Oligomer-containing benzamide-based compounds
View Patent ↗The invention relates to (among other things) oligomer-containing benzamide-based compounds. A compound of the invention exhibits one or more advantages over corresponding compounds lacking the oligomer.
1. A compound having the following structure:
wherein:
R 2 is lower alkyl;
(a) is an integer in the range of from 1 to 4 inclusive;
Y is either O or S;
R 3 is lower alkyl;
R 4 is selected from the group consisting of hydrogen, halo, lower alkoxy, amino, and lower alkylamino;
R 5 is selected from the group consisting of hydrogen, halo, lower alkoxy, amino, and lower alkylamino;
R 6 is selected from the group consisting of hydrogen, halo, lower alkoxy, amino, and lower alkylamino;
X is a stable or releasable linkage; and
POLY is a water-soluble, non-peptidic oligomer having a number of repeating monomers in the range of from 2 to 30,
and pharmaceutically acceptable salts thereof.
2. The compound of claim 1 , wherein the linkage is a stable linkage.
3. The compound of claim 1 , wherein the linkage is a degradable linkage.
4. The compound of claim 1 , wherein the linkage is selected from the group consisting of amine, urea, carbamate and ether.
5. The compound of claim 1 , wherein the weight average molecular weight of the water-soluble, non-peptidic oligomer is less than 400 Daltons.
6. The compound of claim 1 , having the following structure:
wherein n is in the range of 2 to 30, and pharmaceutically acceptable salts thereof.
7. The compound of claim 1 , wherein the water-soluble, non-peptidic oligomer is a poly(alkylene oxide).
8. The compound of claim 7 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).
9. The compound of claim 1 , wherein the water-soluble, non-peptidic oligomer has a number of repeating monomers in the range of from 2 to 10.
10. The compound of claim 7 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxyl end-capping moiety.
11. A composition comprising a compound of claim 1 , and (ii) optionally, a pharmaceutically acceptable excipient.
12. A composition of matter comprising a compound of claim 1 , wherein the compound is present in a dosage form.