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    Pyrimidine compounds
    124.
    发明公开
    Pyrimidine compounds 失效
    吡嗪化合物

    公开(公告)号：EP0180298A3

    公开(公告)日：1987-01-21

    申请号：EP85305902

    申请日：1985-08-20

    申请人： SMITH KLINE & FRENCH LABORATORIES LIMITED

    发明人： Brown, Thomas Henry ,  Durant, Graham John

    IPC分类号： C07D239/52 ,  C07D239/54 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  A61K31/505

    CPC分类号： C07D239/54 ,  C07D239/52 ,  C07D239/545 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： Compounds of the formula (I) :-
    (1) and their salts are histamine H,-antagonists, wher in: R° is 2-guanidinothiazol-4-yl or a group R 1 R 2 N(CH n -Z-wherein R 1 and R 2 are independently hydrogen, C 1-6 alkyl, phenyl(C 1-6 )alkyl, furanyl(C 1-6 )alkyl, thienyl(C 1-8 )alkyl, C 3-10 cycloalkyl, hydroxy( C2-6 )alkyl, or halo(C 2-6 )alkyl (wherein said hydroxy and halo groups are not substituted on the carbon atom adjacent to the nitrogen atom); or R 1 and R 2 together represent - (OH 2 ) r - wherein r is 4 to 7, to form together with the nitrogen atom to which they are attached a 5-8 membered saturated ring; n is an integer from 1 to 6; Z is 2,5-furanyl, 2,5-thienyl, 2,4-pyridyl wherein the R 1 R 2 N(CH 2 ) n group is in the 4-position, 2,4-thiazolyl wherein the R 1 R 2 N(CH 2 ) n group is in the 2-position, or 1,3- or 1,4-phenylene; m is one; or if Z is pyridyl or phenylene m may also be zero; Y is oxygen, sulphur or methylene; or if Z is furanyl, thienyl or thiazolyl Y may also be a bond; p is two, three or four; q is zero c one; R 3 is hydrogen or C 1-6 alkyl; and R 4 is hydrogen, optionally substituted C 1-6 alkyl, C 3-10 -cycloalkyl, C 3 - 10CY - cloalkyl(C 1-6 )alkyl, C 2-6 alkenyl or C 2-6 alkynyl,and when q is zero R 4 may also be -(CH,) s B wherein s is 1 to 6 and B is optionally substituted aryl or heteroaryl. Pharmaceutical compositions containing them are described as are processes for their preparation.

    3-Aryluracile und deren Verwendung zur Unkrautbekämpfung
    125.
    发明公开
    3-Aryluracile und deren Verwendung zur Unkrautbekämpfung 失效
    3-Aryluracile und deren Verwendung zurUnkrautbekämpfung。

    公开(公告)号：EP0195346A2

    公开(公告)日：1986-09-24

    申请号：EP86103188.8

    申请日：1986-03-10

    申请人： CIBA-GEIGY AG

    发明人： Wenger, Jean, Dr. ,  Winternitz, Paul, Dr.

    IPC分类号： C07D239/54 ,  C07D239/70 ,  C07D239/96 ,  C07D239/56 ,  C07D491/04 ,  C07D495/04 ,  A01N43/54 ,  C07C273/04 ,  C07C335/06

    CPC分类号： C07D239/47 ,  A01N43/54 ,  A01N47/16 ,  C07D239/54 ,  C07D239/545 ,  C07D239/553 ,  C07D239/557 ,  C07D239/56 ,  C07D239/70 ,  C07D239/96 ,  C07D491/04 ,  C07D495/04 ,  Y02P20/142

    摘要： Die Erfindung betrifft neue 3-Aryluracile der Formel
    worin R', R 2 , R 3 , R 4 , R 5 , R` und X die in der Beschreibung angegebenen Bedeutungen besitzen, sowie Salze davon und deren Herstellung, Unkrautbekämpfungsmittel, die solche Verbindungen als Wirkstoffe enthalten, und die Verwendung der Wirkstoffe bzw. Mittel zur Unkrautbekämpfung. Die Erfindung betrifft ebenfalls gewisse herbizid wirksame Ausgangsmaterialien und diese enthaltende Unkrautbekämpfungsmittel.

    摘要翻译： 3-芳基脲衍生物。 式（I）化合物及其盐，其中R 1和/或R 2 = H是新的：R 1 = H; 1-4C烷基; 2-4C烯基或炔基; 2-6C烷氧基烷基，烷酰基或烷氧基羰基或甲酰基; R2 = H; 1-6C烷基; 2-4C烯基或炔基; 或2-6C烷氧基烷基; R3 =卤素或NO2; R4 = H或卤素; R5 = H，卤素，1-4C烷基，ClCH2，BrCH2，HOCH2，1-5C（烷氧基或烷硫基）甲基，CN，NO2或硫氰酸酯; R6 = H或1-4C烷基（选自F）; 或R 5和R 6一起为三或四亚甲基，其中CH 2可以被O或S替代，并且环可以被取代。 1-3C烷基; X = O或S; （1）如果R5 = F，则R6不能为H; （2）如果R5 = CN，R6必须是H或1-4C烷基，X = S。 式（I）的中间体也是新的：R2'=除H以外的R2; R'5 = H，F或1-4C烷基，或与R6完成环; R7 = 1-4C烷基。 -

    Pyrimidine derivatives, preparation thereof and use thereof
    127.
    发明公开
    Pyrimidine derivatives, preparation thereof and use thereof 失效
    嘧啶衍生物，其制备及其应用。

    公开(公告)号：EP0123402A2

    公开(公告)日：1984-10-31

    申请号：EP84301741.9

    申请日：1984-03-14

    申请人： FUJISAWA PHARMACEUTICAL CO., LTD.

    发明人： Takaya, Takao ,  Murata, Masayoshi ,  Ito, Kiyotaka

    IPC分类号： C07D239/46 ,  C07D239/52 ,  C07D239/54 ,  C07D239/56 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  A61K31/505

    CPC分类号： C07D239/47

    摘要： New pyrimidine derivatives of the formula:
    wherein Z is a group selected from
    in which R 1 and R 2 are each hydrogen, alkenyl, ar (lower) alkyl or lower alkyl optionally substituted with epoxy, hydroxy, amino and/or lower alkylamino and R 5 is lower alkyl,

    R' is hydrogen, aryl optionally substituted with lower alkyl, lower alkoxy a nd/o r halogen, or pyridyl optionally substituted with lower alkyl,
    R 4 is hydrogen, lower alkyl or phenyl optionally substituted with lower alkoxy, and
    Y is =0, =S or =N-R 6 ,
    in which R 6 is lower alkyl; cyclo(lower)alkyl; ar(lower)alkyl optionally substituted with lower alkoxy; N-containing unsaturated heterocyclic group optionally substituted with lower alkyl; or aryl optionally substituted with hydroxy, lower alkyl, halogen or lower alkoxy, in which lower alkoxy substituent may be substituted with epoxy, hydroxy, amino and/or lower alkylamino,
    provided that Y is =N-R 6 when R 5 and R 4 are each hydrogen, and Y is =S or =N-R 6 when R' and R 2 are each hy d - rogen or lower alkyl and R 5 is phenyl, and pharmaceutically acceptable salts thereof, and processes for preparation thereof nad pharmaceutical composition comprising the same.

    These derivatives and salts thereof are useful as cardiotonic, antihypertensive agent, cerebrovascularvasodilator and anti-platelet agent.