Carboxamide compounds and their use as antagonists of a...

C - Chemistry – Metallurgy – 07 – D

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C07D 295/08 (2006.01) A61K 31/165 (2006.01) A61K 31/381 (2006.01) A61K 31/395 (2006.01) A61K 45/06 (2006.01) A61P 5/48 (2006.01) C07C 233/75 (2006.01) C07C 235/42 (2006.01) C07C 235/48 (2006.01) C07C 235/84 (2006.01) C07C 237/40 (2006.01) C07C 255/57 (2006.01) C07C 317/44 (2006.01) C07C 323/62 (2006.01) C07D 207/08 (2006.01) C07D 211/42 (2006.01) C07D 213/56 (2006.01) C07D 231/12 (2006.01) C07D 241/12 (2006.01) C07D 271/06 (2006.01) C07D 271/10 (2006.01) C07D 295/092 (2006.01) C07D 295/12 (2006.01) C07D 295

Patent

CA 2417638

Compounds of formula (I) in which: each A is independently hydrogen, C1-6alkyl optionally substituted by hydroxyl, C1-6alkoxy, C1-6alkenyl or C1-6acyl group or a halogen atom or hydroxyl, CN or CF3 group; R3 is hydrogen, methyl or ethyl; R4 is an optionally substituted aromatic carbocyclic or heterocyclic ring; Z is an O or S atom, or an NH or CH2 group, or a single bond, at the 3 or 4 position of R4 relative to the carbonyl group; R5 is an optionally substituted aromatic carbocyclic or heterocyclic ring, or an optionally substituted, saturated or unsaturated, carbocyclic or heterocyclic ring; and Q is (a) Where X, Y, R1 and R2 are as defined in claim 1; are antagonists of a human 11CBy receptor.

L'invention concerne des composés de formule (I), dans laquelle chaque A représente indépendamment l'hydrogène, un groupe C¿1-6 ?alkyle facultativement substitué par l'hydroxyle, un groupe C¿1-6 ?alkoxy, un groupe C¿1-6 ?alcényle ou un groupe C¿1-6 ?acyle ou un atome d'halogène ou l'hydroxyle, un groupe CF¿3? ou CN, R3 représente l'hydrogène, le méthyle ou l'éthyle, R4 est un anneau hétérocyclique ou carbocyclique aromatique substitué facultativement, Z représente un atome d'oxygène ou de soufre ou un groupe NH ou CH¿2? ou une liaison unique au niveau de la troisième ou quatrième position de R4 par rapport au groupe carbonyle, R5 est un anneau hétérocylique ou carbocyclique aromatique substitué facultativement ou un anneau hétérocyclique ou carbocyclique, insaturé ou saturé, substitué facultativement, et Q représente (II), où X, Y, R1 et R2 sont tels que définis dans la revendication 1. Lesdits composés sont des antagonistes d'un récepteur 11CBy humain.

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