C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/47, 260/325.
C07D 207/09 (2006.01) A61K 51/04 (2006.01) C07D 405/12 (2006.01) C07F 3/12 (2006.01) C07F 7/10 (2006.01) C07F 7/22 (2006.01)
Patent
CA 2011745
Novel CNS dopamine D-2 receptors of the formulae (see fig. I) (see fig. II) where Y and Y' are independently selected from the group consisting of hydrogen, C1-C5 alkyl; C1-C5 alkenyl and C1-C5 alkynyl; Z is selected from the group consisting of halogen (Hal), CH=CH-Hal; C1-C10 alkylene-Hal; C1-C10 alkylene-CH=CH-Hal; C1-C10 alkylene-phenyl-Hal; C1-C10 alkylene-heteroaryl-Hal; provided that, in Compounds of Formula I, Hal is a radioactive iodine atom; and A is an alkylene moiety of from two to eight carbon atoms, are disclosed. An example of such a compound is 5-iodo-7-N-[(1-ethyl-2-pyrrolidinyl)methyl]carboxamide-2,3- dihydrobenzofuran. These compounds are useful as imaging agents for D-2 receptors in the human brain and exhibit good brain retention and in vivo stability.
De nouveaux récepteurs D-2 de la dopamine dans le SNC, tel que le composé 5-iodo-7-N-[(1-éthyl-2-pyrrolidnyl)méthyl]carboxamide-2, 3-dihydrobenzofurane, sont divulgués. Ces composés sont utiles comme agents d'imagerie des récepteurs D-2 dans le cerveau humain et se caractérisent par une bonne rétention cérébrale et une bonne stabilité in vivo
Kung Hank F.
Murphy Raymond
Smart & Biggar
Trustees Of The University Of Pennsylvania (the)
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