JP2018522867A5 - - Google Patents
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- Publication number
- JP2018522867A5 JP2018522867A5 JP2017567218A JP2017567218A JP2018522867A5 JP 2018522867 A5 JP2018522867 A5 JP 2018522867A5 JP 2017567218 A JP2017567218 A JP 2017567218A JP 2017567218 A JP2017567218 A JP 2017567218A JP 2018522867 A5 JP2018522867 A5 JP 2018522867A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pharmaceutically acceptable
- hydrate
- acceptable salt
- 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
- 150000001875 compounds Chemical class 0.000 claims 29
- 239000013078 crystal Substances 0.000 claims 24
- 239000000651 prodrug Substances 0.000 claims 24
- 229940002612 prodrug Drugs 0.000 claims 24
- 150000003839 salts Chemical class 0.000 claims 24
- 239000012453 solvate Substances 0.000 claims 23
- 125000000623 heterocyclic group Chemical group 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000001072 heteroaryl group Chemical group 0.000 claims 12
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 11
- 125000004452 carbocyclyl group Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000002252 acyl group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 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 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 125000004430 oxygen atom Chemical group O* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 230000001568 sexual effect Effects 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 238000003419 tautomerization reaction Methods 0.000 claims 2
- 229940126062 Compound A Drugs 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 239000000523 sample Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562185366P | 2015-06-26 | 2015-06-26 | |
| US62/185,366 | 2015-06-26 | ||
| PCT/US2016/039302 WO2016210291A1 (en) | 2015-06-26 | 2016-06-24 | Fused bicyclic pyrimidine derivatives and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018522867A JP2018522867A (ja) | 2018-08-16 |
| JP2018522867A5 true JP2018522867A5 (enExample) | 2019-07-25 |
Family
ID=57585794
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017567218A Pending JP2018522867A (ja) | 2015-06-26 | 2016-06-24 | 縮合二環式ピリミジン誘導体およびこれらの使用 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10342798B2 (enExample) |
| EP (1) | EP3313529A4 (enExample) |
| JP (1) | JP2018522867A (enExample) |
| AU (1) | AU2016283100A1 (enExample) |
| CA (1) | CA2988461A1 (enExample) |
| HK (1) | HK1254469A1 (enExample) |
| WO (1) | WO2016210291A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10870651B2 (en) | 2014-12-23 | 2020-12-22 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| CN107427521B (zh) | 2015-03-27 | 2021-08-03 | 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 |
| AU2016283105C1 (en) | 2015-06-26 | 2023-02-02 | Dana-Farber Cancer Institute, Inc. | 4,6-pyrimidinylene derivatives and uses thereof |
| CN107698603B (zh) * | 2016-08-09 | 2022-04-08 | 南京红云生物科技有限公司 | 噻吩并嘧啶类化合物、其制备方法、药用组合物及其应用 |
| CN109384782A (zh) * | 2017-08-04 | 2019-02-26 | 厦门大学 | 取代五元并六元杂环类化合物、其制备方法、药物组合及其用途 |
| CN107557370B (zh) * | 2017-09-25 | 2020-03-17 | 华南农业大学 | 水稻rel1基因在提高植物抗干旱胁迫中的应用 |
