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    Aminoethylation process having improved yield of aryloxyalkylene amine compounds and reduced urea by-products
    1.
    发明授权
    Aminoethylation process having improved yield of aryloxyalkylene amine compounds and reduced urea by-products 有权
    氨基乙基化方法具有提高的芳氧基亚烷基胺化合物的产率和减少的尿素副产物

    公开(公告)号：US09035097B2

    公开(公告)日：2015-05-19

    申请号：US13612595

    申请日：2012-09-12

    申请人： Patrick J. McDougall ,  James Saenz ,  David Lao

    发明人： Patrick J. McDougall ,  James Saenz ,  David Lao

    IPC分类号： C07C215/00 ,  C07C209/78 ,  C07C213/08

    CPC分类号： C07C209/78 ,  C07C213/08 ,  C07C217/16

    摘要： Disclosed is a process for preparing an aryloxyalkylene amine compound via an aminoethylation reaction comprising: a) reacting an aromatic hydroxyl compound in the presence of a basic catalyst with a 2-oxazolidinone compound of the formula II to form an intermediate reaction product; wherein R3 is selected from the group consisting of hydrogen or lower alkyl having 1 to 6 carbon atoms, R4 is selected from the group consisting of hydrogen, straight or branched chain alkyl having from one to six carbon atoms, phenyl, alkaryl, or arylalkyl; and b) reacting the intermediate product of step a) with a polyalkylene polyamine.

    摘要翻译： 公开了通过氨基乙基化反应制备芳氧基亚烷基胺化合物的方法，包括：a）在碱性催化剂存在下使芳族羟基化合物与式II的2-恶唑烷酮化合物反应，形成中间反应产物; 其中R 3选自氢或具有1至6个碳原子的低级烷基，R 4选自氢，具有1至6个碳原子的直链或支链烷基，苯基，烷芳基或芳基烷基; 和b）使步骤a）的中间产物与聚亚烷基多胺反应。

    Hydrazine amide derivative
    6.
    发明授权
    Hydrazine amide derivative 有权
    肼酰胺衍生物

    公开(公告)号：US08344180B2

    公开(公告)日：2013-01-01

    申请号：US12310566

    申请日：2007-08-28

    申请人： Naoki Kouyama

    发明人： Naoki Kouyama

    IPC分类号： C07C303/00 ,  C07C241/00 ,  C07C215/00 ,  C07C211/00

    CPC分类号： C07D209/08 ,  A61K9/1623 ,  A61K9/2018 ,  A61K9/4858 ,  C07C311/07 ,  C07C2601/14 ,  C07D213/77

    摘要： 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.

    摘要翻译： 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。