Rapamycin peptides conjugates: synthesis and uses thereof

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

2004-11-03

2010-02-09

Kosar, Andrew D (Department: 1654)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

C530S317000

Reexamination Certificate

active

07659244

ABSTRACT:
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.

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International Search Report and Written Opinion of the International Searching Authority, corresponding to PCT application No. PCT/CA2004/001918 dated Mar. 14, 2005.

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