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US 2010/0063036 A1Published application
Substituted morpholine and thiomorpholine derivatives
AssigneeH. Lundbeck A/S
InventorsChristian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
Life of this patent
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Abstract
The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.
Claims19
A compound of formula I
- wherein
- q is 0 or 1;
- W is S;
- 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-al k(en/yn)yl, C1-6-alk(en/yn)yloxy, 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 selected from the group consisting of C1-10-alk(en/yn)yl, C3-8-cycloalk(en)yl, C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl, aromatic-C1-6-alk(en/yn)yl, aromatic-C3-8-cycloalk(en)yl, aromatic-C3-8-cycloalk(en)yl-C1-6-alk(en/yn)yl and aromatic;
- wherein each aromatic is an optionally substituted aromatic group of 5-10 carbon atoms, wherein 0, 1, 2, 3 or 4 carbon atoms may be replaced by a heteroatom, each heteroatom independently is N, S, or 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 0, 1, 2, 3 or 4 carbon atoms may be replaced by a heteroatom, each heteroatom independently is N, S, or O;
- or
- a pharmaceutically acceptable salt thereof.
10 more elements
4-5. (canceled)
A compound selected from the group consisting of:
- 2-Cyclopentyl-N-(2,6-dimethyl-4-thiomorpholin-4-yl-phenyl)-acetamide;
- 2-Cyclopentyl-N-[2,6-dimethyl-4-(2-phenyl-thiomorpholin-4-yl)-phenyl]-acetamide;
- 2-Cyclopentyl-N-[2,6-dimethyl-4-(3-pyridin-3-yl-thiomorpholin-4-yl)-phenyl]-acetamide;
- 2-Cyclopentyl-N-{2,6-dimethyl-4-[2-(4-trifluoromethyl-phenyl)-thiomorpholin-4-yl]-phenyl}-acetamide;
- and
- N-{-4-[2-(2-Chloro-phenyl)-thiomorpholin-4-yl]-2,6-dimethyl-phenyl}-2-cyclopentyl-acetamide
3 more elements
14-20. (canceled)
Dependencies are inferred from the claim text.