10 | 2022-08-24 | Yale University | Small-molecule pi5p4k alpha/beta inhibitors and methods of treatment using same |
| CN111039944B (zh) | 2018-10-12 | 2021-11-23 | 中国科学院合肥物质科学研究院 | Mst1激酶抑制剂及其用途 |
| WO2020093162A1 (en) * | 2018-11-07 | 2020-05-14 | Neomed Institute | Treatment of bet inhibitor-resistant cancers and other diseases responsive to dual bet and cbp/ep300 inhibition therapy |
| CN116850165B (zh) * | 2022-03-28 | 2026-04-14 | 广州国家实验室 | 化合物及其药学上可接受的盐在抗冠状病毒中的用途 |
| WO2025207957A1 (en) * | 2024-03-28 | 2025-10-02 | Yale University | Small-molecule pi5p4k alpha/beta inhibitors and methods using same |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CZ200439A3 (cs) * | 2001-07-20 | 2005-03-16 | Novo Nordisk A/S | Farmaceutický prostředek obsahující polypeptidy faktoru Vll a polypeptidy faktoru XI |
| US6806272B2 (en) * | 2001-09-04 | 2004-10-19 | Boehringer Ingelheim Pharma Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| BR0318145A (pt) * | 2003-02-26 | 2006-02-21 | Boehringer Ingelheim Pharma | dihidropteridinonas, processos para a sua preparação e sua aplicação como medicamento |
| US6861422B2 (en) * | 2003-02-26 | 2005-03-01 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions |
| MXPA06003054A (es) * | 2003-09-18 | 2006-05-31 | Novartis Ag | 2,4-di-(fenil-amino)-pirimidinas utiles en el tratamiento de trastornos proliferativos. |
| US20060035903A1 (en) * | 2004-08-14 | 2006-02-16 | Boehringer Ingelheim International Gmbh | Storage stable perfusion solution for dihydropteridinones |
| US20060074088A1 (en) * | 2004-08-14 | 2006-04-06 | Boehringer Ingelheim International Gmbh | Dihydropteridinones for the treatment of cancer diseases |
| US7728134B2 (en) * | 2004-08-14 | 2010-06-01 | Boehringer Ingelheim International Gmbh | Hydrates and polymorphs of 4[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, process for their manufacture and their use as medicament |
| US7759485B2 (en) * | 2004-08-14 | 2010-07-20 | Boehringer Ingelheim International Gmbh | Process for the manufacture of dihydropteridinones |
| US20060058311A1 (en) * | 2004-08-14 | 2006-03-16 | Boehringer Ingelheim International Gmbh | Combinations for the treatment of diseases involving cell proliferation |
| JP2008510771A (ja) * | 2004-08-27 | 2008-04-10 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ジヒドロプテリジノン、その製造方法および医薬薬剤としてのその使用 |
| WO2007014838A1 (en) * | 2005-08-03 | 2007-02-08 | Boehringer Ingelheim International Gmbh | Dihydropteridinones in the treatment of respiratory diseases |
| WO2008009909A1 (en) * | 2006-07-17 | 2008-01-24 | Astrazeneca Ab | Pteridimones as modulators of polo-like kinase |
| ATE543819T1 (de) * | 2006-10-19 | 2012-02-15 | Signal Pharm Llc | Heteroarylverbindungen, zusammensetzungen daraus und behandlungsverfahren damit |
| WO2008050096A1 (en) * | 2006-10-25 | 2008-05-02 | Chroma Therapeutics Ltd. | Pteridine derivatives as polo-like kinase inhibitors useful in the treatment of cancer |
| EP2112152A1 (en) * | 2008-04-22 | 2009-10-28 | GPC Biotech AG | Dihydropteridinones as Plk Inhibitors |
| CN102020643A (zh) * | 2009-09-22 | 2011-04-20 | 上海恒瑞医药有限公司 | 二氢喋啶酮类衍生物、其制备方法及其在医药上的应用 |
| US9358233B2 (en) * | 2010-11-29 | 2016-06-07 | Boehringer Ingelheim International Gmbh | Method for treating acute myeloid leukemia |
| WO2014095774A1 (de) * | 2012-12-20 | 2014-06-26 | Bayer Pharma Aktiengesellschaft | Bet-proteininhibitorische dihydropyridopyrazinone |
-
2015
- 2015-02-02 WO PCT/US2015/014044 patent/WO2015117055A1/en not_active Ceased
- 2015-02-02 MX MX2016009975A patent/MX2016009975A/es unknown
- 2015-02-02 CN CN201580006508.5A patent/CN105939607A/zh active Pending
- 2015-02-02 CA CA2936871A patent/CA2936871A1/en not_active Abandoned
- 2015-02-02 EP EP15743171.9A patent/EP3099171A4/en not_active Withdrawn
- 2015-02-02 KR KR1020167023459A patent/KR20160111520A/ko not_active Withdrawn
- 2015-02-02 RU RU2016133196A patent/RU2673944C2/ru not_active IP Right Cessation
- 2015-02-02 JP JP2016549433A patent/JP2017512186A/ja active Pending
- 2015-02-02 US US15/114,989 patent/US20160347750A1/en not_active Abandoned
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