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US 10,472,372 B2Granted
HIV-1 protease inhibitors and uses thereof
AssigneesPurdue Research Foundation, National University Corporation Kumamoto University
InventorsArun K. Ghosh, Hiroaki Mitsuya
Life of this patent
Estimating the term…
Abstract
Various embodiments relate to a compound of the formula (I): wherein X, X1, R1—R4 and R7 are defined herein, as well as pharmaceutical compositions comprising compounds of the formula (I) and methods of treating an HIV infection comprising administering a therapeutically effective amount of one or more compounds of formula (I), or a pharmaceutical compositions comprising compounds of the formula (I), to a patient in need thereof.
Claims20
A compound of the formula (I):
- or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or ate thereof, wherein:
- n is an integer from 1 to 3;
- X and X1 are each, independently, (—CH2—)m, wherein m is 1 or 2;
- R1 is —N3 or —NR52, wherein each R5 is, independent, H, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl or a nitrogen protecting group;
- R7 is H or unsubstituted or substituted alkyl or R1 and R7, together with the carbon atom to which they are attached, form a heterocycle;
- R2 is unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkoxy, unsubstituted or substituted hydroxyalkyl, halo, unsubstituted or substituted heterocyclylaltyloxy, —O—(CH2)0-2P(O)(OR6)2, wherein each R6 is independently H or unsubstituted or substituted alkyl or substituted or unsubstituted aryl or R1 is —NR52, wherein one R5 and one R2 are joined to represent the group —(CH2)p(CHCH)d(CH2)qO— wherein p is an integer from 0 to 5, d is 0 or 1, and q is an integer from 0 to 5;
- R3 is substituted or unsubstituted alkyl;
- and
- R4 is unsubstituted or substituted aryl, unsubstituted or substituted benzthiazole, unsubstituted or substituted benzoxazole, unsubstituted or substituted benzofuranyl or unsubstituted or substituted indolyl.
6 more elements
A compound of the formula:
- or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof.
A compound of the formula:
- or a pharmaceutically acceptable salt, polymorph, prodrug, solvate or clathrate thereof;
- wherein e is 0 or 1;
- R′ is H or unsubstituted or substituted alkyl;
- and X6 is:
1 more element
Dependencies are inferred from the claim text.