HRP20211446T1 - Formulacije inhibitora pi3k/mtor za intravensko davanje - Google Patents
Formulacije inhibitora pi3k/mtor za intravensko davanje Download PDFInfo
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- HRP20211446T1 HRP20211446T1 HRP20211446TT HRP20211446T HRP20211446T1 HR P20211446 T1 HRP20211446 T1 HR P20211446T1 HR P20211446T T HRP20211446T T HR P20211446TT HR P20211446 T HRP20211446 T HR P20211446T HR P20211446 T1 HRP20211446 T1 HR P20211446T1
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- phenyl
- triazin
- piperidin
- dimethylamino
- carbonyl
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- 239000000203 mixture Substances 0.000 title claims 5
- 238000009472 formulation Methods 0.000 title claims 4
- 238000001990 intravenous administration Methods 0.000 title claims 2
- 239000012823 PI3K/mTOR inhibitor Substances 0.000 title 1
- 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 31
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 claims 28
- 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 25
- 239000008194 pharmaceutical composition Substances 0.000 claims 23
- 239000012931 lyophilized formulation Substances 0.000 claims 21
- 229960000448 lactic acid Drugs 0.000 claims 18
- 239000007864 aqueous solution Substances 0.000 claims 17
- 239000004310 lactic acid Substances 0.000 claims 16
- 235000014655 lactic acid Nutrition 0.000 claims 16
- 235000011007 phosphoric acid Nutrition 0.000 claims 14
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 4
- 239000004202 carbamide Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 150000003013 phosphoric acid derivatives Chemical class 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
- 229930195725 Mannitol Natural products 0.000 claims 2
- 239000000945 filler Substances 0.000 claims 2
- 150000003893 lactate salts Chemical class 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 239000008181 tonicity modifier Substances 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
- 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
- 239000002253 acid Substances 0.000 claims 1
- 239000013011 aqueous formulation Substances 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
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 201000011510 cancer Diseases 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
- 238000007911 parenteral administration Methods 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/17—Amides, e.g. hydroxamic acids having the group >N—C(O)—N< or >N—C(S)—N<, e.g. urea, thiourea, carmustine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5355—Non-condensed oxazines and containing further heterocyclic rings
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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Claims (30)
1. Liofilizirana formulacija koja se može dobiti sušenjem zamrzavanjem farmaceutske formulacije vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ili njenu laktatnu sol, mliječnu kiselinu i vodu, pri čemu 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea je prisutna u otopini u koncentraciji manjoj od 6mg/ml i prisutno je dovoljno mliječne kiseline da bi se osigurala bistra otopina; ili
1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ili njenu fosfatnu sol, ortofosfornu kiselinu i vodu, pri čemu 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea je prisutna u otopini u koncentraciji manjoj od 4mg/ml i prisutno je dovoljno ortofosforne kiseline da bi se postigla bistra otopina.
2. Liofilizirana formulacija prema zahtjevu 1, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ili njenu laktatnu sol, mliječnu kiselinu i vodu, pri čemu je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji manjoj od 6mg/ml i prisutno je dovoljno mliječne kiseline da bi se postigla bistra otopina.
3. Liofilizirana formulacija prema zahtjevu 1 ili 2, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, mliječnu kiselinu i vodu, pri čemu je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji manjoj od 6mg/ml i prisutno je dovoljno mliječne kiseline da bi se osigurala bistra otopina.
4. Liofilizirana formulacija prema bilo kojem od zahtjeva 1 do 3, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u farmaceutskoj formulaciji vodene otopine u koncentraciji otopine od oko 2.5 do 5.5mg/ml.
5. Liofilizirana formulacija prema bilo kojem od zahtjeva 1 do 4 gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u farmaceutskoj formulaciji vodene otopine u koncentraciji otopine od oko 5.0 do 5.5mg/ml i prisutno je bar 2.5 molskih ekvivalenata mliječne kiseline.
6. Liofilizirana formulacija prema zahtjevu 4 gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u farmaceutskoj formulaciji vodene otopine u koncentraciji otopine od oko 5mg/ml.
7. Liofilizirana formulacija prema zahtjevu 6, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u farmaceutskoj formulaciji vodene otopine u koncentraciji otopine od oko 5mg/ml i prisutno je bar 2.5 molskih ekvivalenata mliječne kiseline.
8. Liofilizirana formulacija prema bilo kojem od zahtjeva 1 do 3, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, mliječnu kiselinu i vodu, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u farmaceutskoj formulaciji vodene otopine u koncentraciji otopine od oko 5mg/ml, i prisutno je bar 2.5 molskih ekvivalenata mliječne kiseline u količini koja je dovoljna da bi se osiguralo dobivanje bistre otopine.
9. Liofilizirana formulacija prema zahtjevu 1 ili 2, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea laktat, mliječnu kiselinu i vodu, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u koncentraciji otopine od oko 5mg/ml, i prisutno je bar 1.5 molskih ekvivalenata mliječne kiseline u količini koja je dovoljna da bi se osiguralo dobivanje bistre otopine.
10. Liofilizirana formulacija prema zahtjevu 8, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, mliječnu kiselinu i vodu, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji od oko 5mg/ml, i prisutno je oko 4.1 molskih ekvivalenata mliječne kiseline u količini koja je dovoljna da bi se osiguralo formiranje bistre otopine sa pH ne većom od 3.7.
11. Liofilizirana formulacija prema zahtjevu 1 ili 2, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, mliječnu kiselinu i vodu, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji od oko 2.5 do 5.5mg/ml, i prisutno je više od 2.5 do 8.0 molskih ekvivalenata mliječne kiseline u količini koja je dovoljna da bi se osiguralo dobivanje bistre otopine.
