Reaktion #356890

ord-c770887302674161a3326f12bf9f0eb7

Reaktionsgleichung

CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C
cholesterol
CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C
cholesterol
NCCNc1ccc(NCCN)c2c1C(=O)c1ccncc1C2=O
BBR 2778
NCCNc1ccc(NCCN)c2c1C(=O)c1ccncc1C2=O
BBR 2778
→
CCCCC/C=C\C/C=C\CCCCCCCC(=O)O
linoleic

Edukte

CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C
cholesterol
CC(C)CCC[C@@H](C)[C@H]1CC[C@H]2[C@@H]3CC=C4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C
cholesterol
NCCNc1ccc(NCCN)c2c1C(=O)c1ccncc1C2=O
BBR 2778
NCCNc1ccc(NCCN)c2c1C(=O)c1ccncc1C2=O
BBR 2778
—
Phosphatidylcholine
—
fatty acids
—
phosphatidylcholine

Reagenzien

Keine

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Vorschrift

Therefore, the invention provides a liposome formulation of compound BBR 2778 consisting of liposomes comprising phosphatidylcholine, cholesterol and BBR 2778, in a cholesterol/phospholipide 1:2 to 1:7 weight ratio and in a BBR 2778/phospholipide 1:4 to 1:25 weight ratio. Phosphatidylcholine preferably includes residues of fatty acids selected from palmitic, oleic, linoleic, gamma-linoleic, linolenic and stearic acids, and the liposome is formed by a mixture of hydrogenated and non-hydrogenated phosphatidylcholines, having the fatty acids composition indicated, in a 1:2 to 2:1 ratio, more preferably said mixture consists of hydrogenated phosphatidylcholine having melting point of 120° C. and crystallization point of 90° C., and non-hydrogenated phosphatidylcholine having a thermogram as reported in FIG. 5. The hydrogenated and non-hydrogenated phosphatidylcholines, having the above-indicated composition, are commercially available respectively under the name PHOSPHOLIPON® 90 H and PHOSPHOLIPON® 90.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07449197B2uspto-grants-2008_11