JP2019519593A5 - - Google Patents
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- JP2019519593A5 JP2019519593A5 JP2018568930A JP2018568930A JP2019519593A5 JP 2019519593 A5 JP2019519593 A5 JP 2019519593A5 JP 2018568930 A JP2018568930 A JP 2018568930A JP 2018568930 A JP2018568930 A JP 2018568930A JP 2019519593 A5 JP2019519593 A5 JP 2019519593A5
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- Prior art keywords
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- aryl
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- 125000000217 alkyl group Chemical group 0.000 claims 20
- 125000003118 aryl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 229940124647 MEK inhibitor Drugs 0.000 claims 2
- 239000012828 PI3K inhibitor Substances 0.000 claims 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 2
- 229940043441 phosphoinositide 3-kinase inhibitor Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 1
- UCYLROVJSUACAD-UHFFFAOYSA-N 2-[2,3-bis(2-hydroxyethoxy)propoxy]ethanol Chemical compound OCCOCC(OCCO)COCCO UCYLROVJSUACAD-UHFFFAOYSA-N 0.000 claims 1
- 102000004232 Mitogen-Activated Protein Kinase Kinases Human genes 0.000 claims 1
- 108090000744 Mitogen-Activated Protein Kinase Kinases Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 108091007960 PI3Ks Proteins 0.000 claims 1
- 102000013530 TOR Serine-Threonine Kinases Human genes 0.000 claims 1
- 108010065917 TOR Serine-Threonine Kinases Proteins 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
- 0 *c(cc1)cc(F)c1Nc(c(C(N*N(CC1)CCN1c1nc(cc(cc2)-c3cnc(*)c(NS(c(cc4)ccc4F)(=O)=O)c3)c2nc1)=O)ccc1F)c1F Chemical compound *c(cc1)cc(F)c1Nc(c(C(N*N(CC1)CCN1c1nc(cc(cc2)-c3cnc(*)c(NS(c(cc4)ccc4F)(=O)=O)c3)c2nc1)=O)ccc1F)c1F 0.000 description 16
- KAQSIIOCRZVCIQ-UHFFFAOYSA-N CC(C)(C)OC(NOCCOCCN(C)CCOCCC(O)=O)=O Chemical compound CC(C)(C)OC(NOCCOCCN(C)CCOCCC(O)=O)=O KAQSIIOCRZVCIQ-UHFFFAOYSA-N 0.000 description 1
- MRQVNRJCIOXFLB-UHFFFAOYSA-N CC(C)(C)OC(NOCCOCCN(C)CCOCCOCCC(O)=O)=O Chemical compound CC(C)(C)OC(NOCCOCCN(C)CCOCCOCCC(O)=O)=O MRQVNRJCIOXFLB-UHFFFAOYSA-N 0.000 description 1
- BQULJZSOTNNVMI-UHFFFAOYSA-N CC(C)(C)OC(NOCCOCCOCCCN(C)CCOCCOCCC(O)=O)=O Chemical compound CC(C)(C)OC(NOCCOCCOCCCN(C)CCOCCOCCC(O)=O)=O BQULJZSOTNNVMI-UHFFFAOYSA-N 0.000 description 1
- TVSMLBGFGKLKOO-UHFFFAOYSA-N CC1CCN(C)CC1 Chemical compound CC1CCN(C)CC1 TVSMLBGFGKLKOO-UHFFFAOYSA-N 0.000 description 1
- WRWPPGUCZBJXKX-UHFFFAOYSA-N Cc(cc1)ccc1F Chemical compound Cc(cc1)ccc1F WRWPPGUCZBJXKX-UHFFFAOYSA-N 0.000 description 1
- YXJKFEHSDJWXFA-UHFFFAOYSA-N NC(c(c(Nc(c(F)c1)ccc1I)c1F)ccc1F)=O Chemical compound NC(c(c(Nc(c(F)c1)ccc1I)c1F)ccc1F)=O YXJKFEHSDJWXFA-UHFFFAOYSA-N 0.000 description 1
- VVIJTFDWBOPSTL-UHFFFAOYSA-N O=C(c(c(Nc(c(F)c1)ccc1I)c1F)ccc1F)NOCCOCCOCCOCCNC/[O]=S/N(CC1)CCN1c1nc(cc(cc2)-c(cc3NS(c(cc4)ccc4F)(=O)=O)cnc3Cl)c2nc1 Chemical compound O=C(c(c(Nc(c(F)c1)ccc1I)c1F)ccc1F)NOCCOCCOCCOCCNC/[O]=S/N(CC1)CCN1c1nc(cc(cc2)-c(cc3NS(c(cc4)ccc4F)(=O)=O)cnc3Cl)c2nc1 VVIJTFDWBOPSTL-UHFFFAOYSA-N 0.000 description 1
- CABWOSCBGMOHCF-UHFFFAOYSA-N O=CN(CC1)CCN1c1nc(cc(cc2)-c(cc3NS(c(cc4)ccc4F)(=O)=O)cnc3Cl)c2nc1 Chemical compound O=CN(CC1)CCN1c1nc(cc(cc2)-c(cc3NS(c(cc4)ccc4F)(=O)=O)cnc3Cl)c2nc1 CABWOSCBGMOHCF-UHFFFAOYSA-N 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021190205A JP7475062B2 (ja) | 2016-07-06 | 2021-11-24 | MEK/PI3K及びmTOR/MEK/PI3K生物学的経路の多官能性阻害剤、並びに同多官能性阻害剤を用いた治療方法 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662359001P | 2016-07-06 | 2016-07-06 | |
