Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-09-09
2000-05-23
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 3140
Patent
active
06066665&
DESCRIPTION:
BRIEF SUMMARY
INTRODUCTION
The invention relates to a combination of therapeutic agents, comprising as essential components: derivatives or precursors, for use as a therapeutic agent, particularly for therapy of cancer in humans. The invention further relates to drug formulations containing said combination, and use of same; and methods of treating cancer patients with said combination. Finally, the invention relates to the use of the individual components for therapy of hormone-sensitive prostate carcinoma.
TECHNICAL BACKGROUND
Ger. Pat. 3538619 discloses the use of cis-4-hydroxy-L-proline in the treatment of carcinomas and related tumors. Eur. AS B 0223850 discloses the use of N-methyl-cis-4-hydroxy-L-proline and N-methyl-trans-4-hydroxy-L-proline in treating astrocytoma cells. Said Eur AS refers to various other configurations, OH-positions, and alkylations, of the said derivatives of hydroxyproline and proline. W. Hoerrmann et al., 1987, Abstract No. 2:046, "Differential effects of cis-4-hydroxy-L-proline and methyl-cis-4-hydroxy-L-proline on tumour cells--evidence for redifferentiation and cell growth inhibition", in Cancer detection and prevention, 11, (1-2):66.
BRIEF DESCRIPTION OF DRAWINGS
FIG. 1 is a graphic plot of KTCTL2 cell counts for component A, component B, and the combination K (A+B).
FIG. 2 is a plot of KTCTL2 cell counts for various concentrations of the combination K.
FIG. 3 is a plot of KTCTL2 cell counts for various concentrations of component A.
FIG. 4 is a plot of KTCTL2 cell counts for various concentrations of component B.
FIG. 5 is a plot of RT4 cell counts for various concentrations of component A.
FIG. 6 is a plot of RT4 cell counts for various concentrations of component B.
FIG. 7 is a plot of RT4 cell counts for various concentrations of the combination K.
FIG. 8 is a plot of J82 cell counts for various concentrations of component A.
FIG. 9 is a plot of J82 cell counts for various concentrations of component B.
FIG. 10 is a plot of J82 cell counts for various concentrations of the combination K.
FIG. 11 is a plot of LNCap cell counts for various concentrations of component A.
FIG. 12 is a plot of LNCap cell counts for various concentrations of component B.
FIG. 13 is a plot of LNCap cell counts for various concentrations of the combination K.
FIG. 14 is a plot of PC-3 cell counts for various concentrations of component A.
FIG. 15 is a plot of PC-3 cell counts for various concentrations of component B.
FIG. 16 is a plot of PC-3 cell counts for various concentrations of the combination K.
FIG. 17 is a plot of MCF7 cell counts for various concentrations of component A.
FIG. 18 is a plot of MCF7 cell counts for various concentrations of component B.
FIG. 19 is a plot of MCF7 cell counts for various concentrations of the combination K.
FIG. 20 is a plot of HT 1080 cell counts for various concentrations of component A.
FIG. 21 is a plot of HT 1080 cell counts for various concentrations of the combination K.
FIG. 22 is a plot of HTZ-122 cell counts for various concentrations of component A.
FIG. 23 is a plot of HTZ-122 cell counts for various concentrations of component B.
FIG. 24 is a plot of HTZ-122 cell counts for various concentrations of the combination K.
FIG. 25 is a plot of HTZ-17 cell counts for various concentrations of component A.
FIG. 26 is a plot of HTZ-17 cell counts for various concentrations of component B.
FIG. 27 is a plot of HTZ-17 cell counts for various concentrations of the combination K.
THE INVENTION
It was discovered, surprisingly, that the combination of components (A) and (B), is a valuable therapeutic agent, particularly in the therapy of tumors. The antitumor activity of the combination can be demonstrated particularly clearly in a cell culture of tumor cells, where it results in significant inhibition of cell proliferation. In tests of this nature, the tumor cells in a customary culture medium were treated with concentrations of the combination (molar ratio 1:1) in the range 1-100 .mu.g/mL over a period of 6-10 da. At specific times the cell count was dete
REFERENCES:
patent: 5665371 (1997-09-01), Hoerrmann
Journal of the National Cancer Institute, vol. 75, No. 2, 1985, pp. 353-359, Klohs et al, "Collagen-Production Inhibitors . . . ".
Biology of Reproduction, vol. 33, No. 1, 1985, pp. 213-227, Thornton et al, "Collagen and the Proliferation and . . . ".
Cancer Research, vol. 41, No. 7, 1981, pp. 2855-2862, Lewko et al, "Sensitivity of N-Nitrosomethylurea-induced Mammary . . . ".
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