发明名称 PHOSPHOROUS DERIVATIVES AS KINASE INHIBITORS
摘要 The invention features compounds of the general formula:;;in which the variable groups are as defined herein, and to their preparation and use.
申请公布号 US2015225436(A1) 申请公布日期 2015.08.13
申请号 US201514690916 申请日期 2015.04.20
申请人 ARIAD PHARMACEUTICALS, INC. 发明人 Wang Yihan;Huang Wei-Sheng;Liu Shuangying;Shakespeare William C.;Thomas Ranny M.;Qi Jiwei;Li Feng;Zhu Xiaotian;Kohlmann Anna;Dalgarno David C.;Romero Jan Antoinette C.;Zou Dong
分类号 C07F9/6584;C07F9/6521;C07F9/6558;C07F9/58;C07F9/6512;C07F9/6533 主分类号 C07F9/6584
代理机构 代理人
主权项 1. A compound of the formula VIa: wherein X1 is NRb1 or CRb; X3 is NRd1 or CRd; X4 is NRe1 or CRe; Ring A and Ring E are each an independently selected aryl or heteroaryl ring, the heteroaryl ring being a 5- or 6-membered ring containing 1 to 4 heteroatoms selected from N, O and S(O)r; each occurrence of Ra, Rb, Rd, Re, and Rg is independently selected from the group consisting of halo, —CN, —NO2, —R1, —OR2, —NR1—NR1R2, —NR1—OR2, —C(O)YR2, —OC(O)YR2, —NR1C(O)YR2, —SC(O)YR2, —NR1C(═S)YR2, —OC(═S)YR2, —C(═S)YR2, —YC(═NR1)YR2, —YC(═N—OR1)YR2, —YC(═N—NR1R2)YR2, —YP(═O)(YR3)(YR3), —Si(R3a)3, —NR1SO2R2, —S(O)rR2, —SO2NR1R2 and —NR1SO2NR1R2; or alternatively, each Ra and Rg may also be an independently selected moiety, —P(═O)(R3)2 or a ring system containing the moiety —P(═O)(R3)— as a ring member; Rb1, Rd1 and Re1 are absent; or alternatively two adjacent substituents selected from Rd, Rd1, Re, and Re1, or two adjacent Ra moieties, can form, with the atoms to which they are attached, a fused, 5-, 6- or 7-membered saturated, partially saturated or unsaturated ring, which contains 0-4 heteroatoms selected from N, O and S(O)r and which may bear up to four substituents; at least one of Ra and Rg is or contains a moiety, —P(═O)(R3)2 or a ring system containing the moiety —P(═O)(R3)— as a ring member; L is O or NH; r is 0, 1 or 2; s is 1,2,3,4 or 5; p is 1,2,3 or 4; each occurrence of Y is independently a bond, —O—, —S— or —NR1—; each occurrence of R1 and R2 is independently H or an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroalkyl, heterocyclic or heteroaryl moiety; each occurrence of R3 is independently an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroalkyl, heterocyclic or heteroaryl moiety, or two adjacent R3 moieties combine to form a ring system including a phosphorous atom; each occurrence of R3a is independently selected from alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroalkyl, heterocyclic, and heteroaryl; alternatively, each NR1R2 moiety may be a 5-, 6- or 7-membered saturated, partially saturated or unsaturated ring, which can be optionally substituted and which contains 0-2 additional heteroatoms selected from N, O and S(O)r; and each of the foregoing alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, aryl, heteroaryl and heterocyclic moieties is optionally substituted.
地址 Cambridge MA US