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14 条记录 (耗时 0.025 秒)

    2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapeutics
    1.
    发明授权
    2-aminopyrimidine-4-carboxamide derivatives, their preparation and their use in therapeutics 失效
    2-氨基嘧啶-4-羧酰胺衍生物，其制备及其在治疗中的应用

    公开(公告)号：US5246939A

    公开(公告)日：1993-09-21

    申请号：US903977

    申请日：1992-06-26

    申请人： Pascal George ,  Christian Maloizel ,  Benoit Marabout ,  Jean-Pierre Merly

    发明人： Pascal George ,  Christian Maloizel ,  Benoit Marabout ,  Jean-Pierre Merly

    IPC分类号： A61K31/505 ,  A61K31/506 ,  A61P13/00 ,  A61P13/02 ,  A61P13/08 ,  A61P15/00 ,  C07D211/56 ,  C07D239/42 ,  C07D295/08 ,  C07D401/12 ,  C07D403/12

    CPC分类号： C07D401/12

    摘要： A compound which is a 2-aminopyrimidine carboxamide derivative represented by formula (I) ##STR1## in which X represents hydrogen, fluorine, chlorine, methyl, 1-methylethyl or methoxy, with the proviso that more than one substituent X may be present in which case each X may be the same or different,n represents 2 or 3,m represents 1, in which case p represents 1, or elsem represents 0, in which case p represents 2,q represents 0 or 1, andR.sub.1 represents a hydrogen atom;or a pharmaceutically acceptable acid addition salt thereof.A compound of formula (I) has .alpha..sub.1 -adrenergic receptor antagonist activity and is useful as a therapeutic substance.

    摘要翻译： 作为式（I）表示的2-氨基嘧啶甲酰胺衍生物的化合物，其中X表示氢，氟，氯，甲基，1-甲基乙基或甲氧基，条件是多于一个取代基X可以 在这种情况下，每个X可以相同或不同，n表示2或3，m表示1，在这种情况下p表示1，或者m表示0，在这种情况下p表示2，q表示0或1， R1表示氢原子。 或其药学上可接受的酸加成盐。 式（I）化合物具有α1-肾上腺素能受体拮抗剂活性，可用作治疗物质。

    2-((4-Piperidyl)methyl)-1,2,3,4-tetrahydroisoquinoline derivatives, their preparation and their application in therapy
    4.
    发明授权
    2-((4-Piperidyl)methyl)-1,2,3,4-tetrahydroisoquinoline derivatives, their preparation and their application in therapy 失效
    2 - （（4-哌啶基）甲基）-1,2,3,4-四氢异喹啉衍生物，其制备及其在治疗中的应用

    公开(公告)号：US4885302A

    公开(公告)日：1989-12-05

    申请号：US228748

    申请日：1988-08-05

    申请人： Pascal George ,  Mireille Sevrin ,  Christian Maloizel

    发明人： Pascal George ,  Mireille Sevrin ,  Christian Maloizel

    IPC分类号： A61K31/47 ,  A61K31/475 ,  A61P9/00 ,  A61P9/12 ,  A61P25/04 ,  A61P25/20 ,  A61P25/24 ,  A61P25/26 ,  C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

    摘要： A compound of formula (I) ##STR1## in which R is (a) a hydrogen atom;(b) a linear or branched (C.sub.1 -C.sub.6) alkyl group; an allyl group; a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a phenylmethyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, amino, dimethylamino, cyano, aminocarbonyl, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 2-phenylethyl group; a 3-phenylpropyl group; a 3-phenyl-2-propenyl group; a phenylcarbonylmethyl group; a naphthylmethyl group; a pyridylmethyl group; a furylmethyl group; or a thienylmethyl group; or(c) a linear or branched (C.sub.2 -C.sub.6) alkanoyl group; a cycloalkylcarbonyl group in which the cycloalkyl moiety has from 3 to 6 carbon atoms; a trifluoroacetyl group; a phenyl-carbonyl group unsubstituted or substituted with one to three substituents chosen from halogen atoms and trifluoromethyl, nitro, linear or branched (C.sub.1 -C.sub.3) alkyl, linear or branched (C.sub.1 -C.sub.3) alkoxy and linear or branched (C.sub.1 -C.sub.3) alkylthio groups; a 1-oxo-3-phenyl-2-propenyl group; a naphthylcarbonyl group; a pyridylcarbonyl group; a furylcarbonyl group; a thienylcarbonyl group; a (2-indolyl)-carbonyl group; or a (5-indolyl)carbonyl group; or a pharmacologically acceptable acid addition salt thereof.

    摘要翻译： 式（I）化合物其中R为（a）氢原子; （b）直链或支链（C1-C6）烷基; 烯丙基; 环烷基甲基，其中环烷基部分具有3至6个碳原子; 未取代或被一至三个选自卤素原子和三氟甲基，硝基，氨基，二甲基氨基，氰基，氨基羰基，直链或支链（C 1 -C 3）烷基，直链或支链（C 1 -C 3）烷氧基和直链或支链 支链（C1-C3）烷硫基; 2-苯基乙基; 3-苯基丙基; 3-苯基-2-丙烯基; 苯基羰基甲基; 萘基甲基; 吡啶基甲基; 呋喃甲基; 或噻吩甲基; 或（c）直链或支链（C 2 -C 6）烷酰基; 环烷基部分具有3至6个碳原子的环烷基羰基; 三氟乙酰基; 直链或支链（C1-C3）烷基，直链或支链（C1-C3）烷氧基和直链或支链的（C1-C3）烷基， 烷硫基; 1-氧代-3-苯基-2-丙烯基; 萘基羰基; 吡啶基羰基; 呋喃基羰基; 噻吩基羰基; （2-吲哚基） - 羰基; 或（5-吲哚基）羰基; 或其药理学上可接受的酸加成盐。