SUBSTITUTED (ARYLALKOXYBENZYL)AMINOPROPANAMIDE DERIVATIVES, THEIR PREPARATION AND USE AS ANTI-EPILEPTIC, NEUROPROTECTIVE AND ANTIDEPRESSANT AGENTS
    1.
    发明申请
    SUBSTITUTED (ARYLALKOXYBENZYL)AMINOPROPANAMIDE DERIVATIVES, THEIR PREPARATION AND USE AS ANTI-EPILEPTIC, NEUROPROTECTIVE AND ANTIDEPRESSANT AGENTS 审中-公开
    取代(芳基烷氧基)氨基丙酰胺衍生物,其制备和用作抗真菌,神经保护和抗原剂

    公开(公告)号:WO1994022808A1

    公开(公告)日:1994-10-13

    申请号:PCT/EP1994000802

    申请日:1994-03-15

    CPC classification number: C07C237/00

    Abstract: The invention provides new compounds of formula (I) wherein, subject to a proviso, n is zero or an integer of 1 to 3; each of R and R1, which may be the same or different, is hydrogen, halogen, trifluoromethyl or C1-C4 alkoxy; R2 is hydrogen or C1-C4 alkyl optionally substituted by hydroxy; each of R3 and R4 independently is hydrogen or C1-C4 alkyl; or a pharmaceutically acceptable salt thereof; and of formula (IA), wherein R5 is hydrogen, halogen, trifluoromethyl or C1-C4 alkoxy, or a pharmaceutically acceptable salt thereof, which are active on the central nervous system (CNS) and can be used in therapy as anti-epileptics, anti-Parkinson, neuroprotective, antidepressant, anti-spastic and hypnotic agents.

    Abstract translation: 本发明提供新的式(I)化合物,其中,条件是n为0或1至3的整数; R和R 1可以相同或不同,为氢,卤素,三氟甲基或C 1 -C 4烷氧基; R2是氢或任选被羟基取代的C 1 -C 4烷基; R 3和R 4各自独立地是氢或C 1 -C 4烷基; 或其药学上可接受的盐; 和式(IA)的化合物,其中R5是氢,卤素,三氟甲基或C1-C4烷氧基,或其药学上可接受的盐,它们在中枢神经系统(CNS)上有活性,可用作抗癫痫药, 抗帕金森,神经保护,抗抑郁药,抗痉挛和催眠药。

    DERIVATIVES OF (R) 5-PENTYLAMINO-5-OXOPENTANOIC ACID WITH ANTICHOLECYSTOKININ ACTIVITY
    6.
    发明申请
    DERIVATIVES OF (R) 5-PENTYLAMINO-5-OXOPENTANOIC ACID WITH ANTICHOLECYSTOKININ ACTIVITY 审中-公开
    (R)5-戊基氨基-5-氧代戊酸与抗转氨酶活性的衍生物

    公开(公告)号:WO1988005774A1

    公开(公告)日:1988-08-11

    申请号:PCT/EP1988000061

    申请日:1988-01-28

    Abstract: Optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with formula (I), in which R1 is selected from the groups 2-naphthyl, 3,4-dichlorobenzoyl and 3,4-dimethylbenzoyl and R2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.

    Abstract translation: (R)5-戊基氨基-5-氧代戊酸及其药学上可接受的盐,对缩胆囊素具有拮抗作用并且具有式(I)的光学活性衍生物,其中R 1选自2-萘基,3,4- 二氯苯甲酰基和3,4-二甲基苯甲酰基,R 2是具有4个碳原子的戊基或烷氧基烷基,其中中心手性基团上的取代基(在式(I)中用星号标记))具有R(直角) 构象。

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