发明名称 Tetrahydrocyclopenta[c]acridine derivatives as kinase inhibitors and biological
摘要 The invention relates to kinase inhibitors of the formula (I) in which —R1 to R4═H; ether or polyether, amino; NO2; NH-carbamate; NH—CO—R, with R such as defined above; N3 and derivatives thereof of the 1,2,3-triazole type; —R5=—OH; halogen; —OR with R such as defined above; OH-carbamate; OH-carbonate; NH2, NH-carbamate; NH—CO—R, with R such as defined above; N3 and derivatives thereof of the 1,2,3-triazole type; N(R9,R10); —R5′═H or a C1-C12 alkyl, —R6═H; R; (R or R′)3—Si, with R such as defined above; optionally substituted aryl, heteroaryl; halogen (iodine); alkynyl; —R7 and R8═H, C1-C12 alkyl; —R9 and R10═H, R (or R′) such as defined above. These compounds can be used as kinase inhibitors in particular for treating cancer.
申请公布号 US8999955(B2) 申请公布日期 2015.04.07
申请号 US200912735463 申请日期 2009.01.19
申请人 Centre National de la Recherche Scientifique 发明人 Belmont Philippe Olivier;Meijer Laurent;Cohen Philip;Patin Amaury;Bosson Johann;Goekjian Peter Gregory
分类号 C07D221/18;C07F7/10;A61K31/695;A61K31/473;C07D219/04;C07D215/14;C07D215/20;C07D219/06;C07F7/08 主分类号 C07D221/18
代理机构 Nixon & Vanderhye P.C. 代理人 Nixon & Vanderhye P.C.
主权项 1. A kinase inhibitor compound of formula (I) in which: R1 to R4, which may be identical or different, represent H; an ether radical —OR, wherein R represents a linear or branched C1-C12 alkyl radical; an amino group NH2 or N(R9, R10); NO2; NH-carbamate of —NH—CO-OM type, with M representing R or a salt; NH—CO—R; N3 or derivatives thereof with a 1,2,3-triazole cycle;R5 represents an —OH group; halogen; —OR with R as defined above with respect to R1-R4; OH-carbamate of —O—CO—NHM type, with M representing R, as defined above with respect to R1-R4; OH-carbonate of —O—CO-OM type, with M representing R, as defined above with respect to R1-R4; NH2, NH-carbamate of —NH—CO-OM type, with M representing R, or a salt; NH—CO—R with R as defined above with respect to R1-R4; N3 or derivatives thereof with a 1,2,3-triazole cycle; or N(R9, R10);R5′ represents H or a C1-C12 alkyl radical,or R5/R5′ together represents an ═O group;R6 represents H; the R radical; an (R or R′)3—Si group, R being as defined above with respect to R1-R4; an aryl radical, where appropriate substituted, a heteroaryl radical; a halogen; or an alkynyl radical —C≡C—R;R7 and R8, which may be identical or different, represent an H or a C1-C12 alkyl radical;R9 and R10, which may be identical or different, represent H or the R-radical, with the exception of the compounds in which R1-R4, R7 and R8═H, R5 and R5′ form a —C═O group, and R6═—(CH3)3—Si, —C6H5, or C1 or C4 alkyl; R1-R4, R7 and R8═H, R5═OH and R5′═H, and R6=—(CH3)3—Si, —C6H5, or C1 or C4 alkyl; R1-R4, R7 and R8═H, R5═H and R5′═OH, and R6=—(CH3)3—Si, —C6H5, or C1 or C4 alkyl; R1-R4, R7 and R8═H, R5=—OCH3 and R5′═H, and R6═C4 alkyl; and R1-R4, R7 and R8═H, R5═H and R5′=—OCH3, and R6═C4 alkyl.
地址 Paris Cedex FR