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US 8,507,521 B2Granted
Heterocyclic derivatives
AssigneeMerck Sharp & Dohme Corp.
InventorsJulia Adam, Jonathan Gillespie, Steven Laats, John Kinnaird Ferguson MacLean, Duncan Robert McArthur
Life of this patent
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Abstract
The present invention relates to a heterocyclic derivative of formula (I) wherein the variables are as defined in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention further relates to pharmaceutical compositions comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of disorders mediated by glutamate dysfunction, such as schizophrenia and generalised anxiety disorder.
Claims12
A heterocyclic derivative of formula I
- wherein
- R1 is C1-4alkyl, C0-4alkylC3-8cycloalkyl, or C0-4alkylZ1, said C1-4alkyl and C0-4alkylC3-8cycloalkyl being optionally substituted with one or more substituent independently selected from hydroxy, C1-4alkyl, C1-4alkyloxy, CN and halogen;
- Z1 is a 4-7 membered saturated ring containing a heteroatom selected from O, S and SO2;
- n is 1 or 2;
- each R2 and R3 is independently H or C1-4alkyl;
- Y is O or NR8;
- R4, R5, R6 and R7 are independently H or C1-4alkyl;
- or
- when Y is NR8, either R4 and R5, or R6 and R7, may together represent oxo;
- R8 is C1-4alkyl, C0-4alkylC3-8cycloalkyl, or C0-4alkylZ2, said C1-4alkyl and C0-4alkylC3-8cycloalkyl being optionally substituted with one or more substituent independently selected from hydroxy, C1-4alkyl, C1-4alkyloxy, oxo, CN and halogen;
- Z2 is a 4-7 membered saturated ring containing a heteroatom selected from O, S and SO2;
- X1-X7 are CR9;
- or one of X1 -X7 may be N;
- each R9 is independently selected from H, C1-4alkyl, C1-4alkyloxy, nitrile and halogen, said C1-4alkyl and C1-4alkyloxy being optionally substituted with one or more substituent independently selected from hydroxy and halogen;
- R10 and R11 are independently H or C1-4alkyl;
- or, when R10 is alkyl and X1 is CR9, R10 and R9 together with the atoms to which they are bonded may form a fused ring optionally comprising a heteroatomic moiety selected from O, S and SO2;
- or a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.