N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides
View Patent ↗The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
1. A compound having the following structure:
wherein:
Ar is aryl, optionally substituted with halo;
R 1 is lower alkyl;
the dotted line (“ - - - ”) represents a covalent bond;
X 1 is a spacer moiety; and
POLY 1 is a poly(alkylene oxide),
and pharmaceutically acceptable salts thereof.
2. The compound of claim 1 , encompassed within the formula:
wherein:
Ar is aryl, optionally substituted with halo;
R 1 is lower alkyl;
X 1 is a spacer moiety; and
POLY 1 is a poly(alkylene oxide),
and pharmaceutically acceptable salts thereof.
3. The compound of claim 1 , encompassed within the formula:
wherein:
Ar is aryl, optionally substituted with halo;
R 1 is lower alkyl;
X 1 is a spacer moiety; and
POLY 1 is a poly(alkylene oxide),
and pharmaceutically acceptable salts thereof.
4. The compound of claim 1 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).
5. The compound of any one of claims 1 - 3 and 4 , wherein the poly(alkylene oxide) has from about 2 to about 30 monomers.
6. The compound of claim 5 , wherein the poly(alkylene oxide) has from about 2 to about 10 monomers.
7. The compound of claim 1 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.
8. A compound selected from the group consisting of (2R) N-benzyl-2-carboxy mPEG 1 amino-3-methoxy propionamide, (2R)N-benzyl-2-carboxy mPEG 2 amino-3-methoxy propionamide, (2R)N-benzyl-2-carboxy mPEG 3 amino-3-methoxy propionamide, (2R)N-benzyl-2-carboxy mPEG 4 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 5 amino-3-methoxy propionamide, (2R)N-benzyl-2-carboxy mPEG 6 amino-3-methoxy propionamide, (2R)N-benzyl-2-carboxy mPEG 7 amino-3-methoxy propionamide, (2R)N-benzyl-2-carboxy mPEG 8 amino-3-methoxy propionamide, (2R) N-benzyl-2-carboxy mPEG 9 amino-3-methoxy propionamide, and pharmaceutically acceptable salts of each of the foregoing.
9. A composition of matter comprising a compound encompassed within claim 8 or 1 , wherein the compound is present in a dosage form.
10. A composition comprising a compound encompassed within claim 8 or 1 , and optionally, a pharmaceutically acceptable excipient.