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    • 10. 发明申请
    • Triazole Compounds Suitable for Treating Disorders that Respond to Modulation of the Dopamine D3 Receptor
    • 适用于治疗多巴胺D3受体调节反应的三唑化合物
    • US20080171751A1
    • 2008-07-17
    • US11792596
    • 2005-12-01
    • Liliane UngerAndreas HauptArmin BeyerbachKarla DrescherWilfried BrajeJohn DarbyshireSean C. TurnerGisela Backfisch
    • Liliane UngerAndreas HauptArmin BeyerbachKarla DrescherWilfried BrajeJohn DarbyshireSean C. TurnerGisela Backfisch
    • A61K31/496C07D403/14A61P25/00
    • C07D403/12
    • The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one triazole compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
    • 本发明涉及式I化合物:其中n是1或2,Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基,和 其中一个氮原子上的基团R 1a, R 1是氢,C 1 -C 6烷基,C 3 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, 氟化C 1 -C 6烷基,氟化C 1 -C 6烷基,C 1 -C 6烷基,C 1 -C 6烷基, 氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基, 杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基,C 3 -C 6烷基, 氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及这些化合物的生理上耐受的酸加成盐。 本发明还涉及一种药物组合物,其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐,还涉及治疗有益于多巴胺D 3的病症的方法 受体拮抗剂或多巴胺D 3激动剂,所述方法包括向有需要的受试者施用有效量的至少一种式III的三唑化合物或生理耐受的酸加成盐。