发明公开
EP2864295A2 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
有权
新的2,3-二氢-1H-咪唑并{1,2-A}嘧啶-5-酮和1,2,3,4- TETRAHYDROPYRIMIDO- {1,2-A}嘧啶-6- ON- 与取代的吗啉，及其制备方法和药物用途及其衍生物
- 专利标题： 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
- 专利标题（中）： 新的2,3-二氢-1H-咪唑并{1,2-A}嘧啶-5-酮和1,2,3,4- TETRAHYDROPYRIMIDO- {1,2-A}嘧啶-6- ON- 与取代的吗啉，及其制备方法和药物用途及其衍生物
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申请号： EP13773341.6申请日： 2013-06-21
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公开(公告)号： EP2864295A2公开(公告)日： 2015-04-29
- 发明人: EL-AHMAD, Youssef , FILOCHE-ROMME, Bruno , LETALLEC, Jean-Philippe , MARCINIAK, Gilbert , RONAN, Baptiste , VIVET, Bertrand , BROLLO, Maurice
- 申请人： SANOFI
- 申请人地址： 54, rue La Boétie 75008 Paris FR
- 专利权人： SANOFI
- 当前专利权人： SANOFI
- 当前专利权人地址： 54, rue La Boétie 75008 Paris FR
- 代理机构： Romanowski, Caroline
- 优先权： FR1255917 20120622
- 国际公布： WO2013190510 20131227
- 主分类号： C07D233/46
- IPC分类号： C07D233/46 ; C07D239/14 ; C07D487/04 ; C07D519/00 ; A61K31/5377 ; A61P35/00
摘要：
The invention relates to the novel products of formula (I) with p, q = 0, 1 or 2; R1 = phenyl, pyridyl; -(CH
2 )
m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO
2 -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, CH
3 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.
2 )
m -Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; -SO
2 -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, CH
3 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.
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