Method of making tetrapeptide derivative TZT-1027 crystal

Details Method of making tetrapeptide derivative TZT-1027 crystal Method of making tetrapeptide derivative TZT-1027 crystal

2008-06-10

2008-06-10

Kosar, Andrew D (Department: 1654)

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

Separation or purification

C530S330000, C530S332000, C530S333000, C514S018700

Reexamination Certificate

active

07385029

ABSTRACT:
The invention provides crystals of N2-(N,N-dimethyl-L-valyl)-N-[(1S,2R)-2-methoxy-4-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[(2-phenylethyl)amino]propyl]-1-pyrrolidinyl]-1-[(S)-1-methylpropyl]-4-oxobutyl]-N-methyl-L-valinamide or salts thereof which possess potent antitumor activity and methods for their preparation.

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G. R. Pettit et al., “The Dolastatins. 21. Synthesis, X-ray Crystal Structure, and Molecular Modeling of (6R)-isodolastatin 10”, The Journal of Organic Chemistry, vol. 59, No. 21, pp. 6127-6130, Oct. 21, 1994.
R. Giege et al., “Crystallogenesis of biological macromolecules: facts and perspectives”, Acta. Crystallogr. D. Biol. Crystallogr., vol. 50 (P+4), pp. 339-350, Jul. 1994.
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