IP Library › Patent Application 17309435
Patent Application
App. No. 17/309,435

ANTIVIRAL PRODRUGS AND NANOFORMULATIONS THEREOF

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Quick Facts
Patent No.
US None
App. No.
17/309,435
Abstract

The present invention provides prodrugs and methods of use thereof.

Claims (27)

1 - 36 . (canceled)

37 . A compound, or a pharmaceutically acceptable salt thereof, comprising a first integrase inhibitor and a second integrase inhibitor, wherein said first and second integrase inhibitors are covalently attached by a linker.

38 . The compound of claim 37 , wherein said first and second integrase inhibitors are each independently selected from the group consisting of cabotegravir (CAB), raltegravir (RAL), elvitegravir (EVG), dolutegravir (DTG), bictegravir (BIC), BI 224436, and MK-2048.

39 . The compound of claim 37 , wherein said linker is an optionally substituted aliphatic group, and wherein said linker forms an ester with the oxygen of a hydroxyl moiety of said first and second integrase inhibitors.

40 . The compound of claim 39 , wherein said optionally substituted aliphatic group comprises 1 to 30 carbons.

41 . The compound of claim 37 , wherein the compound is represented by Formula (I), Formula (II), Formula (III), Formula (IV), or Formula (V):

wherein the —(CH 2 ) n — of Formula (I), Formula (II), Formula (III), Formula (IV), or Formula (V) is optionally substituted with at least one heteroatom; and

n is an integer from 1 to 24.

42 . The compound of claim 41 , wherein n is an integer from 6 to 14.

43 . The compound of claim 37 , wherein the compound is

44 . A compound, or a pharmaceutically acceptable salt thereof, comprising an integrase inhibitor conjugated to an amino acid fatty ester, wherein the amino acid fatty ester comprises an aliphatic group.

45 . The compound of claim 44 , wherein said integrase inhibitor is selected from the group consisting of cabotegravir (CAB), raltegravir (RAL), elvitegravir (EVG), dolutegravir (DTG), bictegravir (BIC), BI 224436, and MK-2048.

46 . The compound of claim 44 , wherein the compound is represented by Formula (VI), Formula (VII), Formula (VIII), Formula (IX), or Formula (X):

wherein:

R is an optionally substituted aliphatic group; and

AA is one or more amino acids.

47 . The compound of claim 46 , wherein AA is one amino acid.

48 . The compound of claim 46 , wherein AA is selected from the group consisting of alanine, valine, phenylalanine, proline, tyrosine, and lysine.

49 . The compound of claim 46 , wherein R is a saturated linear aliphatic chain of a length of 11 to 19 carbons.

50 . The compound of claim 44 , wherein said compound is

51 . A nanoparticle, comprising a compound or a pharmaceutically acceptable salt thereof of claim 37 , and at least one polymer or surfactant.

52 . The nanoparticle of claim 51 , wherein said polymer or surfactant is an amphiphilic block copolymer.

53 . The nanoparticle of claim 52 , wherein said amphiphilic block copolymer comprises at least one block of poly(oxyethylene) and at least one block of poly(oxypropylene).

54 . The nanoparticle of claim 51 , wherein the polymer or surfactant is P407.

55 . A pharmaceutical composition, comprising a compound or a pharmaceutically acceptable salt thereof of claim 37 , and at least one pharmaceutically acceptable carrier.

56 . A method of treating a viral infection in a subject in need thereof, comprising administering a therapeutically effective amount of a pharmaceutical composition of claim 55 to the subject.

57 . The method of claim 56 , wherein the viral infection is an HIV infection.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 7, 2021
From: GENDELMAN, HOWARD; EDAGWA, BENSON
To: BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
Reel/Frame 058323/0611 →