Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai
Patent
1999-01-12
2000-11-07
Peselev, Elli
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Carbohydrate doai
536 65, 536 168, A61K 3170
Patent
active
061437263
DESCRIPTION:
BRIEF SUMMARY
The present invention refers to the complexes forming between N'-dimethylaminoacetylpartricin A dimethylaminoethylamide, (SPA-S-752), or the salts thereof, and cholesterol 3-sulphate, and the pharmaceutical compositions containing them, useful in the treatment of systemic mycoses. Examples of a salt are the diaspartate (SPA-S-753), the diascorbate (SPA-S-843) and any other salt that is pharmaceutically acceptable.
At present, the request for antifungal agents is pressing owing to the diffusion of systemic mycoses in patients with debilitating diseases such as cancer, and in immunodeficiency conditions, such as HIV III infections (AIDS). Organ grafting too, in conjunction with the subsequent, indispensable immunosuppressive treatments, is one of the causes of the progressive diffusion of the often lethal mycotic infections. Systemic mycoses, for example, are found as often as nearly 50% in patients having died of acute leukaemia and following renal transplant. These mycoses are caused by a large number of pathogenic microorganisms of the mould and yeast class (Aspergillus, Candidae, Cryptococcus etc.).
The therapeutic measures so far available to the physician are limited to some substances, none of which effective on all of the infecting species. Availability of new systemic antifungal agents is therefore vital, owing also to the high toxicity of those already available, limiting their use to doses insufficient to cure and inadequate to prevent. These drugs high toxicity requires that they be used in hospital only, during even prolonged hospitalisation (several weeks and months), distressing to the patient and costly for the community.
As for the compound N'-dimethylaminoacetylpartricin A dimethylaminoethylamide diaspartate (henceforth mentioned with code name SPA-S-753), for instance, it is a known synthetic derivative (U.S. Pat. No. 5,298,495, Bruzzese T. et al., 1994) of partricin A, a polyene antibiotic obtained through fermentation of a streptomyces aureofaciens strain. SPA-S-753 presents a toxicity definitely much lower than that of partricin which enables its clinical use, a high water-solubility which permits its parenteral administration, and similar microbiological activity against various fungi (Candida albicans, Candida parapsilopsis, Candida rusei, Candida tropicalis, Candida guilliermondi, Candida glabrata, Cryptococcus laurentii, Cryptococcus albidus, Cryptococcus neoformans, Saccharomyces cerevisiae, Syncephalastrum racemosum, Trichosporon cutaneum, Trichophytum mentagrophytes, Trichophytum rubrum, Aspergillus niger, Aspergillus fumigatus) and protozoa (Trichomonas vaginalis), attributable to its capacity of interacting with cell membranes (Strippoli V., Simonetti N., Villa A., Bruzzese T.--European Bulletin of Drug Research, 1, 113, 1992 and Strippoli V., Simonetti N., D'Auria F. D., Bruzzese T.--European Bulletin of Drug Research, 3, 71, 1994).
SPA-S-753 toxicity is however not low enough as to allow its use outside close medical supervision in hospital, nor to exclude important side effects. For example, SPA-S-753 intramuscular administration leads to its partial precipitation which has a negative influence on tolerance of the product. Like all other drugs employed in the pathologies in question, the side effects connected with the use of the product might limit the extent of the doses to be administered, with the risk that in certain cases treatment might not prove effective, with predictable unfavourable outcome.
One of the aims of the present invention is the description of some antimycotic agents exhibiting limited toxicity, negligible side-effects and simple administration in both hospital and at home.
This and other aims evidenced by understanding of the present description are attained by the complexes subject of the present invention.
In the course of studies on this new antibiotic, SPA-S-753, the possibility was demonstrated of complexing it with several substances of biological interest (liposomes, lipids, etc.), and in particular, it was surprisingly found that its complexatio
REFERENCES:
patent: 4822777 (1989-04-01), Abra
patent: 5296597 (1994-03-01), Bruzzese et al.
Bruzzese Tiberio
Mozzi Giovanni
Peselev Elli
Quatex N.V.
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