JP2019527682A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019527682A5 JP2019527682A5 JP2019500570A JP2019500570A JP2019527682A5 JP 2019527682 A5 JP2019527682 A5 JP 2019527682A5 JP 2019500570 A JP2019500570 A JP 2019500570A JP 2019500570 A JP2019500570 A JP 2019500570A JP 2019527682 A5 JP2019527682 A5 JP 2019527682A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- pharmaceutically acceptable
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 34
- 239000000651 prodrug Substances 0.000 claims 32
- 229940002612 prodrug Drugs 0.000 claims 32
- 150000003839 salts Chemical class 0.000 claims 32
- 239000012453 solvate Substances 0.000 claims 31
- 239000013078 crystal Substances 0.000 claims 30
- 229910052739 hydrogen Inorganic materials 0.000 claims 29
- 239000001257 hydrogen Substances 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 28
- 150000002431 hydrogen Chemical class 0.000 claims 26
- 125000000623 heterocyclic group Chemical group 0.000 claims 23
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 17
- 150000002367 halogens Chemical class 0.000 claims 17
- 125000004452 carbocyclyl group Chemical group 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000000304 alkynyl group Chemical group 0.000 claims 11
- 201000010099 disease Diseases 0.000 claims 11
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 10
- 125000004429 atom Chemical group 0.000 claims 8
- 150000004677 hydrates Chemical class 0.000 claims 6
- 102000001253 Protein Kinase Human genes 0.000 claims 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- 108060006633 protein kinase Proteins 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 125000002252 acyl group Chemical group 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 125000004430 oxygen atom Chemical group O* 0.000 claims 3
- 125000004193 piperazinyl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 125000004434 sulfur atom Chemical group 0.000 claims 3
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 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
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 230000001594 aberrant effect Effects 0.000 claims 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 238000003419 tautomerization reaction Methods 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- 208000019838 Blood disease Diseases 0.000 claims 1
- 208000026350 Inborn Genetic disease Diseases 0.000 claims 1
- 208000023178 Musculoskeletal disease Diseases 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease Diseases 0.000 claims 1
- 208000034038 Pathologic Neovascularization Diseases 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 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
- 230000000694 effects Effects 0.000 claims 1
- 208000016361 genetic disease Diseases 0.000 claims 1
- 208000014951 hematologic disease Diseases 0.000 claims 1
- 208000018706 hematopoietic system disease Diseases 0.000 claims 1
- 208000027866 inflammatory disease Diseases 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
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 208000017445 musculoskeletal system disease Diseases 0.000 claims 1
- 230000009826 neoplastic cell growth Effects 0.000 claims 1
- 239000008177 pharmaceutical agent Substances 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
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662358524P | 2016-07-05 | 2016-07-05 | |
| US62/358,524 | 2016-07-05 | ||
| PCT/US2017/040722 WO2018009544A1 (en) | 2016-07-05 | 2017-07-05 | Bicyclic urea kinase inhibitors and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019527682A JP2019527682A (ja) | 2019-10-03 |
| JP2019527682A5 true JP2019527682A5 (enExample) | 2020-08-13 |
