JP2019536820A5 - - Google Patents
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- JP2019536820A5 JP2019536820A5 JP2019549613A JP2019549613A JP2019536820A5 JP 2019536820 A5 JP2019536820 A5 JP 2019536820A5 JP 2019549613 A JP2019549613 A JP 2019549613A JP 2019549613 A JP2019549613 A JP 2019549613A JP 2019536820 A5 JP2019536820 A5 JP 2019536820A5
- Authority
- JP
- Japan
- Prior art keywords
- compound according
- alkyl
- halogen
- compound
- heterocyclyl
- 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
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- 150000001875 compounds Chemical class 0.000 claims 41
- 125000000217 alkyl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 11
- 229910052799 carbon Inorganic materials 0.000 claims 10
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
- 229920006395 saturated elastomer Polymers 0.000 claims 5
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 4
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 4
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- -1 CR 8 Inorganic materials 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- DKYBVKMIZODYKL-UHFFFAOYSA-N 1,3-diazinane Chemical compound C1CNCNC1 DKYBVKMIZODYKL-UHFFFAOYSA-N 0.000 claims 2
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 2
- YPWFISCTZQNZAU-UHFFFAOYSA-N Thiane Chemical compound C1CCSCC1 YPWFISCTZQNZAU-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- BRNULMACUQOKMR-UHFFFAOYSA-N thiomorpholine Chemical compound C1CSCCN1 BRNULMACUQOKMR-UHFFFAOYSA-N 0.000 claims 2
- 125000002947 alkylene group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000004438 haloalkoxy group Chemical group 0.000 claims 1
- 125000001188 haloalkyl group Chemical group 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 0 *c(c1c(*)nc(N(*)*)nc11)c(*)[n]1-c1c(*)c(*)c(*)c(N(*)S(O*)(=O)=O)c1* Chemical compound *c(c1c(*)nc(N(*)*)nc11)c(*)[n]1-c1c(*)c(*)c(*)c(N(*)S(O*)(=O)=O)c1* 0.000 description 4
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662428756P | 2016-12-01 | 2016-12-01 | |
| US62/428,756 | 2016-12-01 | ||
| PCT/CA2017/000258 WO2018098561A1 (en) | 2016-12-01 | 2017-12-01 | Fused pyrimidine compounds as brd4 and jak2 dual inhibitors and methods for use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019536820A JP2019536820A (ja) | 2019-12-19 |
| JP2019536820A5 true JP2019536820A5 (enExample) | 2021-01-14 |
Family
ID=62241001
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019549613A Pending JP2019536820A (ja) | 2016-12-01 | 2017-12-01 | Ｂｒａｄ４およびｊａｋ２の二重阻害剤としての縮合環式ピリミジン化合物、ならびにその使用に関する方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11279703B2 (enExample) |
| EP (1) | EP3548496A4 (enExample) |
| JP (1) | JP2019536820A (enExample) |
| KR (1) | KR20190135464A (enExample) |
| CN (1) | CN110691782A (enExample) |
| AU (1) | AU2017369753A1 (enExample) |
| WO (1) | WO2018098561A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3717475B1 (en) | 2017-11-20 | 2023-06-07 | Icahn School of Medicine at Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| WO2019136320A1 (en) | 2018-01-05 | 2019-07-11 | Icahn School Of Medicine At Mount Sinai | Method of increasing proliferation of pancreatic beta cells, treatment method, and composition |
| AU2019240065A1 (en) | 2018-03-20 | 2020-09-24 | Icahn School Of Medicine At Mount Sinai | Kinase inhibitor compounds and compositions and methods of use |
| WO2020051572A1 (en) * | 2018-09-07 | 2020-03-12 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Brd4-jak2 inhibitors |
| KR102377007B1 (ko) * | 2018-09-20 | 2022-03-22 | 한미약품 주식회사 | 상피세포 성장인자 수용체 돌연변이 저해 효과를 갖는 신규 융합 피리미딘 골격 설폰아마이드 유도체 |
| EP3842435A4 (en) * | 2018-09-20 | 2022-05-11 | Hanmi Pharm. Co., Ltd. | NEW SULFONAMIDE DERIVATIVE PRESENTING A FUSED PYRIMIDINE SKELETON, HAVING AN INHIBITOR EFFECT OF EPIDERMAL GROWTH FACTOR RECEPTOR MUTATION |
