发明名称 Pyrazolylbenzimidazole derivatives, compositions containing them and use thereof
摘要 The disclosure relates to compounds of formula (I):; wherein R1, R2, R3, R4, and R5 are as defined in the disclosure, to the compositions containing them and to the use thereof as medicaments, in particular as anticancer agents. The disclosure also relates to the process for preparing the compounds of formula (I) and to reaction intermediates.
申请公布号 US9126969(B2) 申请公布日期 2015.09.08
申请号 US200812338176 申请日期 2008.12.18
申请人 AVENTIS PHARMA S.A. 发明人 Cherrier Marie-Pierre;Parmantier Eric;Minoux Hervé;Clerc François;Angouillant-Boniface Odile;Brollo Maurice;Schio Laurent
分类号 C07D413/14;C07D401/14;C07D235/04;C07D403/04;C07D403/14;C07D405/14 主分类号 C07D413/14
代理机构 Morrison & Foerster LLP 代理人 Morrison & Foerster LLP
主权项 1. A compound of general formula (I) below: in which: R1 and R4 are independently selected from the group consisting of H, Me, Et, CO2Rc, CH2ORc, ORc, F, Cl and C(═O)NH(Rd); in which Rc is chosen from H, (C1-C6)alkyl, substituted (C1-C6)alkyl, (C3-C7)cycloalkyl, substituted (C3-C7)cycloalkyl, aryl, substituted aryl, heteroaryl and substituted heteroaryl; and in which Rd is chosen from H, (C1-C6)alkyl, substituted (C1-C6)alkyl, (C3-C7)cycloalkyl, substituted (C3-C7)cycloalkyl, and optionally substituted (C3-C7)heterocycloalkyl comprising from 1 to 3 heteroatoms chosen from N, O and S; R3 is O(CH2)nN(Me)2 with n=2, 3 or 4, or NH(CH2)2N(Me)2; and R2 is F; R5 is selected from the group consisting of NMe(Et), NH(iPr), N(Et)2, N(iPr)2, NEt(iPr), pyrrolidinyl, piperidinyl, morpholinyl, N-methylpiperazinyl, NH(Cy), N(Cy)2, NMe(iPr), NH(tBu), NH(iBu), N(nBu)2, piperazinyl, NH(Et), N(nPr)2 and NEt(iPr);or a salt thereof.
地址 Antony FR