JP2016510042A5 - - Google Patents
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- Publication number
- JP2016510042A5 JP2016510042A5 JP2015560533A JP2015560533A JP2016510042A5 JP 2016510042 A5 JP2016510042 A5 JP 2016510042A5 JP 2015560533 A JP2015560533 A JP 2015560533A JP 2015560533 A JP2015560533 A JP 2015560533A JP 2016510042 A5 JP2016510042 A5 JP 2016510042A5
- Authority
- JP
- Japan
- Prior art keywords
- octanoyl
- azabicyclo
- oxa
- pharmaceutically acceptable
- prodrug
- 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
- -1 pyrimidopyrimidine compound Chemical class 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 12
- 150000002148 esters Chemical class 0.000 claims 10
- 239000000651 prodrug Substances 0.000 claims 10
- 229940002612 prodrug Drugs 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 10
- BWESROVQGZSBRX-UHFFFAOYSA-N pyrido[3,2-d]pyrimidine Chemical compound C1=NC=NC2=CC=CN=C21 BWESROVQGZSBRX-UHFFFAOYSA-N 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 7
- 150000002367 halogens Chemical class 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 4
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 3
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 claims 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical group C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 230000019491 signal transduction Effects 0.000 claims 2
- FQUYSHZXSKYCSY-UHFFFAOYSA-N 1,4-diazepane Chemical group C1CNCCNC1 FQUYSHZXSKYCSY-UHFFFAOYSA-N 0.000 claims 1
- ZNGWEEUXTBNKFR-UHFFFAOYSA-N 1,4-oxazepane Chemical group C1CNCCOC1 ZNGWEEUXTBNKFR-UHFFFAOYSA-N 0.000 claims 1
- PVOAHINGSUIXLS-UHFFFAOYSA-N 1-Methylpiperazine Chemical group CN1CCNCC1 PVOAHINGSUIXLS-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000007257 malfunction Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310068888.8 | 2013-03-04 | ||
| CN201310068888.8A CN103588792B (zh) | 2013-03-04 | 2013-03-04 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
| PCT/CN2014/072678 WO2014135028A1 (zh) | 2013-03-04 | 2014-02-28 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016510042A JP2016510042A (ja) | 2016-04-04 |
| JP2016510042A5 true JP2016510042A5 (enExample) | 2016-09-29 |
Family
ID=50079144
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015560533A Pending JP2016510042A (ja) | 2013-03-04 | 2014-02-28 | ピリドピリミジンまたはピリミドピリミジン系化合物、その製造方法、薬剤組成物及びその用途 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9796732B2 (enExample) |
| EP (1) | EP2966079B1 (enExample) |
| JP (1) | JP2016510042A (enExample) |
| CN (1) | CN103588792B (enExample) |
| AU (1) | AU2014225155B2 (enExample) |
| CA (1) | CA2903072C (enExample) |
| DE (1) | DE14760712T1 (enExample) |
| DK (1) | DK2966079T3 (enExample) |
| ES (1) | ES2572105T3 (enExample) |
| RU (1) | RU2662713C2 (enExample) |
| WO (1) | WO2014135028A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103588792B (zh) | 2013-03-04 | 2016-03-23 | 中国科学院上海药物研究所 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
| CN106008559B (zh) * | 2015-03-25 | 2020-10-16 | 中国科学院上海药物研究所 | 取代吡啶并嘧啶类化合物的合成工艺 |
| WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