| BR112020012651A2 (pt) | 2017-12-22 | 2020-12-01 | Ravenna Pharmaceuticals, Inc. | compostos derivados de aril-bipiridina amina como inibidores da fosfatidilinositol fosfato quinase, composição farmacêutica compreendendo os mesmos e usos terapêuticos dos ditos compostos |
| CN111936484A (zh) * | 2017-12-22 | 2020-11-13 | 拉文纳制药公司 | 作为磷脂酰肌醇磷酸激酶抑制剂的色烯并吡啶衍生物 |
| EP3810132A4 (en) | 2018-06-25 | 2022-06-22 | Dana-Farber Cancer Institute, Inc. | TAIRE FAMILY KINASE INHIBITORS AND RELATED USES |
| CN113164477A (zh) | 2018-12-14 | 2021-07-23 | 达纳-法伯癌症研究所股份有限公司 | C-jun-n-末端激酶的吡唑并吡啶抑制剂及其用途 |
| EP3902542A4 (en) | 2018-12-28 | 2022-09-07 | Dana-Farber Cancer Institute, Inc. | CYCLIN DEPENDENT KINASE 7 INHIBITORS AND USES THEREOF |
| CA3136354A1 (en) * | 2019-04-10 | 2020-10-15 | Cornell University | Pip4ks suppress insulin signaling and enhance immune function through a catalytic-independent mechanism |
| CN109879887B (zh) * | 2019-04-16 | 2021-07-20 | 辽宁大学 | 含吲哚结构的噻吩并[3,2-d]嘧啶类衍生物及其应用 |
| CN114133394B (zh) * | 2020-08-12 | 2023-12-08 | 赛诺哈勃药业（成都）有限公司 | 一种选择性针对细胞周期依赖性激酶12活性的化合物、制备方法及医药用途 |
| EP4259128A4 (en) * | 2020-12-09 | 2025-04-30 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| EP4341254A4 (en) * | 2021-05-20 | 2025-04-09 | Dana-Farber Cancer Institute, Inc. | INHIBITORS AND DEGRADERS OF THE PIP4K PROTEIN |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ｃｋ１２抑制劑 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| WO2023227125A1 (zh) * | 2022-05-26 | 2023-11-30 | 杭州德睿智药科技有限公司 | 作为CDKs抑制剂的新型并杂环类新化合物及其应用 |
| WO2023246371A1 (zh) * | 2022-06-24 | 2023-12-28 | 中国科学院基础医学与肿瘤研究所(筹) | 具有嘧啶并噻吩结构的小分子化合物及其应用 |
| CN117338769B (zh) * | 2023-10-30 | 2026-03-20 | 中国科学技术大学 | 罗替戈汀的抗多发性骨髓瘤活性与应用 |
| CN119874680B (zh) * | 2025-03-27 | 2026-02-13 | 浙大城市学院 | 含2-氯丙烯酰胺的2-氨基嘧啶类化合物、其制备方法和应用 |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1465900B1 (en) * | 2002-01-10 | 2008-05-14 | Bayer HealthCare AG | Rho-kinase inhibitors |
| EP2937345B1 (en) * | 2009-12-29 | 2018-03-21 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| JP6106685B2 (ja) * | 2011-11-17 | 2017-04-05 | ダナ−ファーバー キャンサー インスティテュート， インコーポレイテッド | Ｃ−ｊｕｎ−ｎ−末端キナーゼ（ｊｎｋ）の阻害剤 |
| WO2013154778A1 (en) | 2012-04-11 | 2013-10-17 | Dana-Farber Cancer Institute, Inc. | Host targeted inhibitors of dengue virus and other viruses |
| EP2909194A1 (en) * | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| CN103242341B (zh) * | 2013-04-19 | 2015-12-09 | 中国科学院广州生物医药与健康研究院 | 噻吩并2，4取代嘧啶类化合物及其药物组合物与应用 |
| CN104177363B (zh) | 2013-05-24 | 2018-06-05 | 江苏先声药业有限公司 | 双环杂环胺类Hedgehog信号通路抑制剂 |
| WO2015058126A1 (en) | 2013-10-18 | 2015-04-23 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| AU2014337044A1 (en) * | 2013-10-18 | 2016-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| WO2015164614A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
-
2016
- 2016-06-24 HK HK18113555.0A patent/HK1254469A1/zh unknown
- 2016-06-24 WO PCT/US2016/039302 patent/WO2016210291A1/en not_active Ceased
- 2016-06-24 EP EP16815397.1A patent/EP3313529A4/en not_active Withdrawn
- 2016-06-24 CA CA2988461A patent/CA2988461A1/en not_active Abandoned
- 2016-06-24 AU AU2016283100A patent/AU2016283100A1/en not_active Abandoned
- 2016-06-24 JP JP2017567218A patent/JP2018522867A/ja active Pending
- 2016-06-24 US US15/737,683 patent/US10342798B2/en active Active