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    2-amino-N- [[4-(aminocarbonyl)pyrimidin-2-yl]amino]-alkyl]pyrimidine-4-carboxamide derivatives, their preparation and pharmaceutical compositions containing them
    7.
    发明授权
    2-amino-N- [[4-(aminocarbonyl)pyrimidin-2-yl]amino]-alkyl]pyrimidine-4-carboxamide derivatives, their preparation and pharmaceutical compositions containing them 失效
    2-氨基-N - [[4-（氨基羰基）嘧啶-2-基]氨基] - 烷基]嘧啶-4-甲酰胺衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US5330985A

    公开(公告)日：1994-07-19

    申请号：US84493

    申请日：1993-07-01

    申请人： Pascal George ,  Benoit Marabout ,  Jacques Froissant ,  Jean Pierre Merly

    发明人： Pascal George ,  Benoit Marabout ,  Jacques Froissant ,  Jean Pierre Merly

    IPC分类号： A61K31/505 ,  A61K9/08 ,  A61K9/20 ,  A61K31/506 ,  A61P13/02 ,  A61P13/08 ,  A61P15/00 ,  A61P43/00 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/495 ,  A61K31/50 ,  C07D403/02 ,  C07D403/06

    CPC分类号： C07D239/42 ,  C07D401/14

    摘要： A compound which is a pyrimidine-4-carboxamide derivative of the general formula (I) ##STR1## in which n is 0 or 1, m is 0 or 1,R.sub.1 represents a methyl group whenR.sub.2 represents a phenoxy(C.sub.1 -C.sub.4)alkyl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), orR.sub.1 and R.sub.2 form together with the nitrogen atom to which they are attached a 4-phenoxypiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), a phenoxymethylpiperidin-1-yl group (in which the phenoxy group optionally carries 1 or 2 C.sub.1 -C.sub.4 alkyl groups) or a 4-phenylpiperazin-1-yl group (in which the phenyl group optionally carries 1 or 2 substituents selected from halogen atoms and methoxy groups), and R.sub.3 represents a hydrogen atom or only when n is 1 a hydroxyl group or a methoxy group, or is an addition salt thereof with an acid, is useful as an .alpha.-adrenergic antagonist.

    摘要翻译： 作为通式（I）的嘧啶-4-甲酰胺衍生物的化合物，其中n为0或1，m为0或1，当R 2表示 苯氧基（C 1 -C 4）烷基（其中苯氧基任选地带有1或2个选自卤素原子和甲氧基的取代基），或者R 1和R 2与它们所连接的氮原子一起形成4-苯氧基哌啶-1 （其中苯氧基任选地带有1或2个选自卤素原子和甲氧基的取代基），苯氧基甲基哌啶-1-基（其中苯氧基任选地带有1或2个C 1 -C 4烷基）或 4-苯基哌嗪-1-基（其中苯基任选地带有1或2个选自卤素原子和甲氧基的取代基），并且R 3表示氢原子或仅当n为1时为羟基或甲氧基，或 是其与酸的加成盐，可用作α-肾上腺素能拮抗剂。

    2-aminopyrimidine-4-carboxamide derivatives, their preparaton and their application in therapy
    9.
    发明授权
    2-aminopyrimidine-4-carboxamide derivatives, their preparaton and their application in therapy 失效
    2-氨基嘧啶-4-羧酰胺衍生物及其制剂及其在治疗中的应用

    公开(公告)号：US5229392A

    公开(公告)日：1993-07-20

    申请号：US872028

    申请日：1992-04-23

    申请人： Pascal George ,  Philippe Manoury ,  Michel Mangane ,  Jean-Pierre Merly

    发明人： Pascal George ,  Philippe Manoury ,  Michel Mangane ,  Jean-Pierre Merly

    IPC分类号： A61K31/505 ,  A61P13/02 ,  A61P15/00 ,  A61P43/00 ,  C07D239/42

    CPC分类号： C07D239/42

    摘要： A compound which is a 2-aminopyrimidine-4-carboxamide derivative represented by general formula (I) ##STR1## in which m represents 2 or 3,n represents 2 or 3,R.sub.1 represents hydrogen or methyl, andX represents a substituent selected from the group consisting of hydrogen, fluorine, chlorine, methoxy, ethoxy, methyl and 1-methylethyl, with the proviso that more than one substituent X may be present in which case each X may be the same or different, or a pharmaceutically acceptable acid addition salt thereof.

