Aminium salts of 1,2,3-triazoles as prodrugs of drugs including antiviral agents
AssigneeBristol-Myers Squibb Company
InventorsJohn Kadow, Alicia Regueiro-Ren
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Abstract
This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts of 1,2,3-triazoles which can be used as prodrugs to improve the solubility or pharmaceutical properties of 1,2,3-triazole containing compounds. More particularly, the present disclosure relates to compounds containing N-aminium-1,2,3-triazoles that are useful as antiviral agents and specifically for the treatment of HIV and AIDS.
Claims8
A compound of Formula I, including pharmaceutically acceptable salts thereof,
- wherein:
- R1 is selected from the group consisting of hydrogen, halogen and methoxy;
- —W— is selected from the group consisting of
- R4, R5, R6, R7, R8, R9, R10, R11 are each independently H or methyl;
- with the proviso that not more than two are methyl;
- R12 is selected from the group consisting of C(O)-phenyl;
- and
- Y is halogen, O(C)OCH3, OC(O)CF3, or other accept pharmaceutical salt counterion.
A method for treating a mammal infected with the HIV virus comprising administering to said mammal an antiviral effective amount of a compound of Formula I, including pharmaceutically accceptable salts thereof, in combination with an antiviral effective amount of an AIDS treatment agent selected from the group consisting of an AIDS antiviral agent;
- an anti-infective agent;
- an immunomodulator;
- and an HIV entry inhibitor.
The use of an aminium salt of a 1,2,3-triazole as a prodrug for releasing a parent drug containing the 1,2,3-triazole after removal of the aminium moiety in animals or humans.
Dependencies are inferred from the claim text.