发明名称 PYRIMIDOOXAZOCINE DERIVATIVES AS MTOR - INHIBITORS
摘要 The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.;
申请公布号 US2014378433(A1) 申请公布日期 2014.12.25
申请号 US201314374838 申请日期 2013.01.25
申请人 SANOFI 发明人 Braun Alain;Crespin Olivier;Foricher Yann;Marciniak Gilbert;Muzet Nicolas;Nicolai Eric;Pascal Cecile;Vivet Bertrand;Viviani Fabrice
分类号 C07D498/04;C07D519/00 主分类号 C07D498/04
代理机构 代理人
主权项 1. Compound corresponding to formula (I):in which: each of the radicals R1 independently represents a group (C1-C6)-alkyl, it being understood that two groups R1 borne by two different carbon atoms of the morpholinyl ring may be linked together to form, with the morpholinyl ring, a bicyclic heterocyclic structure, R2 and R3 independently represent: H, or a group (C1-C6) alkyl, R4 represents: H,a group (C1-C6)-alkyl, optionally substituted with a hydroxyl group,a group (C1-C6)-alkoxy,a group -L1-R10, in which:L1 represents a group (C1-C6)-alkylene,R10 represents a group chosen from —COOR11, —CO—R12, —OR13, —CONR14R15 and a 5- or 6-atom heterocycle optionally substituted with a group —R16, —COOR17, —CO—R18, —OR19 or —NR20R21, ora 5- or 6-atom heterocycle optionally substituted with a group —R22, —COOR23, —CO—R24, —OR25 or —CONR26R27, G1 represents a divalent phenyl or 5- to 6-atom heteroaryl radical, optionally substituted with 1 to 4 groups R5 independently chosen from a halogen atom, a group —OR30 and a group —(C1-C6)-alkyl optionally substituted with a hydroxyl, X1 represents a group —O— or —NR40—, X2 represents a single bond or a group —CONR50—, —CONR51—O—, —COO—, —CO— or —SO2—, R6 represents: H,a group -L2-R7, in which:-L2- represents a group (C1-C6)-alkylene or (C3-C6)-cycloalkylene,R7 represents a group chosen from:H,OR60,a halogen atom,a group (C1-C6)-haloalkyl,a 5- to 6-atom heterocycle optionally substituted with one or more groups chosen from a group (C1-C6)-alkyl, a group (C1-C6)-alkoxy and a group ═O, ora group -G2-X3-G3, in which:X3 represents a single bond or a group —O—, —CO— or —CH2—,G2 represents a single bond or a 5- to 6-atom divalent cyclic radical optionally substituted with one or more groups R80,G3 represents a 4- to 8-atom ring optionally substituted with one or more groups R81,or -G2-X3-G3 together form a 7- to 10-atom fused bicycle,each radical R80 and each radical R81 is independently chosen from:a halogen atom,a group —COOR70, —CO—R71, —OR72, —NR73R74, —CONR75R76, —CN or —S(O)p—R77,a group (C1-C6)-alkyl optionally substituted with one or more groups R100 and/or optionally interrupted with one or more oxygen atoms,a group (C1-C6)-alkoxy optionally substituted with one or more groups R101 and/or optionally interrupted with one or more oxygen atoms, n represents 0, 1 or 2, m represents 0 or 1, p represents 0, 1 or 2, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R30, R40, R50, R51, R60, R70, R71, R72, R73, R74, R75, R76 and R77 independently represent H or a group (C1-C6)-alkyl optionally substituted with a group R90 and/or optionally interrupted with one or more oxygen atoms, R90 represents a group —OR91 or —NR92R93, R91, R92 and R93 independently represent H or a group (C1-C6)-alkyl, R100 and R101 are independently chosen from a halogen atom and a hydroxyl in the form of the base or of an acid-addition salt.
地址 Paris FR