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US 2016/0002229 A1Published application
Tricyclic lactam derivatives as 11-beta hydroxysteroid dehydrogenase inhibitors
AssigneeJanssen Pharmaceutica NV
InventorsLibuse Jaroskova, Joannes Theodorus Maria Linders, Loius Jozef Elisabeth Van Der Veken, Gustaaf Henri Maria Villemsens
Life of this patent
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Abstract
Compounds of the formula (I) useful as 11-Beta Hydroxysteroid Dehydrogenase Inhibitors
Claims19
A compound having the formula
- the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein
- X represents C;
- Y represents N;
- L represents a methyl or a direct bond;
- Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b);
- Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b);
- R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, —O—(C═O)—C1-4alkyl, hydroxycarbonyl, NR3R4 or C1-4alkyl wherein said C1-4alkyl or —O—(C═O)—C1-4alkyl are optionally substituted with one or more substituents selected from halo, hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or
- R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from halo, hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8;
- R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-;
- R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-;
- R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-;
- R7 and R8 each independently represent hydrogen, C1-4alkyl or
- C1-4alkylcarbonyl-;
- A represents phenyl.
11 more elements
(canceled)
A compound of formula
- the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein
- X represents C;
- Y represents N;
- L represents a methyl or a direct bond;
- Z1 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b);
- Z2 represents a direct bond, C1-2alkyl- or a divalent radical of formula —CH2—CH═ (a) or —CH═ (b);
- R1 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, —O—(C═O)—C1-4alkyl, hydroxycarbonyl, NR3R4 or C1-4alkyl wherein said C1-4alkyl or —O—(C═O)—C1-4alkyl are optionally substituted with one or more substituents selected from halo, hydroxycarbonyl, phenyl, C1-4alkyloxy or NR5R6 or
- R1 represents C1-4alkyloxy- optionally substituted with one or more substituents selected from halo, hydroxycarbonyl, phenyl, C1-4alkyloxy or NR7R8;
- R2 represents hydrogen, halo, C1-4alkyl or C1-4alkyloxy-;
- R3 and R4 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-;
- R5 and R6 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-;
- R7 and R8 each independently represent hydrogen, C1-4alkyl or C1-4alkylcarbonyl-;
- A represents phenyl or a monocyclic heterocycle selected from the group consisting of thiophenyl, furanyl, oxazolyl, thiazolyl, imidazolyl, isoxazolyl, isothiazolyl, pyrridinyl, pyridazinyl, pyrimidinyl and piperazinyl.
10 more elements
Dependencies are inferred from the claim text.