| US 7,541,358 B2 | ||
| 1-aryl-or 1-alkylsulfonylbenzazole derivatives as 5-hydroxytryptamine-6 ligands | ||
| Ping Zhou, Plainsboro, N.J. (US); and Michael Gerard Kelly, Thousand Oaks, Calif. (US) | ||
| Assigned to Wyeth, Madison, N.J. (US) | ||
| Filed on Aug. 14, 2007, as Appl. No. 11/891,961. | ||
| Application 11/891961 is a division of application No. 10/888810, filed on Jul. 09, 2004, granted, now 7,271,180. | ||
| Application 10/695490 is a division of application No. 10/314726, filed on Dec. 09, 2002, granted, now 6,710,069. | ||
| Application 10/314726 is a division of application No. 10/055365, filed on Jan. 22, 2002, granted, now 6,509,357. | ||
| Application 10/888810 is a continuation in part of application No. 10/695490, filed on Oct. 28, 2003, abandoned. | ||
| Claims priority of provisional application 60/263425, filed on Jan. 23, 2001. | ||
| Prior Publication US 2008/0027055 A1, Jan. 31, 2008 | ||
| Int. Cl. A61K 31/5355 (2006.01); A61K 31/404 (2006.01); A61P 25/16 (2006.01); C07D 209/04 (2006.01); C07D 231/56 (2006.01); C07D 401/12 (2006.01) | ||
| U.S. Cl. 514—235.2 [514/322; 514/323; 514/406; 514/414; 514/415; 544/144; 546/201; 548/362.5; 548/465; 548/469; 548/503] | 20 Claims |
1. A compound of formula I
 W is SO2, CO, CONH, CSNH or CH2;
X is CR7 or N;
Y is CR8 ;
Z is O, SOp or NR9;
R1 and R2 are each independently H or C1-C6alkyl;
n is an integer of 2, 3 or 4;
R3 and R4 are taken together with the atom to which they are attached to form an optionally substituted 3- to 6-membered ring optionally
containing an additional heteroatom selected from O, N or S;
R5 is H, halogen, CN, OR13, CO2R14, CONR15R16, CNR17NR18R19, SO2NR20R21, SOqR22 or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, phenyl or heteroaryl group each optionally substituted;
m is an integer of 1, 2 or 3;
p and q are each independently 0 or an integer of 1 or 2;
R6 is an optionally substituted heteroaryl group or an optionally substituted 8- to 13-membered bicyclic or tricyclic ring system
having a N atom at the bridgehead and optionally containing 1, 2 or 3 additional heteroatoms selected from N, O or S;
R7 and R8 are each independently H, halogen or a C1-C6 alkyl, aryl, heteroaryl or C1- C6alkoxy group each optionally substituted;
R9 is H or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, cycloheteroalkyl, aryl or heteroaryl group each optionally substituted;
R15, R16, R17, R18 and R19 are each independently H or C1-C4alkyl;
R13 is H, COR23 or a C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, aryl or heteroaryl group each optionally substituted;
R14 is H or a C1-C6alkyl, aryl or heteroaryl group each optionally substituted;
R20 and R21 are each independently H or a C1-C6alkyl, aryl or heteroaryl group each optionally substituted; and
R22 and R23 are each independently an optionally substituted C1-C6alkyl, aryl or heteroaryl group; or
a pharmaceutically acceptable salt thereof.
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