Back to results
US 9,517,279 B2Granted
2-alkoxy-11-hydroxyaporphine derivatives and uses thereof
AssigneeThe McLean Hospital Corporation
InventorsJohn L. Neumeyer, Yu-Gui Si, Anna W. Sromek
Life of this patent
Estimating the term…
Abstract
The invention features 2-alkoxy-11-hydroxyaporphine derivatives that selectively bind D2high receptors. The compounds are useful for imaging D2high receptors and for the treatment of diseases, such as Parkinson's disease, sexual dysfunction, and depressive disorders.
Claims18
A compound of formula I:
- or a pharmaceutically acceptable salt thereof,
- wherein
- X1 is 2-fluoroethyl, 3-fluoro-n-propyl, 2-iodoethyl, or 3-iodo-n-propyl;
- R1 is H, CH3, CH2CH3, or CH2CH2CH3;
- R2 is H or OY2;
- each of Y1 and Y2 is, independently, selected from H, C(O)—R3, and fatty acid acyl, and
- R3 is selected from H, C1-12 alkyl, C2-12 alkenyl, C2-12 alkynyl, C2-6 heterocyclyl, C6-12 aryl, C7-14 alkaryl, C3-10 alkheterocyclyl, and C1-7 heteroalkyl,
- wherein said compound has an in vitro affinity of between 0.5 nM and 35 nM at D2high receptors.
5 more elements
Dependencies are inferred from the claim text.