Fluorine-containing vitamin D3 analogues and pharmaceutical comp

Details Fluorine-containing vitamin D3 analogues and pharmaceutical comp Fluorine-containing vitamin D3 analogues and pharmaceutical comp

1991-06-05

1993-04-27

Dees, Jose G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

556436, 556449, 552547, A01N 4500, A61K 3159, C07F 704

Patent

active

052062309

ABSTRACT:
Fluorine-containing vitamin D.sub.3 analogues of the formula[I]: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen atom, a chemically inactive hydroxy-protecting group, an acyl having 2 to 8 carbon atoms, or an alkyl having 1 to 8 carbon atoms, X is a straight carbon chain having 4 to 6 carbon atoms which contains at least one double or triple bond, which have excellent vitamin D.sub.3 -like activities, particularly anti-tumor activity owing to differentiation-inducing activity and are useful for the prophylaxis and treatment of various tumors, and intermediates therefor.

REFERENCES:
patent: 4613594 (1986-09-01), Baggiolini et al.
patent: 4717721 (1988-01-01), De Luca et al.
Hirobumi Tamaka et al., Seikagaku (Biochemistry), vol. 55 1323 (1983).
Colton et al., Lancet, Jan. 28, 188 (1989).
Ostrem et al. Proc. Natl. Acad. Sci. 84, 2610, (1987).
Baggiolini et al, JACS 104, 2945 (1982).
Toh et al., J. Org. Chem vol. 48, 1414, 1983.
Wovkulich et al. Tetrahedron vol. 40, 2283, (1984).
Augeron et al., Cancer Res. vol. 44, 3961, 1984.
Kay W. Colston et al, The Lancet, Jan. 28, 1989, pp. 188-191.
Voula K. Ostem et al, Proc. Natl. Acad. Sci., USA, vol. 84 May 1987, pp. 2610-2614.

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