- Patent Title: 2,3-dihydro-1H-imidazo{1,2-a}pyrimidin-5-one and this 1,2,3,4-tetrahydropyrimido{1,2-a}pyrimidin-6-one derivatives comprising a substituted morpholine, preparation thereof and pharmaceutical use thereof
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Application No.: US14409964Application Date: 2013-06-21
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Publication No.: US10253043B2Publication Date: 2019-04-09
- Inventor: Youssef El-Ahmad , Bruno Filoche-Romme , Jean-Philippe Letallec , Gilbert Marciniak , Baptiste Ronan , Bertrand Vivet , Maurice Brollo
- Applicant: SANOFI
- Applicant Address: FR Paris
- Assignee: SANOFI
- Current Assignee: SANOFI
- Current Assignee Address: FR Paris
- Agency: McDonnell Boehnen Hulbert & Berghoff LLP
- Priority: FR1255917 20120622
- International Application: PCT/IB2013/055099 WO 20130621
- International Announcement: WO2013/190510 WO 20131227
- Main IPC: C07D519/00
- IPC: C07D519/00 ; C07D233/46 ; C07D239/14 ; C07D239/70 ; C07D471/04 ; C07D487/04 ; C07D295/04 ; A61K31/5377 ; A61K31/5386 ; A61K31/55 ; A61K45/06

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.
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