US 7,320,989 B2
Pyridine, pyrimidine, quinoline, quinazoline, and naphthalene urotensin-II receptor antagonists
Eric Anderson, Houston, Tex. (US); Brian Dupre, Houston, Tex. (US); Daxin Gao, Houston, Tex. (US); Raymond J. Kessler, Houston, Tex. (US); Wen Li, Santa Clara, Calif. (US); and Chengde Wu, Pearland, Tex. (US)
Assigned to Encysive Pharmaceuticals, Inc., Houston, Tex. (US)
Filed on Aug. 23, 2004, as Appl. No. 10/924,181.
Application 10/924181 is a continuation in part of application No. 10/783916, filed on Feb. 20, 2004.
Claims priority of provisional application 60/451089, filed on Feb. 28, 2003.
Prior Publication US 2005/0054850 A1, Mar. 10, 2005
This patent is subject to a terminal disclaimer.
Int. Cl. A61K 31/44 (2006.01); C07D 215/38 (2006.01); C07D 211/72 (2006.01)
U.S. Cl. 514—313  [546/159; 546/304; 514/353] 4 Claims
 
1. A compound of the formula

OG Complex Work Unit Drawing
wherein Ar is selected from the group consisting of aryl, heteroaryl, benzoheteroaryl, pyridone, pyridazinone, and pyrimidone;
R1 and R2 are independently H, alkyl, cycloalkyl, bicyclic alkyl, adamantyl, aralkyl, aryl, R7CO, or R8OCO;
R3 is H, alkyl or aralkyl;
X is C;
Y is N;
R4 is selected from the group consisting of H, alkyl, aralkyl, aryl, heteroaryl, benzoheteroaryl, hydroxyl, halo, haloalkyl, alkoxy, aminocarbonyl and aminosulfonyl;
R5 and R6 together form a 5-6 membered aromatic ring or a 5-7 membered aliphatic ring;
L1 is O;
L2 and L3 are single bond;
L4 is (Z)n where each Z is CH2; n is an integer from 1 to 6; and
R7 and R8 are independently selected from the group consisting of H, alkyl, aryl and aralkyl, or a pharmaceutically acceptable salt thereof.