Derivative-compound-conjugates and pharmaceutical compositions comprising same

DETAILED DESCRIPTION OF THE INVENTION The introduction of molecules of diagnostic, prophylactic, or therapeutic interest across body surfaces and/or into cells requires the transversal of one or more semi-permeable biological membranes.
The compounds of this invention are useful in permeabilizing biological membranes, thereby assisting body surface and/or membrane transversal of therapeutically-significant-compounds.
In one embodiment, the therapeutically-significant-compound is administered in admixture with a glycosylated steroid derivative of the present invention.
In another embodiment, trans-surface and/or transmembrane transport is facilitated by administering the therapeutically-significant-compound in the form of a derivative-compound-conjugate in which the compound of interest is conjugated to the glycosylated steroid, i.
e.
, R.
sup.
5 is linked to a therapeutically-significant-compound.
Alternatively, the derivative-compound-conjugate may be administered in admixture with a novel glycosylated steroid derivative of the present invention, which may be either the same as, or different from, the derivative of the conjugate.
The novel glycosylated steroid derivatives of the present invention may be expected to enhance the therapeutic efficacy of a wide variety of compounds.
As a result, many therapeutic applications for the compounds of the present invention may be contemplated.
Membrane permeable therapeutic agents could be used in the treatment of a wide variety of illnesses such as AIDS and other chronic viral infections, cancer, bacterial and fungal infections, and metabolic diseases such as lupus, diabetes and rheumatoid arthritis.
The ability of the novel glycosylated steroid derivatives of the present invention to interact with, and/or permeabilize, biological membranes, is believed to result from the compounds' facial amphiphilicity.
The glycosylated surface of the derivatives is hydrophilic; the non-glycosylated surface, hydrophobic.
This facially amphiphilic structure confers unusual properties on the molecules, including an ability to self-associate in both hydrophobic and hydrophilic environments, and to organize at amphiphilic interfaces