| JP7277357B2 JP7277357B2 (ja) | 2023-05-18 |
Family
ID=59351134
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019500570A Active JP7277357B2 (ja) | 2016-07-05 | 2017-07-05 | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (3) | US10954242B2 (enExample) |
| EP (2) | EP3481830B1 (enExample) |
| JP (1) | JP7277357B2 (enExample) |
| KR (1) | KR20190075043A (enExample) |
| CN (1) | CN110225914A (enExample) |
| AU (1) | AU2017291812B2 (enExample) |
| CA (1) | CA3069016A1 (enExample) |
| ES (1) | ES2920823T3 (enExample) |
| IL (1) | IL264106B (enExample) |
| WO (1) | WO2018009544A1 (enExample) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3171874B1 (en) | 2014-07-21 | 2020-11-18 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| JP7277357B2 (ja) | 2016-07-05 | 2023-05-18 | ザ ブロード インスティテュート,インコーポレーテッド | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
| WO2018053373A1 (en) | 2016-09-16 | 2018-03-22 | The General Hospital Corporation | Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis |
| EP3589284A4 (en) | 2017-02-28 | 2020-12-16 | The General Hospital Corporation | USES OF PYRIMIDOPYRIMIDINONES AS SIK INHIBITORS |
| PL3774805T3 (pl) * | 2018-03-30 | 2024-05-06 | Les Laboratoires Servier | Heterobicykliczne inhibitory mat2a i sposoby przydatne do leczenia nowotworu |
| WO2020027200A1 (ja) * | 2018-08-01 | 2020-02-06 | 小野薬品工業株式会社 | 軟骨関連疾患治療剤 |
| WO2021062327A1 (en) * | 2019-09-27 | 2021-04-01 | Jubilant Biosys Limited | Fused pyrimidine compounds, compositions and medicinal applications thereof |
| GB201915829D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| GB201915828D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| GB201915831D0 (en) | 2019-10-31 | 2019-12-18 | Cancer Research Tech Ltd | Compounds, compositions and therapeutic uses thereof |
| CA3169649A1 (en) * | 2020-01-30 | 2021-08-05 | The Regents Of The University Of California | Strad-binding agents and uses thereof |
| EP4143191A2 (en) * | 2020-04-28 | 2023-03-08 | iOmx Therapeutics AG | Bicyclic kinase inhibitors and uses thereof |
| EP4149629B1 (en) | 2020-05-14 | 2025-06-04 | Rhizen Pharmaceuticals AG | Purine derivatives as sik-3 inhibitors |
| KR102673031B1 (ko) * | 2020-09-16 | 2024-06-07 | 주식회사 엑세쏘바이오파마 | 피리미도 피리미디논 화합물 및 그를 포함하는 약제학적 조성물 |
| AU2021343539A1 (en) * | 2020-09-21 | 2023-05-18 | Soltego, Inc. | Sik inhibitors and methods of use thereof |
| CN116801878A (zh) * | 2020-10-05 | 2023-09-22 | 达纳-法伯癌症研究所股份有限公司 | Her2的有效和选择性抑制剂 |
| WO2022120132A1 (en) * | 2020-12-04 | 2022-06-09 | Dyne Therapeutics, Inc. | Antibody-oligonucleotide complexes and uses thereof |
| US20240174662A1 (en) * | 2021-02-01 | 2024-05-30 | Janssen Biotech, Inc. | Small molecule inhibitors of salt inducible kinases |
| KR20230053049A (ko) * | 2021-10-13 | 2023-04-21 | 서울대학교산학협력단 | 류마티스 관절염 예방 또는 치료용 약학적 조성물 및 건강기능식품 |
| CN116813608B (zh) * | 2023-06-08 | 2024-03-22 | 英矽智能科技(上海)有限公司 | 噻唑类化合物及其应用 |
| CN117547615B (zh) * | 2023-09-26 | 2024-12-06 | 首都医科大学宣武医院 | 一种纳米囊泡及其制备方法和应用 |
Family Cites Families (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4231559B2 (ja) | 1997-04-23 | 2009-03-04 | オリザ油化株式会社 | リポキシゲナーゼ阻害剤 |
| ES2310039T3 (es) | 1998-05-26 | 2008-12-16 | Warner-Lambert Company Llc | Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular. |
| NZ510760A (en) | 1998-10-23 | 2003-08-29 | F | Bicyclic nitrogen heterocycles |
| US20050202001A1 (en) | 2002-04-24 | 2005-09-15 | Han-Mo Koo | Enhancement of human epidermal melanogenesis |
| US7084270B2 (en) | 2002-08-14 | 2006-08-01 | Hoffman-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| DE10239042A1 (de) | 2002-08-21 | 2004-03-04 | Schering Ag | Makrozyclische Pyrimidine, deren Herstellung und Verwendung als Arzneimittel |
