Tricyclic heterocyclic derivatives
AssigneeMerck Sharp & Dohme Corp.
InventorsKeneth Davies, Takao Kiyoi, Ashvinkumar Dhirubhai Mistry, Peter Christopher Ray, Mark Reid, Grant Wishart
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Abstract
The present invention relates to a tricyclic heterocyclic derivative according to Formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.
Claims17
1-15. (canceled)
A tricyclic heterocyclic derivative according to Formula I
- wherein
- m is 1 or 2;
- n is 0 or 1;
- R1 is H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-2alkyl, C1-2alkyloxyC1-2alkyl or C6-10arylC1-2alkyl, said C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-2alkyl, C1-2alkyloxyC1-2alkyl and C6-10arylC1-2alkyl each being optionally substituted with one or more halogens;
- R2 is H, C1-4alkyl, C3-5cycloalkyl or C3-5cycloalkylC1-2alkyl said C1-4alkyl, C3-5cycloalkyl and C3-5cycloalkylC1-2alkyl each being optionally substituted with one or more halogens;
- R3 is C1-4alkyl, hydroxyC1-2alkyl or C1-2alkyloxyC1-2alkyl said C1-4alkyl and C1-2alkyloxyC1-2alkyl each being optionally substituted with one or more halogens;
- L1 is C═O or CR4R5;
- L2 is CR4′R5′
- R4, R4′, R5 and R5′ are each independently H, F, C1-4alkyl, C2-4alkenyl, C2-4alkynyl, hydroxy, C1-4alkyloxy, C1-2alkyloxyC1-2alkyl, C3-5cycloalkyl or C3-5cycloalkylC1-2alkyl said C1-4alkyl, C3-5cycloalkyl and C3-5cycloalkylC1-2alkyl each being optionally substituted with one or more halogens or
- one of R4 and R4′ together with one of R5 and R5′ along with the atoms to which they are bonded form a 3-6 membered ring optionally comprising a heteroatom selected from O, S and NR4″, wherein R4″ is H, C1-4alkyl, COC1-4alkyl or SO2C1-4alkyl.
- Y1 is N or CR6;
- Y2 is N or CR7;
- Y3 is N or CR8;
- Y4 is N or CR9 with the proviso that no more than two of Y1-Y4 can be N simultaneously;
- R6, R7 and R8 are each independently selected from H, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C3-7cycloalkylC1-2alkyl, C1-6alkyloxy, SC1-6alkyl, SOC1-6alkyl, SO2C1-6alkyl, NR10R11, CO2R12, C6-10aryl, C6-10arylC1-2alkyloxy, CN, halogen and a 5-6 membered heteroaryl ring system comprising 1-2 heteroatoms independently selected from N, O and S, wherein said C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-2alkyl and C1-6alkyloxy are each optionally substituted with one or more halogens and wherein said C6-10aryl, 5-6 membered heteroaryl ring system comprising 1-2 heteroatoms independently selected from N, O and S and C6-10arylC1-2alkyloxy are optionally independently substituted with one or more substitutents independently selected from methyl and halogen or;
- R6 and R7 or R7 and R8 together with the atoms to which they are bonded form a 5-7
- membered unsaturated ring optionally comprising 1-2 heteroatoms selected from NR6′,
- O and S and optionally substituted with methyl or halogen, wherein R6′ is H or C1-4alkyl;
- R9 is H, C1-6alkyl, C3-7cycloalkyl, C1-6alkyloxy, CN or halogen said C1-6alkyl, C3-7cycloalkyl and C1-6alkyloxy each being optionally substituted with one or more halogens with the proviso that R6-R9 cannot simultaneously be H;
- R10 and R11 are each independently H or C1-6alkyl and
- R12 is C1-6alkyl;
- or a pharmaceutically acceptable salt thereof.
A tricyclic heterocyclic derivative selected from:
- or a pharmaceutically acceptable salt.
Dependencies are inferred from the claim text.