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US 2010/0137428 A1Published application
Oxygen containing heterocycles as glycine transporter inhibiting compounds
AssigneeGlaxo Group Limited
InventorsAndrea Bozzoli, Clive Leslie Branch, Jacqueline Anne MacRitchie, Howard Robert Marshall, Roderick Alan Porter, Simone Spada
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Abstract
The present invention relates to compounds of formula (I), or salts or solvates thereof, their use in the manufacture of medicaments for treating neurological and neuropsychiatric disorders, in particular psychoses, dementia or attention deficit disorder. The invention further comprises processes to make these compounds and pharmaceutical formulations thereof. wherein R1 is a group selected from:
Claims13
A compound of formula (I) or a salt or solvate thereof:
- wherein:
- R1 is a group selected from:
- and wherein
- Each Z is independently selected from hydrogen, halogen, C3-7cycloalkyl, C1-4alkyl, haloC1-4alkyl, C1-4alkoxyC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkylthio, haloC1-4alkylthio, C3-7cycloalkylC1-4alkoxy, C1-4alkylsulphoxy, C1-4 alkylsulphonyl, and cyano;
- and each Z′ is independently selected from hydrogen, fluoro or C1-4alkyl;
- R2 is selected from the group consisting of halogen, cyano, C1-4alkoxy, C1-4alkyl, Alkyl, haloC1-4alkoxy, C3-7cycloalkyl, C(O)NR9R10, (where each of R9 and R10 is independently hydrogen or C1-4alkyl, or R9 and R10 together with the nitrogen atom to which they are attached form a 4-, 5-, 6- or 7-membered saturated carbocyclic ring, the 4-, 5-, 6- or 7-membered saturated ring optionally further comprising an additional heteroatom group selected from O, N and S(O)m (where m is 0, 1, or 2)), C3-7cycloalkylC1-4alkoxy, C1-4alkylthio, and haloC1-4alkylthio;
- n is 0, 1 or 2.
- R3 and R4 are independently selected from hydrogen, C1-4alkyl, optionally substituted with one or more groups Y;
- or R3 and R4 together with the nitrogen atom to which they are attached form a saturated or partially unsaturated carbocyclic 4-, 5- 6- or 7-membered ring optionally substituted with a group Y′;
- Y is selected from the group consisting of C1-4alkoxy, hydroxy, haloC1-4alkoxy and C3-5cycloalkyl and C5-10 aryl;
- Y′ is selected from the group consisting of C1-4alkyl, C1-4alkoxy, halogen, hydroxy, haloC1-4alkoxy, C3-5cycloalkyl and C5-10aryl or Y′ forms a —CH2— or —CH2—CH2— bridge between two atoms on the 4-, 5- or 6-membered ring;
- R5 and R6 are independently C1-4alkyl, optionally substituted with one or more groups X;
- or R5 and R6 together with the carbon atom to which they are attached form a saturated 5- or 6-membered carbocyclic ring optionally substituted with one or more groups X′, in the case of R5 and R6 together with the carbon atom to which they are attached forming a 5-membered saturated carbocyclic ring, that ring may optionally further comprise an additional heteroatom group selected from O, N and S(O)m;
- where m=0, 1 or 2.
- X is selected from the group consisting of halogen, hydroxy, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and C5-10aryl;
- and
- X′ is selected from the group consisting of halogen, hydroxy, C1-4alkoxy, haloC1-4alkyl, haloC1-4alkoxy and C5-10aryl.
14 more elements
Dependencies are inferred from the claim text.