Substituted pyrimidine derivatives, their preparation and...

Details Substituted pyrimidine derivatives, their preparation and... Substituted pyrimidine derivatives, their preparation and...

C - Chemistry, Metallurgy

07

D

C07D 239/48 (2006.01) A61K 31/505 (2006.01) C07D 239/42 (2006.01) C07D 239/46 (2006.01) C07D 239/52 (2006.01) C07D 401/04 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 401/14 (2006.01)

Patent

CA 2305255

The present invention relates to novel derivatives of a series of substituted pyrimidines of formula (I); wherein W is O, CH2, CH2CH2, OCH2, CH2CH2CH2, or a bond; R1 is a hydroxyC1-6alkyloxyC1-6alkylamino, diC1-6alkylamino (wherein the alkyl groups may be the same or different), aminoC1-6alkylamino, morpholino, piperidino, piperazino, piperazinoamino, homopiperazino, homopiperidino, homomorpholino, benzoxazino, indolino, 1,2,3,4-tetrahydroquinolino, benzylamino or anilino wherein C or N atoms may be substituted with one or more substituents; R2 is selected from the group consisting of H; halogen; N3; OR; SR; C1-6alkyl; C6-10aryl; C6-10arylC1-6alkyl; C6-10heteroaryl; NR7R8; N=C(R11)N(R6)2; aziridino; azetidino; pyrrolidino; piperidino; hydroxypiperidino; heptamethyleneimino; piperazino; N-substituted piperazino; homopiperazino; N-substituted homopiperazino; morpholino; homomorpholine; thiomorpholino; and R12C(O)C1-6alkyl; C-substituted piperidino; X is a C6- 10aryl ring or a C6-10 heteroaryl ring optionally substituted with one or more suitable substituents for an aryl ring; R is H, C1-6alkyl, C3-8cycloalkyl, C6- 10aryl or C6-10arylC1-6alkyl; provided that when -W-X is benzyl, R1 is not piperidine; and when R1 is a hydroxyalkyloxyalkylamino, R2 is not a heterocyclic ring; and to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.

L'invention concerne de nouveaux dérivés d'une série de pyrimidines substituées, de formule (I), dans laquelle W est O, CH¿2?, CH¿2?CH¿2?, OCH¿2?, CH¿2?CH¿2?CH¿2? ou une liaison; R?1¿ est hydroxyalkyl C¿1?-C¿6? alkyl C¿1?-C¿6? amino, dialkyl C¿1?-C¿6? amino (où les groupes alkyles peuvent être identiques ou différents), aminoalkyl C¿1?-C¿6? amino, morpholino, pipéridino, pipérazino, pipérazinoamino, homopipérazino, homopipéridino, homomorpholino, benzoazino, indolino, 1,2,3,4-tétrahydroquinolino, benzylamino ou anilino, où les atomes de C et de N peuvent être substitués par un ou plusieurs substituants; R?2¿ est choisi dans le groupe comprenant H, halogène, N¿3?, OR, SR, alkyle C¿1?-C¿6?, aryle C¿6?-C¿10?, aryle C¿6?-C¿10?, alkyle C¿1?-C¿6?, hétéroaryle C¿6?-C¿10?, NR?7¿R?8¿, N=C(R?11¿)N(R?6¿)¿2?, azidino, azétidino, pyrrolidino, pipéridino, hydroxypipéridino, heptaméthylèneimino, pipérazino, pipérazino N-substitué, homopipérazino, homopipérazino N-substitué, morpholino, homomorpholino, thiomorpholino, et R?12¿C(O) alkyle C¿1?-C¿6? ou pipéridino C-substitué; X est un noyau aryle C¿6?-C¿10? ou un noyau hétéroaryle C¿6?-C¿10? portant éventuellement un ou plusieurs substituants pour un noyau aryle; R est H, alkyle C¿1?-C¿6?, cycloalkyle C¿3?-C¿8?, aryle C¿6?-C¿10? ou aryle C¿6?-C¿10? alkyle C¿1?-C¿6?, à condition que quand W-X est benzyle, R?1¿ ne soit pas pipéridine, et que quand R?1¿ est hydroxyalkyloxyalkyamino, R?2¿ ne soit pas un noyau hétérocyclique. L'invention concerne également des compositions pharmaceutiques contenant ces dérivés et des procédés permettant de les préparer, ainsi que leur utilisation thérapeutique, notamment pour le traitement des troubles neurodégénératifs et d'autres troubles neurologiques du système nerveux central et du système nerveux périphérique.

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