C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 15/18 (2006.01) A61K 9/127 (2006.01) C07H 15/10 (2006.01) C07H 19/173 (2006.01) C07H 21/00 (2006.01) C07K 1/107 (2006.01) C07K 7/06 (2006.01) C07K 9/00 (2006.01) C08B 37/00 (2006.01) C08B 37/10 (2006.01)
Patent
CA 2270144
The present invention provides glycophospholipid and peptide-phospholipid conjugates comprising a phospholipid moiety and a saccharide or peptide moiety joined by an ether linkage comprising a secondary or tertiary amine. The conjugate structure of the invention comprises a flexible spacer arm between the phospholipid and saccharide or peptide moieties which, being variable in length, serves to optimize saccharide or peptide bioactivity. This invention further provides a method for the synthesis of such conjugates comprising the step of reductive amination. The method is efficient, economical and provides a high yield of product. Glycophospholipid and peptide-phospholipid conjugates of the invention can be incorporated and, optionally, chemically polymerized in self-assembling systems such as membranes, bilayers, films, liposomes and the like, and find utility diagnostically and therapeutically in medical and immuno-biological applications.
L'invention concerne des conjugués de glycophospholipides et de peptide-phospholipides comprenant une fraction phospholipide et une fraction saccharide ou peptide réunies par une liaison éther comprenant une amine secondaire ou tertiaire. La structure de ce conjugué présente un bras de liaison souple entre les fractions phospholipide et saccharide ou peptide, qui, étant donné sa longueur variable, sert à optimiser la bioactivité des saccharides ou des peptides. Elle concerne, de plus, un procédé de synthèse de ces conjugués consistant en une étape d'amination réductrice. Ce procédé est efficace, économique et permet d'obtenir un rendement élevé. On peut incorporer ces conjugués de glycophospholipides et de peptide-phospholipides et, éventuellement, les polymériser dans des systèmes s'assemblant automatiquement, tels que des membranes, des bicouches, des films, des liposomes, par exemple, et on peut les utiliser dans un but diagnostique ou thérapeutique dans le domaine médical ou immunobiologique.
Chaikof Elliot L.
Sun Lijun
Emory University
Robic
LandOfFree
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