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26 条记录 (耗时 0.031 秒)

    Procedure for the preparation of racemic and enantiomerically pure derivatives O F 1,5 diaryl-3-trifluorromethyl-delta2-pyrazolines
    16.
    发明申请
    Procedure for the preparation of racemic and enantiomerically pure derivatives O F 1,5 diaryl-3-trifluorromethyl-delta2-pyrazolines 失效

    公开(公告)号：US20050096373A1

    公开(公告)日：2005-05-05

    申请号：US11007449

    申请日：2004-12-08

    申请人： Montserrat Alcon-Marrugat ,  Miguel Pericas-Brondo ,  Maria Cuberes-Altisen ,  Jordi Frigola-Constansa

    发明人： Montserrat Alcon-Marrugat ,  Miguel Pericas-Brondo ,  Maria Cuberes-Altisen ,  Jordi Frigola-Constansa

    IPC分类号： C07D231/06 ,  C07D231/12 ,  A61K31/415

    CPC分类号： C07D231/06

    摘要： Procedure for preparation of compounds with the general formula 1, which include the racemic mixtures (±)-1, and the enantiomerically pure compounds (−)-1 and (+)-1, wherein R1 and R3, like or different, represent an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl or methoxy group; R2 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group; R4 represents an atom of hydrogen, chlorine, fluorine, a methyl, trifluoromethyl, methoxy, trifluoromethoxy, methylsulphonyl or aminosulphonyl group, with the condition that one of the substituents R2 or R4 is a methylsulphonyl or aminosulphonyl group; which involves obtaining the racemic mixture with the general formula (±)-1 by reacting an (E)-1,1,1-trifluoro-4-aryl-3-buten-2-one with a phenylhydrazine, followed by a treatment with chlorosulphonic acid, or by reacting with chlorosulphonic acid followed by a reaction with sodium hydroxide and, finally, with thionyl chloride. The product obtained by either of these methods is made to react with ammonium carbonate or ammonia, or with sodium sulphite and methyl iodide or methyl sulphate. In addition, to obtain the enantiomerically pure compounds with the general formula 1 by resolving the racemic mixture with the general formula (±)-1, a reaction is effected with optically active ephedrine, followed by formation of the sodium salt of each enantiomer, reaction with thionyl chloride and ammonium carbonate or ammonia, or instead with thionyl chloride followed by sodium sulphite and methyl iodide or methyl sulphate to thereby obtain separately the enantiomerically pure compounds with the general formulae (−)-1 and (+)-1.

    5-methyl-1-(naphthalen-2-yl)-1H-pyrazoles useful as sigma receptor inhibitors
    18.
    发明授权
    5-methyl-1-(naphthalen-2-yl)-1H-pyrazoles useful as sigma receptor inhibitors 失效
    可用作σ受体抑制剂的5-甲基-1-（萘-2-基）-1H-吡唑

    公开(公告)号：US08492425B2

    公开(公告)日：2013-07-23

    申请号：US12988929

    申请日：2009-04-27

    申请人： Antoni Torrens Jover ,  Maria Rosa Cuberes-Altisent ,  Maria Jose Pretel Sanchez ,  Maria Magdalena Bordas Gelabert

    发明人： Antoni Torrens Jover ,  Maria Rosa Cuberes-Altisent ,  Maria Jose Pretel Sanchez ,  Maria Magdalena Bordas Gelabert

    IPC分类号： A61K31/415 ,  C07D231/22

    CPC分类号： C07D231/22

    摘要： 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.

    摘要翻译： 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。