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US 2014/0235576 A1Published application
Pyrrolidine-2-carboxylic acid derivatives as iglur antagonists
AssigneeKobenhavns Universitet
InventorLennart BUCH
Life of this patent
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Abstract
The present invention relates to compounds of Formula (I), combinations and use thereof for disease therapy, or pharmaceutically acceptable salt or solvate thereof, including all tautomers, stereoismers and polymorphs thereof, which are iGluR receptor inhibitors, and hence are useful in the treatment of psychiatric diseases or neurological disorders or a disease or disorder associated with abnormal activities of iGluR receptors.
Claims19
A compound of Formula (I)
- and pharmaceutically acceptable derivatives, as well as all tautomers and stereoisomers of compound of Formula (I), wherein
- represents compounds of Formula (Ia) or (Ib);
- ---- in each case may represent if appropriate the presence of at least one double bond between T2 and Z2, or between Z2 and Z1, or between Z1 and T1, or between T1 and Z4, or between Z4 and (Z3 or T2), or between Z3 and T2;
- or
- T1 is C, CH,
- T2 is C, CH,
- Z1 is CR2, C(R2)2, N, S, O, or NR3,
- Z2 is CR2, C(R2)2, N, S, O, or NR3,
- Z3 is CR2, C(R2)2, N, S, O, or NR3,
- Z4 is CR2, C(R2)2, N, S, O, or NR3,
- wherein the residues Z1, Z2, Z3 and Z4 can not represent adjacent O or S;
- R1 may together with Z1 or Z4, or
- Z2 may together with Z1, or
- Z3 may together with Z4,
- form a saturated or unsaturated C5- or C6-cycloalkyl, or a saturated or unsaturated heterocyclyl containing 5 or 6 ring atoms, wherein the saturated or unsaturated C5- or C6-cycloalkyl, or the saturated or unsaturated heterocyclyl containing 5 or 6 ring atoms, may be substituted with one or more substituents selected from the group comprising OR4 or R4,
- R1 is H, OR4, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, COOR4, N(OH)H, or NHR4,
- R2 is independently selected among R4, O, OR4, halogen, N(OH)H, N(OH)R4, NHR4, COR4, CONHR4, or SO2NHR4,
- R3 is independently selected among R4, O, OR4, or halogen,
- R4 is independently selected among H, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl, C1-C6-alkylphenyl, or saturated or unsaturated C5- or C6-cycloalkyl, or saturated or unsaturated C1-C6-alkyl C5- or C6-heterocyclyl, wherein C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, phenyl, C1-C6-alkylphenyl, or saturated or unsaturated C5- or C6-cycloalkyl, or saturated or unsaturated C1-C6-alkyl C5- or C6-heterocyclyl may be substituted with one or more substituents selected from the group comprising C1-C6-alkyl, C1-C6-alkoxy, aryl, halogen, and amine,
- halogen represents Cl, Br, or I, and
- with the proviso that Z1, Z2, Z3 and Z4 are not all CH, and T1 and T2 are not both C, when R1 is OH.
18 more elements
Dependencies are inferred from the claim text.