Oxazole derivatives as serotonin-1a receptor agonists

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 413/06 (2006.01) A61K 31/42 (2006.01) C07D 209/00 (2006.01) C07D 221/00 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2317515

This invention provides compounds of Formula (1), wherein R1 is hydrogen, alkyl of 1-6 carbon atoms, alkoxy of 1-6 carbon atoms, benzyloxy, trifluoromethyl, chloro, bromo, or fluoro; a dashed line indicates an optional bond; X is NR4, or no atom; R2 is alkyl of 1-6 carbon atoms, cycloalkyl of 3-8 carbon atoms, cycloalkylalkyl wherein the cycloalkyl moiety is 3-8 cabon atoms and the alkyl moiety is 1-6 carbon atoms, aryl of 5-12 carbon atoms, or arylalkyl of 6-12 carbon atoms; R3 is aryl of 5-12 carbon atoms, arylalkyl of 6-12 carbon atoms, or heteroaryl of 5-12 ring atoms; R4 is hydrogen or alkyl of 1-6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are useful in the treatment of psychosis (e.g. schizophrenia), anxiety, depression and related CNS disorders and other conditions such as the treatment of alcohol and drug withdrawal, sexual dysfunction and memory deficits associated with Alzheimer's disease and other dementias.

La présente invention concerne des composés de la formule (1) dans laquelle R¿1? est un hydrogène, un alkyle renfermant de 1 à 6 atomes de carbone, un benzyloxy, un trifluorométhyle, un chloro, un bromo ou un fluoro; une ligne pointillée indique une liaison facultative; X représente NR¿4? ou aucun atome; R¿2? est un alkyle renfermant de 1 à 6 atomes de carbone, un cycloalkyle renfermant de 3 à 8 atomes de carbone, un cycloalkylalkyle dans lequel le fragment cycloalkyle renferme de 3 à 8 atomes de carbone et le fragment alkyle renferme de 1 à 6 atomes de carbone, un aryle renfermant de 5 à 12 atomes de carbone, ou un arylalkyle renfermant de 6 à 12 atomes de carbone; R¿3? est un aryle renfermant de 5 à 12 atomes de carbone, ou un hétéroaryle renfermant de 5 à 12 atomes cycliques; R¿4? est un hydrogène ou un alkyle renfermant de 1 à 6 atomes de carbone; ou un sel pharmaceutiquement acceptable de ces composés, qui sont utilisés dans le traitement des psychoses (la schizophrénie, par exemple), de l'anxiété, de la dépression et des troubles du SNC associés, et dans le traitement d'autres états tels que ceux qui sont induits par le sevrage d'alcool et de drogue, les difficultés sexuelles et les déficiences de la mémoire associées à la maladie d'Alzheimer et autres démences.

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