JP2016113461A5 - - Google Patents
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- Publication number
- JP2016113461A5 JP2016113461A5 JP2015243831A JP2015243831A JP2016113461A5 JP 2016113461 A5 JP2016113461 A5 JP 2016113461A5 JP 2015243831 A JP2015243831 A JP 2015243831A JP 2015243831 A JP2015243831 A JP 2015243831A JP 2016113461 A5 JP2016113461 A5 JP 2016113461A5
- Authority
- JP
- Japan
- Prior art keywords
- phenyl
- dimorpholin
- piperidin
- dimethylamino
- carbonyl
- 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
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 claims 36
- 239000000243 solution Substances 0.000 claims 30
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 24
- 229960000448 lactic acid Drugs 0.000 claims 18
- DWZAEMINVBZMHQ-UHFFFAOYSA-N 1-[4-[4-(dimethylamino)piperidine-1-carbonyl]phenyl]-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea Chemical compound C1CC(N(C)C)CCN1C(=O)C(C=C1)=CC=C1NC(=O)NC1=CC=C(C=2N=C(N=C(N=2)N2CCOCC2)N2CCOCC2)C=C1 DWZAEMINVBZMHQ-UHFFFAOYSA-N 0.000 claims 16
- 239000004310 lactic acid Substances 0.000 claims 16
- 235000014655 lactic acid Nutrition 0.000 claims 16
- 239000012931 lyophilized formulation Substances 0.000 claims 16
- -1 4-{[4- (dimethylamino) piperidin-1-yl] carbonyl} phenyl Chemical group 0.000 claims 14
- 239000000203 mixture Substances 0.000 claims 14
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 13
- 239000004202 carbamide Substances 0.000 claims 13
- 238000009472 formulation Methods 0.000 claims 13
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 13
- 235000011007 phosphoric acid Nutrition 0.000 claims 12
- 239000007864 aqueous solution Substances 0.000 claims 10
- 239000000825 pharmaceutical preparation Substances 0.000 claims 9
- 238000002360 preparation method Methods 0.000 claims 7
- 238000000034 method Methods 0.000 claims 5
- 239000003186 pharmaceutical solution Substances 0.000 claims 5
- 229910019142 PO4 Inorganic materials 0.000 claims 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 3
- 239000010452 phosphate Substances 0.000 claims 3
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- JVTAAEKCZFNVCJ-REOHCLBHSA-N L-lactic acid Chemical compound C[C@H](O)C(O)=O JVTAAEKCZFNVCJ-REOHCLBHSA-N 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- 239000002253 acid Substances 0.000 claims 2
- 239000004067 bulking agent Substances 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 230000003204 osmotic effect Effects 0.000 claims 2
- NSJFQBFLPMIGFZ-UHFFFAOYSA-N 2-hydroxypropanoic acid;urea Chemical compound NC(N)=O.CC(O)C(O)=O NSJFQBFLPMIGFZ-UHFFFAOYSA-N 0.000 claims 1
- HLAMCZOWCWTIBU-UHFFFAOYSA-N 4-(4-morpholin-4-yl-1,3,5-triazin-2-yl)morpholine Chemical compound C1COCCN1C1=NC=NC(N2CCOCC2)=N1 HLAMCZOWCWTIBU-UHFFFAOYSA-N 0.000 claims 1
- 229930182843 D-Lactic acid Natural products 0.000 claims 1
- JVTAAEKCZFNVCJ-UWTATZPHSA-N D-lactic acid Chemical compound C[C@@H](O)C(O)=O JVTAAEKCZFNVCJ-UWTATZPHSA-N 0.000 claims 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical group OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229940022769 d- lactic acid Drugs 0.000 claims 1
- 239000008121 dextrose Substances 0.000 claims 1
- 238000004108 freeze drying Methods 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462093060P | 2014-12-17 | 2014-12-17 | |
| US62/093,060 | 2014-12-17 | ||
| US201562250633P | 2015-11-04 | 2015-11-04 | |
| US62/250,633 | 2015-11-04 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016113461A JP2016113461A (ja) | 2016-06-23 |
| JP2016113461A5 true JP2016113461A5 (enExample) | 2018-05-10 |
| JP6420753B2 JP6420753B2 (ja) | 2018-11-07 |
Family
ID=54937330
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015243831A Active JP6420753B2 (ja) | 2014-12-17 | 2015-12-15 | 製剤 |
Country Status (25)
| Country | Link |
|---|---|
| US (2) | US10172942B2 (enExample) |
| EP (1) | EP3233054B1 (enExample) |
| JP (1) | JP6420753B2 (enExample) |
| KR (1) | KR102016822B1 (enExample) |
| CN (1) | CN107205923B (enExample) |
| AU (1) | AU2015365497B2 (enExample) |
| CA (1) | CA2915199C (enExample) |
| CY (1) | CY1124527T1 (enExample) |
| DK (1) | DK3233054T3 (enExample) |
| ES (1) | ES2881214T3 (enExample) |
| HR (1) | HRP20211446T1 (enExample) |
| HU (1) | HUE055928T2 (enExample) |
| IL (1) | IL252158B (enExample) |
| LT (1) | LT3233054T (enExample) |