| US20060094013A1 (en) | 2002-08-21 | 2006-05-04 | Hiroshi Takemori | Salt-inducible kinases 2 and use thereof |
| US7129351B2 (en) | 2002-11-04 | 2006-10-31 | Hoffmann-La Roche Inc. | Pyrimido compounds having antiproliferative activity |
| CN1717396A (zh) | 2002-11-28 | 2006-01-04 | 舍林股份公司 | Chk-、Pdk-和Akt-抑制嘧啶,其制备及作为药物的用途 |
| KR100864393B1 (ko) | 2003-04-10 | 2008-10-20 | 에프. 호프만-라 로슈 아게 | 피리미도 화합물 |
| US7504396B2 (en) | 2003-06-24 | 2009-03-17 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| US7442698B2 (en) | 2003-07-24 | 2008-10-28 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| CA2533774A1 (en) | 2003-07-29 | 2005-02-10 | Irm Llc | Compounds and compositions as protein kinase inhibitors |
| BRPI0511978A (pt) | 2004-06-10 | 2008-01-22 | Irm Llc | compostos e composições como inibidores de proteìnas quinases |
| GB0512324D0 (en) | 2005-06-16 | 2005-07-27 | Novartis Ag | Organic compounds |
| MX2007002096A (es) | 2004-08-31 | 2007-03-29 | Hoffmann La Roche | Derivados de amida de 3-fenil-dihidropirimido[4,5-d] pirimidinonas, su fabricacion y su uso como agentes farmaceuticos. |
| WO2006024545A1 (en) | 2004-09-03 | 2006-03-09 | Stichting Voor De Technische Wetenschappen | Fused bicyclic natural compounds and their use as inhibitors of parp and parp-mediated inflammatory processes |
| WO2006074057A2 (en) | 2004-12-30 | 2006-07-13 | Exelixis, Inc. | Pyrimidine derivatives as kinase modulators and method of use |
| US20080096905A1 (en) | 2005-03-25 | 2008-04-24 | Glaxo Group Limited | Process For Preparing Pyrido[2,3-D]Pyrimidin-7-One And 3,4-Dihydropyrimido{4,5-D}Pyrimidin-2(1H)-One Derivatives |
| CA2610598A1 (en) * | 2005-06-10 | 2006-12-21 | Irm Llc | Compounds that maintain pluripotency of embryonic stem cells |
| ME00011A (me) | 2005-12-21 | 2009-02-10 | Novartis Ag | Derivati pirimidinilaril uree kao fgf inhibitori |
| BRPI0711628A2 (pt) * | 2006-05-15 | 2011-12-06 | Irm Llc | composto, composição farmacêutica, uso e processo para preparação do composto |
| WO2008060248A1 (en) | 2006-11-15 | 2008-05-22 | S*Bio Pte Ltd. | Indole sustituted pyrimidines and use thereof in the treatment of cancer |
| ES2610190T3 (es) | 2007-11-28 | 2017-04-26 | Dana-Farber Cancer Institute, Inc. | Inhibidores de miristato de moléculas pequeñas de Bcr-abl y métodos de uso |
| WO2009122180A1 (en) | 2008-04-02 | 2009-10-08 | Medical Research Council | Pyrimidine derivatives capable of inhibiting one or more kinases |
| WO2009152027A1 (en) | 2008-06-12 | 2009-12-17 | Merck & Co., Inc. | 5,7-dihydro-6h-pyrrolo[2,3-d]pyrimidin-6-one derivatives for mark inhibition |
| WO2010017047A1 (en) | 2008-08-05 | 2010-02-11 | Merck & Co., Inc. | Therapeutic compounds |
| EP2376494A4 (en) * | 2008-12-12 | 2012-07-11 | Msd Kk | DIHYDROPYRIMIDOPYRIMIDINDERIVATE |
| CN102656174A (zh) | 2009-10-14 | 2012-09-05 | 百时美施贵宝公司 | 用于治疗丙型肝炎的化合物 |
| CN102816162B (zh) * | 2011-06-10 | 2016-04-27 | 中国科学院广州生物医药与健康研究院 | 嘧啶并嘧啶酮类化合物及其药用组合物和应用 |
| KR20140078710A (ko) | 2011-09-30 | 2014-06-25 | 온코디자인 에스.에이. | 거대고리 flt3 키나제 억제제 |
| 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 |
| GB201204384D0 (en) | 2012-03-13 | 2012-04-25 | Univ Dundee | Anti-flammatory agents |
| SMT201800608T1 (it) | 2012-04-24 | 2019-01-11 | Vertex Pharma | Inibitori di dna-pk |
| GB201212960D0 (en) * | 2012-07-20 | 2012-09-05 | Common Services Agency | Erythroid production |
| JP5683634B2 (ja) * | 2012-11-28 | 2015-03-11 | 株式会社ショーワ | 圧力緩衝装置 |
| US9260426B2 (en) | 2012-12-14 | 2016-02-16 | Arrien Pharmaceuticals Llc | Substituted 1H-pyrrolo [2, 3-b] pyridine and 1H-pyrazolo [3, 4-b] pyridine derivatives as salt inducible kinase 2 (SIK2) inhibitors |