| US62/359,001 | 2016-07-06 | ||
| US201762454163P | 2017-02-03 | 2017-02-03 | |
| US62/454,163 | 2017-02-03 | ||
| PCT/US2017/040866 WO2018009638A1 (en) | 2016-07-06 | 2017-07-06 | MULTIFUNCTIONAL INHIBITORS OF MEK/PI3K AND mTOR/MEK/PI3K BIOLOGICAL PATHWAYS AND THERAPEUTIC METHODS USING THE SAME |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021190205A Division JP7475062B2 (ja) | 2016-07-06 | 2021-11-24 | MEK/PI3K及びmTOR/MEK/PI3K生物学的経路の多官能性阻害剤、並びに同多官能性阻害剤を用いた治療方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019519593A JP2019519593A (ja) | 2019-07-11 |
| JP2019519593A5 true JP2019519593A5 (enExample) | 2020-08-13 |
Family
ID=59363277
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018568930A Pending JP2019519593A (ja) | 2016-07-06 | 2017-07-06 | MEK/PI3K及びmTOR/MEK/PI3K生物学的経路の多官能性阻害剤、並びに同多官能性阻害剤を用いた治療方法 |
| JP2021190205A Active JP7475062B2 (ja) | 2016-07-06 | 2021-11-24 | MEK/PI3K及びmTOR/MEK/PI3K生物学的経路の多官能性阻害剤、並びに同多官能性阻害剤を用いた治療方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021190205A Active JP7475062B2 (ja) | 2016-07-06 | 2021-11-24 | MEK/PI3K及びmTOR/MEK/PI3K生物学的経路の多官能性阻害剤、並びに同多官能性阻害剤を用いた治療方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US10919877B2 (enExample) |
| EP (2) | EP4086250B1 (enExample) |
| JP (2) | JP2019519593A (enExample) |
| CN (1) | CN109563088B (enExample) |
| AU (2) | AU2017291838B2 (enExample) |
| CA (1) | CA3029875C (enExample) |
| ES (2) | ES3002745T3 (enExample) |
| WO (1) | WO2018009638A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11311624B2 (en) | 2017-08-11 | 2022-04-26 | The Regents Of The University Of Michigan | Inhibitors of MEK/PI3K, JAK/MEK, JAK/PI3K/mTOR and MEK/PI3K/mTOR biological pathways and methods for improving lymphatic uptake, bioavailability, and solubility of therapeutic compounds |
| CN112143700B (zh) * | 2019-06-26 | 2024-07-19 | 上海细胞治疗集团股份有限公司 | 制备过表达外源基因的免疫效应细胞的方法 |
| CN117396470A (zh) * | 2021-04-09 | 2024-01-12 | 巴塞尔大学 | 作为pi3k的可逆和不可逆共价抑制剂的三嗪衍生物 |
| JP2024516361A (ja) * | 2021-04-09 | 2024-04-15 | ウニヴェアズィテート バーゼル | Pi3kの可逆的および不可逆的共有結合性阻害剤としてのトリアジン誘導体 |
| WO2023170107A1 (en) | 2022-03-07 | 2023-09-14 | Centre Hospitalier Universitaire Vaudois (Chuv) | Pi3k/akt/mtor inhibitor for improving the cellular uptake of a radiopharmaceutical |
| JP2023180347A (ja) * | 2022-06-09 | 2023-12-21 | 国立大学法人金沢大学 | ハイブリッド型化合物又はその塩 |
| CN116617227A (zh) * | 2023-06-09 | 2023-08-22 | 苏州大学 | 三氟噻吨在治疗脑血管疾病中的应用 |
| WO2025072796A1 (en) * | 2023-09-27 | 2025-04-03 | Totus Medicines Inc. | Pharmaceutical compositions and methods of use thereof |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA197701A (en) | 1920-03-02 | Mcgoldrick Timothy | Arm cushion for crutches | |
| CA85878A (en) | 1903-08-19 | 1904-03-08 | George W. Peyton | Carpenter's gauge |
| US5608110A (en) | 1993-06-15 | 1997-03-04 | Bracco International B.V. | Heteroatom-bearing ligands and metal complexes thereof |
| EE05450B1 (et) | 2000-07-19 | 2011-08-15 | Warner-Lambert Company | 4-jodofenlaminobenshdroksaamhapete oksgeenitud estrid, nende kristallvormid ja farmatseutilised kompositsioonid ning kasutamine |
| TW200505834A (en) | 2003-03-18 | 2005-02-16 | Sankyo Co | Sulfamide derivative and the pharmaceutical composition thereof |
