| US 7,585,996 B2 | ||
| Acyloxyalkyl carbamate prodrugs, methods of synthesis and use | ||
| Mark A. Gallop, Los Altos, Calif. (US); Feng Xu, Palo Alto, Calif. (US); Thu Phan, Fremont, Calif. (US); Usha Dilip, Sunnyvale, Calif. (US); and Ge Peng, Mountain View, Calif. (US) | ||
| Assigned to XenoPort, Inc., Santa Clara, Calif. (US) | ||
| Filed on Sep. 13, 2007, as Appl. No. 11/901,194. | ||
| Claims priority of provisional application 60/844640, filed on Sep. 15, 2006. | ||
| Prior Publication US 2008/0146526 A1, Jun. 19, 2008 | ||
| Int. Cl. C07C 271/06 (2006.01); A61K 31/662 (2006.01) | ||
| U.S. Cl. 560—115 [514/119] | 27 Claims |
1. A compound of Formula (I):
 a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable solvate of any of the foregoing, wherein:
R1 is chosen from acyl, substituted acyl, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl,
cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, substituted cycloheteroalkyl, heteroalkyl, substituted heteroalkyl,
heteroaryl, substituted heteroaryl, heteroarylalkyl, and substituted heteroarylalkyl;
R2 and R3 is chosen from hydrogen, alkyl, substituted alkyl, alkoxycarbonyl, substituted alkoxycarbonyl, aryl, substituted aryl, arylalkyl,
substituted arylalkyl, cycloalkyl, substituted cycloalkyl, heteroaryl, substituted heteroaryl, heteroarylalkyl, and substituted
heteroarylalkyl; or R2 and R3 together with the carbon atom to which they are bonded form a cycloalkyl, substituted cycloalkyl, cycloheteroalkyl, or substituted
cycloheteroalkyl ring;
R4 is chosen from benzyl, substituted benzyl, C4-7 cycloalkyl, C3-7 cycloalkylmethyl, and dialkoxymethyl;
R5 is chosen from hydrogen, hydroxy, mercapto, fluoro, oxo, C1-4 alkyl, substituted C1-4 alkyl, aryl, substituted aryl, C3-6 cycloalkyl, substituted C3-6 cycloalkyl, heteroaryl, substituted heteroaryl, C7-9 phenylalkyl, and substituted C7-9 phenylalkyl;
R6 and R7 is chosen from hydrogen, C1-6 alkyl, C1-6 alkoxy, aryl, substituted aryl, C3-6 cycloalkyl, heteroaryl, substituted heteroaryl, C7-9 phenylalkyl, and substituted C7-9 phenylalkyl; and
R8 is chosen from hydrogen, C1-6 alkyl, substituted C1-6 alkyl, aryl, substituted aryl, C3-6 cycloalkyl, substituted C3-6 cycloalkyl, heteroaryl, substituted heteroaryl, C7-9 phenylalkyl, and substituted C7-9 phenylalkyl.
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