    摘要翻译： 作为通式（I）表示的2-氨基嘧啶-4-甲酰胺衍生物的化合物，其中m表示2或3，n表示2或3，R 1表示氢或甲基，X表示 选自氢，氟，氯，甲氧基，乙氧基，甲基和1-甲基乙基的取代基，条件是可以存在多于一个取代基X，在这种情况下，每个X可以相同或不同，或药学上 其可接受的酸加成盐。

    3-(acylaminomethyl)imidazo[1,2-a]pyridine derivatives and their application in therapy
    10.
    发明授权
    3-(acylaminomethyl)imidazo[1,2-a]pyridine derivatives and their application in therapy 失效
    3-（酰氨基甲基）咪唑并[1,2-a]吡啶衍生物及其在治疗中的应用

    公开(公告)号：US4990506A

    公开(公告)日：1991-02-05

    申请号：US425870

    申请日：1989-10-24

    申请人： Pascal George ,  Claudie Giron ,  Jacques Froissant

    发明人： Pascal George ,  Claudie Giron ,  Jacques Froissant

    IPC分类号： C07D471/04

    CPC分类号： C07D471/04

    摘要： A compound which is a 3-(acylaminomethyl)imidazo[1,2-a]pyridine derivative of formula (I) ##STR1## in which R.sub.1 denotes hydrogen; linear or branched C.sub.1 -C.sub.4 alkyl; or benzyl;R.sub.2 denotes linear or branched C.sub.1 -C.sub.6 alkyl; cyclohexyl; trichloromethyl; 1-propenyl; allyl; phenyl; 4-chlorophenyl; or benzyl:or R.sub.1 and R.sub.2 together denote a C.sub.3 -C.sub.5 aliphatic chain:X denotes halogen; C.sub.1 -C.sub.3 alkyl; methylthio; trifluoromethyl; optionally esterified carboxy of formula --COOR in which R denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.3 R.sub.4 in which R.sub.3 and R.sub.4 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--; alkylamino of formula NHR.sub.5 in which R.sub.5 denotes C.sub.2 -C.sub.6 alkyl; or dialkylamino of formula --NR.sub.6 R.sub.7 in which R.sub.6 and R.sub.7 independently denote C.sub.2 -C.sub.6 alkyl or together denote a chain of formula --(CH.sub.2).sub.2 --Z--(CH.sub.2).sub.2 -- in which Z denotes a direct bond, oxygen, sulphur, or a divalent group of formula --CH.sub.2 --, --NH-- or --N(C.sub.1 -C.sub.4 alkyl)--: and Y denotes hydrogen; halogen; methyl; trifluoromethyl; optionally esterified carboxy of formula --COOR.sub.8 in which R.sub.8 denotes hydrogen or C.sub.1 -C.sub.6 alkyl; cyano; optionally mono- or dialkylated aminocarbonyl of formula --CONR.sub.9 R.sub.10 in which R.sub.9 and R.sub.10 independently hydrogen or C.sub.1 -C.sub.4 alkyl; or optionally mono- or dialkylated amino of formula --NR.sub.11 R.sub.12 in which R.sub.11 and R.sub.12 independently denote hydrogen or C.sub.1 -C.sub.4 alkyl: with the exclusion of compounds in which X denotes halogen; alkyl; or methylthio and Y denotes hydrogen; halogen; or methyl:or a pharmacologically acceptable acid addition salt is useful in therapy.

    摘要翻译： 化合物，其是式（I）的3-（酰氨基甲基）咪唑并[1,2-a]吡啶衍生物，其中R1表示氢; 直链或支链C 1 -C 4烷基; 或苄基; R2表示直链或支链C 1 -C 6烷基; 环己基 三氯甲基 1-丙烯基; 烯丙基 苯基; 4-氯苯基; 或苄基：或R 1和R 2一起表示C 3 -C 5脂族链：X表示卤素; C1-C3烷基; 甲硫基 三氟甲基 任选的式-COOR的酯化羧基，其中R表示氢或C 1 -C 6烷基; 氰基; 任选的式-CONR 3 R 4的单或二烷基化氨基羰基，其中R 3和R 4独立地表示氢或C 1 -C 4烷基或一起表示式 - （CH 2）2 -Z-（CH 2）2 - 的链，其中Z表示直接键 ，氧，硫或式-CH 2 - ， - NH-或-N（C 1 -C 4烷基） - 的二价基团。 式NHR5的烷基氨基，其中R 5表示C 2 -C 6烷基; 或式-NR6R7的二烷基氨基，其中R6和R7独立地表示C2-C6烷基或一起表示式 - （CH2）2-Z-（CH2）2-的链，其中Z表示直接键，氧，硫或 式为-CH 2 - ， - NH-或-N（C 1 -C 4烷基） - 的二价基团，Y表示氢; 卤素; 甲基; 三氟甲基 任选的式-COOR 8的酯化羧基，其中R 8表示氢或C 1 -C 6烷基; 氰基; 任选的式-CONR 9 R 10的单或二烷基化氨基羰基，其中R 9和R 10独立地是氢或C 1 -C 4烷基; 或任选的式-NR 11 R 12的单或二烷基化氨基，其中R 11和R 12独立地表示氢或C 1 -C 4烷基：排除其中X表示卤素的化合物; 烷基; 或甲硫基，Y表示氢; 卤素; 或甲基：或药理学上可接受的酸加成盐可用于治疗。