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    Novel 2,3-Dihydro-1H-imidazopyrimidin-5-one and this 1,2,3,4-tetrahydropyrimidopyrimidin-6-one Derivatives Comprising a Substituted Morpholine, Preparation Thereof and Pharmaceutical Use Thereof
    6.
    发明申请
    Novel 2,3-Dihydro-1H-imidazopyrimidin-5-one and this 1,2,3,4-tetrahydropyrimidopyrimidin-6-one Derivatives Comprising a Substituted Morpholine, Preparation Thereof and Pharmaceutical Use Thereof 审中-公开
    新的2,3-二氢-1H-咪唑并嘧啶-5-酮和该1,2,3,4-四氢嘧啶并嘧啶-6-酮衍生物包括取代的吗啉，其制备方法及其药物用途

    公开(公告)号：US20150148328A1

    公开(公告)日：2015-05-28

    申请号：US14409964

    申请日：2013-06-21

    Applicant: SANOFI

    Inventor： Youssef El-Ahmad ,  Bruno Filoche-Romme ,  Jean-Philippe Letallec ,  Gilbert Marciniak ,  Baptiste Ronan ,  Bertrand Vivet ,  Maurice Brollo

    IPC: C07D519/00 ,  A61K31/5386 ,  A61K45/06 ,  A61K31/55 ,  C07D487/04 ,  A61K31/5377

    CPC classification number: C07D519/00 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/55 ,  A61K45/06 ,  C07D233/46 ,  C07D239/14 ,  C07D239/70 ,  C07D295/04 ,  C07D471/04 ,  C07D487/04

    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)═N—ORc, —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.

    Abstract translation: 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; - （CH 2）m -R a; 亚烷基 环烷基 杂环烷基; 烷基; -SO 2 -Rb; -核心; m = 1或2; R a =芳基，杂芳基，-CO-环烷基，-CO-杂环烷基，-CO-R b，-C（R b）= N-OR c，-CO 2 R d，-CONR x R y; Rb =烷基，芳基，杂芳基; Rc = H，烷基; Rd =烷基，环烷基; Re =烷基，环烷基，芳基，杂芳基; 具有Rx，R y = H，烷基，环烷基，烷氧基，苯基或与具有任选的O，N的N a环形成的NR x R y; R 2，R 3 = H，烷基，CF 3或具有任选O，S和N的C a环的形式; R4 = H，F，Cl，CH3或CN; 吗啉被Me取代，并任选被F，OH取代; 或者是（式1a）和构型R，R（式1b）的异构体，这些产物是全部异构体形式和盐，作为药物，特别是作为抗癌药物。

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