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2. 发明授权

US06395742B1 2,4-diaminopyrimidine derivatives 有权
标题翻译： 2,4-二氨基嘧啶衍生物
公开(公告)号：US06395742B1
公开(公告)日：2002-05-28
申请号：US09667458
申请日：2000-09-22
申请人： Jean-Paul René Marie André Bosmans , Christopher John Love , Guy Rosalia Eugène Van Lommen
发明人： Jean-Paul René Marie André Bosmans , Christopher John Love , Guy Rosalia Eugène Van Lommen
IPC分类号： C07D40112
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： The 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.
摘要翻译：本发明涉及配制N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中Alk是C 1-6烷二基或C 3-6亚烯基; R1是氢或C1-4烷基; R2和R3各自独立地为氢，C1-6烷基或C3-7环烷基; 或者R 2和R 3也可以与它们所连接的氮原子一起，从而形成吡咯烷，哌啶或全氢吖庚因环; R4是氢或卤素; Q是芳基，芳氧基，二（芳基）甲基或杂芳基; 芳基是萘基或苯基，所述萘基和苯基可任选被取代; 异喹啉基，吡啶基，噻吩基，吲哚基，2,3-二氢-1,4-苯并二氧杂环戊烯基，2,3-二氢 - 苯并呋喃基或苯并二氧杂环戊烷基; 所述杂芳基可任选被取代; 它还涉及它们的制备方法，包含它们的组合物以及它们作为药物的用途; 含有放射性同位素的式（I）化合物; 标记多巴胺D4受体位点的过程; 并且公开了用于成像器官的方法。

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