| WO2014138485A1 (en) * | 2013-03-08 | 2014-09-12 | Irm Llc | Ex vivo production of platelets from hematopoietic stem cells and the product thereof |
| CN105209040A (zh) | 2013-03-15 | 2015-12-30 | 昂科迪塞恩股份有限公司 | 大环的盐可诱导的激酶抑制剂 |
| AU2014228746B2 (en) * | 2013-03-15 | 2018-08-30 | Celgene Car Llc | Heteroaryl compounds and uses thereof |
| EP3019491A4 (en) | 2013-07-09 | 2016-12-21 | Dana Farber Cancer Inst Inc | KINASEHEMMER FOR THE TREATMENT OF DISEASES |
| CN104418860B (zh) * | 2013-08-20 | 2016-09-07 | 中国科学院广州生物医药与健康研究院 | 嘧啶并杂环类化合物及其药用组合物和应用 |
| EP3171874B1 (en) | 2014-07-21 | 2020-11-18 | Dana-Farber Cancer Institute, Inc. | Imidazolyl kinase inhibitors and uses thereof |
| CA2954187C (en) | 2014-07-21 | 2022-08-16 | Dana-Farber Cancer Institute, Inc. | Macrocyclic kinase inhibitors and uses thereof |
| EP3177295A4 (en) | 2014-08-08 | 2018-06-13 | Dana Farber Cancer Institute, Inc. | Uses of salt-inducible kinase (sik) inhibitors |
| KR101850282B1 (ko) | 2014-11-26 | 2018-05-31 | 한국과학기술연구원 | 단백질 키나아제 저해제로 유용한 헤테로아릴아민 유도체 |
| CN104482860B (zh) | 2014-12-05 | 2017-10-31 | 浙江大学宁波理工学院 | 鱼类形态参数自动测量装置和方法 |
| JP7277357B2 (ja) | 2016-07-05 | 2023-05-18 | ザ ブロード インスティテュート,インコーポレーテッド | 二環式尿素キナーゼインヒビターおよびそれらの使用 |
| WO2018053373A1 (en) * | 2016-09-16 | 2018-03-22 | The General Hospital Corporation | Uses of satl-inducible kinase (sik) inhibitors for treating osteoporosis |
| EP3589284A4 (en) | 2017-02-28 | 2020-12-16 | The General Hospital Corporation | USES OF PYRIMIDOPYRIMIDINONES AS SIK INHIBITORS |
-
2017
- 2017-07-05 JP JP2019500570A patent/JP7277357B2/ja active Active
- 2017-07-05 AU AU2017291812A patent/AU2017291812B2/en active Active
- 2017-07-05 ES ES17740232T patent/ES2920823T3/es active Active
- 2017-07-05 US US16/315,438 patent/US10954242B2/en active Active
- 2017-07-05 KR KR1020197003642A patent/KR20190075043A/ko not_active Withdrawn
- 2017-07-05 CN CN201780054098.0A patent/CN110225914A/zh active Pending
- 2017-07-05 CA CA3069016A patent/CA3069016A1/en active Pending
- 2017-07-05 EP EP17740232.8A patent/EP3481830B1/en active Active
- 2017-07-05 WO PCT/US2017/040722 patent/WO2018009544A1/en not_active Ceased
- 2017-07-05 EP EP21218204.2A patent/EP4047001A3/en active Pending
-
2019
- 2019-01-06 IL IL264106A patent/IL264106B/en unknown
-
2020
- 2020-11-20 US US16/953,984 patent/US11725011B2/en active Active
-
2023
- 2023-03-27 US US18/126,676 patent/US12398145B2/en active Active
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019527682A5 (enExample) | ||
| JP2018522866A5 (enExample) | ||
| JP6342805B2 (ja) | 置換ピラゾロ[3,4−d]ピリミジンおよびその用途 | |
| JP6806562B2 (ja) | eIF2α経路の調節因子 | |
| JP2018522867A5 (enExample) | ||
| JP5576485B2 (ja) | 新生物疾患又は自己免疫疾患を処置するためのプロドラッグとしてのフラザノベンゾイミダゾール | |
| BR112020008817B1 (pt) | Compostos moduladores da via de estresse integrada referência cruzada a pedidos relacionados | |
| CA3080948A1 (en) | Modulators of the integrated stress pathway | |
| JP2017502006A5 (enExample) | ||
| JP2018515434A5 (enExample) | ||
| CA3080964A1 (en) | Modulators of the integrated stress pathway | |
| CA3080808A1 (en) | Modulators of the integrated stress pathway | |
| EP3724165B1 (en) | New benzamide derivatives as ppar-gamma modulators | |
| JP2017537940A5 (enExample) | ||
| JP2020534373A5 (enExample) | ||
| EP4050008A1 (en) | Pyridazinone or pyridazine compound and derivative and pharmaceutical composition thereof | |
| JP2015508092A5 (enExample) | ||
| JP2020516616A5 (enExample) | ||
| JP2017537886A5 (enExample) | ||
| JP2017534572A5 (enExample) | ||
| JP2025118609A (ja) | Nurr1受容体調節因子 | |
| JP2019521964A5 (enExample) | ||
| TW201641492A (zh) | 經取代1,2,3-三唑、其用途、以及包含其之醫藥組成物 | |
| JPWO2021133896A5 (enExample) | ||
| US20200009175A1 (en) | Nucleobase analogue derivatives and their applications |