12. Liofilizirana formulacija prema bilo kojem od zahtjeva 1 do 11 pri čemu su DL-mliječna kiselina, L-mliječna kiselina ili D-mliječna kiselina korištene u farmaceutskoj formulaciji vodene otopine.
13. Liofilizirana formulacija prema bilo kojem od zahtjeva 1 do 12 pri čemu je DL-mliječna kiselina korištena u farmaceutskoj formulaciji vodene otopine.
14. Liofilizirana formulacija prema zahtjevu 1, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ili njenu fosfatnu sol, ortofosfornu kiselinu i vodu, pri čemu je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji koja je manja od 4 mg/ml i prisutno je dovoljno ortofosforne kiseline da se dobije bistra otopina.
15. Liofilizirana formulacija prema zahtjevu 1 ili 14, farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ortofosfornu kiselinu i vodu, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji koja je manja od 4 mg/ml i prisutno je dovoljno ortofosforne kiseline da se dobije bistra otopina.
16. Liofilizirana formulacija prema zahtjevu 15 gdje 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea je prisutna u farmaceutskoj formulaciji vodene otopine u koncentraciji otopine od oko 3.0 do 3.5mg/ml.
17. Liofilizirana formulacija prema zahtjevu 15 ili 16 gdje je korišteno najmanje 5 molskih ekvivalenata ortofosforne kiseline u farmaceutskoj formulaciji vodene otopine.
18. Liofilizirana formulacija prema zahtjevu 17 gdje je korišteno 5 do 7 molskih ekvivalenata ortofosforne kiseline u farmaceutskoj formulaciji vodene otopine.
19. Liofilizirana formulacija prema bilo kojem od zahtjeva 1 do 18 koja dodatno sadrži sredstvo za punjenje.
20. Liofilizirana formulacija prema zahtjevu 19 pri čemu sredstvo za punjenje je manitol.
21. Postupak za dobivanje farmaceutske formulacije vodene bistre otopine rekonstitucijom ili konstitucijom liofilizirane formulacije prema bilo kojem od zahtjeva 1 do 20 upotrebom vode ili vodene otopine koji sadrži modifikator toničnosti.
22. Postupak prema zahtjevu 21 pri čemu je modifikator toničnosti dekstroza, saharoza ili manitol, ili je smjesa bilo koja 2 ili više spomenutih.
23. Postupak prema zahtjevu 21 ili 22, koji je podešen, po potrebi, da ima pH pogodnu za intravensko ili parenteralno davanje.
24. Postupak prema zahtjevu 23 pri čemu je pH od 3 do 4.5.
25. Farmaceutska formulacija vodene otopine koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ili njenu fosfatnu sol, ortofosfornu kiselinu i vodu, pri čemu je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea prisutna u otopini u koncentraciji koja je manja od 4 mg/ml i prisutno je dovoljno ortofosforne kiseline da bi se ostvarila bistra otopina.
26. Farmaceutska formulacija vodene otopine prema zahtjevu 25 koja sadrži 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]ureu, ortofosfornu kiselinu i vodu, gdje je 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil] urea prisutna u otopini u koncentraciji koja je manja od 4 mg/ml i prisutno je dovoljno ortofosforne kiseline da bi se ostvarila bistra otopina.
27. Farmaceutska formulacija vodene otopine prema zahtjevu 26 gdje 1-(4-{[4-(dimetilamino)piperidin-1-il]karbonil}fenil)-3-[4-(4,6-dimorfolin-4-il-1,3,5-triazin-2-il)fenil]urea je prisutna u otopini u koncentraciji od oko 3.0 do 3.5mg/ml.
28. Farmaceutska formulacija vodene otopine prema zahtjevu 26 ili 27 pri čemu je korišteno najmanje 5 molskih ekvivalenata ortofosforne kiseline.
29. Farmaceutska formulacija vodene otopine prema zahtjevu 28 pri čemu je korišteno od 5 do 7 molskih ekvivalenata ortofosforne kiseline.
30. Formulacija prema bilo kojem od zahtjeva 1 do 20 i 25 do 29 za upotrebu u liječenju karcinoma.
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US201462093060P | 2014-12-17 | 2014-12-17 | |
US201562250633P | 2015-11-04 | 2015-11-04 | |
PCT/IB2015/059515 WO2016097949A1 (en) | 2014-12-17 | 2015-12-10 | Formulations of a pi3k/mtor-inhibitor for intravenous administration |
EP15813578.0A EP3233054B1 (en) | 2014-12-17 | 2015-12-10 | Formulations of a pi3k/mtor-inhibitor for intravenous administration |
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WO2019234632A1 (en) * | 2018-06-07 | 2019-12-12 | Pfizer Inc. | 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 |
CA3227191A1 (en) | 2021-07-26 | 2023-02-02 | Celcuity Inc. | 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea (gedatolisib) and its combinations for use in the treatment of cancer |
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WO2006125540A1 (en) * | 2005-05-27 | 2006-11-30 | Bayer Healthcare Ag | Combination therapy comprising a diaryl urea compound and a pi3, akt kinase or mtor inhibitors (rapamycins) for cancer treatment |
US20080234262A1 (en) * | 2007-03-21 | 2008-09-25 | Wyeth | Pyrazolopyrimidine analogs and their use as mtor kinase and pi3 kinase inhibitors |
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WO2009146406A1 (en) * | 2008-05-30 | 2009-12-03 | Genentech, 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 |
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