C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 271/12 (2006.01) A61K 51/04 (2006.01) C07D 285/14 (2006.01)
Patent
CA 2520278
The present invention relates to novel benzo[1,2,5]oxadiazoles and benzo[1,2,5]thiadiazoles of formula (I) wherein X is O or S, R1 is 5-(2-fluoro- ethylamino)-thiazol-2-yl, 5-(2-18F-ethylamino)- thiazol-2-yl or a group of formula (a) wherein Y is CH or N, R2 is NHCH3, NH11CH3, N(CH3)11CH3, N(CH3)2, N(11CH3)2, NH(CH2)nF, NH(CH2)n18F, N(CH3)~(CH2)nF, N(CH3)-(CH2)n 18F, O- (CH2)nF, O-(CH2)n 18F, CONH(CH2)nF or CONH(CH2)n18F (n being in each case 2 to 4) and R3 is hydroxy, (C1-4)alkoxy, hydrogen or nitro, in free base or acid addition salt form; their preparation, their use as markers in diagnosis and compositions containing them.
L'invention concerne de nouveaux benzo[1,2,5]oxadiazoles et benzo[1,2,5]thiadiazoles représentés par la formule (I) dans laquelle X représente O ou S; R¿1? représente 5-(2-fluoro-ethylamino)-thiazol-2-yl, 5-(2-?18¿F-ethylamino)- thiazol-2-yl ou un groupe représenté par la formule (a) où Y représente CH ou N; R¿2? représente NHCH¿3?, NH?11¿CH¿3?, N(CH¿3?)?11¿CH¿3?, N(CH¿3?)¿2?, N(?11¿CH¿3?)¿2?, NH(CH¿2?)¿n?F, NH(CH¿2?)¿n??18¿F, N(CH¿3?)-(CH¿2?)¿n?F, N(CH¿3?)-(CH¿2?)¿n? ?18¿F, O-(CH¿2?)¿n?F, O-(CH¿2?)¿n? ?18¿F, CONH(CH¿2?)nF ou CONH(CH¿2?)¿n??18¿F (n étant dans chaque cas compris entre 2 et 4); et R¿3? représente hydroxy, (alcoxy C¿1-4?), hydrogène ou nitro sous forme d'une base libre ou d'un sel d'addition acide. L'invention concerne également la préparation de ces composés, leur utilisation comme marqueurs dans un diagnostic ou dans des compositions les renfermant.
Auberson Yves
Hintermann Samuel
Zimmermann Kaspar
Fetherstonhaugh & Co.
Novartis Ag
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