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US 2010/0076016 A1Published application
Isoquinolinone derivatives as nk3 antagonists
AssigneeH. Lundbeck A/S
InventorsNikolay Khanzhin, Karsten Juhl, Soren Moller Nielsen, Klaus Baek Simonsen
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Abstract
The invention relates to compounds useful in therapy, in particular in the treatment of psychosis, to compositions comprising said compounds, and to methods of treating diseases comprising the administration of said compounds.
Claims39
A compound according to formula I
- wherein A represents N, CH or CR1;
- each R1 independently represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, —C(O)—C1-6alkyl, —C(O)—C2-6alkenyl, —C(O)—C2-6alkynyl, —C(O)—O—C1-6alkyl, —C(O)—O—C2-6alkenyl, —C(O)—O—C2-6alkynyl or phenyl, wherein said phenyl, C1-6alkyl, C2-6alkenyl or C2-6alkynyl is optionally substituted with one or more substituents selected from halogen, hydroxyl, haloC1-6alkyl, nitro, C1-6alkoxy, and NR2R3;
- X represents hydrogen, C1-6alkyl optionally substituted with F, or —CRaRb—X′, wherein X′ represents a monocyclic saturated moiety having 5-6 ring atoms one of which is N and wherein one or two additional ring atom may be a hetero atom selected from N, O and S, which monocyclic ring may be substituted with one or more substituent W, wherein W is selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C1-6haloalkyl or (═O);
- Ra and Rb) each individually represent hydrogen, —CH3 or halogen;
- Q represents a bond, —CH2—, —NH—, or —O—;
- Y represents C1-6alkyl, C2-6alkenyl or C2-6alkynyl, wherein said alkyl, alkenyl or alkynyl may be substituted with one or more substituents P, wherein P is selected from halogen, hydroxy, C1-6alkoxy, cyano, —S—C1-6alkyl, and a monocyclic saturated moiety having 5-6 ring atoms one ring atom of which may be N and the rest is C;
- or Y may represent a monocyclic saturated moiety having 4-6 ring atoms, wherein one of said ring atoms may be selected from N and O, the rest being C, and which monocyclic saturated moiety may be substituted with one or more substituents Z, wherein Z is selected from C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C(O)H, —C(O)—C1-6alkyl, halogen, C1-6alkoxy, C1-6hydroxyalkyl and hydroxy;
- wherein each of R2 and R3 independently represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, hydroxyC1-6alkyl, or haloC1-6alkyl;
- each of R4-R8 and R9-R12 independently represents hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, halogen, NR2R3, hydroxy, cyano, nitro, C1-6alkoxy, haloC1-6alkyl or hydroxyC1-6alkyl;
- provided said compound is different from 2-methyl-1-oxo-1,2-dihydro-isoquinoline-4-carboxylic acid (1-phenyl-ethyl)-amide;
- and pharmaceutically acceptable salts thereof.
8 more elements
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Dependencies are inferred from the claim text.