C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 277/82 (2006.01) A61K 31/495 (2006.01) A61K 51/04 (2006.01) C07B 59/00 (2006.01) C07D 263/58 (2006.01)
Patent
CA 2253453
The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is O or S; n is 2, 3, 4 or 5; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R2 is hydrogen, C1-6alkyl, phenyl, phenylC1-6alkyl or phenylcarbonyl; R3 and R4 each independently are selected from hydrogen, halo, nitro, C1-6alkyl, C1-6alkyloxy, haloC1-6alkyl, aminosulfonyl, mono-or di(C1- 4alkyl)aminosulfonyl; or R3 and R4 may also be taken together to form a bivalent radical of formula -CH=CH-CH=CH-; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.
La présente invention concerne les composés de la formule (I), les formes N-oxyde, les sels d'addition d'acide pharmaceutiquement acceptables et les formes stéréochimiquement isomériques de ces derniers. Dans la formule, X est O ou S; n est 2, 3, 4 ou 5; R<1> est hydrogène, C1-6alkyle, C1-6alkyloxy ou halo; R<2> est hydrogène, C1-6alkyle, phényle, phénylC1-6alkyle ou phénylcarbonyle,; R<3> et R<4> sont chacun indépendamment sélectionnés parmi hydrogène, halo, nitro, C1-6alkyle, C1-6alkyloxy, haloC1-6alkyle, aminosulfonyle, mono ou di(C1-4alkyl)aminosulfonyle; ou R<3> et R<4> peuvent être pris ensemble pour former un radical bivalent de la formule -CH=CH-CH=CH-. L'invention traite aussi de procédés pour leur préparation, de compositions les comprenant ainsi que de leur utilisation comme médicaments. L'invention a aussi pour objet des composés de la formule (I) comprenant un isotope radioactif, un procédé de marquage des sites du récepteur D4 de la dopamine et un procédé pour observer un organe par imagerie.
Kennis Ludo Edmond Josephine
Mertens Josephus Carolus
Pieters Serge Maria Aloysius
Gowling Lafleur Henderson Llp
Janssen Pharmaceutica N.v.
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