Fused pyridine derivatives
    5.
    发明授权
    Fused pyridine derivatives 有权
    融合吡啶衍生物

    公开(公告)号:US08680089B2

    公开(公告)日:2014-03-25

    申请号:US13522304

    申请日:2011-01-17

    摘要: Fused pyridine derivatives shown as the general formula (I), and their pharmaceutically acceptable salts, stereoisomers or solvates thereof are disclosed, which belong to the technical field of medicines. The R1, R2, R3, Q, X and Y substituents in formula (I) are defined as in the description. Also disclosed are the preparation methods, pharmaceutical compositions comprising the compounds and uses of the compounds in the manufacture of the medicine for the treatment and/or prevention of noninsulin-dependent diabetes, hyperglycemia, hyperlipidemia and insulin resistance.

    摘要翻译: 公开了以通式(I)表示的稠合吡啶衍生物及其药学上可接受的盐,立体异构体或溶剂化物,属于药物技术领域。 式(I)中的R 1,R 2,R 3,Q,X和Y取代基如描述中所定义。 还公开了制备方法,包含该化合物的药物组合物和该化合物在制备用于治疗和/或预防非胰岛素依赖型糖尿病,高血糖,高脂血症和胰岛素抵抗的药物中的用途。

    Tyrosine-derived compounds as calcium channel antagonists
    9.
    发明授权
    Tyrosine-derived compounds as calcium channel antagonists 失效
    酪氨酸衍生化合物作为钙通道拮抗剂

    公开(公告)号:US06180677B2

    公开(公告)日:2001-01-30

    申请号:US09381938

    申请日:1999-09-27

    IPC分类号: A61K3803

    摘要: The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

    摘要翻译: 本发明提供了阻断钙通道并具有式I的化合物及其药学上可接受的盐,酯和前药,其中R 1和R 2独立地为H,苯基环戊基羰基,C 1 -C 7烷基,环己基甲基,苄基,C 1 -C 5烷基苄基 或C 1 -C 5烷氧基苄基,A是-C(O) - 或-CH 2 - ; R 3是H或-CH 3; R 4是C 1 -C 4烷基或哌啶-1-基乙基; R 5是苯基 - (CH 2) C 1 -C 4烷基苯基 - (CH 2)n - 或卤代苯基 - (CH 2)n - 并且n为1或2.本发明还提供了含有式I化合物的药物组合物及其用于治疗中风,脑缺血,头部创伤和癫痫的方法。