Malignant tumor metastasis inhibitors

Details Malignant tumor metastasis inhibitors Malignant tumor metastasis inhibitors

1998-06-10

2003-05-20

Goldberg, Jerome D. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

Reexamination Certificate

active

06566351

ABSTRACT:

TECHNICAL FIELD
The present invention relates to malignant tumor metastasis inhibitors. More specifically, it relates to malignant tumor metastasis inhibitors containing an active vitamin D or a derivative thereof as an active ingredient.
BACKGROUND ART
The cure rate of malignant tumors is more and more increasing by early diagnosis and progress of therapies, but metastases of malignant tumors are often beyond current therapies and pose one of important medical problems. At present, chemotherapies are used to arrest metastases following removal of tumors with unsatisfactory results, so that it would be desirable to develop more effective inhibitors against malignant tumor metastases.
Bone tissues are one of the most favored sites of metastases of malignant tumors, as a report shows that bone metastases occurred in about 30% of all the cancer cases from autopsy. Among malignant tumors, cancers of the lung, breast, prostate or the like are particularly known to be likely to metastasize to bone.
Vitamin D compounds are known to show a wide variety of physiological activities such as calcium metabolism regulation, growth inhibition or differentiation-inducing of tumor cells or the like, and immunoregulation. Vitamin D derivatives having an oxygen atom at the 22-position which are particularly preferred compounds as malignant tumor metastasis inhibitors of the present invention are known to have very few side effects commonly associated with this type of vitamin D compounds which induce hypercalcemia and they have been reported to be effective for psoriasis, secondary hyperparathyroidism or the like (for example, see JP No. 183534A/1988, JP No. 86382/1994, etc.). They are also known to have antitumor effects, but have not been reported yet to show inhibitory effects against metastases of malignant tumors.
It is an object of the present invention to provide a malignant tumor metastasis inhibitors, and particularly a pharmaceutical agents for inhibiting bone metastases of a malignant tumors.
DISCLOSURE OF THE INVENTION
As a result of extensive research of malignant tumor metastasis inhibitors, it has been found that vitamin D derivatives of the general formula (I):
wherein R
1
represents —O—R
2
, —S—R
2
,—CH
2
—R
2
or —CH═R
2
where R
2
represents a C
1
-C
10
chain hydrocarbon group which may be substituted by one or more hydroxyl groups, and R
3
represents a hydrogen atom or a hydroxyl group are effective as malignant tumor metastasis inhibitors, particularly as inhibitors against bone metastases of malignant tumors, and thus accomplished the present invention.
Therefore, the present invention relates to malignant tumor metastasis inhibitors containing a compound of the general formula (I):
wherein R
1
represents —O—R
2
, —S—R
2
—CH
2
—R
2
or —CH═R
2
where R
2
represents a C
1
-C
10
chain hydrocarbon group which may be substituted by one or more hydroxyl groups, and R
3
represents a hydrogen atom or a hydroxyl group, as an active ingredient.


REFERENCES:
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Olkawa et al., Anti-Cancer Drugs, 2, pp 475-480, 1991.*
Franceschi et al., J. of Biological Chemistry, 262, 9, pp 4165-4171, 1987.*
Young et al, “Treating tumor-bearing mice with vitamin D3diminishes tumor-induced myelopoiesis and associated immunosuppression, and reduces tumor metastasis and recurrence”,Cancer Immunol Immunother41:37-45, (1995).
Hamada et al., “Novel vitamin D3analogs and their potential for inhibiting cancer cell growth”,Drugs of the Future, (1993), pp. 1057-1061, vol. 18, No. 11, Prous Science.
Abe et al., Endocrinology, 129(2), pp832-837 Abstract Only, 1991.

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