TRITERPENOIDS WITH HIV MATURATION INHIBITORY ACTIVITY
Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C 4-8 cycloalkyl, C 4-8 cycloalkenyl, C 4-9 spirocycloalkyl, C 4-9 spirocycloalkenyl, C 4-8 oxacycloalkyl, C 4-8 dioxacycloalkyl, C 6-8 oxacycloalkenyl, C 6-8 dioxacycloalkenyl, C 6 cyclodialkenyl, C 6 oxacyclodialkenyl, C 6-9 oxaspirocycloalkyl and C 6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is —C 1-6 alkyl-halo. These compounds are useful for the treatment of HIV and AIDS.
1 . A pharmaceutical composition which comprises the compound
together with one or more pharmaceutically acceptable carriers, excipients and/or diluents, and which comprises an additional AIDS treatment agent selected from the group consisting of: (a) an AIDS antiviral agent; (b) an anti-infective agent; (c) an immunomodulator; and (d) an HIV entry inhibitor.
2 . A pharmaceutical composition according to claim 1 wherein said additional AIDS treatment agent dolutegravir.
3 . A pharmaceutical composition according to claim 2 wherein said additional AIDS treatment agent is cabotegravir.
4 . A pharmaceutical composition according to claim 2 wherein said additional AIDS treatment agent is 3TC.
5 . A method for treating a mammal infected with the HIV virus comprising administering to said mammal the compound
and which comprises administration of an additional AIDS treatment agent selected from the group consisting of: (a) an AIDS antiviral agent; (b) an anti-infective agent; (c) an immunomodulator; and (d) an HIV entry inhibitor.
6 . The method of claim 4 wherein said additional AIDS treatment agent is dolutegravir.
7 . The method of claim 5 wherein said additional AIDS treatment agent is cabotegravir.
8 . The method of claim 5 wherein said additional AIDS treatment agent is 3TC.