| US 7,501,414 B2 | ||
| Substituted morpholine and thiomorpholine derivatives | ||
| Christian Wenzel Tornøe, Copenhagen (Denmark); Mario Rottländer, Greve (Denmark); Nikolay Khanzhin, Frederiksberg (Denmark); Andreas Ritzèn, Vanløse (Denmark); and William Patrick Watson, Vanløse (Denmark) | ||
| Assigned to H. Lundbeck A/S, Valby-Copenhagen (Denmark) | ||
| Filed on Dec. 21, 2005, as Appl. No. 11/314,802. | ||
| Application 11/314802 is a continuation of application No. PCT/DK2005/000159, filed on Mar. 09, 2005. | ||
| Claims priority of provisional application 60/552574, filed on Mar. 12, 2004. | ||
| Claims priority of application No. 2004 00412 (DK), filed on Mar. 12, 2004. | ||
| Prior Publication US 2006/0167248 A1, Jul. 27, 2006 | ||
| Int. Cl. C07D 279/12 (2006.01); C07D 417/02 (2006.01); C07D 265/30 (2006.01); A61K 31/5377 (2006.01) | ||
| U.S. Cl. 514—237.2 [544/124; 544/163; 544/165; 514/237.8] | 15 Claims |
1. A compound of formula I
 q is 0 or 1;
W is O;
X is CO;
Z is O;
R1 is selected from the group consisting of halogen, cyano, C1-6-alk(en/yn)yl, C3-8-cycloalk(en)yl, C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl, halo-C1-6-alk(en/yn)yl, halo-C3-8-cycloalk(en)yl, halo-C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl, C1-3-alk(en/yn)yloxy, C5-6-alk(en/yn)yloxy, C4-alkenyloxy, C4-alkynyloxy, C3-8-cycloalk(en)yloxy and C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yloxy;
R2 is selected from the group consisting of halogen, cyano, C1-6-alk(en/yn)yl, C3-8-cycloalk(en)yl, C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl, halo-C1-6-alk(en/yn)yl, halo-C3-8-cycloalk(en)yl, halo-C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl, C1-6-alk(en/yn)yloxy, C3-8-cycloalk(en)yloxy, C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yloxy, phenyl and pyridyl; wherein the phenyl and the pyridyl are optionally substituted with one or more substituents
that are independently halogen, C1-6-alk(en/yn)yl, C3-8-cycloalk(en)yl or C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl;
R3 is C1-10-alk(en/yn)yl; and
R4, R5, R6 and R7 are each independently selected from the group consisting of hydrogen and an optionally substituted aromatic
group of 5-10 carbon atoms, wherein:
1, 2, 3 or 4 carbon atoms may be replaced by a heteroatom, each heteroatom independently being N, S, or O;
the aromatic group is selected from the group consisting of phenyl, naphthyl, pyridine, thiophene, furan, thiazole, quinoline,
indole, 2,3-dihydro-benzofuran, pyrimidine, pyrrole, and oxazole; and
the optional substituent is selected from the group consisting of hydroxy, halogen, C1-6alk(en/yn)yl, C3-8-cycloalk(en)yl, C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl, halo-C1-6-alk(en/yn)yl, C1-6-alk(en/yn)yloxy, C3-8-alk(en/yn)yloxy, acyl, nitro, cyano, —CO—NH—C1-6-alk(en/yn)yl, —CO—N(C 1-6-alk(en/yn)yl)2, —NH2, —NH—C1-6-alk(en/yn)yl, —N(C1-6-alk(en/yn)yl)2, —S—C1-6-alk(en/yn)yl, —SO2—C1-6-alk(en/yn)yl, —SO2N(C1-6-alk(en/yn)yl)2 and —SO2NH—C1-6-alk(en/yn)yl; or
a pharmaceutically acceptable salt thereof.
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