Fluoro taxols

Details Fluoro taxols Fluoro taxols

1992-07-01

1993-03-09

Reamer, James H.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

549510, A01N 4302

Patent

active

051927969

ABSTRACT:
This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is benzoyl or t-butyloxycarbonyl; R.sup.2 is acetoxy, hydrogen or hydroxy; and the wavy line indicates either the .alpha.- or the .beta.-configuration.
Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.

REFERENCES:
patent: 4814470 (1989-03-01), Colin et al.
patent: 4960790 (1990-10-01), Stella et al.
patent: 5136060 (1992-08-01), Holton
Welch, Tetrahedron, vol. 43, #14, pp. 3123-3197 (1987).
Francioise Gueritte-Voegelein et al, "Relationships between the Structure of Taxol Analogues and Their Antimitotic Activity," Journal of Medicinal Chemistry, 1991, 34, pp. 992-998.
William P. McGuire, M.D. et al, "Taxol: A Unique Antineoplastic Agent with Significant Activity in Advanced Ovarian Epithelial Neoplasms," Annals of Internal Medicine, Aug. 15, 1989, vol. 111, No. 4, pp. 273-279.
Charles S. Swindell et al, "Biologically Active Taxol Analogues with Deleted A-Ring Side Chain Substituents and Variable C-2' Configurations," Journal of Medicinal Chemistry, 1991, 34, pp. 1176-1184.

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