Tetrapeptide derivative TZT-1027 crystal

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Peptide containing doai

Reexamination Certificate

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Details

C530S330000

Reexamination Certificate

active

07008928

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.

REFERENCES:
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patent: 0598129 (1994-05-01), None
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patent: 93/03054 (1993-02-01), None
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Website: http://web.archive.org/web/20010222115331/http://www.chem.vt.edu/chem-ed/diffraction/powder.html.
George R. Petitt, Jayaram K. Srirangam, Delbert L. Herald, and Ernest Hamel, The Dolastatins. 21. Synthesis, X-ray Crystal Structure, and Molecular Modeling of (6R)-Isodolastatin 10, Oct. 21, 1994, 59 (21), pp. 6127-6130.
Richard Giege, Bernard Lorber, and Anne Theobald-Dietrich, Crystallogenesis of biological macromolecules: facts and perspectives, Acta Crystallogr D Biol Crystallogr. Jul. 1994;50(Pt 4):339-50. □□.
K. Miyazaki et al., “Synthesis and Antitumor Activity of Novel Dolastatin 10 Analogs”, Chem. Phar. Bull., vol. 43, No. 10, pp. 1706-1718, 1995.
G. R. Pettit et al., “The Doplastatins. 21. Synthesis, X-ray Crystal Structure, and Molecular Modeling of (6R)-Isodolastatin 101a”, The Journal of Organic chemistry, vol. 59, No. 21, Oct. 21, 1994, pp. 6127-6130.

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