Process for...

Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system

Reexamination Certificate

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Reexamination Certificate

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07915407

ABSTRACT:
The present invention is concerned with a process for the preparation of the compound {3-[2(R)-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3(S)-(4-fluorophenyl) -morpholin-4-yl]methyl]-5-oxo-4,5-dihydro-[1,2,4]-triazol-1-yl}phosphonic acid, and pharmaceutically acceptable salts thereof. This compound is useful as a substance P (neurokinin-1) receptor antagonist. In particular, the compound is useful e.g., in the treatment of emesis and inflammatory diseases.

REFERENCES:
patent: 5691336 (1997-11-01), Dorn et al.
patent: 5780467 (1998-07-01), Dorn et al.
J.J. Hale et al., “Phosphorylated Morpholine Acetal Human Neurokinin-1- Receptor Antagonists as Water-Soluble Prodrugs”, J. Med. Chem., 2000, vol. 43, pp. 1234-1241.
T. D. Nelson et al., “Tetrabenzyl Pyrophosphate [{Diphosphoric Acid, Tetrakis (phenylmethyl) ester]}”, Organic Syntheses, 2000, vol. 80, p. 219.

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