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    • 8. 发明申请
    • DIAMINE DERIVATIVES HAVING SELECTIVE AFFINITY FOR SIGMA RECEPTORS
    • 具有SIGMA受体选择性亲和力的DIAMINE衍生物
    • WO1993022279A1
    • 1993-11-11
    • PCT/CH1993000106
    • 1993-04-22
    • BATTELLE MEMORIAL INSTITUTEROCHER, Jean-Philippe
    • BATTELLE MEMORIAL INSTITUTE
    • C07C233/40
    • C07D207/325C07C211/27C07C233/36C07C233/37C07C233/40C07C2603/74C07D295/125
    • Diamine derivatives of formula (I), wherein n = 0-8; R1 is hydrogen or a C1-3 alkyl residue; each of R2, R3, R4, R5 and R6 is hydrogen, a C1-6 alkyl residue, branched C4-12 alkyl or alkenyl; R2 and R3 together may form a C3-8 ring optionally including a heteroatom and optionally partially or wholly unsatured; R5 and R6 taken together may form a C2-8 ring; X is a single bond, -CH2-, -C (=O)-, -S (O)-, or -S (O)2-; Y is an alkyl residue, cycloalkyl, cycloalkylalkyl, adamantyl, optionally substituted phenyl or an aromatic heterocyclic ring; Ar is an optionally substituted phenyl radical, naphtyl or an aromatic heterocyclic ring. Said derivatives are psychotropic agents particularly suitable for treating psychotic disorders, convulsion, dyskinesia, brain distress (ischaemia, hypoxia) and anxiety, and further have anti-inflammatory properties.
    • 式(I)的二胺衍生物,其中n = 0-8; R1是氢或C1-3烷基残基; R2,R3,R4,R5和R6各自为氢,C1-6烷基,支链C4-12烷基或烯基; R2和R3一起可以形成任选地包括杂原子并且任选地部分或全部不成熟的C 3-8环; R5和R6一起可以形成C2-8环; X是单键,-CH 2 - , - C(= O) - , - S(O) - 或-S(O)2 - Y是烷基残基,环烷基,环烷基烷基,金刚烷基,任选取代的苯基或芳族杂环; Ar是任选取代的苯基,萘基或芳族杂环。 所述衍生物是特别适用于治疗精神病,惊厥,运动障碍,脑窘迫(缺血,缺氧)和焦虑的精神药物,并且还具有抗炎特性。