NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-a]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS
AssigneeJanssen Pharmaceutica NV
InventorsFrançois Paul Bischoff, Henricus Jacobus Maria Gijsen, Frans Alfons Maria Van den Keybus, Frederik Jan Rita Rombouts
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Abstract
The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) wherein R1, R2, R3, R4, L, Y, Z and X have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said compounds as an active ingredient as well as the use of said compounds as a medicament.
Claims15
A compound of Formula (I)
- a tautomer or a stereoisomeric form thereof, wherein
- R1 is phenyl, napthyl, indolyl, benzothienyl, benzothiazolyl or benzofuranyl;
- each optionally substituted with one, two or three substituents each independently selected from the group consisting of halo and C1-4alkyl optionally substituted with one, two or three halo substituents;
- L is attached at position a or b;
- L is selected from the group consisting of a covalent bond, —C1-6alkanediyl- and —O—C1-6alkanediyl-;
- Y is -Q-(CH2)m—, —CH2-Q-CH2—, —(CH2)n—,
- —(CH2)n— wherein one —CH2— is substituted with hydroxyl and C1-4alkyl, or
- —(CH2)n— wherein one —CH2— is substituted with one hydroxyl;
- n represents 1, 2 or 3;
- m represents 1 or 2;
- Q is O or NR6;
- R6 is hydrogen or C1-4alkyl;
- Z is methylene or 1,2-ethanediyl, wherein methylene or 1,2-ethanediyl is optionally substituted with one or two C1-4alkyl substituents;
- R2 is hydrogen, halo or C1-4alkyl;
- R3 is hydrogen or C1-4alkyl;
- R4 is hydrogen, halo or C1-4alkyl;
- X is CR5 or N;
- R5 is hydrogen or C1-4alkyl;
- or a pharmaceutically acceptable addition salt thereof.
(canceled)
Dependencies are inferred from the claim text.