Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Patent
1992-02-14
1994-06-21
Raymond, Richard L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
514331, 514428, 514445, 514616, 514630, 514895, 546231, 548566, 549 65, 564157, 564220, 564233, 564234, C07C27926, C07C32128, A61K 31155
Patent
active
053228588
ABSTRACT:
There are provided compounds of the formula ##STR1## wherein R.sup.1 is a substituted or unsubstituted divalent aliphatic group of 1 to 16 carbon atoms; wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, aryl and arlkyl, R.sup.3 is selected from the group consisting of same group of values as R.sup.5, R.sup.5 is selected from the group consisting of substituted and unsubstituted alkyl of 1-10 carbon atoms, aryl, cycloalkyl and heterocycloalkyl of 3-8 carbon atoms, wherein the substituents are mono or poly and are selected from the group consisting of lower alkyl, cycloalkyl of 3-8 carbon atoms, lower alkenyl, lower alkynyl, nitro, lower alkoxy, lower alkoxycarbonyl, phenyl loweralkyl, phenyl, mono and polyhalophenyl, phenoxy, mono and polyhalophenoxy, R.sup.6 and R.sup.7 may be the same or different and are hydrogen, alkanoyl or alkoxyalkanoyl, R.sup.7 may also have the same value as R.sup.5, Y is oxygen or sulfur, m is 0 or 1, q is 0 or 1, wherein the prefix alk designates moieties which are straight chain or branched chain, and the term lower designates 1-6 carbon atoms and the unmodified term alk signifies 1-24 carbon atoms, the respective tautomers thereof, the pharmaceutically acceptable salts and addition salts thereof and the hydrates of said salts and addition salts. There are further provided methods of protecting subjects liable thereto from infections caused by an organism of the group Plasmodium sp., Mycobacterium sp. and Pneumocystis carinii by administering to a subject liable to such infection, a prophylactically effective amount of a compound of the foregoing formula. These compounds will also reduce the level of infection where said subjects have already been infected.
REFERENCES:
patent: 3660394 (1972-05-01), Mamalis et al.
patent: 3723429 (1973-03-01), Mamalis et al.
International Search Report, Apr. 22, 1993 (PCT/US93/00395).
Bajwa et al. "The Chemistry of Drugs III, etc." Heterocycles, vol. 20, No. 5 (1983) pp. 839-843.
Mamalis et al I. "Amino-oxy-derivatives, etc." J. Chem. Soc. (1962) pp. 3915-3926.
Weinberg, "The Anti-Microbial Activity of N.sup.1,N.sup.5 Substituted Biguanides", Antibiotics & Chemotherapy 11 (1961) pp. 572-582.
Canfield Craig
Jacobus David P.
Lewis Neil J.
Behr Omri M.
Jacobus Pharmaceutical Co. Inc.
McDonald Matthew J.
O'Sullivan Peter G.
Raymond Richard L.
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