Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-10-02
2000-07-04
Rotman, Alan L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514316, 514397, 514398, A61K 31415, A61K 31445, A61K 3147
Patent
active
060839589
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to pharmaceutical compositions comprising two or more anti-HIV compounds.
BACKGROUND ART
AIDS (Acquired immunodeficiency syndrome) has been sweeping worldwide as an intractable disease caused by HIV (human immunodeficiency virus). The research and development of the therapeutic agents are also performed globally, however, have not given satisfaction yet. At present, anti-HIV compositions which have been used or tested clinically are exemplified by nucleoside derivatives such as azidodeoxythymidine (AZT), dideoxyinosine (ddI), dideoxycytidine (ddC), dideoxydidehydrothymidine (d4T), 3'-thiacytidine (3TC), and the like as main therapeutic agents.
But all of these agents have serious side effects such as pancreatitis, anemia, leukopenia, neutropenia, emesis, aphagia, gastric disorder, anthema, insomnia, illusion, myospasm, dyspnea, dysuria, renal insufficiency, hypacusis, and the like. The agents have many problems such as the emergence of drug resistant viruses by the prolonged administration and followed by reduction of efficacy of agents, and the like.
In order to reduce these problems, at present, the treatment with multiple anti-HIV compositions have been generally adopted.
Under these situations, it has been reported that administration of multiple anti-HIV compounds show synergy. The examples of the synergy are combination of 3TC with non-nucleoside anti-HIV compounds such as {[(benzoxazol-2-yl)methyl]amino}-5-alkyl-6-alkyl-2-(1H)-pyridinone and the like disclosed in JP-A 7-508997, and similar combination of 3TC with 11-cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,3-b;21,31-e][1,4]diazep in-6-one disclosed in JP-A 7-508998.
Problems such as serious side effects of anti-HIV compounds, the emergency of resistant viruses, and the like are pointed out. New combination of anti-HIV compounds which show synergy, that is, compositions comprising the compounds as an active ingredient have been desired.
DISCLOSURE OF INVENTION
The present inventors found that administration of 2-carbamoyloxymethyl-5-(3,5-dichlorophenylthio)-4-iropropyl-1-(pyridin-4-y l) methyl-1H-imidazole (referred to as a CDIMI hereinafter) or the pharmaceutical acceptable salt thereof in combination with other one or more anti-HIV compounds gives synergy by raising anti-HIV activity of each other.
Accordingly, one of the objects of the present invention is to provide an anti-HIV composition comprising CDIMI or the pharmaceutical acceptable salt thereof and other one or more anti-HIV compounds. The present invention also provides a method for treating or preventing of AIDS which comprises administering CDIMI or the pharmaceutical acceptable salt thereof simultaneously or continuously with other one or more anti-HIV compounds.
Another object of the present invention is to provide a use of CDIMI or the pharmaceutical acceptable salt thereof and anti-HIV compounds, for the manufacture of a medicament for treating or preventing of AIDS. The present invention further relates to a method for inhibiting propagation of HIV by contacting HIV virus to CDIMI or the pharmaceutical acceptable salt thereof in combination with other one or more anti-HIV compounds. The present invention relates to combination of CDIMI or the pharmaceutical acceptable salt thereof with other one ore more anti-HIV compounds.
CDIMI of the present invention is described in WO 96/10019 and the synthesis and the anti-HIV activity of the compound have been disclosed in the specification.
BRIEF DESCRIPTION OF DRAWING
FIG. 1 shows correlation a concentration of an anti-HIV compound and a toxicity (CC.sub.50) CEM cells.
FIG. 2 shows correlation between a concentration of an anti-HIV compound and a toxicity (CC.sub.50) to U937 cells.
FIG. 3 shows correlation between a concentration of an anti-HIV compound and a growth inhibition (IC.sub.50) to CEM cells.
FIG. 4 shows correlation between a concentration of an anti-HIV compound and a growth inhibition (IC.sub.50) to U937 cells.
BEST MODE FOR CARRYING OUT THE INVENTION
In the pre
REFERENCES:
patent: 5910506 (1999-06-01), Sugimoto et al.
Eric DeClerck, Journal of Medicinal Chemistry, vol. 38 (14),pp. 2491-2517, Jul. 1995.
Decker et al.,Research Articles, Metabolism of Amprenavir in Liver Microsomes,pp. 803-807, Apr. 16, 1998.
Rotman Alan L.
Shionogi & Co. Ltd.
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