2-AMINOQUINOLINE DERIVATIVES HAVING D4-AGONISTIC ACTIVITY
    9.
    发明申请
    2-AMINOQUINOLINE DERIVATIVES HAVING D4-AGONISTIC ACTIVITY 审中-公开
    具有D4-激活活性的2-氨基喹啉衍生物

    公开(公告)号:WO9940068A2

    公开(公告)日:1999-08-12

    申请号:PCT/EP9900855

    申请日:1999-02-05

    CPC classification number: C07D215/38 C07D401/12 C07D405/12

    Abstract: The present invention relates to a group of novel 2-aminoquinoline derivatives which are potent and selective agonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 1 or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)-amino, or two groups R1 at adjacent carbon atoms together with the benzene ring may form the benzdioxane group or benzofuran group, X represents nitrogen or carbon, and the dotted line may represent a double bond, (R2)p represents 0, 1 or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)p is a methylene bridge or ethylene bridge, R3 is hydrogen or methyl, and (R)m represents 0, 1, or 2 substituents, which can be the same or different and can be located at all available positions of the quinolyl group, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, and mono- or dialkyl (C1-2)-amino, on the understanding that R1 cannot represent o-OCH3 when X is nitrogen, (R2)p and R3 are hydrogen, m is 0 and n is 1.

    Abstract translation: 本发明涉及一组新的2-氨基喹啉衍生物,其是多巴胺D4-受体的有效和选择性激动剂。 化合物具有通式(I),其中(R1)n表示1或2个可以相同或不同的取代基,可以是C1-3 - 烷基或烷氧基,卤素,三氟甲基,硝基,氨基和单 - 或 二烷基(C1-2) - 氨基或两个相邻碳原子的R1与苯环一起形成苯并二恶烷基或苯并呋喃基,X表示氮或碳,虚线表示双键,(R2) p表示0,1或2个与甲基和乙基基团相同或不同的取代基,或(R2)p是亚甲基桥或乙烯桥,R3是氢或甲基,(R)m表示0 ,1或2个取代基,其可以相同或不同,并且可以位于喹啉基的所有可用位置,C 1-3 - 烷基或烷氧基,卤素,三氟甲基,硝基,氨基和单 - 或 二烷基(C 1-2) - 氨基,但应理解,当X为氮时,R 1不能表示o-OCH 3,(R 2)p和R 3为氢,m为0,n为 是1。

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