Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...
Patent
1982-12-17
1986-05-27
Goldberg, Jerome D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Phosphorus containing other than solely as part of an...
A61K 3166
Patent
active
045915830
ABSTRACT:
A pharmaceutical preparation containing as active ingredient a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are the same or different, and each is selected from the group consisting of hydrogen, alkyl groups containing 1-6 carbon atoms; cycloalkyl groups containing 3-6 carbon atoms; cycloalkyl-alkyl groups containing 4-6 carbon atoms; 1-adamantyl; 2-adamantyl, benzyl; and phenyl groups of the formula ##STR2## wherein R.sub.4 and R.sub.5 are the same or different and each is selected from the group consisting of hydrogen, halogen, alkyl having 1, 2, or 3 carbon atoms, alkoxy having 1, 2, or 3 carbon atoms, alkoxycarbonyl having 2-7 carbon atoms and alkylcarbonyl groups having 2-7 carbon atoms; or R.sub.4 and R.sub.5 together form a straight saturated alkylene chain having 3 or 4 carbon atoms and being bound to adjacent positions, i.e. 2,3- or 3,4- in the phenyl ring; and R.sub.3 is selected from the group consisting of hydrogen, alkyl groups containing 1-8 carbon atoms; cycloalkyl groups containing 3-8 carbon atoms; cycloalkyl-alkyl groups containing 4-8 carbon atoms; 1-adamantyl; 2-adamantyl; benzyl; and phenyl groups of the formula ##STR3## wherein R.sub.4 and R.sub.5 have the meaning given above; provided that at least one of the groups R.sub.1, R.sub.2 and R.sub.3 is alkyl, cycloalkyl, or cycloalkyl-alkyl as defined above, or 1-adamantyl, 2-adamantyl, or benzyl; and provided that when R.sub.3 is H, then one of R.sub.1 and R.sub.2 is alkyl, cycloalkyl, or cycloalkyl-alkyl as defined above, or 1-adamantyl, 2-adamantyl, or benzyl and the other of R.sub.1 and R.sub.2 is H; or a physiologically acceptable salt or an optical isomer thereof; novel compounds within formula I, methods for their preparation and their medicinal use.
REFERENCES:
Alenius, et al., "Therapeutic Effect of Trisodium Phosphonoformate on Cutaneus Herpes Virus Infection in Guinea Pigs," Antimicrobial Agents and Chemotherapy, Sep. 1978.
Palmer, et al., "Disodium Phosphonoacetate in Cream Base as a Possible Topical Treatment for Skin Lesions at Herpes Simplex Virus in Cebus Monkeys," Antimicrobial Agents and Chemotherapy, Oct. 1977.
Chemical Abstracts, vol. 50, No. 2, 794d, (1956).
Galasso, "An Assessment of Antiviral Drugs for the Management of Infectious Diseases in Humans," Antiviral Research, 1 (1981), 73-96.
Kern et al., "Treatment of Experimental Herpesvirus Infections with Phosphonoformate and Some Comparisons with Phosphonoacetate", Antimicrobial Agents and Chemotherapy, 14 (Dec. 1978), 817-823.
Helgstrand Ake J. E.
Johansson Karl N.
Misiorny Alfons
Noren Jan O.
Stening Goran B.
Astra Lakemedel Aktiebolag
Goldberg Jerome D.
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