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US 2010/0305147 A1Published application
Chemically modified small molecules
AssigneeNektar Therapeutics
InventorsMichael D. Bentley, Tracey X. Viegas, Richard R. Goodin, Lin Cheng, Xuan Zhao
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Abstract
The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer obtained from a monodisperse or bimodal water-soluble oligomer composition. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a reduced biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.
Claims18
-55. (canceled)
A compound selected from the group consisting of:
- 6-CH3—(OCH2CH2)5—O-naloxol;
- 6-CH3—(OCH2CH2)6—O-naloxol;
- 6-CH3—(OCH2CH2)8—O-naloxol;
- and
- 6-CH3—(OCH2CH2)9—O-naloxol;
- or pharmaceutically acceptable salt thereof, wherein the compound is an α-6 isomer, a β-6 isomer or a mixture of α-6 and β-6 isomers.
3 more elements
Dependencies are inferred from the claim text.