发明名称 2,4-diaminopyrimidine derivates as dopamine D4 receptor antagonist
摘要 PCT No. PCT/EP97/02506 Sec. 371 Date Nov. 9, 1998 Sec. 102(e) Date Nov. 9, 1998 PCT Filed May 2, 1997 PCT Pub. No. WO97/43279 PCT Pub. Date Nov. 20, 1997The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl or C3-6alkenediyl; R1 is hydrogen or C1-4alkyl; R2 and R3 each independently are hydrogen, C1-6alkyl or C3-7cycloalkyl; or R2 and R3 may also be taken together with the nitrogen atom to which they are attached, thus forming a pyrrolidine, a piperidine or a perhydro azepine ring; R4 is hydrogen or halo; Q is aryl, aryloxy, di(aryl)methyl or heteroaryl; aryl is naphthyl or phenyl, said naphthyl and phenyl may optionally be substituted; and heteroaryl is quinolinyl, isoquinolinyl, pyridinyl, thienyl, indolyl, 2,3-dihydro-1,4-benzodioxinyl, 2,3-dihydro-benzofuranyl or benzodioxolanyl; said heteroaryls may optionally be substituted: 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.
申请公布号 US6159982(A) 申请公布日期 2000.12.12
申请号 US19980180364 申请日期 1998.11.09
申请人 JANSSEN PHARMACEUTICA N. V. 发明人 BOSMANS, JEAN-PAUL RENEMARIE ANDRE;LOVE, CHRISTOPHER JOHN;VAN LOMMEN, GUY ROSALIA EUGENE
分类号 A61K31/505;C07D401/12;C07D401/14;C07D405/14;C07D409/14;(IPC1-7):C07D401/12 主分类号 A61K31/505
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