C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 215/18 (2006.01) A61K 31/47 (2006.01) C07D 215/04 (2006.01) C07D 215/12 (2006.01) C07D 215/14 (2006.01) C07D 215/22 (2006.01) C07D 215/227 (2006.01) C07D 215/36 (2006.01) C07D 215/38 (2006.01) C07D 215/48 (2006.01) C07D 215/50 (2006.01) C07D 215/54 (2006.01) C07D 221/10 (2006.01) C07D 221/12 (2006.01) C07D 221/16 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 405/04 (2006.01) C07D 405/06 (2006.01) C07D 405/12 (2006.01) C07D 409/04 (2006.01) C07D 409/06 (2006.01) C07D 4
Patent
CA 2421782
The present invention concerns compounds of formula. In a preferable embodiment, X represents O; R1 represents C1-6alkyl; cycloC3-12alkyl or (cycloC3-12alkyl)C1-6alkyl, wherein one or more hydrogen atoms in a C1-6alkyl- moiety or in a cycloC3-12alkyl-moiety optionally may be replaced by C1- 6alkyloxy, aryl, halo or thienyl; R2 represents hydrogen; halo; C1-6alkyl or amino; R3 and R4 each independently represent hydrogen or C1-6alkyl; or R2 and R3 may be taken together to form -R2-R3-, which represents a bivalent radical of formula -Z4-CH2-CH2-CH2- or -Z4-CH2-CH2- with Z4 being O or NR11 wherein R11 is C1-6alkyl; and wherein each bivalent radical is optionally substituted with C1-6alkyl; or R3 and R4 may be taken together to form a bivalent radical of formula -CH2-CH2-CH2-CH2- ; R5 represents hydrogen; Y represents O; and aryl represents phenyl optionally substituted with halo. The invention also relates to the use of a compound according to the invention as a medicament and in the manufacture of a medicament for treating or preventing glutamate- induced diseases of the central nervous system, as well as formulations comprising such a compound and processes for preparing such a compound.
L'invention porte sur des composés de formules (I-A) et (I-B). Dans l'une variantes préférables, X représente O; R?1¿ représente C¿1-6? alkyle; cyclo C¿3-12? alkyle ou (cyclo C¿3-12 ?alkyle) C¿1-6 ?alkyle, où un ou plusieurs atomes d'hydrogène du fragment C¿1-6 ?alkyle ou cyclo C¿3-12 ?alkyle peuvent facultativement être remplacés par C¿1-6? alkyloxy, aryle, halo ou thiényle; R?2¿ représente hydrogène; halo; C¿1-6? alkyle ou amino; R?3¿ et R?4¿ représentent chacun indépendamment hydrogène ou C¿1-6? alkyle; ou R?2¿ et R?3¿ peuvent être pris ensemble pour former -R?2¿-R?3¿-, qui représente un radical bivalent de formule -Z¿4?-CH¿2?-CH¿2?-CH¿2?- ou -Z¿4?-CH¿2?-CH¿2?- où Z¿4? est O ou NR?11¿ ou R?11¿ est C¿1-6? alkyle; et où chaque radical bivalent est facultativement substitué par C¿1-6? alkyle; ou R?3¿ et R?4¿ peuvent être pris ensemble pour former un radical bivalent de formula -CH¿2?-CH¿2?-CH¿2?-CH¿2?-; R?5¿ représente hydrogène; Y représente O; et aryle représente phényle facultativement substitué par halo. L'invention porte également sur l'utilisation d'un tel composé comme médicament, et sur la fabrication d'un médicament traitant ou prévenant les maladies du SNC induites par le glutamate, ainsi que sur des préparations comprenant un tel composé, et sur les procédés de préparation de ce composé.
Coupa Sophie
Lesage Anne Simone Josephine
Mabire Dominique Jean-Pierre
Poncelet Alain Philippe
Venet Marc Gaston
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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