5-METHYL-1-(NAPHTHALEN-2-YL)-1H-PYRAZOLES USEFUL AS SIGMA RECEPTOR INHIBITORS
    20.
    发明申请
    5-METHYL-1-(NAPHTHALEN-2-YL)-1H-PYRAZOLES USEFUL AS SIGMA RECEPTOR INHIBITORS 失效
    作为SIGMA受体抑制剂有用的5-甲基-1-(萘-2-基)-1H-吡咯烷

    公开(公告)号:US20110118253A1

    公开(公告)日:2011-05-19

    申请号:US12988929

    申请日:2009-04-27

    CPC classification number: C07D231/22

    Abstract: The invention relates to compounds having the formula (I): wherein the dashed line (represented by - - - - -) represents an optional double bond; R1 is hydrogen and R2 is hydroxyethyl; or R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl ring optionally substituted with one or two hydroxy groups; each R3 is independently hydroxy or C1-6alkoxy; n is selected from 0, 1, and 2; or a N-oxide, salt, prodrug, solvate or stereoisomer thereof; with the proviso that the compound where the dashed line represents a double bond, R1 and R2 together with the nitrogen atom to which they are attached form a morpholinyl ring, and n is 0, is excluded. Also provided are methods for the preparation of compounds of formula (I); their uses as a medicaments, particularly for the treatment or prophylaxis of a sigma receptor mediated diseases or conditions.

    Abstract translation: 本发明涉及具有式(I)的化合物:其中虚线(由 - - - - 表示)表示任选的双键; R1是氢,R2是羟乙基; 或R 1和R 2与它们所连接的氮原子一起形成任选被一个或两个羟基取代的吗啉基; 每个R 3独立地是羟基或C 1-6烷氧基; n选自0,1和2; 或其N-氧化物,盐,前药,溶剂合物或立体异构体; 条件是虚线表示双键的化合物,R 1和R 2与它们所连接的氮原子一起形成吗啉基环,n为0。 还提供了制备式(I)化合物的方法; 它们作为药物的用途,特别是用于治疗或预防σ受体介导的疾病或病症。

Patent Agency Ranking