Derivatives of dehydrodidemnin B
AssigneePharma Mar, S.A.
InventorsKenneth L. Rinehart, Anna M. Lithgow-Bertelloni
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Abstract
Dehydrodidemnin with useful biological activity has formula (1). It can be isolated from natural sources or synthesized, and it forms active derivatives. 1
Claims6
The substantially pure compound, Dehydrodidemnin B, essentially free of the cellular debris of the Mediterranean tunicate, Aplidium albicans, said compound having the formula:
- 3
An acylated, alkylated or arylated derivative of dehydrodidemnin B wherein the acyl, alkyl, or aryl groups are selected from C1 to C6 alkyl, C1 to C6 acyl, phenyl, benzyl, or C1 to C6 alkylphenyl.
A pharmaceutical composition which comprises dehydrodidemnin B or an active acylated, alkylated or arylated derivative thereof, together with a pharmaceutically acceptable carrier, wherein the acyl, alkyl, or aryl groups are selected from either C1 to C6 alkyl, C1 to C6 acyl, phenyl, benzyl, or C1 to C6 alkylphenyl.
A semisynthetic process for the preparation of dehydrodidemnin B, which comprises the coupling of pyruvyl-proline to didemnin A.
A method for isolation of dehydrodidemnin B which comprises extraction from a dehydrodidemnin B-containing tunicate.
The monoacetyl derivative of dehydrodidemnin B.
Dependencies are inferred from the claim text.