| JP2022515650A (ja) * | 2018-12-31 | 2022-02-21 | アイカーン スクール オブ メディシン アット マウント サイナイ | キナーゼ阻害剤化合物及び組成物ならびに使用方法 |
| CN110305140B (zh) * | 2019-07-30 | 2020-08-04 | 上海勋和医药科技有限公司 | 二氢吡咯并嘧啶类选择性jak2抑制剂 |
| WO2021030238A2 (en) * | 2019-08-09 | 2021-02-18 | Ohm Oncology | Method of synthesis of compound for dual inhibition of jak2 and bet |
| EP3800188A1 (en) | 2019-10-02 | 2021-04-07 | Bayer AG | Substituted pyrazolopyrimidines as irak4 inhibitors |
| GB201914910D0 (en) * | 2019-10-15 | 2019-11-27 | Sentinel Oncology Ltd | Pharmaceutical compounds |
| JP7621351B2 (ja) * | 2019-11-08 | 2025-01-24 | ネクセラ・ファーマ・ユーケイ・リミテッド | Ｇｐｒ５２モジュレーター化合物 |
| CN114728978A (zh) * | 2019-11-22 | 2022-07-08 | 南京明德新药研发有限公司 | 作为dna-pk抑制剂的嘧啶并吡咯类螺环化合物及其衍生物 |
| WO2022083560A1 (zh) * | 2020-10-19 | 2022-04-28 | 南京药石科技股份有限公司 | Tyk2选择性抑制剂及其用途 |
| CN117295743A (zh) * | 2021-04-30 | 2023-12-26 | 微境生物医药科技(上海)有限公司 | 作为Wee-1抑制剂的吡咯并嘧啶衍生物 |
| GB202113079D0 (en) * | 2021-09-14 | 2021-10-27 | Ucl Business Ltd | New therapy |
| JP2024540921A (ja) * | 2021-10-19 | 2024-11-06 | 上海瑛派▲薬▼▲業▼有限公司 | Ｕｓｐ１阻害剤としての置換トリアゾロヘテロアリール化合物及びその応用 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
| CN118574832A (zh) * | 2022-01-19 | 2024-08-30 | 上海奕拓医药科技有限责任公司 | 三并环化合物、其制备、药物组合物及应用 |
| CN116731035A (zh) * | 2022-03-08 | 2023-09-12 | 广州再极医药科技有限公司 | 一种噻吩并嘧啶类化合物、中间体、其制备方法、组合物和应用 |
| CN114957248B (zh) * | 2022-05-09 | 2023-12-29 | 南开大学 | 一种吡咯并嘧啶化合物及其制备方法、药物组合物和应用 |
| CN116813624B (zh) * | 2023-06-29 | 2025-10-03 | 成都金瑞基业生物科技有限公司 | 一种jak2抑制剂的晶型及制备方法 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB9903762D0 (en) * | 1999-02-18 | 1999-04-14 | Novartis Ag | Organic compounds |
| AU2008323628B2 (en) * | 2007-11-15 | 2013-10-17 | Ym Biosciences Australia Pty Ltd | N-containing heterocyclic compounds |
| WO2009131687A2 (en) * | 2008-04-22 | 2009-10-29 | Portola Pharmaceuticals, Inc. | Inhibitors of protein kinases |
| TW201035100A (en) * | 2008-12-19 | 2010-10-01 | Cephalon Inc | Pyrrolotriazines as ALK and JAK2 inhibitors |
| ES2487542T3 (es) * | 2009-05-22 | 2014-08-21 | Incyte Corporation | Derivados de N-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo[2,3-d]pirimidinas y pirrol-3-il-pirrolo[2,3-d]pirimidinas como inhibidores de cinasas Janus |
| KR101147550B1 (ko) * | 2009-10-22 | 2012-05-17 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| KR101094446B1 (ko) * | 2009-11-19 | 2011-12-15 | 한국과학기술연구원 | 단백질 키나아제 저해활성을 가지는 2,4,7-치환된 티에노［3,2-ｄ］피리미딘 화합물 |
| EP2947084B8 (en) * | 2013-01-18 | 2021-03-10 | Guangzhou Maxinovel Pharmaceuticals Co. | Five-and-six-membered heterocyclic compound, and preparation method, pharmaceutical composition and use thereof |
| KR101704386B1 (ko) * | 2013-06-28 | 2017-02-08 | 한국과학기술연구원 | 티에노[3,2-ｄ]피리미딘 유도체의 Ｔ315Ｉ-Ｂｃｒ-Ａｂｌ 점돌연변이종의 저해 활성 |
| WO2015038417A1 (en) * | 2013-09-10 | 2015-03-19 | Asana Biosciences, Llc | Compounds for regulating fak and/or src pathways |
| WO2015151006A1 (en) * | 2014-03-29 | 2015-10-08 | Lupin Limited | Substituted purine compounds as btk inhibitors |
| WO2016022460A1 (en) * | 2014-08-03 | 2016-02-11 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Potent dual brd4-kinase inhibitors as cancer therapeutics |
| US10947201B2 (en) * | 2015-02-17 | 2021-03-16 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| 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 |
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2017
- 2017-12-01 KR KR1020197018280A patent/KR20190135464A/ko not_active Ceased
- 2017-12-01 EP EP17875551.8A patent/EP3548496A4/en not_active Withdrawn
- 2017-12-01 CN CN201780085399.XA patent/CN110691782A/zh active Pending
- 2017-12-01 AU AU2017369753A patent/AU2017369753A1/en not_active Abandoned
- 2017-12-01 JP JP2019549613A patent/JP2019536820A/ja active Pending
- 2017-12-01 WO PCT/CA2017/000258 patent/WO2018098561A1/en not_active Ceased
- 2017-12-01 US US16/465,880 patent/US11279703B2/en active Active