PYRIDOPYRIMIDONE DERIVATIVES, PREPARATION THEREOF, THERAPEUTIC USE THEREOF
    3.
    发明申请
    PYRIDOPYRIMIDONE DERIVATIVES, PREPARATION THEREOF, THERAPEUTIC USE THEREOF 失效
    吡咯烷酮衍生物,其制备方法,其治疗方法

    公开(公告)号:US20090048277A1

    公开(公告)日:2009-02-19

    申请号:US12166431

    申请日:2008-07-02

    CPC classification number: C07D471/04

    Abstract: The disclosure relates to pyrido[2,3-d]pyrimidone compounds, to the preparation thereof and to the therapeutic use thereof, wherein said compounds are of general formula (I): in the form of a base or of an addition salt with an acid which is pharmaceutically acceptable, in the form of hydrates or of solvates, and also in the form of enantiomers, diastereoisomers and a mixture thereof. The disclosure also relates to processes for preparing said compounds, to pharmaceutical compositions containing a compound of general formula (I), and to the therapeutic use of said compounds and compositions.

    Abstract translation: 本公开涉及吡啶并[2,3-d]嘧啶酮化合物,其制备方法及其治疗用途,其中所述化合物为通式(I):以碱的形式或加成盐与 其为药学上可接受的,为水合物或溶剂化物形式,也为对映异构体,非对映异构体及其混合物的形式。 本公开还涉及制备所述化合物的方法,含有通式(I)化合物的药物组合物以及所述化合物和组合物的治疗用途。

    Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof
    6.
    发明授权
    Pyrido-pyrimidine derivatives, preparation thereof, and therapeutic use thereof 有权
    吡啶并嘧啶衍生物及其制备方法及其治疗用途

    公开(公告)号:US07893259B2

    公开(公告)日:2011-02-22

    申请号:US12415256

    申请日:2009-03-31

    CPC classification number: C07D471/04

    Abstract: The disclosure concerns pyrido[2,3-d]pyrimidine derivatives, their preparation and their therapeutic application, of general formula (I): and acid addition salts, hydrates and solvates thereof, as well as in the form of enantiomers, diastereoisomers and mixtures thereof. The disclosure also concerns methods for preparing said derivatives, pharmaceutical compositions containing a compound of general formula (I), and their therapeutic use.

    Abstract translation: 本公开涉及通式(I)的吡啶并[2,3-d]嘧啶衍生物及其制备方法及其治疗应用:及其酸加成盐,水合物和溶剂化物,以及对映异构体,非对映异构体和混合物的形式 其中。 本公开还涉及制备所述衍生物的方法,含有通式(I)的化合物的药物组合物及其治疗用途。

    Dinitrogen heterocyclic derivatives N-substituted by a biphenylmethyl
group, and the pharmaceutical compositions in which they are present
    8.
    发明授权
    Dinitrogen heterocyclic derivatives N-substituted by a biphenylmethyl group, and the pharmaceutical compositions in which they are present 失效
    通过联苯甲基N-取代的二氮杂环衍生物及其存在的药物组合物

    公开(公告)号:US5268375A

    公开(公告)日:1993-12-07

    申请号:US843239

    申请日:1992-02-28

    Abstract: This invention relates to compounds of formula ##STR1## in which: R.sub.1 and R.sub.2 are similar or different and are each independently hydrogen or a group selected from CO.sub.2 N.dbd.C(NH.sub.2).sub.2, CONHNHCONH.sub.2, CONHNHCSNH.sub.2, C(OC.sub.2 H.sub.5).dbd.NCO.sub.2 CH.sub.3, COCH.sub.2 CO.sub.2 H.sub.5, N(OH)-CONHCOOC.sub.2 NCO.sub.2 CH.sub.3, COCH.sub.2 CO.sub.2 H.sub.5, N(OH)-CONHCOOC.sub.2 H.sub.5, C(OC.sub.2 H.sub.5).dbd.NH or a nitrogen heterocycle; with the proviso that at least one of the substituents R.sub.1 or R.sub.2 is other than hydrogen;R.sub.3 is a hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.2 -C.sub.6 alkenyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl, a phenylalkyl, or a phenylalkenyl;R.sub.4 and R.sub.5 are each independently a C.sub.1 -C.sub.6 alkyl, a C.sub.3 -C.sub.7 cycloalkyl, a phenyl or a phenylalkyl; orR.sub.4 and R.sub.5, bonded together, are either a group of the formula (CH.sub.2).sub.n or a group of the formula (CH.sub.2).sub.p Y (CH.sub.2).sub.q, in which Y is either an oxygen atom, or a sulfur atom, or a substituted carbon atom, or a group N-R.sub.6, in which R.sub.6 is a hydrogen, a C.sub.1 -C.sub.4 alkyl, a phenylalkyl, a C.sub.1 -C.sub.4 alkylcarbonyl, a C.sub.1 -C.sub.4 halogenoalkylcarbonyl, a C.sub.1 -C.sub.4 polyhalogenoalkylcarbonyl, a benzolyl, an .alpha.-aminoacyl or a N-protecting group, or R.sub.4 and R.sub.5, together with the carbon atom to which they are bonded, form an indane or an adamantine; p+q=m; n is an integer between 2 and 11; m is an integer between 2 and 5; X is an oxygen or a sulfur atom; and z and t are zero or z+t=1; and its salts.

    Abstract translation: 本发明涉及式(I)的化合物,其中:R 1和R 2相同或不同,各自独立地为氢或选自CO 2 N = C(NH 2)2,CONHNHCONH 2,CONHNHCSNH 2,C(OC 2 H 5)= NCO2CH3,COCH2CO2H5,N(OH)-CONHCOOC2NCO2CH3,COCH2CO2H5,N(OH)-CONHCOOC2H5,C(OC2H5)= NH或氮杂环; 条件是至少一个取代基R 1或R 2不是氢; R 3是氢,C 1 -C 6烷基,C 2 -C 6烯基,C 3 -C 7环烷基,苯基,苯基烷基或苯基烯基; R 4和R 5各自独立地为C 1 -C 6烷基,C 3 -C 7环烷基,苯基或苯基烷基; 或者R 4和R 5键合在一起,是式(CH 2)n的基团或式(CH 2)p Y(CH 2)q的基团,其中Y是氧原子或硫原子,或 取代的碳原子或基团N-R6,其中R6是氢,C1-C4烷基,苯基烷基,C1-C4烷基羰基,C1-C4卤代烷基羰基,C1-C4多卤代烷基羰基,苯甲酰基, α-氨基酰基或N-保护基,或R 4和R 5与它们所键合的碳原子一起形成二氢化茚或金刚烷; p + q = m; n是2和11之间的整数; m是2和5之间的整数; X是氧或硫原子; z和t为零或z + t = 1; 及其盐。

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