申请人:BHARAT BIOTECH INTERNATIONAL LIMITED
公开号:US20180360957A1
公开(公告)日:2018-12-20
The invention relates to novel Muramyl Dipeptide (MDP) derivative compound of structural Formula-VIII, a process for synthesis, intermediates used in the synthesis and use thereof;
wherein R
1
and R
2
both are hydrogen; or R
1
is hydrogen and R
2
is alkyl or aryl; or R
1
is alkyl or aryl and R
2
is hydrogen; or R
1
and R
2
both are alkyl or aryl (same or different groups); wherein alkyl group constitute C1-C6 alkyl or higher (both linear and branched) with or without heteroatoms; and aryl group constitute phenyl, substituted phenyl, heteraryl, arylalkyl and polynuclear aromatics. These compounds possess excellent pharmacological properties, in particular immunomodulating properties for use as adjuvant in vaccine formulations. These compounds are, particularly useful as adjuvants in vaccines.
该发明涉及结构式-VIII的新型Muramyl二肽(MDP)衍生物化合物,以及用于合成的过程、合成中使用的中间体和其用途;其中R1和R2均为氢;或者R1为氢且R2为烷基或芳基;或者R1为烷基或芳基且R2为氢;或者R1和R2均为烷基或芳基(相同或不同基团);其中烷基基团包括C1-C6烷基或更高碳数(线性和支链)且可能含有杂原子;芳基基团包括苯基、取代苯基、杂芳基、芳基烷基和多核芳香族。这些化合物具有出色的药理特性,特别是作为疫苗配方中的辅助免疫调节剂的用途。这些化合物在疫苗中作为辅助剂特别有用。