Rapamycin peptides conjugates: synthesis and uses thereof

Details Rapamycin peptides conjugates: synthesis and uses thereof Rapamycin peptides conjugates: synthesis and uses thereof

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 31/436 (2006.01) A61K 38/04 (2006.01) A61L 31/08 (2006.01) A61L 31/16 (2006.01) A61P 37/00 (2006.01) C07D 498/14 (2006.01) C07K 1/00 (2006.01) C07K 5/04 (2006.01)

Patent

CA 2544731

The present invention relates to new rapamycin derivatives for the inhibition of cell proliferation. The compounds can advantageously target two proteins in dividing cells and interfere with cell cycle. There is thus provided derivatives of rapamycin in which the 42 position of rapamycin is linked to an amino acid or a peptide through a carbamate ester linkage. These rapamycin derivatives can be synthesized by reacting 42-O-(4-Nitrophenoxycarbonyl) rapamycin and an amino acid or a free amino peptide under basic conditions. These rapamycin derivatives can be used to inhibit the cell cycle and are therefore useful for treating cell proliferation disorders.

La présente invention concerne de nouveaux dérivés de rapamycine destinés à inhiber la prolifération cellulaire. Ces composés peuvent avantageusement cibler deux protéines dans la division cellulaire, et intervenir dans le cycle cellulaire. L'invention concerne ainsi des dérivés de rapamycine dans lesquels la 42 ème position de la rapamycine est liée à un acide aminé ou un peptide par une liaison carbamate ester. Ces dérivés de rapamycine peuvent être synthétisés par mise en réaction de 42-O-(4-Nitrophénoxycarbonyl) rapamycine et d'un acide aminé ou d'un aminopeptide libre dans des conditions de base. Lesdits dérivés de rapamycine peuvent être utilisés pour inhiber le cycle cellulaire et sont, par conséquent, utilisés dans le traitement des troubles associés à la prolifération cellulaire.

Affiliated with

Also associated with

Rating

Rapamycin peptides conjugates: synthesis and uses thereof does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Rapamycin peptides conjugates: synthesis and uses thereof, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Rapamycin peptides conjugates: synthesis and uses thereof will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-1438348