Novel compounds as metabotropic glutamate receptor antagonists
    45.
    发明申请
    Novel compounds as metabotropic glutamate receptor antagonists 失效
    新型化合物作为代谢型谷氨酸受体拮抗剂

    公开(公告)号:US20070072879A1

    公开(公告)日:2007-03-29

    申请号:US11524135

    申请日:2006-09-20

    IPC分类号: A61K31/519 C07D487/04

    CPC分类号: C07D487/04 C07D471/04

    摘要: The present invention relates to compounds of formula (I) wherein A, E G, J, L, M, R1, R2, and R3 are as defined in the specification and claims. The invention also relates to pharmaceutical compositions containing such compounds and methods for preparing the compounds and compositions. The compounds are metabotropic glutamate receptor antagonists and are useful for the treatment of a variety of CNS disorders.

    摘要翻译: 本发明涉及式(I)的化合物,其中A,EG,J,L,M,R 1,R 2和R 3, SUP>如说明书和权利要求中所定义。 本发明还涉及含有这些化合物的药物组合物和用于制备化合物和组合物的方法。 化合物是代谢型谷氨酸受体拮抗剂,可用于治疗各种CNS疾病。

    β-lactam compounds and process for producing the same
    46.
    发明授权
    β-lactam compounds and process for producing the same 失效
    β-内酰胺化合物及其制备方法

    公开(公告)号:US07163936B2

    公开(公告)日:2007-01-16

    申请号:US10416334

    申请日:2001-11-06

    IPC分类号: A61K31/40 C07D487/04

    CPC分类号: C07D477/20 C07D477/06

    摘要: 1. A β-lactam compound of the formula [1]; wherein R1 is a lower alkyl, a lower alkyl substituted by a hydroxy; R2 is a hydrogen, a lower alkyl; X is O, S, NH; m and n are 0 to 4, Y1 is a halogen, cyano, a hydroxy, an amino, a lower alkyloxy, a lower alkylamino, a carboxy, a carbamoyl, a lower alkyl, etc., Y2 is hydrogen, an alkyl, cyano, —C(R3)═NR4 (wherein R3 and R4 are hydrogen, an amino, an alkyl, etc., or R3 and R4 may combine each other together with the nitrogen atom to form a 5- to 7-membered heterocyclic group), or a pharmaceutically acceptable salt thereof, or a non-toxic ester thereof, which has an excellent antibacterial activity against Gram-positive bacteria, especially against MRSA and MRCNS.

    摘要翻译: 1.式[1]的β-内酰胺化合物; 其中R 1是低级烷基,被羟基取代的低级烷基; R 2是氢,低级烷基; X是O,S,NH; m和n为0〜4,Y 1为卤素,氰基,羟基,氨基,低级烷氧基,低级烷基氨基,羧基,氨基甲酰基,低级烷基等, Y 2是氢,烷基,氰基,-C(R 3) - NR 4(其中R 3 O) >和R 4是氢,氨基,烷基等,或R 3和R 4可以彼此结合, 氮原子形成5-至7-元杂环基)或其药学上可接受的盐或其无毒性酯,其对革兰氏阳性细菌,特别是抗MRSA和MRCNS具有优异的抗菌活性。

    Pyrrazolo-pyrimidine derivatives
    48.
    发明申请
    Pyrrazolo-pyrimidine derivatives 失效
    吡唑并嘧啶衍生物

    公开(公告)号:US20060183756A1

    公开(公告)日:2006-08-17

    申请号:US11348105

    申请日:2006-02-06

    IPC分类号: A61K31/519 C07D487/04

    CPC分类号: C07D487/04

    摘要: The present invention relates to pyrrazolo-pyrimidine derivatives of formula (I): wherein R1 to R4 and A are as defined in the specification, a process for the manufacture thereof, their use for treating or preventing metabotropic glutamate receptors mediated disorders, their use for the preparation of medicaments for treating such disorders and pharmaceutical compositions containing said derivatives.

    摘要翻译: 本发明涉及式(I)的吡唑并嘧啶衍生物:其中R 1至R 4和A如说明书中所定义,其制备方法 ,它们用于治疗或预防代谢型谷氨酸受体介导的病症,其用于制备用于治疗这种病症的药物的用途和含有所述衍生物的药物组合物。