| WO2019091400A1 (zh) * | 2017-11-07 | 2019-05-16 | 中国科学院上海药物研究所 | 吡啶并嘧啶类化合物的盐型和晶型及其制备方法 |
| CN109867667B (zh) * | 2017-12-05 | 2021-06-11 | 中国药科大学 | 含有吡啶并嘧啶结构的parp和pi3k双靶点抑制剂 |
| US20220306622A1 (en) * | 2019-05-06 | 2022-09-29 | Medshine Discovery Inc. | Salt and crystal form of mtorc1/2 dual kinase activity inhibitor and preparation method therefor |
| US20240208964A1 (en) * | 2020-06-03 | 2024-06-27 | Pyridopyrimidines And Methods Of Their Use | Pyridopyrimidines and methods of their use |
| WO2022061251A1 (en) * | 2020-09-18 | 2022-03-24 | Plexxikon Inc. | Compounds and methods for kras modulation and indications therefor |
| WO2022228576A1 (zh) * | 2021-04-30 | 2022-11-03 | 上海医药集团股份有限公司 | 一种靶向蛋白调节剂的化合物及其应用 |
| CA3228579A1 (en) * | 2021-08-10 | 2023-02-16 | Amgen Inc. | Heterocyclic compounds and methods of use |
| MX2024001893A (es) * | 2021-08-10 | 2024-02-29 | Amgen Inc | Compuestos heterociclicos y metodos de uso. |
| KR20250024077A (ko) * | 2022-06-15 | 2025-02-18 | 미라티 테라퓨틱스, 인크. | Pan-kras 억제제의 전구약물 |
| WO2024057013A1 (en) * | 2022-09-12 | 2024-03-21 | Exscientia Ai Limited | Nlrp3 modulators |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2008531538A (ja) * | 2005-02-25 | 2008-08-14 | クドス ファーマシューティカルズ リミテッド | ２，４−ジアミノ−ピリドピリミジン誘導体とｍＴＯＲ阻害剤としてのその使用 |
| UA96745C2 (en) * | 2005-11-22 | 2011-12-12 | Кудос Фармасьютикалз Лимитед | PYRIDO-, PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS |
| BRPI0714908B8 (pt) * | 2006-08-08 | 2021-05-25 | Chugai Pharmaceutical Co Ltd | derivados de pirimidina como inibidor de pi3k, composição farmacêutica e agente preventivo ou agente terapêutico de uma doença proliferativa que os compreende |
| CN101558067B (zh) * | 2006-08-23 | 2014-05-28 | 库多斯药物有限公司 | 作为mtor抑制剂的2-甲基吗啉吡啶并、吡唑并和嘧啶并-嘧啶衍生物 |
| US20080233127A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Imidazolopyrimidine analogs and their use as pi3 kinase and mtor inhibitors |
| WO2010120987A1 (en) * | 2009-04-17 | 2010-10-21 | Wyeth Llc | Ring fused, ureidoaryl- and carbamoylaryl-bridged morpholino-pyrimidine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
| CN102887895B (zh) * | 2011-07-22 | 2016-08-24 | 山东轩竹医药科技有限公司 | 吡啶并嘧啶类mTOR抑制剂 |
| CN102911172A (zh) * | 2011-08-04 | 2013-02-06 | 上海恒瑞医药有限公司 | 杂芳基并嘧啶类衍生物、其制备方法和用途 |
| CN103588792B (zh) * | 2013-03-04 | 2016-03-23 | 中国科学院上海药物研究所 | 吡啶并嘧啶或嘧啶并嘧啶类化合物、其制备方法、药物组合物及其用途 |
-
2013
- 2013-03-04 CN CN201310068888.8A patent/CN103588792B/zh active Active
-
2014
- 2014-02-28 JP JP2015560533A patent/JP2016510042A/ja active Pending
- 2014-02-28 DK DK14760712.1T patent/DK2966079T3/da active
- 2014-02-28 RU RU2015140387A patent/RU2662713C2/ru active
- 2014-02-28 AU AU2014225155A patent/AU2014225155B2/en not_active Ceased
- 2014-02-28 WO PCT/CN2014/072678 patent/WO2014135028A1/zh not_active Ceased
- 2014-02-28 DE DE14760712.1T patent/DE14760712T1/de active Pending
- 2014-02-28 CA CA2903072A patent/CA2903072C/en active Active
- 2014-02-28 ES ES14760712T patent/ES2572105T3/es active Active
- 2014-02-28 EP EP14760712.1A patent/EP2966079B1/en active Active
-
2015
- 2015-09-01 US US14/842,682 patent/US9796732B2/en active Active
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