| GB0510390D0 (en) | 2005-05-20 | 2005-06-29 | Novartis Ag | Organic compounds |
| AR059339A1 (es) | 2006-02-09 | 2008-03-26 | Chugai Pharmaceutical Co Ltd | Derivados de la cumarina para trastornos proliferativos de celulas, composicion farmaceutica y agente terapeutico que los contiene |
| WO2008032162A1 (en) | 2006-09-15 | 2008-03-20 | Pfizer Products Inc. | Pyrido (2, 3-d) pyrimidin0ne compounds and their use as pi3 inhibitors |
| US8569378B2 (en) | 2007-07-20 | 2013-10-29 | Toshiyuki Sakai | p27 protein inducer |
| EP2276750A2 (en) | 2008-03-27 | 2011-01-26 | Auckland Uniservices Limited | Substituted pyrimidines and triazines and their use in cancer therapy |
| WO2009155121A2 (en) * | 2008-05-30 | 2009-12-23 | Amgen Inc. | Inhibitors of pi3 kinase |
| EP2143819A1 (de) | 2008-07-11 | 2010-01-13 | Siemens Aktiengesellschaft | Beschichtungsverfahren und Korrosionsschutzbeschichtung für Turbinen-Komponenten |
| TW201038567A (en) | 2009-03-27 | 2010-11-01 | Pathway Therapeutics Ltd | Pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides and their use in cancer therapy |
| TW201105662A (en) | 2009-07-07 | 2011-02-16 | Pathway Therapeutics Ltd | Pyrimidinyl and 1,3,5-triazinyl benzimidazoles and their use in cancer therapy |
| US20110166191A1 (en) | 2010-01-07 | 2011-07-07 | Shijun Zhang | 3-(2-amino-ethyl)-5-(3-cyclohexyl-propylidene)-thiazolidine-2,4-dione and its derivatives as multiple signaling pathway inhibitors and for the treatment of cancer |
| GB201007227D0 (en) | 2010-04-30 | 2010-06-16 | Univ Basel | Piperazinotriazines |
| EP2604601B1 (en) * | 2010-08-10 | 2016-02-24 | Astellas Pharma Inc. | Hetero ring compound |
| EP2640367A2 (en) | 2010-11-15 | 2013-09-25 | Exelixis, Inc. | Benzoxazepines as inhibitors of pi3k/mtor and methods of their use and manufacture |
| US9284334B2 (en) * | 2011-05-19 | 2016-03-15 | Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii | Macrocyclic compounds as protein kinase inhibitors |
| EP2781520B1 (en) | 2011-11-17 | 2016-05-04 | Xuanzhu Pharma Co., Ltd. | Three-ring pi3k and/or mtor inhibitor |
| EP2968345B1 (en) | 2013-03-13 | 2017-12-13 | The Regents of The University of Michigan | Dual mek/pi3k inhibitors and their application in the treatment of cancer diseases |
| KR20150143672A (ko) * | 2013-04-12 | 2015-12-23 | 아사나 바이오사이언시스 엘엘씨 | Ras/raf/mek/erk 및 pi3k/akt/pten/mtor 경로의 이중 억제제로서의 퀴나졸린 및 아자퀴나졸린 |
| CN105130960B (zh) * | 2015-07-31 | 2018-07-06 | 沈阳药科大学 | 1,3,5-三嗪类衍生物及其应用 |
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2017
- 2017-07-06 JP JP2018568930A patent/JP2019519593A/ja active Pending
- 2017-07-06 US US16/313,923 patent/US10919877B2/en active Active
- 2017-07-06 EP EP22179630.3A patent/EP4086250B1/en active Active
- 2017-07-06 ES ES22179630T patent/ES3002745T3/es active Active
- 2017-07-06 EP EP17740578.4A patent/EP3481822B1/en active Active
- 2017-07-06 ES ES17740578T patent/ES2922898T3/es active Active
- 2017-07-06 CN CN201780049835.8A patent/CN109563088B/zh active Active
- 2017-07-06 WO PCT/US2017/040866 patent/WO2018009638A1/en not_active Ceased
- 2017-07-06 AU AU2017291838A patent/AU2017291838B2/en active Active
- 2017-07-06 CA CA3029875A patent/CA3029875C/en active Active
-
2021
- 2021-04-28 AU AU2021202619A patent/AU2021202619B2/en active Active
- 2021-11-24 JP JP2021190205A patent/JP7475062B2/ja active Active