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:
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:
The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in claim 1. These compounds are pharmacologically active.
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:
The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in Claim 1. These compounds are pharmacologically active.
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。
Abstract:
Derivatives of pyrido[2,3-d]pyrimidine are provided having formula (I) with Ar1, Ar2 and R1 as defined herein, which are useful for treating cell proliferative conditions, and to the preparation thereof, and to the therapeutic application of the same.