	US 7,538,110 B2
	Opioid antagonists
Roland E. Dolle, King of Prussia, Pa. (US); Bertrand Le Bourdonnec, East Fallowfield, Pa. (US); and Allan James Goodman, Media, Pa. (US)
Assigned to Adolor Corporation, Exton, Pa. (US)
Filed on Oct. 25, 2006, as Appl. No. 11/552,827.
Claims priority of provisional application 60/730609, filed on Oct. 27, 2005.
Prior Publication US 2007/0105863 A1, May 10, 2007
Int. Cl. A01N 43/60 (2006.01); A61K 31/495 (2006.01); C07D 241/36 (2006.01)

U.S. Cl. 514—249 [544/349]

90 Claims

1. A compound of formula I:

wherein:

R¹is —OH, —OR^a, —CH₂OH, —C(═O)OR⁶, —C(═O)NR⁶R⁷, or —NR⁶R⁷;

R²and R³are each independently alkyl or alkenyl;

R⁴is H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, aralkyl, alkylaralkyl, or heteroarylalkyl;

R⁵is H, alkyl, cycloalkyl, cycloalkylalkyl, aryl, heteroaryl, aralkyl, alkylaralkyl, heteroarylalkyl, —C(═O)OR^8a, —S(═O)₂R^8a, —C(═O)R^8b, or —C(═O)NR^8bR^8c;

R⁶is H, alkyl, cycloalkyl, alkylcycloalkyl, or aralkyl;

R⁷is H, alkyl, aralkyl, or aryl;

R^8ais alkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, aralkyl, or aryl;

R^8band R^8care each independently H, alkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, aralkyl, or aryl; or R^8band R^8ctaken together with the nitrogen atom to which they are connected form a 4- to 8-membered heterocycloalkyl ring;

R^ais a hydroxyl protecting group; and

m and n are each 1;

or a pharmaceutically acceptable salt thereof.