HIV matrix protein tyrosine position 29 pocket binders
AssigneeThe Picower Institute for Medical Research
InventorsSenliang Pan, Michael Bukrinsky, Omar K. Haffar
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Abstract
There is disclosed a structural genus of compounds, defined according to coordinates in three-dimensional space, that binds amino moieties on neighboring lysine residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV preintegration complex (PIC), thereby preventing the PIC from binding to karyopherin .alpha. and preventing nuclear importation and integration of the HIV viral genome into the host cell DNA, thereby preventing viral infection.
Claims15
A compound having the formula I:
- ##STR4## wherein R is --X--CO--Z, wherein Z is C.sub.4-6 (straight of branched) alkoxy, wherein X is (CH.sub.2).sub.n or --S--(CH.sub.2).sub.n, wherein n is an integer from 0 to 6, and wherein Y is H or C.sub.1-6 alkyl (straight or branched chain).
A pharmaceutical formulation for the treatment of HIV infection, comprising a compound of formula I:
- ##STR5## wherein R is --X--CO--Z, wherein Z is C.sub.1-6 (straight of branched) alkoxy, wherein X is (CH.sub.2).sub.n or --S--(CH.sub.2).sub.n, wherein n is an integer from 0 to 6, and wherein Y is H or C.sub.1-6 alkyl (straight or branched chain), and a pharmaceutically acceptable carrier.
A method for treating HIV infection, comprising administering an effective amount of a compound from formula I:
- ##STR6## wherein R is --X--CO--Z, wherein Z is C.sub.1-6 (straight of branched) alkoxy, wherein X is (CH.sub.2).sub.n or --S--(CH.sub.2).sub.n, wherein n is an integer from 0 to 6, and wherein Y is H or C.sub.1-6 alkyl (straight or branched chain), and a pharmaceutically acceptable carrier.
A combination therapeutic treatment regimen for the treatment of HIV infection, comprising a compound of formula I:
- ##STR7## wherein R is --X--CO--Z, wherein Z is C.sub.1-6 (straight of branched) alkoxy, wherein X is (CH.sub.2).sub.n or --S--(CH.sub.2).sub.n, wherein n is an integer from 0 to 6, and wherein Y is H or C.sub.1-6 alkyl (straight or branched chain), and a reverse transcriptase inhibitor.
A method for treating HIV infection, comprising administering an effective amount of a compound of formula I:
- ##STR8## wherein R is --X--CO--Z, wherein Z is C.sub.1-6 (straight of branched) alkoxy, wherein X is (CH.sub.2).sub.n or --S--(CH.sub.2).sub.n, wherein n is an integer from 0 to 6, and wherein Y is H or C.sub.1-6 alkyl (straight or branched chain), and an effective amount of a reverse transcriptase inhibitor.
Dependencies are inferred from the claim text.