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    • 6. 发明授权
    • Hydrazine amide derivative
    • 肼酰胺衍生物
    • US08344180B2
    • 2013-01-01
    • US12310566
    • 2007-08-28
    • Naoki Kouyama
    • Naoki Kouyama
    • C07C303/00C07C241/00C07C215/00C07C211/00
    • C07D209/08A61K9/1623A61K9/2018A61K9/4858C07C311/07C07C2601/14C07D213/77
    • Disclosed are compound having NPY Y5 receptor antagonistic activity of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is optionally substituted lower alkyl, R2 and R8 are each independently hydrogen or lower alkyl, X is optionally substituted cycloalkylene, or —NR2—X— may be a group of the formula: wherein a group of the formula: is piperidinediyl, piperazinediyl, pyridindiyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl, U is a bond, lower alkylene or lower alkenylene, Y is —OCONR7—, —CONR7— or —CSNR7—, R7 is hydrogen or lower alkyl, Z is optionally substituted carbocyclyl, or optionally substituted heterocyclyl, W is —S(═O)n-, n is 2, provided that Z is not carbocyclyl substituted with non-halogeno lower alkoxy, and provided that 5-Methyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid [2-[(5-chloro-1H-indole-2-carbonyl)-amino]-5 -(N′,N′-dimethyl-hydrazinocarbonyl)-cyclohexyl]-amide and 5-Methyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid [2-[(5-chloro-4-fluoro-1H-indole-2-carbonyl)-amino]-5-(N′,N′-dimethyl-hydrazinocarbonyl) -cyclohexyl]-amide are excluded.
    • 公开了具有式(I)的NPY Y5受体拮抗活性的化合物或其药学上可接受的盐,其中R 1为任选取代的低级烷基,R 2和R 8各自独立地为氢或低级烷基,X为任选取代的亚环烷基或-NR 2 -X-可以是下式的基团:其中下式的基团是哌啶二基,哌嗪二基,吡啶二基,吡嗪二基,吡咯烷二基或吡咯二基,U是一个键,低级亚烷基或低级亚烯基,Y是-OCONR7-,-CONR7 - 或-CSNR 7 - ,R 7是氢或低级烷基,Z是任选取代的碳环基或任选取代的杂环基,W是-S(= O)n - ,n是2,条件是Z不是被非卤素取代的碳环基 并且条件是5-甲基-4,5,6,7-四氢 - 噻唑并[5,4-c]吡啶-2-甲酸[2 - [(5-氯-1H-吲哚-2-羰基 ) - 氨基] -5 - (N',N'-二甲基 - 肼基羰基) - 环己基] - 酰胺和5-甲基-4,5,6,7-四氢 - 噻唑 o [5,4-c]吡啶-2-甲酸[2 - [(5-氯-4-氟-1H-吲哚-2-羰基) - 氨基] -5-(N',N'-二甲基 - 肼基羰基) - 环己基] - 酰胺。