发明名称 SANGUINARINE ANALOG PP2C INHIBITORS FOR CANCER TREATMENT
摘要 Sanguinarine analogs as PP2C inhibitors are disclosed for the treatment of various cancers, as well as methods of synthesizing such analogs.
申请公布号 US2016009727(A1) 申请公布日期 2016.01.14
申请号 US201414772327 申请日期 2014.02.27
申请人 KOVACH John S.;JOHNSON Francis;SAMUDRALA Ramakrishna 发明人 KOVACH John S.;JOHNSON Francis;SAMUDRALA Ramakrishna
分类号 C07D491/153 主分类号 C07D491/153
代理机构 代理人
主权项 1. A compound having the structure: wherein: bond “a” is a single bond or a double bond; bond “b” is a single bond or a double bond; bond “c” is a single bond which is present or absent; bond “d” is a single bond which is present or absent; bond “e” is a single bond, a double bond or a triple bond; bond “f” is a single bond which is present or absent; bond “g” is a single bond which is present or absent; Q is R1 is present or absent, wherein when R1 is present, then bond “f” is present, and when R1 is absent, then bond “f” is absent; R2 is present or absent, wherein when R2 is present, then bond “g” is present, and when R2 is absent, then bond “g” is absent; wherein when bond “d” is absent, then bond “a” is a single bond, bond “b” is a single bond, bond “c” is absent, bond “e” is a triple bond, R1 is absent, R2 is absent and Q is wherein when bond “d” is present, then bond “b” is a double bond, bond “e” is a single bond or a double bond and R2 is present; wherein when bond “c” is absent and bond “d” is present, then bond “a” is a single bond, “e” is a double bond and Q is wherein when bond “c” is present, than bond “e” is a single bond or a double bond and Q is wherein when bond “e” is a single bond, then bond “a” is a double bond and R1 is present; wherein when R1 is present, then N is N+ and R1 is C1-C10 alkyl other than methyl, C2-C10 alkenyl, C3-C10 alkynyl, C3-C7 cycloalkyl, C2-C10 acyl, C2-C10 heteroalkyl, aryl or arylmethyl, any one of which is unsubstituted or substituted at one or more positions with halogen, C1-C5 alkyl, C1-C5 heteroalkyl, C2-C7 acyl, C3-C7 cycloalkyl or aryl; wherein when R2 is present, then R2 is hydrogen, halogen or amino, wherein the amino is unsubstituted or substituted with one or more C1-C5 alkyl, C2-C7 acyl, aryl or arylmethyl; wherein R3, R4, R5 and R6 are each independently hydrogen, hydroxyl, C1-C5 alkoxy, C2-C7 acyloxy, aryloxy, arylmethyloxy, thiol, C1-C5 alkylthiol, C2-C7 acylthiol, arylthiol, arylmethylthiol, amino, C1-C5 monoalkylamino, C1-C5 dialkylamino, C2-C7 acylamino or arylmethylamino, wherein at least one of R3, R4, R5 and R6 are other than hydrogen, or R3 and R4 are linked so as to form —O—(CX2)n—O—, or R4 and R5 are linked so as to form —O—(CX2)n—O—, or R5 and R6 are linked so as to form —O—(CX2)n—O—, wherein X is hydrogen, methyl or fluorine and n is 1-2; wherein R7, RB, R9 and R10 are each independently hydrogen, hydroxyl, C1-C5 alkoxy, C2-C7 acyloxy, aryloxy, arylmethyloxy, thiol, C1-C5 alkylthiol, C2-C7 acylthiol, arylthiol, arylmethylthiol, amino, C1-C5 monoalkylamino, C1-C5 dialkylamino, C2-C7 acylamino or arylmethylamino, wherein at least one of R7, R8, R9 and R10 are other than hydrogen, or R7 and R8 are linked so as to form —O—(CX2)n—O—, R8 and R9 are linked so as to form —O—(CX2)n—O—, or R9 and R10 are linked so as to form —O—(CX2)n—O—, wherein X is hydrogen, methyl or fluorine and n is 1-2; and wherein when bond “c” is present and R2 is hydrogen, then R1 is present, or a pharmaceutically acceptable salt thereof.
地址 US