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7 条记录 (耗时 0.037 秒)

    Substituted tetrahydroisoquinolines and uses thereof
    5.
    发明授权
    Substituted tetrahydroisoquinolines and uses thereof 失效
    取代的四氢异喹啉及其用途

    公开(公告)号：US07196088B2

    公开(公告)日：2007-03-27

    申请号：US10791578

    申请日：2004-03-02

    申请人： David George Putman

    发明人： David George Putman

    IPC分类号： A61K31/496 ,  C07D401/04

    CPC分类号： C07D401/12 ,  C07D217/08 ,  C07D217/24

    摘要： The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein, n, X, Y, R1, R2, R3, R4 and R5 are as defined herein. The subject compounds are useful for treatment of 5-HT6 receptor antagonist-mediated diseases. Also provides are methods for preparing, compositions comprising, and methods for using the subject compounds.

    摘要翻译： 本发明提供下式的化合物：

    Aryl pyrimidine derivatives and uses thereof
    7.
    发明授权
    Aryl pyrimidine derivatives and uses thereof 失效
    芳基嘧啶衍生物及其用途

    公开(公告)号：US5958934A

    公开(公告)日：1999-09-28

    申请号：US976418

    申请日：1997-11-21

    申请人： Jacob Berger ,  Lee Allen Flippin ,  Robert Greenhouse ,  Saul Jaime-Figueroa ,  Yanzhou Liu ,  Aubry Kern Miller ,  David George Putman ,  Klaus Kurt Weinhardt ,  Shu-Hai Zhao

    发明人： Jacob Berger ,  Lee Allen Flippin ,  Robert Greenhouse ,  Saul Jaime-Figueroa ,  Yanzhou Liu ,  Aubry Kern Miller ,  David George Putman ,  Klaus Kurt Weinhardt ,  Shu-Hai Zhao

    IPC分类号： A61K31/505 ,  C07D239/42

    CPC分类号： A61K31/505 ,  C07D239/42

    摘要： The aryl pyrimidine derivatives and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, including utility as selective 5HT.sub.2B -antagonists. The 5-HT.sub.2B antagonist is a compound of the formula: ##STR1## wherein: R.sup.1 is hydrogen, alkyl, lower alkoxy, hydroxyalkyl, cycloalkyl, cycloalkyl lower alkyl, alkenyl, lower thioalkoxy, halo, fluoroalkyl, --NR.sup.6 R.sup.7, --CO.sub.2 R.sup.8, --O(CH.sub.2).sub.n R.sup.9, or lower alkyl optionally substituted with hydroxy, alkoxy, halo, or aryl; in whichn is 1, 2, or 3;R.sup.6 and R.sup.7 are hydrogen or lower alkyl;R.sup.8 is hydrogen or lower alkyl; andR.sup.9 is hydrogen, lower alkyl, hydroxy, hydroxy lower alkyl, lower alkenyl, or lower alkoxy;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, or lower fluoroalkyl;R.sup.3 is optionally substituted aryl other than pyridyl, thienyl, or furanyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, alkenyl, acyl, amino, amido, aryl, --(CH.sub.2).sub.m NR.sup.10 R.sup.11, or lower alkyl optionally substituted by amino, monosubstituted amino, disubstituted amino, hydroxy, carboxy, aryl, lower alkoxy, amido, alkoxy carbonyl, tetrahydrofuran-2-yl, hydroxyalkoxy, or sulfonamido;in whichR.sup.10 and R.sup.11 are hydrogen or lower alkyl; andR.sup.5 is hydrogen or lower alkyl; provided that:(i) when R.sup.3 is naphthyl, indol-1-yl, or 2,3-dihydroindol-1-yl, and R.sup.2, R.sup.4 and R.sup.5 are all hydrogen, R.sup.1 is not methyl;(ii) when R.sup.3 is phenyl or naphthyl, R.sup.1 is not --NR.sup.6 R.sup.7 ;(iii) when R.sup.3 is phenyl, R.sup.2 is not lower alkoxy, and R.sup.1 and R.sup.2 are not halo;(iv) when R.sup.3 is phenyl and R.sup.1 is H, R.sup.2 is not methyl; and(v) when R.sup.3 is 1,2,3,4-tetrahydroquinolinyl, R.sup.4 and R.sup.5 are hydrogen;or a pharmaceutically acceptable salt or N-oxide thereof.

    摘要翻译： 芳基嘧啶衍生物及其药学上可接受的盐和N-氧化物显示出有用的药理学性质，包括作为选择性5HT2B拮抗剂的用途。 5-HT2B拮抗剂是下式的化合物：其中：R 1是氢，烷基，低级烷氧基，羟基烷基，环烷基，环烷基低级烷基，烯基，低级硫代烷氧基，卤素，氟代烷基，-NR 6 R 7，-CO 2 R 8，-O ）n R 9或任选被羟基，烷氧基，卤素或芳基取代的低级烷基; 其中n为1,2或3; R6和R7是氢或低级烷基; R8是氢或低级烷基; 且R 9为氢，低级烷基，羟基，羟基低级烷基，低级烯基或低级烷氧基; R2是氢，低级烷基，低级烷氧基，卤素或低级氟代烷基; R 3是除吡啶基，噻吩基或呋喃基以外的任选取代的芳基; R4是氢，低级烷基，环烷基，烯基，酰基，氨基，酰氨基，芳基， - （CH2）mNR10R11或任选被氨基，单取代的氨基，二取代的氨基，羟基，羧基，芳基，低级烷氧基， 烷氧基羰基，四氢呋喃-2-基，羟基烷氧基或磺酰氨基; 其中R10和R11是氢或低级烷基; R5是氢或低级烷基; 条件是：（i）当R 3是萘基，吲哚-1-基或2,3-二氢吲哚-1-基时，R 2，R 4和R 5都是氢，R 1不是甲基; （ii）当R3是苯基或萘基时，R1不是-NR6R7; （iii）当R3是苯基时，R2不是低级烷氧基，R1和R2不是卤素; （iv）当R3是苯基且R1是H时，R2不是甲基; 和（v）当R 3是1,2,3,4-四氢喹啉基时，R 4和R 5是氢; 或其药学上可接受的盐或N-氧化物。