Oligomer-anticholinergic agent conjugates
View Patent ↗The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different as compared to the characteristics of the small molecule drug not attached to the water-soluble oligomer.
1. A compound having the following structure:
wherein:
R 1 is selected from the group consisting of cyclopentyl, 1-hydroxyl cyclopentyl, cyclohexyl and phenyl;
R 3 is selected from the group consisting of cyclopentyl, 1-hydroxyl cyclopentyl, cyclohexyl and phenyl;
L 2 is —CH 2 —C≡C—CH 2 —;
R 4 is selected from the group consisting of —CH 3 and —CH 2 CH 3 ;
R 5 is selected from the group consisting of —CH 3 and —CH 2 CH 3 ;
X is —O—; and
POLY is a poly(alkylene oxide), and charged species of the compound.
2. The compound of claim 1 , wherein R 1 is cyclohexyl and R 3 is phenyl.
3. The compound of claim 1 , wherein the poly(alkylene oxide) is a poly(ethylene oxide).
4. The compound of claim 1 , wherein the poly(alkylene oxide) has between 1 and 30 monomers.
5. The compound of claim 4 , wherein the poly(alkylene oxide) has between 1 and 10 monomers.
6. The compound of claim 1 , wherein the poly(alkylene oxide) includes an alkoxy or hydroxy end-capping moiety.
7. A composition comprising a compound of claim 1 , and optionally, a pharmaceutically acceptable excipient.
8. A composition of matter comprising a compound of claim 1 , wherein the compound is present in a dosage form.