초록 ▼

Disclosed are specific dipeptidyl 2-amino-1,2-dideoxy-D-glucoses which, either alone, or in combintion with an anti-AIDS drug, e.g. azidothymidine, protect an immunocompromised human host, resulting from an AIDS-related virus, against opportunistic, bacterial, fungal and viral infections, as well as

Disclosed are specific dipeptidyl 2-amino-1,2-dideoxy-D-glucoses which, either alone, or in combintion with an anti-AIDS drug, e.g. azidothymidine, protect an immunocompromised human host, resulting from an AIDS-related virus, against opportunistic, bacterial, fungal and viral infections, as well as help to suppress the AIDS-related virus itself.

대표청구항 ▼

A composition for enhancing host resistance against opportunistic bacterial, fungal and viral infection in an AIDS-immunocompromised human host comprising a compound of the formula: [Figure] wherein: R1 is C1-7 alkyl, substituted Cl-7 alkyl; phenyl; or substituted phenyl; R2 is hydrogen; or C1-10 al

A composition for enhancing host resistance against opportunistic bacterial, fungal and viral infection in an AIDS-immunocompromised human host comprising a compound of the formula: [Figure] wherein: R1 is C1-7 alkyl, substituted Cl-7 alkyl; phenyl; or substituted phenyl; R2 is hydrogen; or C1-10 alkyl; R3 and R4 may be the same or different and are each independently hydrogen, or acyl of the formula: [Figure] where X is －O－, －S－, －CH2－, [Figure] R9, R10, and R12 may be the same or different and are each independently hydrogen; C1-20 alkyl; C2-20 alkenyl; C1-20 alkylcarbonyloxy; amino; phenyl; benzyl; C1-20alkoxymethyl; or C1-20 alkylamido; R11 is hydrogen; C1-30alkyl; C2-30 alkenyl; C1-30 alkoxy; phenyl; C1-20 alkylsulfonyl; or cholesteryl; and m is 0-90; and n is 0 or 1, provided that when n is 0, R1 may additionally be phenyl, substituted phenyl, 1-adamantyl, or heterocycle selected from the group consisting of 2- or 3-furyl, 2- or 3- thienyl, 2- or 3-pyrrolidinyl, 2-, 3-, or 4-pyridyl, and 1-tetrazolyl, said heterocycle optionally substituted with C1-20 alkylcarbonyl; R5 is hydrogen; or R5-R6 together is －CH2－CH2－CH2; R6 is hydrogen; C1-7 alkyl, hydroxymethyl; mercaptomethyl; benzyl; or substituted benzyl; R7 and R8 may be the same or different and are each independently COOR or CONR′R″, where R is hydrogen or Cl-7 alkyl, and R′and R″are each independently hydrogen or C1-3 alkyl; when R2 is C1-10 alkyl, the stereochemistry at asymmetric center I can be either D or L; when R6 is not hydrogen, the stereochemistry at asymmetric center II is L; the stereochemistry at asymmetric center III is D; or pharmaceutically acceptable acid addition salts thereof; and an anti-viral, anti-AIDS drug selected from the group consisting of azidothymidine, ansamycin, ribavarin, deoxycytdine, HPA-23, AL-721, and foscarnet; in a physiologically acceptable medium in an amount effective to impart resistance against opportunistic infection.