DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1
    6.
    发明申请
    DI-AROMATIC SUBSTITUTED AMIDES AS INHIBITORS FOR GLYT1 审中-公开
    作为GLYT1抑制剂的DI-AROMATIC取代的氨基酸

    公开(公告)号:WO2008022938A1

    公开(公告)日:2008-02-28

    申请号:PCT/EP2007/058350

    申请日:2007-08-13

    Abstract: The present invention relates to compounds of the general Formula (I) wherein (A) is a 5 or 6-membered aromatic or heteroaromatic ring; R 1 is cycloalkyl or is aryl or heteroaryl, wherein at least one ring is aromatic in nature, unsubstituted or substituted by 1 to 3 substituents selected from the group consisting of halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, -C(O) -lower alkyl, -S(O) 2 -lower alkyl, nitro or cyano; R 2 is hydrogen or lower alkyl; R 3 is hydrogen or lower alkyl; R 4 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or nitro; R 5 is hydrogen, halogen, lower alkyl or lower alkyl substituted by halogen; X is a bond, -(CH 2 ) m -, -CH 2 O- or -CH 2 NH-; The dotted line denotes a bond or not; n is 1 or 2; m is 1, 2 or 3; and pharmaceutically acceptable acid addition salts thereof and their use in the treatment of neurological and neuropsychiatric disorders.

    Abstract translation: 本发明涉及通式(I)的化合物,其中(A)是5或6元芳族或杂芳族环; R 1是环烷基或芳基或杂芳基,其中至少一个环在本质上是芳族的,未被取代或被1至3个选自以下的取代基取代:卤素,低级烷基,被 卤素,低级烷氧基,被卤素取代的低级烷氧基,-C(O) - 低级烷基,-S(O)2 - 低级烷基,硝基或氰基; R 2是氢或低级烷基; R 3是氢或低级烷基; R 4是卤素,低级烷基,被卤素取代的低级烷基,低级烷氧基,被卤素或硝基取代的低级烷氧基; R 5是氢,卤素,被卤素取代的低级烷基或低级烷基; X是一个键, - (CH 2)2 - , - CH 2 O-或-CH 2 - NH-; 虚线表示不是键; n为1或2; m为1,2或3; 及其药学上可接受的酸加成盐及其在治疗神经和神经精神障碍中的用途。

    NOVEL QUATERNARY AMMONIUM DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL USE
    10.
    发明申请
    NOVEL QUATERNARY AMMONIUM DERIVATIVES, METHOD FOR PREPARING SAME AND PHARMACEUTICAL USE 审中-公开
    新的季铵衍生物,其制备方法和药物使用方法

    公开(公告)号:WO01000621A1

    公开(公告)日:2001-01-04

    申请号:PCT/FR2000/001731

    申请日:2000-06-22

    Abstract: The invention concerns compounds of formulae (Ia) or (Ib) wherein M: represents a molecule for use in the treatment or diagnosis of pathologies affecting the cartilage; R1, R2, R3 represent an alkyl group, or R1, R 2, R3 together with the nitrogen atom which bears them form a heterocycle; X represents a C1-C6 alkyl chain wherein one or several -CH2- groups are optionally substituted by a sulphur, an oxygen atom, a -NR, -CO-, -CO-NH-, -CO2-, SO- or SO2- group; n represents 0 or 1; Hal represents a halogen atom, or the formula (Ib); R4 represents an alkyl group; Hal represents a halogen atom. General formula (F1) represents a molecule for use in the treatment or diagnosis of pathologies affecting the cartilage, provided that the nitrogen atom can optionally be included in a saturated or unsaturated nitrogenous heterocyclic system, or involved in a double bond.

    Abstract translation: 本发明涉及式(Ia)或(Ib)化合物,其中M:代表用于治疗或诊断影响软骨病理的分子; R 1,R 2,R 3表示烷基,或者R 1,R 2,R 3与它们的氮原子一起形成杂环; X表示C1-C6烷基链,其中一个或多个-CH 2 - 基团任选被硫,氧原子,-NR,-CO-,-CO-NH-,-CO 2 - ,SO-或SO 2 - 组; n表示0或1; Hal表示卤素原子,或式(Ib); R4表示烷基; Hal代表卤原子。 通式(F1)表示用于治疗或诊断影响软骨的病理学的分子,条件是氮原子可以任选地包括在饱和或不饱和的含氮杂环体系中或参与双键。

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