Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-07-21
1996-01-09
Prescott, Arthur C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514212, 514278, 514885, A61K 31405, A61K 31445, C07D21300
Patent
active
054829593
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/UP93/00730 Jan. 27, 1993.
This invention relates to a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans which comprises administering to such human an effective therefore amount of a substituted azaspirane.
BACKGROUND OF THE INVENTION
The use of immunosuppressive/immunomodulatory agents has been shown to suppress viral replication. Specifically, immunomodulating CD8 lymphocytes have been shown to suppress replication of HIV in peripheral blood mononuclear cells (Waler et al. Science, 23:1563-6 (1986)) and activated CD8+ T cells have been shown to inhibit the replication of HIV in cultures of CD4+ cells from asymptomatic HIV seropositive individuals (Brinchmann et al. CD8+ T cells J. Immunol. 144 2961-2966 (1990)). Further, the immunosuppressive compound cyclosporin A (CsA) has demonstrated a protective effect in several animal models of viral infection. Particularly, chronic treatment with CsA before and after infection with LP-BM5 murine leukemia virus has proven effective against the development of immunodeficiency disease (Cerny, A. et al. Eur. J. Immunol. 21:1747-50 (1991)). Evidence that treatment of AIDS and HIV-seropositive non-AIDS patients with CsA increases T4 cells and inhibits lymphadenopathy has also been reported. (Andrieu et al. Clin. Immunol. and Immumopathol. 46:181-198 (1988)) .
Badger, et al., U.S. Pat. No. 4,963,557 (Badger I) discloses compounds of the formula ##STR1## wherein: n is 3-7; m is 1 or 2; R.sup.1 and R.sup.2 are the same or different and are selected from hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 5-10; or R.sup.1 and R.sup.2 together form a cyclic alkyl group having 3-7 carbon atoms; R.sup.3 and R.sup.4 are the same or different and are selected from hydrogen or straight chain alkyl having 1-3 carbon atoms; or R.sup.3 and R.sup.4 are joined together with the nitrogen atom to form a heterocyclic group having 5-8 atoms; or a pharmaceutically acceptable salt or hydrate or solvate thereof.
Badger I discloses compounds of Formula I as a novel class of compounds which induce an immunomodulatory effect which is characterized by the stimulation of suppressor cell activity.
Badger I does not disclose the compounds of Formula I as agents for preventing or delaying the occurrence of AIDS in HIV seropositive humans.
SUMMARY OF THE INVENTION
This invention relates to a method of preventing or delaying the occurrence of AIDS in HIV seropositive humans which comprises administering to such mammal an effective therefor amount of a compound of the formula ##STR2## wherein: n is 3-7; hydrogen or straight or branched chain alkyl, provided that the total number of carbon atoms contained by R.sup.1 and R.sup.2 when taken together is 5-10; or R.sup.1 and R.sup.2 together form a cyclic alkyl group having 3-7 carbon atoms; hydrogen or straight chain alkyl having 1-3 carbon atoms; or R.sup.3 and R.sup.4 are joined together with the nitrogen atom to form a heterocyclic group having 5-8 atoms;
DETAILED DESCRIPTION OF THE INVENTION
The preparation of all compounds of Formula (I) and pharmaceutically acceptable salts, hydrates and solvates and formulations thereof is disclosed in U.S. Pat. No. 4,963,557, the entire disclosure of which is hereby incorporated by reference.
A preferred compound used in the novel method is the dihydrochloride salt of a compound of Formula (I) where R.sup.1 and R.sup.2 are propyl, R.sup.3 and R.sup.4 are methyl, m is 1 and n is 3 which is N,N-dimethyl-8,8-dipropyl-2-azaspiro[4,5]decane-2-propanamine dihydrochloride.
A preferred compound used in the novel method is a compound of Formula (I) where R.sup.1 and R.sup.2 are propyl, R.sup.3 and R.sup.4 are ethyl, m is 1 and n is 3 which is N,N-diethyl-8,8-dipropyl-2-azaspiro[4,5]decane-2-propanamine and salts thereof.
This invention discloses compounds of Formula (I) and pharmaceutica
REFERENCES:
patent: 3733412 (1973-05-01), deBock
patent: 4411904 (1983-10-01), Pattison
patent: 4963557 (1990-10-01), Badger et al.
patent: 5395848 (1995-03-01), Bugelski et al.
patent: 5399553 (1995-03-01), Yokomoto et al.
Badger et al, "Antiarthritic . . . Agents", Chem. Abstr., vol. 113, No. 21, Nov. 1990, No. 191085r, p. 696.
Badger et al, "Preparation . . . Immunosuppressants", Chem. Abstr., vol. 111, No. 17, pp. 702-703, No. 153616r, Oct. 1989.
El-Telbany, "Synthesis . . . Study. Part II", Chem. Abstr., vol. 86, No. 9, p. 419, Feb. 1977.
Dustman Wayne J.
Lentz Edward T.
Prescott Arthur C.
SmithKline Beecham Corporation
Venetianer Stephen
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