| MX (1) | MX380172B (enExample) |
| NZ (1) | NZ731518A (enExample) |
| PL (1) | PL3233054T3 (enExample) |
| PT (1) | PT3233054T (enExample) |
| RS (1) | RS62337B1 (enExample) |
| RU (1) | RU2672875C1 (enExample) |
| SG (1) | SG11201703826TA (enExample) |
| SI (1) | SI3233054T1 (enExample) |
| TW (1) | TWI660729B (enExample) |
| WO (1) | WO2016097949A1 (enExample) |
| ZA (1) | ZA201703764B (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2895370T3 (es) | 2017-08-25 | 2022-02-21 | Pfizer | Formulación farmacéutica acuosa que comprende 1-(4-{[4-(dimetilamino)piperidin-1-il]carbonil}fenil)-3-[4-(4,6- dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea |
| NZ805649A (en) * | 2018-06-07 | 2024-11-29 | Pfizer | Aqueous formulation comprising 1-(4-{ [4-(dimethylamino)piperidin-1-yl]carbonyl} phenyl)-3- [4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea |
| TW202320795A (zh) | 2021-07-26 | 2023-06-01 | 美商凱爾科迪股份有限公司 | 使用1-(4-{[4-(二甲胺基)哌啶-1-基]羰基}苯基)-3-[4-(4,6-二嗎啉-4-基-1,3,5-三-2-基)苯基]脲治療癌症之方法 |
| WO2025128712A1 (en) | 2023-12-12 | 2025-06-19 | Celcuity Inc. | Treatment of ocular diseases using 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl)phenyl)-3-[4-(4,6- dimorpholin-4- yl-1,3,5-triazin-2-yl)phenyl]urea |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0852951A1 (de) * | 1996-11-19 | 1998-07-15 | Roche Diagnostics GmbH | Stabile lyophilisierte pharmazeutische Zubereitungen von mono- oder polyklonalen Antikörpern |
| MX2007014726A (es) * | 2005-05-27 | 2008-02-14 | Bayer Healthcare Ag | Tratamiento combinado que comprende un compuesto diarilurea y una pi3, akt cinasa o inhibidores mtor (rapamicina) para tratamiento de cancer. |
| US20080234262A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
| DE202008001253U1 (de) * | 2008-01-28 | 2008-04-10 | Mirror Image Ag | Bildanzeigegerät |
| EP2300483A1 (en) * | 2008-05-23 | 2011-03-30 | Wyeth LLC | Triazine compounds as p13 kinase and mtor inhibitors |
| US8158624B2 (en) * | 2008-05-30 | 2012-04-17 | Genetech, Inc. | Purine PI3K inhibitor compounds and methods of use |
| WO2010096619A1 (en) | 2009-02-23 | 2010-08-26 | Wyeth Llc | Process, purification and crystallization of 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea |
| WO2014078522A1 (en) * | 2012-11-14 | 2014-05-22 | Ohio State Innovation Foundation | Materials and methods useful for treating glioblastoma |
| EP2968191B1 (en) * | 2013-03-14 | 2021-06-16 | Abraxis BioScience, LLC | Methods of treating bladder cancer |
| MX378984B (es) * | 2014-03-14 | 2025-03-11 | Pfizer | Nanoparticulas terapeuticas que comprenden un agente terapeutico, y metodos para su elaboracion y uso. |
-
2015
- 2015-12-10 US US15/534,999 patent/US10172942B2/en active Active
- 2015-12-10 SG SG11201703826TA patent/SG11201703826TA/en unknown
- 2015-12-10 KR KR1020177016417A patent/KR102016822B1/ko active Active
- 2015-12-10 EP EP15813578.0A patent/EP3233054B1/en active Active
- 2015-12-10 MX MX2017008072A patent/MX380172B/es unknown
- 2015-12-10 CN CN201580068063.3A patent/CN107205923B/zh active Active
- 2015-12-10 RS RS20211128A patent/RS62337B1/sr unknown
- 2015-12-10 PT PT158135780T patent/PT3233054T/pt unknown
- 2015-12-10 NZ NZ731518A patent/NZ731518A/en unknown
- 2015-12-10 SI SI201531687T patent/SI3233054T1/sl unknown
- 2015-12-10 HU HUE15813578A patent/HUE055928T2/hu unknown
- 2015-12-10 PL PL15813578T patent/PL3233054T3/pl unknown
- 2015-12-10 DK DK15813578.0T patent/DK3233054T3/da active
- 2015-12-10 LT LTEPPCT/IB2015/059515T patent/LT3233054T/lt unknown
- 2015-12-10 WO PCT/IB2015/059515 patent/WO2016097949A1/en not_active Ceased
- 2015-12-10 ES ES15813578T patent/ES2881214T3/es active Active
- 2015-12-10 RU RU2017119282A patent/RU2672875C1/ru active
- 2015-12-10 HR HRP20211446TT patent/HRP20211446T1/hr unknown
- 2015-12-10 AU AU2015365497A patent/AU2015365497B2/en active Active
- 2015-12-14 TW TW104141933A patent/TWI660729B/zh active
- 2015-12-14 CA CA2915199A patent/CA2915199C/en active Active
- 2015-12-15 JP JP2015243831A patent/JP6420753B2/ja active Active
-
2017
- 2017-05-08 IL IL252158A patent/IL252158B/en active IP Right Grant
- 2017-06-01 ZA ZA201703764A patent/ZA201703764B/en unknown
-
2018
- 2018-11-13 US US16/189,009 patent/US10660959B2/en active Active
-
2021
- 2021-09-28 CY CY20211100851T patent/CY1124527T1/el unknown
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