发明名称 Diarylamino diazine and triazine derivatives are telomerase inhibitors and G-quadruplex stabilizers, useful in the treatment of cancers
摘要 Arylamine derivatives (I) and their salts, especially (I'), which are capable of fixing the G-quadruplex structure of telomers. Arylamine derivatives of formula N-containing aromatic ring - NR<3> - dividing group - NR'<3> - aromatic ring (I) and their salts, which are capable of fixing the G-quadruplex structure of telomers. N-containing aromatic ring = quinoline optionally substituted by N(Ra)(Rb), or 1-4C alkoxy, quinolinium, benzamidine, or pyridine; Ra and Rb = H or 1-4C alkyl or alkoxy; aromatic ring = N-containing aromatic ring as defined above, phenyl optionally substituted by a halo, 1-4C alkoxy, CN, carbonylamino optionally substituted by one or two 1-4C alkyl groups, guanyl, 1-4C alkylthio, amino, 1-4C mono- or dialkyl amino, NO2, 1-4C alkylene amino, or 2-4C alkenylene amino, or a mono- di- or tri-cyclic heterocyclic ring having 0-2 hetero atoms per ring so at least one hetero atom is present, optionally substituted by one or more 1-4C alkyl or alkylene groups or 2-4C alkenylene groups; R<3> and R'<3> = H or 1-4C alkyl; dividing group = triazine optionally substituted by one 1-4C alkyl group, thio, oxy, amino, which may themselves be substituted by one or more 1-4C alkyl groups or halo, carbonyl, -C(=NH)-NH-C(=NH)- 3-7 alkyl diyl, or diazine optionally substituted by the same groups as for the triazine An Independent claim is also included for an arylamine derivative of formula (I') with the exception of 2-amino-bis-4,6-((4'-amino-6'-quinaldinyl)amino)triazine dihydrochloride and 2-amino-bis-4,6-(p-amidino anilino) triazine. A = NR<1>R<2>, OR<1>, SR<1>, 1-4C alkyl, CF3, H, F, Cl, Br, or I; R<1>, R<2> = H or 1-4C alkyl; R<3> and R'<3> = H or 1-4C alkyl; Ar<1> and Ar<2> when they are identical = quinoline optionally substituted by N(Ra)(Rb), or 1-4C alkoxy, quinolinium, benzamidine, or pyridine attached through the 4-position or fused with an aryl or heteroaryl group and optionally substituted by 1-4C alkyl; Ar1, Ar2, when they are different = a group as defined above, or Ar2 may be phenyl optionally substituted by one halo, 1-4C alkoxy, CN, carbonylamino optionally substituted by one or two 1-4C alkyl groups, guanyl, 1-4C alkylthio or alkylamino, amino, di-(1-4C alkyl)amino, NO2, 1-4C alkylene amino or 2-4C alkenylene amino, or a mono- di- or tri-cyclic heterocyclic ring as defined above.
申请公布号 FR2801588(A1) 申请公布日期 2001.06.01
申请号 FR19990015031 申请日期 1999.11.29
申请人 AVENTIS PHARMA S.A. 发明人 MAILLIET PATRICK;RIOU JEAN FRANCOIS;MERGNY JEAN LOUIS;LAOUI ABDELAZIZE;LAVELLE FRANCOIS;PETITGENET ODILE
分类号 A61P35/00;C07D215/42;C07D215/46;C07D251/70;C07D401/12;C07D401/14 主分类号 A61P35/00
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