首页> 外国专利> NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF

NOVEL 2,3-DIHYDRO-1H-IMIDAZO{1,2-a}PYRIMIDIN-5-ONE and this1,2,3,4-TETRAHYDROPYRIMIDO{1,2-a}PYRIMIDIN-6-ONE DERIVATIVES COMPRISING A SUBSTITUTED MORPHOLINE, PREPARATION THEREOF AND PHARMACEUTICAL USE THEREOF

机译:新型2,3-二氢-1H-咪唑并{1,2-a}吡咯烷酮-5-一和该1,2,3,4-四氢吡咯烷酮{1,2-a}吡咯烷酮-6-一衍生物,包括取代的吗啉,制备及其医药用途

摘要

The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; (CH2)mRa; alkylene; cycloalkyl; heterocycloalkyl; alkyl; SO2 Rb; CORe; m=1 or 2; Ra=aryl, heteroaryl, CO-cycloalkyl, CO-heterocycloalkyl, CORb, C(Rb)NORc, CO 2 Rd, CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
机译:本发明涉及具有p,q = 0、1或2的式(I)的新产物。 R1 =苯基,吡啶基; (CH2)mRa;亚烷基环烷基杂环烷基烷基; SO 2 Rb;核心; m = 1或2; Ra =芳基,杂芳基,CO-环烷基,CO-杂环烷基,CORb,C(Rb)NORc,CO 2 Rd,CONRxRy; Rb =烷基,芳基,杂芳基; R c = H,烷基; Rd =烷基,环烷基; Re =烷基,环烷基,芳基,杂芳基; NR x R y与R x,R y = H,烷基,环烷基,烷氧基,苯基,或与N形成带有任选O,N的环; R 2,R 3 = H,烷基,CF 3,或与C形成具有任选的O,S和N的环; R4 = H,F,Cl,CH3或CN;吗啉被Me取代,并任选被F,OH取代;或是(式1a)和构型R,R的异构体(式1b),这些产物是所有异构体形式和盐,作为药物,特别是作为抗癌药物。

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