Anti-glucocorticoid drug

Details Anti-glucocorticoid drug Anti-glucocorticoid drug

1997-09-26

1999-10-12

Travers, Russell

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

C-o-group doai

514 78, 514724, 514703, 514722, A61K 31045, A61K 31685, A61K 3111, A61K 3108

Patent

active

059656239

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND OF THE INVENTION

The invention relates to medicine, specifically to antiglucocorticoid preparations of a non-steroid nature, i.e. preparations whose chemical structure contains no steran nucleus. The purpose of the invention is to defend somatic mammary cells from the action of glucocorticoid hormones.
The following glucocorticoid-suppressive substances are known to be in use in medicine:
1. Substances which suppress the synthesis of steroid hormones at various stages (inhibitors of enzymes which catalyze various stages of the synthesis of steroid hormones [1]): synthesis of steroid hormones at stages 11-.beta.-, 17- and 21- of hydroxylase); synthesis at stage 11-.beta. of hydroxylase); impedes the synthesis of pregnenolon from cholesterine through suppression of 20-.alpha.-hydroxylase and C20, C-22-liase; steroid-3.beta.-hydroxy-5-androsten-17-one), which suppresses 3.beta.-desoxysteroidhydrogenase-5.4-isomerase [4].
2. Substances which suppress the interaction of glucocorticoid hormones with hormone receptors: dimethyl-aminophenyl)-17.beta.-hydroxy-17.alpha.-(prop-1-inyll)-estra4.9di en-3-one), which acts on receptors of glucocorticoid hormones to form a complex incapable of initiating mechanisms of the glucocorticoid effect [3]; of isoquinoline-1-(3.4-dietoxibene zilidene)-6.7-dietoxy-1,2,3,4-tetrahydrizoquinoline) or acetylsalicic acid [5].
The above-named preparations have a determinate antiglucocorticoid effect when taken as an ingredient in various medicines.
It is also known that the above-listed preparations have a number of significant drawbacks:
1. Preparations which inhibit the synthesis of glucocorticoids also inhibit, depending upon the target enzymes, the synthesis of other steroid hormones (i.e. sexual steroids and/or mineralocorticoids) and elicit an accumulation of the predecessor substrates of inhibited enzymes, which substrates also display hormonal activity.
2. The level of specificity of effect of preparations in the second group is very low, i.e. in addition to an antiglucocorticoid effect, they also have other steroidal antihormonal effects as well.
3. All steroid substances in one way or another upset the balance of steroids in the human organism. Such substances may form metabolites possessing active characteristics different to those of the substance initially administered to the patient.
Of the above-listed preparations Mifepriston (RU 486), a medicine containing a steran nucleus, is the most free of the above-named defects, is the most specific in its ability to block glucocorticoid receptors, and is closest in its pharmacological action to the group of medicines which are the subject of the present application. Mifepriston is described in greater detail in, for example, [3] and [6]. Hereafter in the present application Mifepriston will be used as the most frequent comparison for the effectiveness of the antiglucocorticoid medicine which is the subject of this application (hereinafter called `the proposed drug`). Together with its great advantages, Mifepriston, like other analogues, possesses a number of weak points:
Also known are insect pheromones, i.e. substances produced and excreted into the environment by insects and having a specific smell that acts upon specific (pheromone) receptors in sensitive members of the same insect type, eliciting in the latter a typical behavioral reaction or process, e.g. attraction of insects of the opposite sex to a meeting site, preparations for fertilization etc. [8].
One group of pheromones comprises, specifically, long-chain aliphatic unsaturated alcohols, ethers and acetates containing in a linear hydrocarbon chain between 10 and 21 carbon atoms. Pheromones of this group are used as domestic and agricultural insecticides [7,8].
The specific physical and chemical characteristics of the above-named pheromones and their synthetic analogues and derivatives (specifically, the pronounced hydrophobic property of the long-chain hydrocarbon structure) give them the ability easily to dissolve in fats and to incorporate themselves into

REFERENCES:
Bartelt et al.; J. Chem. Ecol. , 9 (9), 1343-52 (Abstract), 1983.
Dunkelblum et al. ; Insect Biochem., 19 (5), 523-6 (Abstract), 1989.
Sweeney et al. J. Chem. Ecol., 16(5), 1517-30 (Abstract), 1990.

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