Apoptosis inducer

Details Apoptosis inducer Apoptosis inducer

2000-06-09

2003-02-25

Goldberg, Jerome D. (Department: 1614)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

C514S396000, C548S345100

Reexamination Certificate

active

06525082

ABSTRACT:

TECHNICAL FIELD
The present invention relates to a substance for inducing apoptosis useful in the field of pharmaceuticals having a physiological activity such as anticancer action and use thereof.
PRIOR ART
In recent years, a mode of apoptosis has been drawing the attention concerning the death of cell tissues.
Unlike necrosis which is a pathological cell death, apoptosis is a death which is initially programmed in the gene of the cell itself. Thus, the gene which programs the apoptosis is activated by certain external or internal causes whereby programmed cell death gene protein is produced based upon said gene and then the cell itself is decomposed and dead by the resulting programmed death protein.
If such apoptosis can be expressed in desired tissues or cells, it will be now possible to exclude the unnecessary or harmful cells from living body in their natural form and that will be significantly meaningful.
PROBLEMS TO BE SOLVED BY THE INVENTION
Pharmaceuticals which have been used in clinical therapy include many agents such as anticancer agents, antibiotic substances, immunopotentiators, immunomodulators, etc. (such as alkylating agents, antimetabolites and plant alkaloids) but it can be hardly said that such a drug therapy has been completely established already.
An object of the present invention is to develop the highly-safe substance having a physiological function such as apoptosis-inducing action, etc. and to offer a method for the manufacture of said substance and pharmaceuticals containing said substance.
MEANS TO SOLVE THE PROBLEMS
The present invention will be summarized to be as follows. Thus, the first feature of the present invention relates to a substance for inducing apoptosis represented by the respective following formulae [I]~[VIII] or an optically active substance or a salt thereof.
(In the formula [III], R
1
is H, an amino group, a lower alkyl group or a lower alkyl group having a substituent in an amino acid; R
2
is a divalent residue after removal of carboxyl group and amino group participating in a peptide bond in an amino acid; X is O
−
or an amino group; Y
k−
is an anion having valence(s) of k; m is an integer of 0-4; n is 0 or a positive integer; k is a positive integer; and when n is 2 or more, two or more R
2
existing therein may be same or different while, when X is O
−
, the substance is an inner salt whereby Y
k−
does not exist.)
(In the formula [VI], R
3
and R
4
may be same or different and each is an alkyl group having 1-3 carbons.)
(In the formula [VII], R
5
and R
6
may be same or different and each is an aromatic ring of an aromatic amino acid.)
The second feature of the present invention relates a pharmaceutical composition which is characterized in containing the substance for inducing apoptosis, an optically active substance or a salt thereof of the first feature of the present invention.
In a preferred embodiment of the second feature of the present invention, said pharmaceutical composition is an anticancer agent.


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Arnau et al., J. Heterocycl. Chem., 34(1), p. 233-239 (1997).
Saville-Stones et al., J. Chem. Soc., Perkin Trans. 1, (10), p. 2603-2604 (1991).
Sakai et al, Journal of Pesticide Science, 18(3), p. 217-223 (1993).
Norris et al, Can. J. Chem., 55(10), p. 1687-1695 (1977).
Groenneberg et al., Acta Chem. Scand., 26(5), p. 1847-1850 (1972).

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